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Last update 23 Jan 2025

Cabergoline

Last update 23 Jan 2025

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(8R)-6-allyl-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)ergoline-8-carboxamide, (8β)-N-[3-(dimethylamino)propyl]-N-[(ethylamino)carbonyl]-6-(2-propenyl)-ergoline-8-carboxamide, 1-((6-allylergolin-8β-yl)carbonyl)-1-(3-(dimethylamino)propyl)-3-ethylurea

+ [14]

Target

D2 receptor

Mechanism

D2 receptor agonists(Dopamine D2 receptor agonists)

Therapeutic Areas

Nervous System DiseasesEndocrinology and Metabolic DiseaseSkin and Musculoskeletal Diseases+ [1]

Active Indication

Lactation DisordersParkinson DiseaseHyperprolactinemia

Inactive Indication

Restless Legs Syndrome

Originator Organization

Pfizer Inc.

Active Organization

Pfizer Japan, Inc.

Pfizer Inc.Strides Pharma Global Pte Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

AU (21 Apr 1995),

Hyperprolactinemia

Regulation-

Structure/Sequence

Molecular FormulaC26H37N5O2

InChIKeyKORNTPPJEAJQIU-KJXAQDMKSA-N

CAS Registry81409-90-7

Clinical Trials associated with Cabergoline

ChiCTR2400088093

/ SuspendedNot ApplicableIIT

A Non-Interventional Real-World Study on the Use of Cabergoline in the Treatment of Locally Advanced or Metastatic Prostate Cancer

Start Date20 Aug 2024

Sponsor / Collaborator-

CTRI/2024/08/071776

/ Not yet recruitingNot Applicable

To study the efficacy of Cabergoline as an adjunct to Metformin in management of overweight & obese women with PCOS

Start Date17 Aug 2024

Sponsor / Collaborator-

IRCT20240305061171N1

/ CompletedPhase 3IIT

Comparing the effects of cabergoline and hydroxychloroquine to prevent ovarian hyperstimulation syndrome (OHSS) in PCOS patients undergoing infertility treatment.

Start Date03 Apr 2024

Sponsor / Collaborator

Tehran University of Medical Sciences

100 Clinical Results associated with Cabergoline

100 Translational Medicine associated with Cabergoline

100 Patents (Medical) associated with Cabergoline

1,924

Literatures (Medical) associated with Cabergoline

01 Jan 2025·Journal of Clinical Sleep Medicine

Treatment of restless legs syndrome and periodic limb movement disorder: an American Academy of Sleep Medicine clinical practice guideline

Review

Author: Shelgikar, Anita V. ; Kazmi, Uzma ; Sharon, Denise ; Falck-Ytter, Yngve ; Koo, Brian B. ; DelRosso, Lourdes M. ; Trotti, Lynn Marie ; Berkowski, J. Andrew ; Walters, Arthur S. ; Zak, Rochelle S. ; Winkelman, John W. ; Scharf, Matthew T.

