Last update 21 Nov 2024

Allopurinol

Last update 21 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

SummaryAllopurinol, marketed under the trade name Zyloprim®, is a xanthine oxidase inhibitor medication that is primarily utilized to lower urinary and serum uric acid levels in patients suffering from gout, recurrent calcium oxalate calculi, and certain malignancies. The mechanism of action of this medication involves inhibiting the enzyme xanthine oxidase. Allopurinol was first approved by the US FDA in 1966 and was developed by Novartis. Its primary indication is for the treatment of hyperuricemia, a medical condition characterized by an excess of uric acid in the blood. Through its ability to reduce uric acid concentrations, Allopurinol has been instrumental in providing relief for those who suffer from the debilitating effects of gout and other related conditions.

Drug Type

Small molecule drug

Synonyms

1,5-Dihydro-4H-pyrazolo(3,4-d)pyrimidin-4-one, 1,5-Dihydro-4H-pyrazolo(3,4-d)pyrimidine-4-one, 1H-Pyrazolo(3,4-d)pyrimidin-4-ol

+ [23]

Target

Mechanism

XO inhibitors(Xanthine dehydrogenase inhibitors)

Therapeutic Areas

Immune System DiseasesCongenital DisordersEndocrinology and Metabolic Disease+ [3]

Active Indication

GoutNephrolithiasisHyperuricemia

Inactive Indication

Chronic Kidney DiseasesHand-Foot SyndromeHeart failure with normal ejection fraction

Originator Organization

Sebela Ireland Ltd.

Active Organization

GlaxoSmithKline KK

Sumitomo Pharma Co., Ltd.

Casper Pharma LLC

+ [1]

Inactive Organization

AstraZeneca PLC

Ardea Biosciences, Inc.

Advancell Advanced In Vitro Cell Technologies SL

Drug Highest PhaseApproved

First Approval Date

US (19 Aug 1966),

Hyperuricemia

Regulation-

Structure

Molecular FormulaC5H4N4O

InChIKeyOFCNXPDARWKPPY-UHFFFAOYSA-N

CAS Registry315-30-0

274

Clinical Trials associated with Allopurinol

IRCT20170609034406N12 / SuspendedPhase 3IIT

The effect of allopurinol in preventing liver fibrosis in non-alcoholic fatty liver disease: A Randomized Placebo-Controlled Clinical Trial

Start Date21 Nov 2024

Sponsor / Collaborator

Tabriz University of Medical Sciences

NCT05888233 / RecruitingPhase 2IIT

Allopurinol Improves Diastolic Function in African Americans With Resistant Hypertension

African American adults in the United States have the highest prevalence rate of high blood pressure (hypertension) and heart failure in the world. African Americans with treatment resistant hypertension have higher levels of the enzyme - xanthine oxidase compared to Caucasians. This trial will test if administration of the xanthine oxidase inhibitor - Allopurinol (commonly used in the treatment of gout), given over a period of 8 weeks, will improve heart function, exercise ability and quality of life in African American Veterans with resistant hypertension.

Start Date30 Sep 2024

Sponsor / Collaborator

VA Office of Research and Development

CTRI/2024/08/073056 / Not yet recruitingPhase 2IIT

A Controlled clinical study to evaluate the efficacy of navkarshik kwath in vatashonita w.s.t to gouty arthritis - nil

Start Date28 Sep 2024

Sponsor / Collaborator-

100 Clinical Results associated with Allopurinol

100 Translational Medicine associated with Allopurinol

100 Patents (Medical) associated with Allopurinol

8,508

Literatures (Medical) associated with Allopurinol

01 Feb 2025·Journal of Ethnopharmacology

Anti-inflammatory effects and mechanism of Plantago asiatica L. and Lonicera japonica Thunb. extracts based on canine and feline kidney cell models

Article

Author: Liu, Tong ; Bai, Huasong ; Li, Yunliang ; Wang, Hengyan ; Wang, Zhanzhong

