Last update 27 Dec 2024

Rosuvastatin Calcium

Last update 27 Dec 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

SummaryRosuvastatin, a drug sold under the trade names of Ezallor and Crestor, is a small molecule that functions as an inhibitor of HMG-CoA reductase, an enzyme responsible for cholesterol synthesis in the liver. By inhibiting the production of cholesterol, rosuvastatin helps to reduce the level of cholesterol and triglycerides in the bloodstream. This drug is primarily used to treat hypercholesterolemia, hyperlipidemias, and heart failure. Although it is available in several countries, including the US, China, Japan, and the Netherlands, it has been granted Priority Review and Orphan Drug status by the FDA. Ongoing research is evaluating the effectiveness of rosuvastatin in treating other conditions, and its active indication is expanding. Nevertheless, rosuvastatin may cause side effects, and patients should be closely monitored during treatment to avoid adverse effects.

Drug Type

Small molecule drug

Synonyms

(3R,5S,6E)-7-(4-(4-fluorophenyl)-6-(1-methylethyl)-2-(ethyl(methylsulfonyl)amino)-5-pyrimidinyl)-3,5-dihydroxy-6-heptenoic acid, (3R,5S,6E)-7-{4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl}-3,5-dihydroxyhept-6-enoic acid, Rosuvastatin

+ [18]

Target

HMG-CoA reductase

Mechanism

HMG-CoA reductase inhibitors(HMG-CoA reductase inhibitors)

Therapeutic Areas

Nervous System DiseasesCardiovascular DiseasesCongenital Disorders+ [2]

Active Indication

AtherosclerosisDyslipidemiasHyperlipidemias+ [12]

Inactive Indication

Acute Coronary SyndromeAmnesiaAortic Valve Stenosis+ [20]

Originator Organization

Shionogi & Co., Ltd.

Active Organization

AstraZeneca PLCIPR Pharmaceuticals, Inc.A. Menarini Australia Pty Ltd.

+ [5]

Inactive Organization

Sun Pharmaceutical Industries Ltd.

AstraZeneca Pharmaceuticals Co. Ltd.

Drug Highest PhaseApproved

First Approval Date

NL (06 Nov 2002),

Homozygous familial hypercholesterolemiaHyperlipoproteinemia Type III

RegulationOrphan Drug (US), Priority Review (CN)

Structure

Molecular FormulaC44H56CaF2N6O12S2

InChIKeyGGPPBULYISSAKA-BGRFNVSISA-N

CAS Registry147098-20-2

607

Clinical Trials associated with Rosuvastatin Calcium

NCT06686615 / Not yet recruitingNot Applicable

Effectiveness and Safety of Bempedoic Acid in Combination With Ezetimibe and Either Rosuvastatin or Atorvastatin in Patients With Primary Hypercholesterolemia or Mixed Dyslipidemia: an Observational Study

Data on the real-world use and effectiveness and safety of bempedoic acid combined with both a statin and ezetimibe in clinical practice is limited. There is an increased focus on using combination therapy to lower LDL-C.

Start Date03 Mar 2025

Sponsor / Collaborator

Daiichi Sankyo Europe GmbH

NCT06742853 / Not yet recruitingPhase 1

A Phase 1, Randomized, Single-blind, Placebo-controlled Study to Investigate the Pharmacokinetics, Safety, Tolerability, and Efficacy of AZD0780 in Combination With Ezetimibe, Ezetimibe/Rosuvastatin, or Ezetimibe/Bempedoic Acid in Healthy Male and Female Participants 18 to 75 Years of Age With Elevated LDL-C.

The main aim of this study is to assess the effects of AZD0780 when added on top of ezetimibe or ezetimibe and rosuvastatin or ezetimibe and bempedoic acid.

Start Date20 Dec 2024

Sponsor / Collaborator

AstraZeneca PLC

ChiCTR2400092884 / RecruitingNot ApplicableIIT

Effect of anticoagulation combined with Rosuvastatin on DVT and prevention of PTS

Start Date01 Dec 2024

Sponsor / Collaborator

Shanxi Bethune Hospital

100 Clinical Results associated with Rosuvastatin Calcium

100 Translational Medicine associated with Rosuvastatin Calcium

100 Patents (Medical) associated with Rosuvastatin Calcium

4,384

Literatures (Medical) associated with Rosuvastatin Calcium

01 Mar 2025·MICROVASCULAR RESEARCH

Statin-treated RBC dynamics in a microfluidic porous-like network

Article

Author: König, Carola ; König, Carola S ; Stathoulopoulos, Antonios ; Balabani, Stavroula ; Ramachandran, Sudarshan

The impact of therapeutic interventions on red blood cell (RBC) deformability and microscale transport is investigated, using statins as an exemplar. Human RBCs were treated in vitro with two commonly prescribed statins, atorvastatin and rosuvastatin, at clinically relevant concentrations. Changes in RBC deformability were quantified using a microfluidic-based ektacytometer and expressed in terms of the elongation index. Dilute suspensions of the statin-treated RBCs were then perfused through a microfluidic pillar array, at a constant flow rate and negligible inertia, and imaged. Particle Tracking Velocimetry (PTV) was applied to track RBCs, identify preferential paths and estimate their velocities, whereas image processing was used to estimate cell dynamics, perfusion metrics and distributions. The findings were compared against those of healthy, untreated cells. Statins enhanced RBC deformability in agreement with literature. The extent of enhancement was found to be statin-dependent. The softer statin-treated cells were found to flow in straight, less tortuous paths, spend more time inside the pillar array and exhibit lower velocities compared to healthy RBCs, attributed to their enhanced deformation and longer shape recovery time upon impact with the array posts. The in vitro microfluidic approach demonstrated here may serve as a monitoring tool to personalise and maximise the outcome of a therapeutic treatment.

01 Feb 2025·Current medicinal chemistry

Effect of Statins on Superoxide Dismutase Level: A Systematic Review

Article

Author: Daliri, Mahla ; Jamialahmadi, Tannaz ; Reiner, Željko ; Kesharwani, Prashant ; Sahebkar, Amirhossein ; Simental-Mendía, Luis E

Background and Objective::

The literature suggests that statins may increase superoxide dismutase (SOD) levels by different mechanisms. These effects may contribute to the antioxidant and anti-inflammatory effects of statins, which are thought to be beneficial in preventing cardiovascular events. However, there are also conflicting results concerning the effect of statins on SOD levels. The goal of this systematic review was to evaluate the effect of statin therapy on SOD activity.

Methods::

This systematic review was performed based on the PRISMA statement. The terms ("statin" or "HMG-CoA reductase inhibitor" OR "lipid-lowering agents" OR "Atorvastatin" OR "Simvastatin" OR "Pravastatin" OR "Fluvastatin" OR "Lovastatin") AND ("superoxide dismutase" OR "SOD" OR "anti-oxidative" OR "oxidative stress") were searched in database systems Google Scholar, PubMed/MEDLINE, and Scopus from inception to April 2022.

Results::

This systematic review was performed based on the PRISMA statement. The terms (“statin” or “HMG-CoA reductase inhibitor” OR “lipid-lowering agents” OR “Atorvastatin” OR “Simvastatin” OR “Pravastatin” OR “Fluvastatin” OR “Lovastatin”) AND (“superoxide dismutase” OR “SOD” OR “anti-oxidative” OR “oxidative stress”) were searched in database systems Google Scholar, PubMed/MEDLINE, and Scopus from inception to April 2022.