INTRODUCTIONThis guideline establishes clinical practice recommendations for treatment of restless legs syndrome (RLS) and periodic limb movement disorder (PLMD) in adults and pediatric patients.METHODSThe American Academy of Sleep Medicine (AASM) commissioned a task force of experts in sleep medicine to develop recommendations and assign strengths based on a systematic review of the literature and an assessment of the evidence using the grading of recommendations assessment, development, and evaluation methodology. The task force provided a summary of the relevant literature and the certainty of evidence, the balance of benefits and harms, patient values and preferences, and resource use considerations that support the recommendations. The AASM Board of Directors approved the final recommendations.GOOD PRACTICE STATEMENTThe following good practice statement is based on expert consensus, and its implementation is necessary for the appropriate and effective management of patients with RLS.1. In all patients with clinically significant RLS, clinicians should regularly test serum iron studies including ferritin and transferrin saturation (calculated from iron and total iron binding capacity). Testing should ideally be administered in the morning avoiding all iron-containing supplements and foods at least 24 hours prior to blood draw. Analysis of iron studies greatly influences the decision to use oral or intravenous (IV) iron treatment. Consensus guidelines, which have not been empirically tested, suggest that supplementation of iron in adults with RLS should be instituted with oral or IV iron if serum ferritin ≤ 75 ng/mL or transferrin saturation < 20%, and only with IV iron if serum ferritin is between 75 and 100 ng/mL. In children, supplementation of iron should be instituted for serum ferritin < 50 ng/mL with oral or IV formulations. These iron supplementation guidelines are different than for the general population.2. The first step in the management of RLS should be addressing exacerbating factors, such as alcohol, caffeine, antihistaminergic, serotonergic, antidopaminergic medications, and untreated obstructive sleep apnea.3. RLS is common in pregnancy; prescribers should consider the pregnancy-specific safety profile of each treatment being considered.RECOMMENDATIONSThe following recommendations are intended as a guide for clinicians in choosing a specific treatment for RLS and PLMD in adults and children. Each recommendation statement is assigned a strength ("strong" or "conditional"). A "strong" recommendation (ie, "We recommend…") is one that clinicians should follow under most circumstances. The recommendations listed below are ranked in the order of strength of recommendations and grouped by class of treatments within each PICO (Patient, Intervention, Comparator, Outcome) question. Some recommendations include remarks that provide additional context to guide clinicians with implementation of this recommendation.ADULTS WITH RLS1. In adults with RLS, the AASM recommends the use of gabapentin enacarbil over no gabapentin enacarbil (strong recommendation, moderate certainty of evidence).2. In adults with RLS, the AASM recommends the use of gabapentin over no gabapentin (strong recommendation, moderate certainty of evidence).3. In adults with RLS, the AASM recommends the use of pregabalin over no pregabalin (strong recommendation, moderate certainty of evidence).4. In adults with RLS, the AASM recommends the use of IV ferric carboxymaltose over no IV ferric carboxymaltose in patients with appropriate iron status (see good practice statement for iron parameters) (strong recommendation, moderate certainty of evidence).5. In adults with RLS, the AASM suggests the use of IV low molecular weight iron dextran over no IV low molecular weight iron dextran in patients with appropriate iron status (see good practice statement for iron parameters) (conditional recommendation, very low certainty of evidence).6. In adults with RLS, the AASM suggests the use of IV ferumoxytol over no IV ferumoxytol in patients with appropriate iron status (see good practice statement for iron parameters) (conditional recommendation, very low certainty of evidence).7. In adults with RLS, the AASM suggests the use of ferrous sulfate over no ferrous sulfate in patients with appropriate iron status (see good practice statement for iron parameters) (conditional recommendation, moderate certainty of evidence).8. In adults with RLS, the AASM suggests the use of dipyridamole over no dipyridamole (conditional recommendation, low certainty of evidence).9. In adults with RLS, the AASM suggests the use of extended-release oxycodone and other opioids over no