ETHNOPHARMACOLOGICAL RELEVANCEStone symptoms are one of the most common health problems in pets. Inflammation in the kidneys causes the pet's urine to form a hard substance that blocks the urinary tract. Plantago asiatica L. and Lonicera japonica Thunb., as traditional Chinese diuretics, have remarkable effects on anti-inflammatory and analgesia. However, their mechanism of action remains unclear.PURPOSEThe alleviating effect of Plantago asiatica and Lonicera japonica extracts upon lipopolysaccharide (LPS)-induced inflammation in canine and feline kidney cells was investigated in this work.MATERIALS AND METHODSInflammatory factor concentrations and oxidative stress indicators were used to evaluate the inflammatory response. The mechanism by which two extracts reduced inflammation was explored using quantitative real-time polymerase chain reaction (RT-qPCR) and high performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) metabolome assay.RESULTSThe results demonstrated that Plantago asiatica or Lonicera japonica extract at safe concentration (25-200 μg/mL for canine kidney cell and 1-20 μg/mL for feline kidney cell, respectively) could significantly reduce the release of nitric oxide (p < 0.05) and oxidative damage (p < 0.05) after LPS stimulation, inhibit the production of inflammatory factors (p < 0.05), and improve cell migration ability (p < 0.05). The RT-qPCR results confirmed that Plantago asiatica and Lonicera japonica extracts significantly reduced the mRNA expressions of TLR4, MyD88, NF-kB, Caspase9 and Bax (p < 0.05), and enhanced the mRNA expression of Bcl-2 (p < 0.05). Non-targeted metabolomics results indicated that the cells treated with two extracts raised the contents of allopurinol, further inhibited uric acid and gout and lowered the contents of adenosine and adenine. Moreover, it was revealed that the Plantago asiatica and Lonicera japonica participated in purine metabolism, glycerophospholipid metabolism, protein digestion and absorption, nucleotide metabolism pathways to alleviate kidney cell inflammation.CONCLUSIONSThe interaction mechanism was revealed to reduce the content of inflammatory factors by inhibiting TLR4-MyD88-NF-kB signaling pathway, and participate in purine metabolism to reduce the inflammation of kidney cells. These findings could provide significant insight into alleviating nephritis in canine and feline, and strategies for preventing urinary tract and kidney stones using Plantago asiatica and Lonicera japonica extracts.

01 Jan 2025·Joint Bone Spine

Pediatrics hyperuricemia in clinical practice: A retrospective analysis in 1753 children and adolescents with hyperuricemia

Article

Author: Stiburkova, Blanka ; Zeman, Jiri ; Lukesova, Marketa

OBJECTIVESSerum levels of uric acid (S-UA) are influenced by the interaction of genetic and environmental factors; detailed studies of hyperuricemia in children are rare. This retrospective study aimed to analyze the causes, risk factors, and therapeutic approaches associated with the development of hyperuricemia in childhood.METHODSIn a single-center study, serum uric acid levels were analyzed in 33,900 samples from 13,890 children and adolescents ˂ 19 years (6,760 girls and 7,130 boys) obtained between 2013 and 2023. Hyperuricemia was defined as S-UA > 370 μmol/L (6.22 mg/dl) in girls and > 420 μmol/L (7.06 mg/dl) in boys; mild hyperuricemia was defined as 370-420 μmol/L in boys ˂ 13 years.RESULTSIn the analyzed group, hyperuricemia was found in 1,753 patients (12.6%), including 586 girls and 864 boys; mild hyperuricemia was found in 303 boys ˂ 13 years. The most common associated conditions were obesity with body mass index > 95^th percentile (27.8% of girls, 26.3% of boys) and chronic kidney disease (18.6% of boys, 11.4% of girls). Hyperuricemia was also relatively common in children with connective tissue disorders (10.6%) or different inherited metabolic disorders (10.7%). Transitory hyperuricemia was found in 19.1% of girls and 10.1% of boys with acute gastroenteritis. Urate-lowering therapy was used in 73 children and adolescents with severe hyperuricemia (S-UA 556±107 µmol/L, fraction excretion of UA 3.27±1.98%). Eight treated children had chronic kidney disease, nine were extremely obese, one had combined antiepileptic therapy, and 55 had inherited metabolic diseases, including 26 children with disorders of purine metabolism. The initial daily dose of allopurinol (50-100 mg) normalized the S-UA (350±80 µmol/L) in a majority of children, except for extremely obese adolescents (weight 98-149 kg), where the dose had to be increased to 200-300 mg. Conclusions Asymptomatic hyperuricemia is a relatively common biochemical finding in pediatric clinical practice. The etiology of hyperuricemia should be carefully analyzed, and the value of individualized hyperuricemia management and the eventual benefits of urate-lowering therapy in children must be carefully considered.

31 Dec 2024·Gut Microbes

Empowering probiotics with high xanthine transport for effective hyperuricemia management

Article

Author: Zhang, Yi-Fan ; Li, Ju-Ling ; Zhou, Ying ; Ye, Bang-Ce ; Zou, Zhen-Ping

Hyperuricemia, a prevalent metabolic disorder, poses a susceptibility to various complications. The conventional pharmacotherapeutic approaches for hyperuricemia often entail notable adverse effects, posing substantial clinical challenges. Hence, the imperative lies in the development of novel, safe and effective strategies for preventing and treating hyperuricemia. Here, we developed a probiotic Escherichia coli Nissle 1917 strain, designated as YES301, which contains a rationally designed xanthine importer XanQ, enabling efficient uptake of xanthine and hypoxanthine, consequently leading to reduced serum uric acid concentrations and amelioration of renal impairments in a murine model of hyperuricemia. Importantly, YES301 exhibited a therapeutic efficacy comparable to allopurinol, a conventional uric acid-lowering agent, and manifesting fewer adverse effects and enhanced biosafety. These findings highlight the promising potential of engineered probiotics in the management of hyperuricemia through reducing intestinal purine levels.