Conclusion::

Our systematic review suggests that treatment with statins has a positive effect on SOD activity. However, evidence from further randomized controlled trials is required to confirm the potential antioxidant effect of statin therapy.

01 Feb 2025·ANNALS OF OTOLOGY RHINOLOGY AND LARYNGOLOGY

The Effect of Rosuvastatin on Facial Nerve Regeneration After Facial Nerve Injury: An Experimental Animal Study

Article

Author: Gürsan, Nilüfer ; Dincer, Uğur ; Toros, Sema Zer ; Verim, Ayşegül ; Tepe Karaca, Çiğdem ; Becerik, Çağrı

Objectives::

Rosuvastatin is an antihyperlipidemic statin group pharmacological agent with antioxidant, neuroprotective, and anti-inflammatory effects. In this study, we aimed to examine the functional, electrophysiological, and histopathological effects of rosuvastatin or in combination with corticosteroids on facial nerve regeneration in rats with traumatic peripheral facial paralysis (PFP).

Methods::

PFP was induced in 28 female Sprague Dawley rats that we divided into 4 groups: group 1, control group; group 2, methylprednisolone group; group 3, rosuvastatin group; group 4, rosuvastatin and methylprednisolone group. Electrophysiological, functional, and histopathological examinations were performed before and after the medications.

Results::

Electrophysiological threshold values of group 3 and group 4 were found to be significantly lower than the control group on day 21 after treatment ( P = .002, P = .001; P < .01).In the histopathological evaluation, axonal degeneration, macrovacuolization, and vascular congestion levels were compared between the groups, and a statistically significant difference was observed in group 4 compared to the control group. The recovery time of the eye corneal reflex was found to be significantly higher in the control group than in groups 3 and 4 when comparing postoperative day 1 to day 7 and postoperative day 1 to day 14.

Conclusion::

Rosuvastatin, especially when combined with methylprednisolone was found to significantly increase the facial nerve electrophysiological, functional, and histopathological recovery in injury-induced traumatic PFP.

News (Medical) associated with Rosuvastatin Calcium

13 Dec 2024

·www.globenewswire.com

HUTCHMED to Receive Milestone Payment from Takeda following First European Reimbursement for FRUZAQLA® (fruquintinib)