opioids (conditional recommendation, moderate certainty of evidence).10. In adults with RLS, the AASM suggests the use of bilateral high-frequency peroneal nerve stimulation over no peroneal nerve stimulation (conditional recommendation, moderate certainty of evidence).11. In adults with RLS, the AASM suggests against the standard use of levodopa (conditional recommendation, very low certainty of evidence).Remarks: levodopa may be used to treat RLS in patients who place a higher value on the reduction of restless legs symptoms with short-term use and a lower value on adverse effects with long-term use (particularly augmentation).12. In adults with RLS, the AASM suggests against the standard use of pramipexole (conditional recommendation, moderate certainty of evidence).Remarks: pramipexole may be used to treat RLS in patients who place a higher value on the reduction of restless legs symptoms with short-term use and a lower value on adverse effects with long-term use (particularly augmentation).13. In adults with RLS, the AASM suggests against the standard use of transdermal rotigotine (conditional recommendation, low certainty of evidence).Remarks: transdermal rotigotine may be used to treat RLS in patients who place a higher value on the reduction of restless legs symptoms with short-term use and a lower value on adverse effects with long-term use (particularly augmentation).14. In adults with RLS, the AASM suggests against the standard use of ropinirole (conditional recommendation, moderate certainty of evidence).Remarks: ropinirole may be used to treat RLS in patients who place a higher value on the reduction of restless legs symptoms with short-term use and a lower value on adverse effects with long-term use (particularly augmentation).15. In adults with RLS, the AASM suggests against the use of bupropion for the treatment of RLS (conditional recommendation, moderate certainty of evidence).16. In adults with RLS, the AASM suggests against the use of carbamazepine (conditional recommendation, low certainty of evidence).17. In adults with RLS, the AASM suggests against the use of clonazepam (conditional recommendation, very low certainty of evidence).18. In adults with RLS, the AASM suggests against the use of valerian (conditional recommendation, very low certainty of evidence).19. In adults with RLS, the AASM suggests against the use of valproic acid (conditional recommendation, low certainty of evidence).20. In adults with RLS, the AASM recommends against the use of cabergoline (strong recommendation, moderate certainty of evidence).SPECIAL ADULT POPULATIONS WITH RLS21. In adults with RLS and end-stage renal disease (ESRD), the AASM suggests the use of gabapentin over no gabapentin (conditional recommendation, very low certainty of evidence).22. In adults with RLS and ESRD, the AASM suggests the use of IV iron sucrose over no IV iron sucrose in patients with ferritin < 200 ng/mL and transferrin saturation < 20% (conditional recommendation, moderate certainty of evidence).23. In adults with RLS and ESRD, the AASM suggests the use of vitamin C over no vitamin C (conditional recommendation, low certainty of evidence).24. In adults with RLS and ESRD, the AASM suggests against the standard use of levodopa (conditional recommendation, low certainty of evidence).Remarks: levodopa may be used to treat RLS in patients who place a higher value on the reduction of restless legs symptoms with short-term use and a lower value on adverse effects with long-term use (particularly augmentation).25. In adults with RLS and ESRD, the AASM suggests against the standard use of rotigotine (conditional recommendation, very low certainty of evidence).Remarks: rotigotine may be used to treat RLS in patients who place a higher value on the reduction of restless legs symptoms with short-term use and a lower value on adverse effects with long-term use (particularly augmentation).ADULTS WITH PLMD26. In adults with PLMD, the AASM suggests against the use of triazolam (conditional recommendation, very low certainty of evidence).27. In adults with PLMD, the AASM suggests against the use of valproic acid (conditional recommendation, very low certainty of evidence).CHILDREN WITH RLS28. In children with RLS, the AASM suggests the use of ferrous sulfate over no ferrous sulfate in patients with appropriate iron status (see good practice statement for iron parameters) (conditional recommendation, very low certainty of evidence).CITATIONWinkelman JW, Berkowski JA, DelRosso LM, et al. Treatment of restless legs syndrome and periodic limb movement disorder: an American Academy of Sleep Medicine clinical practice guideline. J Clin Sleep Med. 2025;21(1):137-152.