News (Medical) associated with Allopurinol

28 Aug 2024

·www.prnewswire.com

Innovent Announces 2024 Interim Results and Business Updates

Strong commercial performance and significant pipeline milestones support sustained growth and innovation SAN FRANSISCO and SUZHOU, China, Aug. 28, 2024 /PRNewswire/ -- Innovent Biologics, Inc. (Innovent) (HKEX: 01801), a world-class biopharmaceutical company that develops, manufactures and commercializes high-quality medicines for the treatment of cancer, cardiovascular and metabolic, autoimmune, ophthalmology and other major diseases, announces its 2024 interim results and major business updates. Dr. Michael Yu, Founder, Chairman and CEO of Innovent, stated: "For the first half of 2024, our company's strategy of sustainable growth and global innovation continue executing very well: we achieved strong revenue growth, improved operational efficiency in all areas, and reached significant milestones in our late-stage pipeline to support our sustained growth. We also reported promising data readouts from early-stage assets, reinforcing our confidence in achieving global innovation and contributing to new long-term opportunities. The successful first half of 2024 has laid a solid foundation for achieving our full-year's growth. With strong commercial and financial execution, a high-value late-stage pipeline, and disciplined investments in next-generation innovation, we are well-positioned to deliver long-term value for patients, employees, shareholders and society." Enhanced operational efficiency and strong financial performance S trong revenue growth momentum: total revenue was RMB3,952.3 million in the first half of 2024, with a strong year-over-year growth of 46.3%, reflecting robust demand for our innovative portfolio and the advantage of our sustainable business model. Significantly improved financial performance: EBITDA Loss was significantly reduced, driven by strong revenue growth, enhanced operational efficiency and notable financial improvement. The gross profit margin of total revenue was 84.1%, a year-over-year increase of 1.8 percentage points The selling and marketing expenses of product revenue was 48.6%, a year-over-year decrease of 5.9 percentage points The administration and expenses of total revenue was 5.2%, a year-over-year decrease of 4.9 percentage points R&D expenses were RMB1,293.9 million; cash and short-term financial assets were RMB10,112.3 million, or approximately over USD1.4 billion, which enables us to focus on the long-term sustainable development EBITDA loss was RMB160.8 million, a notable year-over-year decrease of 39.9% Strong product revenue growth; preparing for CVM commercialization Product sales revenue reached RMB3 ,811.4 million in the first half of 2024, a strong year-over-year growth of 55.1%. Expansion of commercial portfolio into new approved products, new indications and broader NRDL coverage [1] , [2] and patient access: Eleven approved products: TYVYT®, BYVASDA®, SULINNO®, HALPRYZA®, PEMAZYRE®, Olverembatinib, CYRAMZA®, Retsevmo®, FUCASO® , SINTBILO® and DUPERT® (new product, KRAS G12C inhibitor) . TYVYT® and PEMAZYRE® were newly approved in the Macau market. TYVYT® and BYVASDA® were included in the NRDL for the treatment of EGFR-mutated NSCLC. Solidify oncology leadership; in active preparation for new commercial opportunities in general biomedicine. Oncology: we strengthened our leadership with a robust product portfolio, including TYVYT® (sintilimab injection), and expanded out oncology business with a 10th product, a ROS1 inhibitor, set for approval in the second half of 2024. General biomedicines: Following the approval of the first CVM product SINTBILO® (tafolecimab injection) in 2023, we have successfully submitted three new drug applications (NDA)—two for mazdutide, targeting obesity/overweight population and T2D, and one for IBI311 (IGF-1R) for thyroid eye disease (TED). As a key strategic priority, we are steadily building our commercialization capabilities in the CVM field with systematic approaches, aiming to unlock substantial commercial opportunities and drive sustainable growth. Material innovation delivery supports strategic goals 7 new assets are in NDA review or pivotal registrational clinical trials, and 18 assets are in early-phase clinical studies Substantial milestones delivered for key late-stage assets Encouraging progress in the next wave innovation of "IO+ADC" TYVYT® (sintilimab): submitted an NDA for its eighth indication, 2L endometrial cancer (EMC). New registrational clinical trials for neoadjuvant therapy in colon cancer and perioperative therapy in NSCLC have been initiated. Additionally, we are exploring the potential of combination therapies through multiple collaborations with novel modalities. IBI310 (CTLA-4 )：initiated a Phase 3 clinical trial for IBI310 in combination with sintilimab as neoadjuvant therapy in treating colon cancer. IBI343 (CLDN18.2 ADC)：Phase 1b positive data readout in GC and a Phase 3 trial is in preparation. Accelerating new launch momentum in general biomedicine to unlock significant opportunities Mazdutide (GLP-1R/GCGR) : first NDA for weight management in obese or overweight populations and second NDA for T2D treatment, both under NMPA review. We plan to develop new indications, including adolescent obesity, metabolic dysfunction-associated steatohepatitis (MASH), obstructive sleep apnea (OSA), and heart failure with preserved ejection fraction (HFpEF). Teprotumumab (IGF-1R) : the NDA for TED is under NMPA review. With a longstanding lack of innovative TED treatments in China, Teprotumumab is set to be a transformative therapy for this significant unmet need once approved. Picankibart (IL-23p19) : the only IL-23p19 that reported over 80% subjects achieving ≥90% improvement in Psoriasis and Severity Index (PASI90) in 16 weeks of treatment, along with strong long-term skin clearance maintenance and quarterly