— US$10 million milestone payment to HUTCHMED follows first national reimbursement in Europe — — Follows June 2024 European approval of FRUZAQLA® (fruquintinib), the first novel oral targeted therapy in the EU for metastatic colorectal cancer regardless of biomarker status in over a decade — HONG KONG and SHANGHAI and FLORHAM PARK, N.J., Dec. 12, 2024 (GLOBE NEWSWIRE) -- HUTCHMED (China) Limited (“HUTCHMED”) (Nasdaq/AIM:HCM; HKEX:13) today announces that it will receive a US$10 million milestone payment by its partner Takeda (TSE:4502/NYSE:TAK). Takeda received a national reimbursement recommendation for FRUZAQLA® (fruquintinib) for patients with previously treated metastatic colorectal cancer (“CRC”) in Spain in December 2024, the first national reimbursement recommendation in Europe. CRC is the second most common cause of cancer-related deaths in Europe. FRUZAQLA® was approved by the European Commission (“EC”) of the European Union (“EU”) in June 2024. Takeda has the exclusive worldwide license to further develop, commercialize and manufacture fruquintinib outside of mainland China, Hong Kong and Macau. “We are delighted for both our partner, Takeda, and patients in Spain who will now be able to receive reimbursement for this innovative treatment. This is an important step forward in improving patient access across Europe more broadly,” said Dr Weiguo Su, Chief Executive Officer and Chief Scientific Officer of HUTCHMED. “It also underscores our ongoing collaboration with Takeda and reinforces our shared commitment to addressing the needs of patients with metastatic colorectal cancer.” The approvals by the EC were primarily based on results from the Phase III multiregional FRESCO-2 trial. Data from FRESCO-2 were published in The Lancet in June 2023. FRUZAQLA® was approved in the US in November 2023, in the EU in June 2024, in Switzerland in August 2024, in Canada, Japan and the United Kingdom in September 2024 and in Argentina, Australia and Singapore in October 2024. Regulatory applications are progressing in many other jurisdictions. About CRC CRC is a cancer that starts in either the colon or rectum. According to the International Agency for Research on Cancer/World Health Organization, CRC is the third most prevalent cancer worldwide, associated with more than 1.9 million new cases and 900,000 deaths in 2022. In Europe, CRC was the second most common cancer in 2022, with approximately 538,000 new cases and 248,000 deaths.1,2 In the US, it is estimated that 153,000 patients will be diagnosed with CRC and 53,000 deaths from the disease will occur in 2024.3 In Japan, CRC was the most common cancer, with an estimated 146,000 new cases and 60,000 deaths, in 2022.2 Although early-stage CRC can be surgically resected, metastatic CRC remains an area of high unmet need with poor outcomes and limited treatment options. Some patients with metastatic CRC may benefit from personalized therapeutic strategies based on molecular characteristics; however, most patients have tumors that do not harbor actionable mutations.4,5,6,7,8 About Fruquintinib Fruquintinib is a selective oral inhibitor of all three VEGF receptors (VEGFR-1, -2 and -3). VEGFR inhibitors play a pivotal role in inhibiting tumor angiogenesis. Fruquintinib was designed to have enhanced selectivity that limits off-target kinase activity, allowing for drug exposure that achieves sustained target inhibition and flexibility for potential use as part of a combination therapy. About Fruquintinib Approvals Global regulatory submissions are based on data from two large, randomized, controlled Phase III trials, the global, multi-regional FRESCO-2 trial and the FRESCO trial conducted in China, showing consistent benefit among a total of 734 patients treated with fruquintinib. Safety profiles were consistent across trials. Results from the FRESCO-2 trial were published in The Lancet in June 2023,9 while results from the FRESCO trial were published in The Journal of the American Medical Association, JAMA.10 In mainland China, Hong Kong and Macau, fruquintinib is co-marketed by HUTCHMED and Eli Lilly and Company under the brand name ELUNATE®. It was included in the China National Reimbursement Drug List (NRDL) in January 2020. Since its launch in China, over 100,000 patients with colorectal cancer have been treated with fruquintinib. About HUTCHMED HUTCHMED (Nasdaq/AIM:HCM; HKEX:13) is an innovative, commercial-stage, biopharmaceutical company. It is committed to the discovery and global development and commercialization of targeted therapies and immunotherapies for the treatment of cancer and immunological diseases. It has approximately 5,000 personnel across all its companies, at the center of which is a team of about 1,800 in oncology/immunology. Since inception it has focused on bringing cancer drug candidates from in-house discovery to patients around the world, with its first three medicines marketed in China, the first of which is also approved in the US, Europe and Japan. For more information, please visit: www.hutch-med.com or follow us on LinkedIn. E.U. IMPORTANT SAFETY INFORMATION Please consult the FRUZAQLA (fruquintinib) Summary of Product Characteristics (SmPC) before prescribing. Guidance for use: FRUZAQLA should be initiated by a physician experienced in the administration of anticancer therapy. Patients should be given the package leaflet. CONTRAINDICATIONS: Hypersensitivity to the active substance or to any of the excipients. SPECIAL POPULATIONS: Renal impairment: No dose adjustment is required for patients with mild, moderate, or severe renal impairment; Hepatic impairment: No dose adjustment is required for patients with mild or moderate hepatic impairment. FRUZAQLA is not recommended for use in patients with severe hepatic impairment as FRUZAQLA has not been studied in this population; Elderly: No dose adjustment is required in patients aged 65 years or above; Pediatric population: There is no relevant use of FRUZAQLA in the pediatric population for the indication of metastatic colorectal cancer; Women of childbearing potential / Contraception in females: Women of childbearing potential should be advised to use highly effective contraception during treatment and for at least 2 weeks following the last dose of FRUZAQLA; Pregnancy: There are no clinical data available on the use of FRUZAQLA in pregnant women. Based on its mechanism of action, FRUZAQLA has the potential to cause fetal harm. Animal studies have shown reproductive toxicity, including fetal malformations. FRUZAQLA should not be used during pregnancy unless the clinical condition of the woman requires treatment with FRUZAQLA. If FRUZAQLA is used during pregnancy or if the patient becomes pregnant while on treatment, the patient must be informed of the potential hazard to the fetus; Breast-feeding: The safe use of FRUZAQLA during breast-feeding has not been established. It is not known whether FRUZAQLA or its metabolites are excreted in human milk. There are no animal data on the excretion of FRUZAQLA in animal milk. A risk to the breastfeeding newborns/infants cannot be excluded. Breastfeeding should be discontinued during treatment and for 2 weeks after the last dose; Fertility: There are no data on the effects of FRUZAQLA on human fertility. Results from animal studies indicate that FRUZAQLA may impair male and female fertility. SPECIAL WARNINGS AND PRECAUTIONS FOR USE Hypertension: Hypertension, including hypertensive crisis, has been reported in patients treated with FRUZAQLA. Pre-existing hypertension should be monitored and adequately controlled in accordance with standard medical practices before starting FRUZAQLA treatment. Hypertension should be medically managed with antihypertensive medicinal products and adjustment of the FRUZAQLA dose, if necessary. FRUZAQLA should be permanently discontinued for hypertension that cannot be controlled with antihypertensive therapy or in patients with hypertensive crisis. Hemorrhagic events: Hemorrhagic events have been reported in patients treated with FRUZAQLA, including gastrointestinal (GI) tract events. Serious and sometimes fatal bleeding events have been reported in patients after treatment with FRUZAQLA. Hematologic and coagulation profiles should be monitored in accordance with standard medical practices in patients at risk for bleeding, including those treated with anticoagulants or other concomitant medicinal products that increase the risk of bleeding. In the event of severe bleeding requiring immediate medical intervention, FRUZAQLA should be permanently discontinued. Gastrointestinal perforation: GI perforation events, including fatal events, have been reported in patients treated with FRUZAQLA. Symptoms of GI perforation should be periodically monitored during treatment with FRUZAQLA. FRUZAQLA should be permanently discontinued in patients developing GI perforation. Proteinuria: Proteinuria events have occurred in patients treated with FRUZAQLA. Proteinuria should be monitored before initiation and during treatment with FRUZAQLA in accordance with standard medical practices. If urine dipstick proteinuria ≥ 2 g / 24 hours is detected, dose interruptions, adjustments, or discontinuation may be necessary. FRUZAQLA should be permanently discontinued in patients developing