31 Dec 2024·Gynecological Endocrinology

Expression of Concern: Laparoscopic ovarian drilling versus GnRH antagonist combined with cabergoline as a prophylaxis against the re-development of ovarian hyperstimulation syndrome

Article

22 Dec 2024·Neuro endocrinology letters

Analysis of oxytocin and oxytocin receptor expressions after hand therapy treatment in a mouse model of chemotherapy-induced peripheral neuropathy .

Article

Author: Shinouchi, Ryosuke ; Nobe, Koji ; Kiuchi, Yuji ; Sasaki, Akiko

OBJECTIVESTriple negative breast cancer (TNBC) is a distinct subtype of breast cancer that has a poor prognosis due to the lack of effective therapeutic agents. Since a significant proportion of human surgical samples of TNBC expressed mRNA for the growth hormone (GH), growth hormone-releasing hormone (GHRH), and gonadotropin-releasing hormone (GnRH) receptors, and the mitogenic proliferative activity of GH, GHRH, and GnRH, have been identified as effective therapeutic targets for somatostatin and its analogs and GnRH analogs, Di Bella Method (DBM), a combination of hormonal analogs and vitamins, was introduced to target and inhibit solid tumors. The present study aimed to improve the prognosis of TNBC using DBM in women with TNBC.METHODSThis retrospective observational clinical study was done on women with TNBC who were diagnosed based on histology, nuclear grade, and immunohistochemical testing for estrogen receptor, HER2/neu, and progesterone receptor. Patients were either treated with standard oncology protocol, including chemotherapy and radiotherapy plus DBM, or with DBM alone. The DBM included a daily combination of somatostatin, octreotide, melatonin, retinoids solubilized in alpha tocopheryl acetate, dopaminergic agonists, bromocriptine, cabergoline, aromatase inhibitors for anti-estrogen function, and low metronomic doses of cyclophosphamide.RESULTSIn this study, 35 patients were enrolled, and their survival was monitored for 5 years during which they received DBM and standard chemotherapy/radiotherapy protocol. These patients had a survival rate of 64% at 5 years, 76% at 3 years, 87% at 2 years, and 100% after 1 year of therapy. On the other hand, 13 patients who received only DBM had a survival rate of 60% at 5 years, 67% at 3 years, 75% at 2 years and 100% after 1 year of therapy. None of the patients had significant adverse events.CONCLUSIONSCompared to published clinical trials, the DBM improved the prognosis of women with TNBC. However, more standardized clinical trials, including DBM with and without standard therapeutic protocols for TNBC, are warranted.

News (Medical) associated with Cabergoline

02 Dec 2024

·www.drugs.com

Guidelines Developed for Treatment of Restless Legs Syndrome

MONDAY, Dec. 2, 2024 -- In a clinical practice guideline issued by the American Academy of Sleep Medicine and published online Sept. 26 in the Journal of Clinical Sleep Medicine , recommendations are presented for the treatment of restless legs syndrome (RLS). John W. Winkelman, M.D., Ph.D., from Massachusetts General Hospital in Boston, and colleagues developed recommendations for treatment of RLS and periodic limb movement disorder in adults and pediatric patients. The researchers developed three good practice statements that were based on expert consensus. They recommend all clinicians should regularly test serum iron studies, including ferritin and transferrin saturation, in all patients with clinically significant RLS, ideally in the morning; analysis of these studies influences the decision to use oral or intravenous (IV) iron treatment. The authors also state that addressing exacerbating factors, including alcohol, caffeine, antihistaminergic, serotonergic, and anti-dopaminergic medications, should be the first step in RLS management. They note RLS is common in pregnancy and the pregnancy-specific safety profile of each treatment should be considered. Recommendations for adults with RLS include use of gabapentin enacarbil over no gabapentin enacarbil; use of gabapentin over no gabapentin; use of pregabalin over no pregabalin; and use of IV ferric carboxymaltose over no IV ferric carboxymaltose for those with appropriate iron status (strong recommendations; moderate certainty of evidence). In addition, there is a strong recommendation against use of cabergoline. "Guided by the best evidence in the scientific literature, we've provided recommendations that will improve the ability of clinicians to provide patient-centered care for people who have RLS," Winkelman said in a statement. One author disclosed ties to the pharmaceutical and medical device industries. Abstract/Full Text Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

20 May 2021

·www.globenewswire.com

Chiasma to Present Encore and New Data from MPOWERED™ Phase 3 Trial at Upcoming e-ECE and AACE Virtual Conferences