dosing interval advantage. We plan to submit an NDA in the second half of 2024. IBI128 (XOI) : potential best-in-class XOI for the treatment of hyperuricemia in gout patients. It is currently undergoing overseas Phase 3 clinical trials overseas with our partner LG Chem, and we have completed patient enrollment for a Phase 2 clinical trial in China. IBI302 (VEGF/C) : Phase 3 study initiated for the treatment of nAMD, following stable and robust visual benefit observed with an extended dosing interval and potential macular atrophy inhibition in two Phase 2 studies. Abundant early-stage pipeline to support long-term growth and global ambition Encouraging data readouts from multiple oncology assets in Phase 1 studies, eyeing most difficult-to-treat cancers IBI363 (PD-1/IL-2 α -bias ) : preliminary positive signals in multiple IO-failed/cold tumor types; further investigations across different rumor types are ongoing; a Phase 2 clinical trial in the U.S. has been initiated. IBI343 (CLDN18.2 ADC) : encouraging positive signal in pancreatic cancer, with FDA fast track designation granted. Plans are underway for a clinical trial in the U.S. IBI389 (CLDN18.2/CD3) : encouraging and differentiated signals in GC and PDAC in Phase 1 studies; Phase 1b study is continuing. Multiple programs ongoing including IBI3003 (GPRC5D/BCMA/CD3), IBI115 (DLL3/CD3); IBI3004 (DR5/CEA); IBI3001 (EGFR/B7H3 ADC), IBI130 (TROP2 ADC), IBI133 (HER3 ADC) Develop next-generation general biomedicine programs to improve chronic disease treatment IBI3016 （ AGT siRNA ） : a new-generation siRNA drug candidate, entered into a Phase 1 clinical trial for hypertension. IBI355 (CD40L), IBI356 (OX40L) and IBI3002 (IL-4R α / TSLP) : innovative autoimmune molecules entered into first-in-human studies to explore other unmet medical needs in various types of autoimmune diseases. IBI324 (VEGF-A/ANG-2) and IBI333 (VEGF-C/VEGF-A) : both are in the Phase 1 stage to explore the potential differentiation clinical values versus existing therapy. Research innovation published in high-impact scientific journals and medical conferences, such as: AACR, ASCO, ESMO GI and ESMO plenary for oncology pipeline innovation, including 10+ oral presentations ADA, APAO, ICE, CSE for general biomedicine pipeline material progress, such as mazdutide and teprotumumab Facilitates and Manufacturing capacity adhering to high-standard quality: Shanghai R&D center (medical) is newly operational in August 2024 First manufacturing site: 60,000L antibody production capacity and ADC production lines in operation Second manufacturing site: first phase of 80,000L completed construction to secure CDMO business Devoted to responsible business practices and enhancing ESG management practices We remain committed to sustainable development, corporate responsibility and ethical business practices. We newly launched our ESG website to enhance our efforts in sustainability, corporate responsibility and ethical business conduct. The new platform highlights our initiatives, policies and performance in key ESG areas, including "Excellent Governance", "Enjoying Good Health", "Ensuring High-Quality Products", "Empowering Employees", and "Embracing Ecology". Innovent is graded 'A' level in MSCI ESG rating, ranking at the forefront of the biotechnology industry. About Innovent Innovent is a leading biopharmaceutical company founded in 2011 with the mission to empower patients worldwide with affordable, high-quality biopharmaceuticals. The company discovers, develops, manufactures and commercializes innovative medicines that treat some of the most intractable diseases. Its pioneering therapies treat cancer, cardiovascular and metabolic, autoimmune and eye diseases. Innovent has 11 products in the market, 3 new drug applications under the NMPA review, 4 assets in Phase III or pivotal clinical trials and 18 more molecules in early clinical stage. Innovent partners with over 30 global healthcare leaders, including Eli Lilly, Roche, Sanofi, Adimab, Incyte and MD Anderson Cancer Center. Guided by the motto, "Start with Integrity, Succeed through Action," Innovent maintains the highest standard of industry practices and works collaboratively to advance the biopharmaceutical industry so that first-rate pharmaceutical drugs can become widely accessible. For more information, visit , or follow Innovent on Facebook and LinkedIn. Statement: Innovent does not recommend the use of any unapproved drug (s)/indication (s). Forward-looking statement This news release may contain certain forward-looking statements that are, by their nature, subject to significant risks and uncertainties. The words "anticipate", "believe", "estimate", "expect", "intend" and similar expressions, as they relate to Innovent Biologics ("Innovent"), are intended to identify certain of such forward-looking statements. The Company does not intend to update these forward-looking statements regularly. These forward-looking statements are based on the existing beliefs, assumptions, expectations, estimates, projections and understandings of the management of the Company with respect to future events at the time these statements are made. These statements are not a guarantee of future developments and are subject to risks, uncertainties and other factors, some of which are beyond the Company's control and are difficult to predict. Consequently, actual results may differ materially from information contained in the forward-looking statements as a result of future changes or developments in our business, the Company's competitive environment and political, economic, legal and social conditions. The Company, the Directors and the employees of the Company assume (a) no obligation to correct or update the forward-looking statements contained in this site; and (b) no liability in the event that any of the forward-looking statements does not materialize or is otherwise inaccurate. SOURCE Innovent Biologics