nephrotic syndrome. Palmar-plantar erythrodysesthesia syndrome (PPES): PPES is the most frequently reported dermatological adverse reaction. If Grade ≥2 skin reactions are detected, dose interruptions, adjustments, or discontinuation may be necessary. Posterior reversible encephalopathy syndrome (PRES): PRES has been reported in 1 patient (0.1%) treated with FRUZAQLA in clinical studies. PRES is a rare neurologic disorder that can present with headache, seizure, lethargy, confusion, altered mental function, blindness, and other visual or neurological disturbances, with or without associated hypertension. A diagnosis of PRES requires confirmation by brain imaging, preferably magnetic resonance imaging (MRI). In patients developing PRES, discontinuation of FRUZAQLA, along with control of hypertension and supportive medical management of other symptoms, are recommended.Impaired wound healing: Impaired wound healing has been reported in 1 patient (0.1%) treated with FRUZAQLA in clinical studies. Patients are recommended to withhold FRUZAQLA for at least 2 weeks prior to surgery. FRUZAQLA should not be resumed for at least 2 weeks after surgery, as clinically indicated when there is evidence of adequate wound healing. Arterial and venous thromboembolic events: It is recommended to avoid starting treatment with FRUZAQLA in patients with a history of thromboembolic events (including deep vein thrombosis and pulmonary embolism) within the past 6 months or if they have a history of stroke and/or transient ischemic attack within the last 12 months. If arterial thrombosis is suspected, FRUZAQLA should be discontinued immediately. INTERACTIONS Effects of other medicinal products on the pharmacokinetics of FRUZAQLA CYP3A inducers Co-administration of FRUZAQLA with rifampicin (a strong CYP3A inducer) 600 mg once daily decreased FRUZAQLA AUCinf by 65% and decreased Cmax by 12%. The concomitant use of FRUZAQLA with strong and moderate CYP3A inducers should be avoided. CYP3A inhibitors Co-administration of FRUZAQLA with itraconazole (a strong CYP3A inhibitor) 200 mg twice daily did not result in clinically meaningful changes in the area under the concentration-time curve (AUC) and Cmax of FRUZAQLA. No dose adjustment of FRUZAQLA is needed during concomitant use with CYP3A inhibitors. Gastric acid lowering agents Co-administration of FRUZAQLA with rabeprazole (a proton pump inhibitor) 40 mg once daily did not result in clinically meaningful changes in the AUC of FRUZAQLA. No dose adjustment of FRUZAQLA is needed during concomitant use with gastric acid lowering agents. Effect of FRUZAQLA on the pharmacokinetics of other medicinal products Medicinal products that are substrates of P-glycoprotein (P-gp) Co-administration of a single dose of dabigatran etexilate 150 mg (a P-gp substrate) with a single dose of FRUZAQLA 5 mg decreased AUC of dabigatran by 9%. No dose adjustment is recommended for P-gp substrates during concomitant use with FRUZAQLA. Medicinal products that are substrates of breast cancer resistance protein (BCRP) Co-administration of a single 10 mg dose of rosuvastatin (a BCRP substrate) with a single 5 mg dose of FRUZAQLA decreased AUC of rosuvastatin by 19%. No dose adjustment is recommended for BCRP substrates during concomitant use with FRUZAQLA. UNDESIRABLE EFFECTS: The most commonly reported adverse reactions with FRUZAQLA are: Very common(frequency ≥1/10)Thrombocytopenia, hypothyroidism, anorexia, hypertension, dysphonia, diarrhea, stomatitis, aspartate aminotransferase increased, total bilirubin increased, alanine aminotransferase increased, palmar-plantar erythrodysesthesia syndrome, musculoskeletal discomfort, arthralgia, proteinuria, asthenia, and fatigueCommon(≥1/100 to <1/10)Pneumonia, upper respiratory tract infection, bacterial infections, leukopenia, neutropenia, hypokalemia, epistaxis, throat pain, gastrointestinal hemorrhage, gastrointestinal perforation, pancreatic enzymes increased, oral pain, rash, and mucosal inflammation For US Prescribing Information: https://www.fruzaqla.com/sites/default/files/resources/fruzaqla-prescribing-information.pdf For Japan Prescribing Information: https://www.pmda.go.jp/PmdaSearch/iyakuDetail/ResultDataSetPDF/400256_42910H0M1028_1_01 For EU Prescribing Information: https://www.ema.europa.eu/en/documents/product-information/fruzaqla-epar-product-information_en.pdf Forward-Looking Statements This press release contains forward-looking statements within the meaning of the “safe harbor” provisions of the US Private Securities Litigation Reform Act of 1995. These forward-looking statements reflect HUTCHMED’s current expectations regarding future events, including its expectations regarding the therapeutic potential of fruquintinib for the treatment of such patients with CRC and the further clinical development of fruquintinib in this and other indications. Forward-looking statements involve risks and uncertainties. Such risks and uncertainties include, among other things, assumptions regarding the sufficiency of clinical data to support approval of fruquintinib for the treatment of patients with CRC or other indications in jurisdictions such as Europe, its potential to gain approvals from regulatory authorities, the safety profile of fruquintinib, HUTCHMED and/or Takeda’s ability to fund, implement and complete its further clinical development and commercialization plans for fruquintinib, the timing of these events, each party’s ability to satisfy the terms and conditions under the license agreement; actions of regulatory agencies, which may affect the initiation, timing and progress of clinical trials or the regulatory pathway for fruquintinib; and Takeda’s ability to successfully develop and commercialize fruquintinib. In addition, as certain studies rely on the use of other drug products as combination therapeutics with fruquintinib, such risks and uncertainties include assumptions regarding the safety, efficacy, supply and continued regulatory approval of these therapeutics. Existing and prospective investors are cautioned not to place undue reliance on these forward-looking statements, which speak only as of the date hereof. For further discussion of these and other risks, see HUTCHMED’s filings with the US Securities and Exchange Commission, The Stock Exchange of Hong Kong Limited and on AIM. HUTCHMED undertakes no obligation to update or revise the information contained in this press release, whether as a result of new information, future events or circumstances or otherwise. Medical Information This press release contains information about products that may not be available in all countries, or may be available under different trademarks, for different indications, in different dosages, or in different strengths. Nothing contained herein should be considered a solicitation, promotion or advertisement for any prescription drugs including the ones under development. CONTACTS Investor Enquiries+852 2121 8200 /ir@hutch-med.com Media Enquiries Ben Atwell / Alex Shaw, FTI Consulting+44 20 3727 1030 / +44 7771 913 902 (Mobile) / +44 7779 545 055 (Mobile) /HUTCHMED@fticonsulting.comZhou Yi, Brunswick+852 9783 6894 (Mobile) /HUTCHMED@brunswickgroup.com Nominated Advisor Atholl Tweedie / Freddy Crossley / Rupert Dearden, Panmure Liberum+44 (20) 7886 2500 ___________________________ 1Bray F,et al. Global cancer statistics 2022: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 Countries.CA Cancer J Clin.2024;74(3):229-263. doi:10.3322/caac.21834.2Ferlay J,et al. Global Cancer Observatory: Cancer Today. Lyon, France: International Agency for Research on Cancer. Available from:https://gco.iarc.who.int/today, accessed 12 June 2024.3American Cancer Society. Cancer Facts & Figures 2024. Atlanta,American Cancer Society; 2024.4Bando H, et al. Therapeutic landscape and future direction of metastatic colorectal cancer.Nat Rev Gastroenterol Hepatol2023; 20(5)306-322. doi:10.1038/s41575-022-00736-1.5D'Haene N, et al. Clinical application of targeted next-generation sequencing for colorectal cancer patients: a multicentric Belgian experience.Oncotarget.2018;9(29):20761-20768. Published 2018 Apr 17. doi:10.18632/oncotarget.25099.6Venderbosch S, et al. Mismatch repair status and BRAF mutation status in metastatic colorectal cancer patients: A pooled analysis of the CAIRO, CAIRO2, COIN, and FOCUS Studies.Clinical Cancer Res.2014; 20(20):5322–5330. doi:10.1158/1078-0432.ccr-14-0332.7Koopman M, et al. Deficient mismatch repair system in patients with sporadic advanced colorectal cancer.Br J Cancer.2009;100(2), 266–273. doi:10.1038/sj.bjc.6604867.8Ahcene Djaballah S, et al. HER2 in Colorectal Cancer: The Long and Winding Road From Negative Predictive Factor to Positive Actionable Target.Am Soc Clin Oncol Educ Book.2022;42:1-14. doi:10.1200/EDBK_351354.9Dasari NA, et al. Fruquintinib versus placebo in patients with refractory metastatic colorectal cancer (FRESCO-2): an international, multicentre, randomised, double-blind, Phase III study.Lancet.2023;402(10395):41-53. doi:10.1016/S0140-6736(23)00772-9.10Li J,et al. Effect of Fruquintinib vs Placebo on Overall Survival in Patients With Previously Treated Metastatic Colorectal Cancer: The FRESCO Randomized Clinical Trial.JAMA. 2018;319(24):2486-2496. DOI:10.1001/jama.2018.7855.