-- New clinical data accepted for oral and e-Poster presentation at AACE -- -- e-ECE clinical data previously presented at Endocrine Society’s 2021 annual meeting -- NEEDHAM, Mass., May 20, 2021 (GLOBE NEWSWIRE) -- Chiasma, Inc. (NASDAQ: CHMA), (“Chiasma” or the “Company”), a commercial-stage biopharmaceutical company utilizing its delivery platform technology to develop and commercialize oral therapies to improve the lives of patients with rare diseases currently treated with burdensome and painful injections, today announced that it will virtually present encore data from its MPOWERED™ Phase 3 clinical trial at the 23rd European Congress of Endocrinology (e-ECE) (May 22-26, 2021) and new data from the MPOWERED trial at the 30th Annual American Association of Clinical Endocrinology (AACE) Meeting (May 26-29, 2021). Oral presentations and posters for display are summarized below: e-ECE 2021 Oral PresentationTitle: A Phase 3 Large International Noninferiority Trial (MPOWERED): Assessing Maintenance of Response to Oral Octreotide Capsules in Comparison to Injectable Somatostatin Receptor LigandsPresenter: Maria Fleseriu, M.D., FACE, Professor, Medicine and Neurological Surgery, Director OHSU Northwest Pituitary CenterSession Date/Time: Wednesday, May 26, 2021, 8:30 a.m. – 9:30 a.m. EDT e-ECE 2021 e-Poster PresentationsTitle: Safety Results from MPOWERED, a Phase 3 Trial of Oral Octreotide Capsules in Adults with AcromegalyPresenter: Pamela Freda, M.D., Columbia University Session Date/Time: Monday, May 24, 2021, 8:00 a.m. – 8:30 a.m. EDT Title: Oral Octreotide Capsules Lowered Incidence and Improved Severity of Acromegaly Symptoms Compared to Injectable Somatostatin Receptor Ligands—Results from the MPOWERED TrialPresenter: Nienke Biermasz, M.D., Ph.D., Leiden University Medical Center Session Date/Time: Tuesday, May 25, 2021, 8:00 a.m. – 8:30 a.m. EDT Title: Addition of Cabergoline to Oral Octreotide Capsules May Improve Biochemical Control in Patients with Acromegaly Who Are Inadequately Controlled with MonotherapyPresenter: Maria Fleseriu, M.D., FACE, Professor, Medicine and Neurological Surgery, Director OHSU Northwest Pituitary CenterSession Date/Time: Tuesday, May 25, 2021, 8:00 a.m. – 8:30 a.m. EDT Title: Improved Acromegaly Patient Satisfaction with Oral Octreotide Capsules Compared with Injectable Somatostatin Receptor Ligands in the MPOWERED TrialPresenter: Murray B. Gordon, M.D., Allegheny General HospitalSession Date/Time: Wednesday, May 26, 2021, 8:00 a.m. – 8:30 a.m. EDT AACE 2021 Oral PresentationTitle: Improved Quality of Life and Work Productivity in Patients with Acromegaly Receiving Oral Octreotide Capsules in the Phase 3 MPOWERED TrialPresenter: Nienke Biermasz, M.D., Ph.D., Leiden University Medical CenterSession Date/Time: Thursday, May 27, 2021, 1:30 p.m. – 1:45 p.m. EDT AACE 2021 Late-Breaker e-Posters - Available online via the virtual e-Poster Gallery beginning May 26Title: Effects of Prior Injectable Somatostatin Receptor Ligand Type and Dose in Patients with Acromegaly Receiving Oral Octreotide Capsules in the Phase 3 MPOWERED TrialLead Author: Murray B. Gordon, M.D., Allegheny General Hospital Title: Injection Site Reactions and Their Impact in Patients with Acromegaly Receiving Injectable Somatostatin Receptor Ligands in the Phase 3 MPOWERED TrialLead Author: Murray B. Gordon, M.D., Allegheny General Hospital To register and view the full schedules as well as abstracts, visit e-ECE’s website here and AACE’s website here. Chiasma will sponsor a product theatre presentation at the AACE annual meeting titled “Understanding the Management of Acromegaly with MYCAPSSA® (octreotide) Delayed-Release Oral Capsules” on Wednesday, May 26 at 2:45 p.m. EDT. Anthony P. Heaney, M.D., Ph.D., Professor, UCLA, will lead the presentation and a live Q&A session. About the MPOWERED™ Trial The MPOWERED trial was a global, non-inferiority, randomized, open-label and active-controlled, 15-month trial intended to support approval of MYCAPSSA in the European Union. Chiasma completed enrollment of 146 adult acromegaly patients into the trial in June 2019, of which 92 patients were deemed responders to octreotide capsules per the protocol following a six-month run-in were randomized to either octreotide capsules (n=55) or injectable somatostatin receptor ligands (octreotide LAR or lanreotide autogel) (n=37), and then followed for an additional nine months. The trial was designed to evaluate the proportion of patients who maintain their biochemical response to octreotide capsules and patient-reported outcomes in patients treated with octreotide capsules, compared to patients treated with leading injectable somatostatin analogs. About MYCAPSSA INDICATION AND IMPORTANT SAFETY INFORMATION INDICATION AND USAGE MYCAPSSA (octreotide) delayed-release capsules, for oral use, is a somatostatin analog indicated