Phase 1Phase 3Financial StatementPhase 2Fast Track

23 Aug 2024

·www.prnewswire.com

Arthrosi to Present Additional Positive Phase 2 Program Data for AR882 at the 26th Asia-Pacific League of Associations for Rheumatology Congress (APLAR)

—AR882 demonstrated safe and efficacious long-term reduction of serum urate (sUA) levels and elimination of urate crystal deposition in a sub-analysis of gout patients from the Asia-Pacific region— SAN DIEGO, Calif., Aug. 23, 2024 /PRNewswire/ -- Arthrosi Therapeutics, Inc., a late-stage biotechnology company developing a potentially best-in-class, highly potent and selective next generation URAT1 inhibitor to reduce serum urate levels, flares and tophi in patients with gout, today announced additional positive data from a sub-population analysis for its Phase 2 clinical program in gout patients from the Asia-Pacific region. These data are being presented as a poster at the 26th Asia-Pacific League of Associations for Rheumatology Congress, being held August 21-25 in Suntec, Singapore. "We are excited to present new sub-population data from our previously reported positive Phase 2 clinical program for AR882 at APLAR as there remains a significant unmet need for patients suffering from gout worldwide," said Robert T. Keenan, MD, MPH, MBA, Chief Medical Officer at Arthrosi Therapeutics. "The data to be showcased further reinforces AR882's potential to drive robust, durable sUA and tophi reduction, while achieving an improved safety profile compared to existing standard of care to date. Most notably, 83% of patients who received 75mg of AR882 achieved serum urate levels below 5 mg/dL, which is essential for resolving debilitating tophi, crystal burden and flares. We look forward to continuing to evaluate AR882 in our pivotal Phase 3 REDUCE 2 study, initiated in June, and we expect to initiate a second confirmatory Phase 3 study in the second half of this year." Clinical Data for AR882, Arthrosi's URAT1 Inhibitor In a poster presentation, Dr. Keenan will highlight sub-group data from the company's Phase 2 program that demonstrates that long-term administration of AR882 is safe and efficacious in reducing sUA and eliminating urate crystal deposition in 68 gout patients from Australia, New Zealand and Taiwan. 53 of these patients were enrolled in the Phase 2 gout study and randomized equally into three treatment groups to receive once-daily AR882 50 mg, AR882 75 mg, or placebo for 3 months. The other 15 patients were enrolled in the Phase 2b subcutaneous tophi study and received once-daily AR882 75 mg, AR882 50 mg in combination with allopurinol 300 mg for 12 months, or allopurinol 300 mg for 6 months then in combination with AR882 75 mg for 6 months. Serum urate levels were measured at 3, 6 and 12-month visits. In the subcutaneous tophi study, caliper measurements and dual energy computed tomography (DECT) were performed at baseline, months 6 and 12. Safety assessments were collected throughout the study. The data showed: AR882 75 mg and the AR882 50 mg + allopurinol groups demonstrated a substantial and durable decrease in sUA through 3, 6 and 12 months. The pooled mean baseline sUA level was 8.7 mg/dL. At the 3-month visit, median sUA levels were 4.9 and 3.4 mg/dL for AR882 50 mg and AR882 75 mg, respectively, corresponding to a 43.3% and 63.7% reduction. 92% and 83% of the patients achieved sUA < 6 and <5 mg/dL, respectively, when taking AR882 75 mg as a monotherapy. Patients receiving AR882 monotherapy or AR882 in combination with allopurinol showed greater sUA response than allopurinol alone. DECT urate crystal volume was reduced by 50% in the AR882 75 mg group after 6 months of treatment versus 25% in the allopurinol group. AR882 was well tolerated. The most frequently reported adverse event was gout flare, which appeared less often in AR882 groups compared to controls. Details for the poster presentation is as follows: Title: Efficacy of AR882, a Selective Uric Acid Transporter 1 (URAT1) inhibitor in Gout Patients from the Asia-Pacific Region in Two Phase 2 Studies Presenting Author: Robert Keenan, M.D., Chief Medical Officer