Drug ApprovalPhase 3ImmunotherapyClinical ResultLicense out/in

11 Dec 2024

·www.echemi.com

Heng Rui Pharma Launches Phase III Trial for ANGPTL3 Monoclonal Antibody

According to information from the U.S. clinical trial registry Clinicaltrials on December 10, Chinese company Heng Rui Pharma has launched its first Phase III clinical trial (SHR-1918-301) for the ANGPTL3 monoclonal antibody SHR-1918. This drug marks the first domestic ANGPTL3 monoclonal antibody to enter the Phase III clinical trial stage. SHR-1918 is an ANGPTL3 monoclonal antibody developed by Heng Rui Pharma, which works by inhibiting ANGPTL3 activity to lower triglycerides (TG) and low-density lipoprotein cholesterol (LDL-C) levels in serum. LDL-C and TG are significant risk factors for the development of atherosclerotic cardiovascular diseases. ANGPTL3 plays a key role in lipid metabolism regulation by inhibiting lipoprotein lipase and endothelial lipase, thereby reducing the clearance of TG and LDL-C. In September this year, Heng Rui Pharma announced the results of its first Phase I study (SHR-1918-101) at the European Society of Cardiology (ESC) annual meeting. The study showed that SHR-1918 (100-1200mg, subcutaneously) demonstrated good tolerance and pharmacokinetic characteristics in healthy subjects, with a peak time of 8.0-10.0 days and a half-life of 29.4-53.5 days. Additionally, SHR-1918 effectively and durably reduced LDL-C and TG levels: patients receiving doses of SHR-1918 of 300mg or higher had LDL-C levels reduced by over 30% (up to 49.1%), lasting more than 64 days; TG levels were reduced by over 50% (up to 82.8%), lasting more than 85 days. Given the potential of SHR-1918 for treating rare dyslipidemia disorders, the drug received breakthrough therapy designation for homozygous familial hypercholesterolemia (HoFH) from the Chinese National Medical Products Administration (NMPA) in September. The launched Phase III study is a multicenter, randomized, double-blind, placebo-controlled clinical trial (n=45), aimed at evaluating the efficacy and safety of SHR-1918 in treating homozygous familial hypercholesterolemia (HoFH). The primary endpoint is the percentage change in LDL-C levels from baseline at week 12. Homozygous familial hypercholesterolemia (HoFH) is a rare and severe genetic disorder where patients accumulate LDL-C in the blood due to defects or deficiencies in low-density lipoprotein receptors (LDLR), increasing the risk of heart disease and stroke. Currently, available treatment options for these patients include statins (simvastatin, atorvastatin, and rosuvastatin), ezetimibe, lomitapide, mipomersen, PCSK9 monoclonal antibodies (evolocumab and alirocumab), and evinacumab. Among these, evinacumab (Regeneron/Ultragenyx) is the only marketed ANGPTL3 monoclonal antibody, with global sales of $80.9 million in 2023.