for long-term maintenance treatment in acromegaly patients who have responded to and tolerated treatment with octreotide or lanreotide. CONTRAINDICATIONS Hypersensitivity to octreotide or any of the components of MYCAPSSA. Anaphylactoid reactions, including anaphylactic shock, have been reported in patients receiving octreotide. IMPORTANT SAFETY INFORMATION WARNINGS AND PRECAUTIONS MYCAPSSA can cause problems with the gallbladder. Monitor patients periodically. Discontinue if complications of cholelithiasis are suspected. Blood sugar, thyroid levels, and vitamin B12 levels should be monitored and treated accordingly. Bradycardia, arrhythmia, or conduction abnormalities may occur. Treatment with drugs that have bradycardia effects may need to be adjusted. ADVERSE REACTIONS The most common adverse reactions (incidence >10%) are nausea, diarrhea, headache, arthralgia, asthenia, hyperhidrosis, peripheral swelling, blood glucose increased, vomiting, abdominal discomfort, dyspepsia, sinusitis, and osteoarthritis. DRUG INTERACTIONS The following drugs require monitoring and possible dose adjustment when used with MYCAPSSA: cyclosporine, insulin, antidiabetic drugs, calcium channel blockers, beta blockers, lisinopril, digoxin, bromocriptine, and drugs mainly metabolized by CYP3A4. Counsel women to use an alternative non-hormonal method of contraception or a back-up method when MYCAPSSA is used with combined oral contraceptives. Patients taking proton pump inhibitors, H2-receptor antagonists, or antacids concomitantly with MYCAPSSA may require increased dosages of MYCAPSSA. PREGNANCY Advise premenopausal females of the potential for an unintended pregnancy. To report SUSPECTED ADVERSE REACTIONS, contact the product information department at 1-844-312-2462 or FDA at 1-800-FDA-1088 or The full Prescribing Information for MYCAPSSA is available at . About Acromegaly Acromegaly typically develops when a benign tumor of the pituitary gland produces too much growth hormone, ultimately leading to significant health problems. Common features of acromegaly are facial changes, intense headaches, joint pain, impaired vision and enlargement of the hands, feet, tongue and internal organs. Serious health conditions associated with the progression of acromegaly include type 2 diabetes, hypertension, respiratory disorders and cardiac and cerebrovascular disease. Chiasma estimates that approximately 8,000 adult acromegaly patients are chronically treated with somatostatin analog injections in the United States. About Chiasma Chiasma is a commercial-stage biopharmaceutical company focused on developing and commercializing oral therapies to improve the lives of patients who face challenges associated with their existing treatments for rare and serious chronic diseases. Employing its Transient Permeability Enhancer (TPE®) technology platform, Chiasma seeks to develop oral medications that are currently available only as injections. In June 2020, Chiasma received FDA approval of MYCAPSSA for long-term maintenance therapy in acromegaly patients who have responded to and tolerated treatment with octreotide or lanreotide. MYCAPSSA, the first and only oral somatostatin analog approved by the FDA, is available for commercial sale. Chiasma is headquartered in Needham, MA with a wholly owned subsidiary in Israel. MYCAPSSA, TPE and CHIASMA are registered trademarks of Chiasma. For more information, please visit the company’s website at . Forward-Looking Statements This release contains “forward-looking statements” within the meaning of the Private Securities Litigation Reform Act of 1995, including, but not limited to, statements regarding the data from the MPOWERED trial and the therapeutic potential of MYCAPSSA. Such statements are subject to numerous important factors, risks and uncertainties, many of which are beyond the company’s control, that may cause actual events or results to differ materially from the company’s current expectations. Management’s expectations and, therefore, any forward-looking statements in this press release could be affected by risks and uncertainties. For a discussion of these and other risks and uncertainties, and other important factors, any of which could cause the company’s actual results to differ from those contained in the forward-looking statements, see the section entitled “Risk Factors” in Chiasma’s Quarterly Report on Form 10-Q for the quarter ended March 31, 2021, and in subsequent filings with the Securities and Exchange Commission. All information in this press release is as of the date of the release, and Chiasma undertakes no duty to update this information unless required by law. Investor Relations and Corporate Communications:Ashley RobinsonLifeSci Advisors, LLC617-430-7577arr@lifesciadvisors.com Media Relations:Patrick BurseyLifeSci Communications646-876-4932pbursey@lifescicomms.com