of Arthrosi Therapeutics Poster Number: 597 Date/Time: Friday, August 23 at 10:45-11:10am and 4:15-4:45pm SGT The poster presentation will be available in the "Publications" section of Arthrosi's website: . About the AR882-202 Phase 2b Study The Phase 2b study was a global, multicenter, 12-week, randomized, double-blind, placebo-controlled study of 140 gout patients who met the gout classification according to the American College of Rheumatology (ACR) and The European Alliance of Associations for Rheumatology (EULAR). The mean baseline serum urate (sUA) among the participants was 8.6 mg/dL. Patients who participated in the study had several major comorbidities, including hypertension (47%), hyperlipidemia (35%), renal insufficiency (34%), arthritis (23%), diabetes (19%), cardiovascular disease (15%), lung disease (11%), and liver disease (5%). In the study, patients received a daily dose of 50 mg AR882, 75 mg AR882, or matching placebo. The sUA levels (< 6, <5, <4, or <3 mg/dL) were evaluated following 12 weeks of dosing, and safety and tolerability were assessed throughout the study. About the AR882-203 Phase 2 Study The Phase 2 study of AR882 in patients with tophaceous gout was a six-month, 1:1:1 randomized, global, placebo-controlled study of 42 patients with subcutaneous tophi. The mean baseline sUA among the participants ranged between 9.1-9.6 mg/dL. In the study, patients received a once daily dose of either 75 mg AR882, 50mg AR882 + allopurinol, or allopurinol up to 300mg. Serum uric acid levels (< 6, <5, <4, or <3 mg/dL) were evaluated monthly through month 6, and safety and tolerability were assessed throughout the study. Tophi measurements with calipers were completed every 4 weeks for 6 months. Patients were also imaged using Dual-Energy Computed Tomography (DECT), DECT a specialized imaging technique that is able to differentiate and identify uric acid crystals in the joints and soft tissue, allowing for quantifying uric acid crystals and tophi at baseline and 6 months. The primary efficacy endpoint was sUA change at 3 months. Secondary endpoints included complete resolution of at least one target tophus with no new tophi and no tophus showing progression. Safety assessments, including vital signs and electrocardiograms, were collected throughout the study. The trial also included a 6-month extension period designed to evaluate longer-term patient outcomes. About Gout: In the U.S., an estimated 13 million individuals are diagnosed with gout. Gout is a form of inflammatory arthritis that can significantly diminish mobility, functionality, and overall quality of life. Gout emerges from the crystallization of uric acid within the joints and soft tissue, instigating painful flare-ups and chronic symptoms. The kidneys play a pivotal role in the process, as they are responsible for filtering out and excreting uric acid from the body. In over 90% of gout patients, underexcretion of uric acid results in the imbalanced and elevated sUA levels that can lead to the deposition of uric acid crystals. It's essential to monitor and manage sUA levels as part of comprehensive gout treatment and prevention strategies. About Arthrosi: Arthrosi Therapeutics, Inc., headquartered in San Diego, CA, is focused on developing AR882, a potentially best-in-class, highly potent and selective next generation URAT1 inhibitor to reduce serum urate levels, flares and tophi in patients with gout. Gout remains a large and growing market with ~ 13M patients in the U.S. alone, ~2M of which have tophaceous gout. AR882 has demonstrated encouraging efficacy and safety compared to SOC in Phase 2 studies as well as impressive results in achieving complete resolution of tophi in a Phase 2b study. Arthrosi is currently advancing AR882 in a pivotal Phase 3 program. Media Contact: Shunqi Yan, PhD Founder & Chief Operating Officer [email protected] Investor Contact: Precision AQ Alex Lobo 212-698-8802 [email protected] SOURCE Arthrosi Therapeutics

Clinical ResultPhase 2

05 Aug 2024

·www.prnewswire.com

Shanton Reaches Full Enrollment in Phase 2b Refractory/Tophaceous Gout Study with SAP-001