Phase 3Clinical ResultPhase 1Breakthrough TherapyPhase 2

05 Nov 2024

·www.prnewswire.com

Rigel Announces Six Poster Presentations at the 66th American Society of Hematology Annual Meeting and Exposition

- Initial data from the ongoing Phase 1b study evaluating R289, a dual IRAK1/4 inhibitor, in LR-MDS - Additional data for REZLIDHIA® (olutasidenib) in patients with mIDH1 AML and MDS SOUTH SAN FRANCISCO, Calif., Nov. 5, 2024 /PRNewswire/ -- Rigel Pharmaceuticals, Inc. (Nasdaq: RIGL), a commercial stage biotechnology company focused on hematologic disorders and cancer, today announced upcoming presentations of six posters highlighting data from their commercial and clinical-stage hematology-oncology portfolio at the 66th American Society of Hematology (ASH) Annual Meeting and Exposition being held December 7-10, 2024, in San Diego, California and virtually. Rigel's presentations will include data from the ongoing Phase 1b dose escalation/expansion study evaluating R2891, a potent and selective dual inhibitor of IRAK1 and IRAK4, in patients with lower-risk myelodysplastic syndrome (LR-MDS) who are relapsed or refractory (R/R) to prior therapies; REZLIDHIA® (olutasidenib) for the treatment of R/R mutated isocitrate dehydrogenase-1 (mIDH1) acute myeloid leukemia (AML); and TAVALISSE® (fostamatinib disodium hexahydrate) for the treatment of chronic immune thrombocytopenia (ITP). "We look forward to the presentation of posters at ASH from across our product portfolio. We are very encouraged by the preliminary safety and efficacy data from our ongoing Phase 1b study of R289 in lower risk MDS. R289 was generally well tolerated and demonstrated responses in heavily pretreated LR-MDS patients, a population with a critical unmet need," said Raul Rodriguez, Rigel's president and CEO. "In addition, data from olutasidenib will be presented that adds to the growing body of evidence showing the benefits of its use in patients with mIDH1 AML." ASH Annual Meeting abstracts may be accessed online at . Details of the poster presentations and publications, which will be available in the poster hall and via the virtual event platform, are as follows: Abstract #: 4595 Title: R289, a Dual IRAK 1/4 Inhibitor, in Patients with Relapsed/Refractory (R/R) Lower-Risk Myelodysplastic Syndrome (LR-MDS): Initial Results from a Phase 1b Study Presenter: Guillermo Garcia-Manero, M.D. Time: Monday, December 9, 2024, 6:00pm to 8:00pm PT Initial data from the dose escalation phase using a July 15, 2024 data cutoff date indicate that R289 was generally well tolerated in a heavily pretreated LR-MDS patient population (median number of prior therapies was 4; 79% had received an hypomethylating agent), the majority of whom were high transfusion burden (received ≥8 units red blood cells in 16 weeks prior to enrollment) at study entry. Fourteen of 19 patients were evaluable for efficacy (received ≥1 dose of study drug with ≥1 efficacy assessment). Per International Working Group (IWG) 2018, RBC-transfusion independence (RBC-TI)/hematologic improvement (HI-E) occurred in 36% of patients receiving R289 doses ≥500 mg QD, with a median duration of RBC-TI of 29 weeks (range 12.4-35.9 weeks). RBC-TI >24 weeks was achieved in 2 high transfusion burden patients following 3 and 5 prior therapies, including a hypomethylating agent. Updated data as of October 25, 2024 data cutoff will be presented during the poster session. Abstract #: 1514 Title: Time to Response and Overall Survival in Patients with mIDH1 Relapsed/Refractory Acute Myeloid Leukemia Treated with Olutasidenib Presenter: Stéphane de Botton, M.D., Ph.D. Time: Saturday, December 7, 2024, 5:30pm to 7:30pm PT Results show that while some patients with mIDH1 R/R AML achieve response to olutasidenib very quickly, within 1-2 months of treatment, other patients responded after 6 months of treatment for complete remission (CR) plus CR with partial hematologic recovery (CRh) and up to 10 months for overall response. These results support the prescribing information that suggests treating for at least 6 months to allow time for clinical response in patients without disease progression or unacceptable toxicity. A Cox regression model showed no significant association between time to response and overall survival in the overall responders and those with a CR/CRh response. Abstract #: 2886 Title: Combination of Olutasidenib and Azacitidine Induces Durable Complete Remissions in mIDH1 Acute Myeloid Leukemia: A Multicohort Open-Label Phase 1/2 Trial Presenter: Jorge E. Cortes, M.D. Time: Sunday, December 8, 2024, 6:00pm to 8:00pm PT Olutasidenib plus azacitidine induced high response rates and durable remissions with a tolerable side effect profile in patients with R/R mIDH1 AML, in the first reported analysis of a combination therapy with an mIDH1 inhibitor and a hypomethylating agent focused on the R/R AML setting. CR/CRh was achieved in 31% (21/67) of patients and median duration of CR/CRh was 15 months. Abstract #: 4600 Title: Olutasidenib Alone or in Combination with Azacitidine in Patients with mIDH1 Myelodysplastic Syndromes/Neoplasms: Final 5-Year Data Presenter: Jorge E. Cortes, M.D. Time: Monday, December 9, 2024, 6:00pm to 8:00pm PT Olutasidenib demonstrated encouraging response rates with durable remissions and an acceptable and manageable safety profile in patients with intermediate to very high-risk mIDH1 MDS treated with olutasidenib monotherapy or in combination with azacitidine. In a sub analysis of the 19 efficacy evaluable patients, 79% (11/14) of patients responded to combination therapy and 40% (2/5) responded to monotherapy, which included both patients (2/2) using the approved dose of 150 mg BID olutasidenib. Abstract #: 1525 Title: Effectiveness of Olutasidenib Versus Ivosidenib in Patients with Mutated Isocitrate Dehydrogenase 1 Acute Myeloid Leukemia Who Are Relapsed or Refractory to Venetoclax: The 2102-HEM-101 Trial Versus a US Electronic Health Record-Based External Control Arm Presenter: Catherine E. Lai, M.D. Time: Sunday, December 8, 2024, 6:00pm to 8:00pm PT This study provides the first evidence suggesting favorable effectiveness of olutasidenib versus ivosidenib in patients with mIDH1 AML who were R/R to a venetoclax-based regimen. As with any real-world experience study, limitations include risk of unmeasured confounding and differential outcome reporting. Abstract #: 5080 Title: Real-World Experience with Combination Therapy of Fostamatinib and Thrombopoetin Receptor Agonists (TPO-RAs) for Treatment of Immune Thrombocytopenia (ITP): Patient-Reported Outcomes Presenter: Elizabeth Bowhay-Carnes, M.D. Time: Monday, December 9, 2024, 6:00pm to 8:00pm PT This real-world study treating patients with fostamatinib and a thrombopoetin receptor agonist (TPO-RA) demonstrated that the combination led to a clinically meaningful response in a majority of patients with ITP. ASH Publication Abstract #: 7908 Title: Treatment Patterns and Outcomes of Olutasidenib in Patients with Relapsed/Refractory (R/R) mutated IDH1 Acute Myeloid Leukemia (AML) in the Real World Authors: Aaron Sheppard, Ph.D.; Lixia Wang, Ph.D.; Ravi Potluri, MBA; Eros Papademetriou, MA About R289 R289 is a prodrug of R835, an IRAK1/4 dual inhibitor, which has been shown in preclinical studies to block inflammatory cytokine production in response to toll-like receptor (TLR) and interleukin-1 receptor (IL-1R) family signaling. TLRs and IL-1Rs play a critical role in the innate immune response and dysregulation of these pathways can lead to various inflammatory conditions. Chronic stimulation of both these receptor systems is thought to cause the pro-inflammatory environment in the bone marrow responsible for persistent cytopenias in lower-risk MDS patients.2 About AML Acute myeloid leukemia (AML) is a rapidly progressing cancer of the blood and bone marrow that affects myeloid cells, which normally develop into various types of mature blood cells. AML occurs primarily in adults and accounts for about 1 percent of all adult cancers. The American Cancer Society estimates that there will be about 20,800 new cases in the United States, most in adults, in 2024.3 Relapsed AML affects about half of all patients who, following treatment and remission, experience a return of leukemia cells in the bone marrow.4 Refractory AML, which affects between 10 and 40 percent of newly diagnosed patients, occurs when a patient fails to achieve remission even after intensive treatment.5 Quality of life declines for patients with each successive line of treatment for AML, and well-tolerated treatments in relapsed or refractory disease remain an unmet need. About ITP In patients with ITP (immune thrombocytopenia), the immune system attacks and destroys the body's own blood platelets, which play an active role in blood clotting and healing. Common symptoms of ITP are excessive bruising and bleeding. People suffering with chronic ITP may live with an increased risk of severe bleeding events that can result in serious medical complications or even death. Current therapies for ITP include steroids, blood platelet production boosters (TPO-RAs), and splenectomy. However, not all patients respond to existing therapies. As a result, there remains a significant medical need for additional treatment options for patients with ITP. About REZLIDHIA® INDICATION REZLIDHIA is indicated for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) with a susceptible isocitrate dehydrogenase-1 (IDH1) mutation as detected by an FDA-approved test. IMPORTANT SAFETY INFORMATION WARNINGS AND PRECAUTIONS Differentiation Syndrome REZLIDHIA can cause differentiation syndrome. In the clinical trial of REZLIDHIA in patients with relapsed or refractory AML, differentiation syndrome occurred in 16% of patients, with grade 3 or 4 differentiation syndrome occurring in 8% of patients treated, and fatalities in 1% of patients. Differentiation syndrome is associated with rapid proliferation and differentiation of myeloid cells and may be life-threatening or fatal. Symptoms of differentiation syndrome in patients treated with REZLIDHIA included leukocytosis, dyspnea, pulmonary infiltrates/pleuropericardial effusion, kidney injury, fever, edema, pyrexia, and weight gain. Of the 25 patients who experienced differentiation syndrome, 19 (76%) recovered after treatment or after dose interruption of REZLIDHIA. Differentiation syndrome occurred as early as 1 day and up to 18 months after REZLIDHIA initiation and has been observed with or without concomitant leukocytosis. If differentiation syndrome is suspected, temporarily withhold REZLIDHIA and initiate systemic corticosteroids (e.g., dexamethasone 10 mg IV every 12 hours) for a minimum of 3 days and until resolution of signs and symptoms. If concomitant leukocytosis is observed, initiate treatment with hydroxyurea, as clinically indicated. Taper corticosteroids and hydroxyurea after resolution of symptoms. Differentiation syndrome may recur with premature discontinuation of corticosteroids and/or hydroxyurea treatment. Institute supportive measures and hemodynamic