20 Mar 2021

·www.globenewswire.com

Chiasma Presents New Positive Data for MYCAPSSA from Phase 3 Trial MPOWERED™ for the Maintenance Treatment of Acromegaly at ENDO 2021

--Data supports MYCAPSSA® as non-inferior to long-acting injectable somatostatin receptor ligands (iSRLs)-- --Data demonstrated patients taking MYCAPSSA had significant improvement in acromegaly related symptoms and patient reported outcomes after switching from iSRLs-- NEEDHAM, Mass., March 20, 2021 (GLOBE NEWSWIRE) -- Chiasma, Inc. (NASDAQ: CHMA), (“Chiasma” or the “Company”), a commercial-stage biopharmaceutical company utilizing its delivery platform technology to develop and commercialize oral therapies to improve the lives of patients with rare diseases currently treated with burdensome and painful injections, as evidenced by its recent phased launch of MYCAPSSA® as the first oral therapy for the treatment of acromegaly, today announced the presentation of new positive clinical data from its MPOWERED™ Phase 3 trial of MYCAPSSA at the Endocrine Society’s annual meeting, ENDO 2021, being held virtually March 20-23, 2021. The data from MPOWERED showed that MYCAPSSA improved clinical symptoms and other patient-reported outcomes compared to long-acting injectable somatostatin receptor ligands (iSRLs) in patients with acromegaly. In addition, MYCAPSSA met the pre-specified non-inferiority margin compared to long-acting iSRLs in maintenance of biochemical response. “The new encouraging data from all five late-breaking poster presentations further expand our understanding of oral octreotide capsules’ potential positive impact for patients with acromegaly who would otherwise need monthly, frequently burdensome SRLs injections,” said Maria Fleseriu, M.D., FACE, lead investigator of the MPOWERED study, Professor of Medicine and Neurological Surgery, Director of the Pituitary Center at Oregon Health and Science University in Portland, Oregon, and Immediate Past President of the Pituitary Society. “As a practicing endocrinologist, I believe that these data provide valuable insights to physicians on the potential benefit of a twice daily oral drug versus long-acting injections for most patients.” Raj Kannan, Chief Executive Officer of Chiasma, added, “We are pleased to characterize further the MYCAPSSA product profile with the positive results from Chiasma’s MPOWERED study at ENDO 2021 for the medical community. This is the first head-to-head large, non-inferiority Phase 3 trial in acromegaly that has been done to assess safety and efficacy, including the effect on acromegaly symptoms, and on patient satisfaction. Based on these data, we remain focused on submitting a marketing authorization application for MYCAPSSA to the European Medicines Agency planned for mid-2021.” Data highlights from the five late-breaking poster presentations are outlined below: A Phase 3 Large International Noninferiority Trial (MPOWERED): Assessing Maintenance of Response to Oral Octreotide Capsules In Comparison to Injectable Somatostatin Receptor Ligands Data showed that MYCAPSSA demonstrated non-inferiority to iSRLs in maintaining biochemical response, 91% (CI, 80%-97%) of the MYCAPSSA patients maintained insulin-like growth factor 1 (IGF-1) response during the randomized controlled treatment (RCT) phase. MYCAPSSA demonstrated stable IGF-1 levels during the RCT phase comparable to iSRLs, supporting efficacy of MYCAPSSA. Oral Octreotide