SAP-001 is Shanton's lead investigational compound with Best-in-Class potential in uncontrolled gout PRINCETON, N.J., Aug. 5, 2024 /PRNewswire/ -- Shanton Pharma, a clinical-stage biotech company developing a groundbreaking treatment for refractory and tophaceous gout patients, today announced full enrollment of a Phase 2b study for its investigational drug SAP-001. "Reaching full enrollment is an important milestone in our 6-month gout study" Shanton's CEO Dr. Bing Li said, "as this sets the clock for topline data readout in Q1 2025. The study aims to show similar good efficacy and safety results that we saw in our Phase 1 and 2a studies in regular gout patients, but now in the more challenging target population of truly refractory patients that often have a more severe form of gout with limited treatment options. The challenge of this study was to just enroll patients that do not respond to a maximum tolerable dose of conventional Xanthine Oxidase Inhibitors such as allopurinol or febuxostat, which we have now accomplished through full enrollment of the Phase 2b study." About Gout Gout is the most common form of inflammatory arthritis, and the second most prevalent metabolic disease caused by too much uric acid in the bloodstream, with over 10 million adult patients diagnosed in the US alone.1 Hyperuricemia, elevated serum uric acid levels, can over time result in gout when urate crystals are deposited in joints (tophi) and other body tissues, causing inflammatory responses and painful gout attacks (flares). Recurrent gout flares are debilitating and can lead to joint destruction and joint disfigurement. About 29% of diagnosed gout patients in the US are treated with urate lowering therapies (ULTs), but only half of those patients sufficiently respond to or can tolerate current treatment options. It is estimated that up to 20% of US gout patients on standard-of-care allopurinol or febuxostat are physiologically refractory to these treatments, and that up to a third of gout patients develop tophi. 2,3,4 About Shanton's Phase 2b Gout Study Shanton's Phase 2b study is a six-month, multi-center, randomized, double-blind, placebo-controlled, dose-ranging clinical study in refractory gout patients with or without tophi, to evaluate the efficacy and safety of a 10, 30, or 60 mg tablet dose of SAP-001. The study has now reached full enrollment with 87 patients from 21 US sites. The Primary objective is to assess the effectiveness of SAP-001 in lowering serum urate levels in gout patients that are refractory to standard-of-care Xanthine Oxidase Inhibitor (XOI) therapy. Secondary study objectives include safety and tolerability assessments, frequency of gout flares, and change in tophi number, size, and mass. About Shanton Pharma Shanton Pharma is a privately held, clinical-stage biotech founded in 2016 by experienced pharma entrepreneurs, with a research focus on unmet needs associated with hyperuricemia and gout. The company is headquartered in the US with research and development activities in the US, China, and Singapore. SAP-001 is Shanton's lead investigational compound for once-a-day oral urate-lowering therapy that targets refractory and tophaceous gout. SAP-001's urate lowering properties are based on a unique mechanism-of-action and the product has shown unparalleled efficacy and safety in Phase 1 and Phase 2a clinical studies in gout patients with hyperuricemia. Based on its clinical profile and mechanism, SAP-001 has the potential to become the Best-in-Class treatment for refractory and tophaceous gout. To learn more about Shanton Pharma, go to . References Chen-Xu, M., Yokose, C., Rai, S.K., Pillinger, M.H. and Choi, H.K. (2019), Contemporary Prevalence of Gout and Hyperuricemia in the United States and Decadal Trends: The National Health and Nutrition Examination Survey, 2007–2016. Arthritis Rheumatol, 71: 991-999. Juraschek SP, Kovell LC, Miller ER 3rd, Gelber AC. Gout, urate-lowering therapy, and uric acid levels among adults in the United States. Arthritis Care Res (Hoboken). 2015 Apr;67(4):588-92. doi: 10.1002/acr.22469. PMID: 25201123; PMCID: PMC4362996. Clarivate Incidence and Prevalence Data Base. Kasper, I.R., Juriga, M.D., Giurini, J.M., Shmerling, R.H., Treatment of tophaceous gout: When medication is not enough, Seminars in Arthritis and Rheumatism, Volume 45, Issue 6, 2016, 669-674. Media Contact Pieter de Ridder VP of Business Development [email protected] SOURCE Shanton Pharma

Phase 2Clinical ResultPhase 1

100 Deals associated with Allopurinol

External Link

KEGG	Wiki	ATC	Drug Bank
D00224	Allopurinol	M04AA01	DB00437

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Gout	CN	Jiangsu Meitong Pharmaceutical Co. Ltd.	01 Jan 1985
Nephrolithiasis	CN	Jiangsu Meitong Pharmaceutical Co. Ltd.	01 Jan 1985
Hyperuricemia	US	Casper Pharma LLC	19 Aug 1966