monitoring until improvement; withhold dose of REZLIDHIA and consider dose reduction based on recurrence. Hepatotoxicity REZLIDHIA can cause hepatotoxicity, presenting as increased alanine aminotransferase (ALT), increased aspartate aminotransferase (AST), increased blood alkaline phosphatase, and/or elevated bilirubin. Of 153 patients with relapsed or refractory AML who received REZLIDHIA, hepatotoxicity occurred in 23% of patients; 13% experienced grade 3 or 4 hepatotoxicity. One patient treated with REZLIDHIA in combination with azacitidine in the clinical trial, a combination for which REZLIDHIA is not indicated, died from complications of drug-induced liver injury. The median time to onset of hepatotoxicity in patients with relapsed or refractory AML treated with REZLIDHIA was 1.2 months (range: 1 day to 17.5 months) after REZLIDHIA initiation, and the median time to resolution was 12 days (range: 1 day to 17 months). The most common hepatotoxicities were elevations of ALT, AST, blood alkaline phosphatase, and blood bilirubin. Monitor patients frequently for clinical symptoms of hepatic dysfunction such as fatigue, anorexia, right upper abdominal discomfort, dark urine, or jaundice. Obtain baseline liver function tests prior to initiation of REZLIDHIA, at least once weekly for the first two months, once every other week for the third month, once in the fourth month, and once every other month for the duration of therapy. If hepatic dysfunction occurs, withhold, reduce, or permanently discontinue REZLIDHIA based on recurrence/severity. ADVERSE REACTIONS The most common (≥20%) adverse reactions, including laboratory abnormalities, were aspartate aminotransferase increased, alanine aminotransferase increased, potassium decreased, sodium decreased, alkaline phosphatase increased, nausea, creatinine increased, fatigue/malaise, arthralgia, constipation, lymphocytes increased, bilirubin increased, leukocytosis, uric acid increased, dyspnea, pyrexia, rash, lipase increased, mucositis, diarrhea and transaminitis. DRUG INTERACTIONS Avoid concomitant use of REZLIDHIA with strong or moderate CYP3A inducers. Avoid concomitant use of REZLIDHIA with sensitive CYP3A substrates unless otherwise instructed in the substrates prescribing information. If concomitant use is unavoidable, monitor patients for loss of therapeutic effect of these drugs. LACTATION Advise women not to breastfeed during treatment with REZLIDHIA and for 2 weeks after the last dose. GERIATRIC USE No overall differences in effectiveness were observed between patients 65 years and older and younger patients. Compared to patients younger than 65 years of age, an increase in incidence of hepatotoxicity and hypertension was observed in patients ≥65 years of age. HEPATIC IMPAIRMENT In patients with mild or moderate hepatic impairment, closely monitor for increased probability of differentiation syndrome. Click here for Full Prescribing Information, including Boxed WARNING. To report side effects of prescription drugs to the FDA, visit or call 1-800-FDA-1088 (800-332-1088). About TAVALISSE® Indication TAVALISSE (fostamatinib disodium hexahydrate) tablets is indicated for the treatment of thrombocytopenia in adult patients with chronic immune thrombocytopenia (ITP) who have had an insufficient response to a previous treatment. Important Safety Information Warnings and Precautions Hypertension can occur with TAVALISSE treatment. Patients with pre-existing hypertension may be more susceptible to the hypertensive effects. Monitor blood pressure every 2 weeks until stable, then monthly, and adjust or initiate antihypertensive therapy for blood pressure control maintenance during therapy. If increased blood pressure persists, TAVALISSE interruption, reduction, or discontinuation may be required. Elevated liver function tests (LFTs), mainly ALT and AST, can occur with TAVALISSE. Monitor LFTs monthly during treatment. If ALT or AST increase to ≥3 x upper limit of normal, manage hepatotoxicity using TAVALISSE interruption, reduction, or discontinuation. Diarrhea occurred in 31% of patients and severe diarrhea occurred in 1% of patients treated with TAVALISSE. Monitor patients for the development of diarrhea and manage using supportive care measures early after the onset of symptoms. If diarrhea becomes severe (≥Grade 3), interrupt, reduce dose or discontinue TAVALISSE. Neutropenia occurred in 6% of patients treated with TAVALISSE; febrile neutropenia occurred in 1% of patients. Monitor the ANC monthly and for infection during treatment. Manage toxicity with TAVALISSE interruption, reduction, or discontinuation. TAVALISSE can cause fetal harm when administered to pregnant women. Advise pregnant women the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment and for at least 1 month after the last dose. Verify pregnancy status prior to initiating TAVALISSE. It is unknown if TAVALISSE or its metabolite is present in human milk. Because of the potential for serious adverse reactions in a breastfed child, advise a lactating woman not to breastfeed during TAVALISSE treatment and for at least 1 month after the last dose. Drug Interactions Concomitant use of TAVALISSE with strong CYP3A4 inhibitors increases exposure to the major active metabolite of TAVALISSE (R406), which may increase the risk of adverse reactions. Monitor for toxicities that may require a reduction in TAVALISSE dose. It is not recommended to use TAVALISSE with strong CYP3A4 inducers, as concomitant use reduces exposure to R406. Concomitant use of TAVALISSE may increase concentrations of some CYP3A4 substrate drugs and may require a dose reduction of the CYP3A4 substrate drug. Concomitant use of TAVALISSE may increase concentrations of BCRP substrate drugs (eg, rosuvastatin) and P-Glycoprotein (P-gp) substrate drugs (eg, digoxin), which may require a dose reduction of the BCRP and P-gp substrate drug. Adverse Reactions Serious adverse drug reactions in the ITP double-blind studies were febrile neutropenia, diarrhea, pneumonia, and hypertensive crisis, which occurred in 1% of TAVALISSE patients. In addition, severe adverse reactions occurred including dyspnea and hypertension (both 2%), neutropenia, arthralgia, chest pain, diarrhea, dizziness, nephrolithiasis, pain in extremity, toothache, syncope, and hypoxia (all 1%). Common adverse reactions (≥5% and more common than placebo) from FIT-1 and FIT-2 included: diarrhea, hypertension, nausea, dizziness, ALT and AST increased, respiratory infection, rash, abdominal pain, fatigue, chest pain, and neutropenia. Please see for Full Prescribing Information. To report side effects of prescription drugs to the FDA, visit or call 1-800-FDA-1088 (800-332-1088). REZLIDHIA and TAVALISSE are registered trademarks of Rigel Pharmaceuticals, Inc. About Rigel Rigel Pharmaceuticals, Inc. (Nasdaq: RIGL) is a biotechnology company dedicated to discovering, developing and providing novel therapies that significantly improve the lives of patients with hematologic disorders and cancer. Founded in 1996, Rigel is based in South San Francisco, California. For more information on Rigel, the Company's marketed products and pipeline of potential products, visit . R289 is an investigational compound not approved by the FDA. Sallman DA et al. Unraveling the Pathogenesis of MDS: The NLRP3 Inflammasome and Pyroptosis Drive the MDS Phenotype. Front Oncol. June 16, 2016. Accessed September 30, 2024. DOI: The American Cancer Society. Key Statistics for Acute Myeloid Leukemia (AML). Revised June 5, 2024. Accessed September 30, 2024: Leukaemia Care. Relapse in Acute Myeloid Leukaemia (AML). Version 3. Reviewed October 2021. Accessed September 30, 2024: Thol F, Schlenk RF, Heuser M, Ganser A. How I treat refractory and early relapsed acute myeloid leukemia. Blood (2015) 126 (3): 319-27. Accessed September 30, 2024. doi: Forward-Looking Statements This press release contains forward-looking statements relating to, among other things, clinical information regarding studies of Rigel's products, including; the progress of the Phase 1b clinical trial of R289 for the treatment of lower-risk myeloid dysplastic syndrome; olutasidenib as a treatment for mIDH1 Relapsed/Refractory Acute Myeloid Leukemia, use of olutasidenib with azacitidine, and use of olutasidenib versus ivosidenib; and, fostamatinib in combination with thrombopoetin receptor agonists for treatment of immune thrombocytopenia, and fostamatinib as early treatment of immune thrombocytopenia. Any statements contained in this press release that are not statements of historical fact may be deemed to be forward-looking statements. Forward-looking statements can be identified by words such as "plan", "potential", "may", "look to", "expects", "will" and similar expressions in reference to future periods. Forward-looking statements are neither historical facts nor assurances of future performance. Instead, they are based on Rigel's current beliefs, expectations, and assumptions and hence they inherently involve significant risks, uncertainties and changes in circumstances that are difficult to predict and many of which are outside of our control. Therefore, you should not rely on any of these forward-looking statements. Actual results and the timing of events could differ materially from those anticipated in such forward looking statements as a result of these risks and uncertainties, which include, without limitation, risks and uncertainties associated with the commercialization and marketing of fostamatinib, olutasidenib and pralsetinib; risks that the FDA, European Medicines Agency, PMDA or other regulatory authorities may make adverse decisions regarding fostamatinib, pralsetinib or olutasidenib; risks that clinical trials may not be predictive of real-world results or of results in subsequent clinical trials; risks that fostamatinib, pralsetinib or olutasidenib may have unintended side effects, adverse reactions or incidents of misuses; the availability of resources to develop Rigel's product candidates; market competition; as well as other risks detailed from time to time in Rigel's reports filed with the Securities and Exchange Commission, including its Quarterly Report on Form 10-Q for the quarter ended June 30, 2024 and subsequent filings. Any forward-looking statement made by us in this press release is based only on information currently available to us and speaks only as of the date on which it is made. Rigel does not undertake any obligation to update forward-looking statements, whether written or oral, that may be made from time to time, whether as a result of new information, future developments or otherwise, and expressly disclaims any obligation or undertaking to release publicly any updates or revisions to any forward-looking statements contained herein, except as required by law. Contact for Investors & Media: Investors: Rigel Pharmaceuticals, Inc. 650.624.1232 [email protected] Media: David Rosen Argot Partners 646.461.6387 [email protected] SOURCE Rigel Pharmaceuticals, Inc. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Clinical ResultPhase 1ASH

100 Deals associated with Rosuvastatin Calcium

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KEGG	Wiki	ATC	Drug Bank
D01915	Rosuvastatin Calcium	C10AA07	DB01098

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Heterozygous familial hypercholesterolemia	US	Sun Pharmaceutical Industries Ltd.	04 Aug 2023
Primary Hyperlipidemia	US	Sun Pharmaceutical Industries Ltd.	04 Aug 2023
Atherosclerosis	US	IPR Pharmaceuticals, Inc.	08 Nov 2007
Dyslipidemias	US	IPR Pharmaceuticals, Inc.	08 Nov 2007
Hyperlipidemias	US	IPR Pharmaceuticals, Inc.	08 Nov 2007
Hypertriglyceridemia	US	IPR Pharmaceuticals, Inc.	08 Nov 2007
Myocardial Infarction	AU	A. Menarini Australia Pty Ltd.	26 Apr 2006
Stroke	AU	A. Menarini Australia Pty Ltd.	26 Apr 2006
Hypercholesterolemia	JP	Shionogi & Co., Ltd.	19 Jan 2005
Hypercholesterolemia	JP	AstraZeneca KK	19 Jan 2005
Hyperlipoproteinemia Type II	JP	AstraZeneca KK	19 Jan 2005
Hyperlipoproteinemia Type II	JP	Shionogi & Co., Ltd.	19 Jan 2005
Hyperlipidemia Type IIa	US	IPR Pharmaceuticals, Inc.	12 Aug 2003
Hyperlipoproteinemia Type IIb	US	IPR Pharmaceuticals, Inc.	12 Aug 2003
Hyperlipoproteinemia Type IV	US	IPR Pharmaceuticals, Inc.	12 Aug 2003
Complex dyslipidemia	NL	Grünenthal GmbH	07 Mar 2003
Primary hypercholesterolemia	NL	Grünenthal GmbH	07 Mar 2003
Homozygous familial hypercholesterolemia	NL	AstraZeneca UK Ltd.	06 Nov 2002
Hyperlipoproteinemia Type III	NL	AstraZeneca UK Ltd.	06 Nov 2002

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Pulmonary Embolism	Phase 3	-	AstraZeneca PLC	01 Feb 2011
Recurrent deep vein thrombosis	Phase 3	-	AstraZeneca PLC	01 Feb 2011
Acute Coronary Syndrome	Phase 3	US	AstraZeneca PLC	01 Dec 2003
Acute Coronary Syndrome	Phase 3	CR	AstraZeneca PLC	01 Dec 2003
Acute Coronary Syndrome	Phase 3	SV	AstraZeneca PLC	01 Dec 2003
Acute Coronary Syndrome	Phase 3	MA	AstraZeneca PLC	01 Dec 2003
Acute Coronary Syndrome	Phase 3	PA	AstraZeneca PLC	01 Dec 2003
Chronic systolic heart failure	Phase 3	BE	AstraZeneca PLC	01 Sep 2003
Chronic systolic heart failure	Phase 3	BG	AstraZeneca PLC	01 Sep 2003
Chronic systolic heart failure	Phase 3	CZ	AstraZeneca PLC	01 Sep 2003

Clinical Result

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05788328 (CTgov)	Phase 1	Obesity	16	DE (Period 1: DE 150 mg)	dbtznclmeh(iczghejsng) = zxdafekfic yyvbjaokfk (xdnaalakue, kblexorrxb - wxxnwmstvn) View more	-	15 Nov 2024
				DE+PF-07081532 (Period 4: DE 150 mg + PF-07081532 80 mg QD)	dbtznclmeh(iczghejsng) = jugqrlwmsf yyvbjaokfk (xdnaalakue, leokaydhfo - rzuvolhepw) View more
NCT04964544 (TACTiC, CTgov)	Phase 3	Hypercholesterolemia	1,196	Rosuvastatin	hlnonaswds(jmiqzvimtx) = lzrsdsfukf ugcbvuvrgy (usesttozye, rvicdxawij - pybruelrrc) View more	-	30 Oct 2024
NCT05898672 (CTgov)	Phase 1	COVID-19	12	Rosuvastatin (Period 1: Rosuvastatin 10 mg)	rycbxtflja(xjxvojmbkf) = illnjxnomj aplvfdgmrr (fkstmuqllj, zlqrdmcebj - zaxkkaulxn) View more	-	28 Oct 2024
				Rosuvastatin+Nirmatrelvir+Ritonavir (Period 2: Rosuvastatin 10 mg + Nirmatrelvir 300 mg/ Ritonavir 100 mg)	rycbxtflja(xjxvojmbkf) = ldwhomauov aplvfdgmrr (fkstmuqllj, haxnvvxkjp - zsetoxumel) View more
NCT02740699 (CTgov)	Phase 4	Cardiovascular Diseases	79	Cardiac Magnetic Resonance Image (MRI)+Atorvastatin+Rosuvastatin	fwxdvjfrkr(tqyzcfaako) = fmdsgkkpsl unbhpizzlk (owgumzqgnu, cnbwqaqqct - coredlgyxl) View more	-	09 Oct 2024
NCT05895123 (retrospectively registered, Pubmed \| Cardiovasc Drugs Ther)	Phase 2	ST Elevation Myocardial Infarction sST2 \| MMP9 \| CRP	-	Rosuvastatin 20mg	ugbymzhffq(vifxpmrnho) = fbfdxjygeq luhukzyzlx (bjkfapevas ) View more	Positive	12 Sep 2024
				Atorvastatin 40mg	ugbymzhffq(vifxpmrnho) = gsuyjlhorh luhukzyzlx (bjkfapevas ) View more
ESC2024	Not Applicable	Atherosclerosis	-	Moderate-intensity statin plus ezetimibe (MIS+EZT)	nlqmcfzemo(mioegewpsy): RR = 1.19 (95% CI, 0.79 - 1.78), P-Value = 0.404 View more	-	01 Sep 2024
				High-intensity statin monotherapy (HIS)
ESC2024	Not Applicable	-	-	Rosuvastatin	mswtoamget(vwzbebiyzf) = euwfwfustj priwnmvrrr (bfyuqohuts ) View more	-	01 Sep 2024
				Other statins	mswtoamget(vwzbebiyzf) = dvicjohzba priwnmvrrr (bfyuqohuts ) View more
ESC2024	Not Applicable	Neoplasm Metastasis	-	Moderate-intensity statin + ezetimibe	vmzczmilrs(addkuagkkj): RR = 1.26 (95% CI, 1.19 - 1.34) View more	-	31 Aug 2024
				High-intensity statin
ADA2024	Not Applicable	Hyperglycemia	-	Rosuvastatin	jjjtehtqrk(rejnqwdvkv) = fazxnvrpzj fvjvgexcuo (lpdmnpyesu )	-	14 Jun 2024
ADA2024	Not Applicable	Chronic Kidney Diseases	-	Rosuvastatin	gsgnmdbrmx(tlfotfifmi) = ideamxxzhy qmopxwabtt (fgwpakwsmz ) View more	-	14 Jun 2024
				Atorvastatin	gsgnmdbrmx(tlfotfifmi) = lmbiaztjzu qmopxwabtt (fgwpakwsmz ) View more

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