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hyperuricemia	Preclinical	US	AstraZeneca PLC	23 Jul 2019
Hyperuricemia	Preclinical	RO	AstraZeneca PLC	23 Jul 2019
Hyperuricemia	Preclinical	IT	AstraZeneca PLC	23 Jul 2019
Hyperuricemia	Preclinical	ZA	AstraZeneca PLC	23 Jul 2019
Hyperuricemia	Preclinical	PL	AstraZeneca PLC	23 Jul 2019
Gout	Preclinical	US	Ardea Biosciences, Inc.	28 Jul 2015
Hand-Foot Syndrome	Preclinical	IT	Advancell Advanced In Vitro Cell Technologies SL	01 Feb 2011
Hand-Foot Syndrome	Discovery	ES	Advancell Advanced In Vitro Cell Technologies SL	01 Feb 2011
Hand-Foot Syndrome	Discovery	DE	Advancell Advanced In Vitro Cell Technologies SL	01 Feb 2011
Hand-Foot Syndrome	Discovery	BE	Advancell Advanced In Vitro Cell Technologies SL	01 Feb 2011

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


UEGW	Not Applicable	Inflammatory Bowel Diseases 6-TGN \| 6-MMP \| FC (fecal calprotectin)	237	Low-dose azathioprine plus allopurinol	(holruwtyzu): OR = 2.46 (95% CI, 1.43 - 4.25), P-Value = 0.001	Positive	13 Oct 2024
				Azathioprine monotherapy
ESC2024	Not Applicable	-	-	Allopurinol + hydration	qqtjkflxwa(yfnnzahybc) = xnajbvtikv blrnhcqcmy (llkygegxvs )	-	31 Aug 2024
				allopurinol (Hydration only)	qqtjkflxwa(yfnnzahybc) = rhcjcfabse blrnhcqcmy (llkygegxvs )
NCT05119686 \| NCT05253833 (AR882-203, PRNewswire) Manual	Phase 2	Gout	-	AR882 50 mg	(dfglwoiwxc) = hgliunpezh wpdeuunydl (umlpxtmmpo ) View more	Positive	23 Aug 2024
				AR882 75 mg	(dfglwoiwxc) = popxgkknwg wpdeuunydl (umlpxtmmpo ) View more
NCT04327024 (AMETHYST, Pubmed \| JAMA Cardiol) Manual	Phase 2	Heart failure with normal ejection fraction	159	Verinurad plus Allopurinol	(uuidrqmczq) = qwximirarx ojmckgqfef (dhmfpcyqwp, -0.56 to 1.10) View more	Negative	14 Aug 2024
				Allopurinol	(uuidrqmczq) = yoipurotqb ojmckgqfef (dhmfpcyqwp, -1.03 to 0.69) View more
NCT05253833 (EULAR2024) Manual	Phase 2	Arthritis, Gouty	42	AR882 75 mg	(tyuxjhsoer) = bvmttmfgdm nhhfdqledk (jhomwvsame ) View more	Positive	12 Jun 2024
				AR882 50 mg + allopurinol	(tyuxjhsoer) = djrxpdiuyb nhhfdqledk (jhomwvsame ) View more
EULAR2024	Not Applicable	fractional excretion of uric acid (FEUA)	1,465	Allopurinol	vhyuhwmjec(synhvyqepz) = aallgluhnc epmcuvkemt (xqeygcttmj ) View more	Positive	05 Jun 2024
				Febuxostat	vhyuhwmjec(synhvyqepz) = zzrbwhougd epmcuvkemt (xqeygcttmj )
ISN WCN2024	Not Applicable	Chronic Kidney Diseases serum uric acid levels ≥6 mg/dl	5,000	Allopurinol 100 mg/day	vttxqknorx(azgzfilvjb) = gohmiwbzkn qvgmketgej (zwlntucgyh ) View more	Positive	01 Apr 2024
ACR2023	Not Applicable	-	-	Allopurinol	nhoqnwexaj(icyahbnrok) = yfjbvtfpcb nnuobigaga (boceculflj )	-	12 Nov 2023
				Allopurinol	nhoqnwexaj(icyahbnrok) = zwzvejarnt nnuobigaga (boceculflj )
AR882-203 (Biospace) Manual	Phase 2	Chronic tophaceous gout	42	AR882 75mg	(mxwhvczsxo) = awwgvioyke nhuyfphtqm (bhfcqqbyuz ) View more	Positive	08 Nov 2023
				AR882 50mg+allopurinol	(mxwhvczsxo) = roandgqqps nhuyfphtqm (bhfcqqbyuz ) View more
ESMO2023	Not Applicable	Neoplasms	715	Rasburicase	mjjejrqmkl(acgwemjiam) = yrvrvoinfv fvhorodcxe (axovhvaqsi ) View more	-	23 Oct 2023
				Allopurinol	mjjejrqmkl(acgwemjiam) = rigtihllsl fvhorodcxe (axovhvaqsi ) View more

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