Capsules Lowered Incidence and Improved Severity of Acromegaly Symptoms Compared to Injectable Somatostatin Receptor Ligands—Results from the MPOWERED Trial A statistically significant (p = 0.001) reduction from baseline (time of first dose of MYCAPSSA in run-in) was noted in the number of active acromegaly symptoms. Reduction in the number of active symptoms by individual symptom was statistically significant for swelling of extremities (p = 0.01) and fatigue (p = 0.03). The overall mean symptom score decreased from 4.5 to 3.5; the mean change from baseline was statistically significant (p < 0.001) and clinically meaningful (> 1 point reduction is equal to a shift of 1 symptom from severe to moderate, or moderate to mild or resolution of 1 symptom). Overall, 80.4% of the randomized patients maintained or improved their symptoms score during the run-in phase compared to baseline. We believe these findings validate previous results from the open-label, Phase 3 CH-ACM-01 study of MYCAPSSA in which patients switching to MYCAPSSA from iSRLs reported significant reduction in joint pain, extremity swelling and fatigue. Improved Acromegaly Patient Satisfaction with Oral Octreotide Capsules Compared with Injectable Somatostatin Receptor Ligands in The MPOWERED Trial For the 92 patients randomized, 3 of 5 domains (emotional reaction, treatment convenience, and treatment satisfaction) of the Acromegaly Treatment Satisfaction Questionnaire (Acro-TSQ) showed significant improvement at the end of the run-in (n=37) phase (reflecting outcomes on MYCAPSSA) as compared to baseline (reflecting outcomes on iSRLs). Improvements not reaching statistical significance were also noted for symptom interference and GI interference. Patients receiving MYCAPSSA demonstrated a significant improvement in the Acro-TSQ domain of treatment convenience over the RCT phase in comparison to those receiving iSRLs (p = 0.04). At the end of the RCT phase, breakthrough acromegaly symptoms were reported by 15% of patients in octreotide capsules group and 31% of patients in the iSRLs group. Of note, 47% of patients receiving SRL injections during the RCT phase reported injection site reactions via the Acro-TSQ. 81% of these patients reported that iSLRs interfered with their daily activities. Addition of Cabergoline to Oral Octreotide Capsules May Improve Biochemical Control in Patients with Acromegaly Who Are Inadequately Controlled with Monotherapy IGF-1 levels improved in most patients over the 36-week study (n=12; 85.7%). Of nine patients with IGF-1 ≥1.3 × ULN at sub-study start, five patients (55.6%; 95% CI, 21.2% -86.3%) exhibited decreases to predefined responder range (<1.3 × ULN) by week 36. Adverse event incidence and nature were similar to the known octreotide safety profile and acromegaly disease burden. For the first time, a study demonstrated the potential benefit of an all-oral combination treatment for acromegaly with avoidance of injection-related burdens. Safety Results From MPOWERED, A Phase 3 Trial of Oral Octreotide Capsules in Adults with Acromegaly No new or unexpected safety signals were identified during the trial. 39 patients (70.9%) in the MYCAPSSA group and 26 (70.3%) in the iSRL group had ≥1 treatment-emergent adverse events (TEAE). Gastrointestinal AEs were the most common TEAEs within both groups. Safety results were similar between both groups, but the MYCAPSSA group did not have injection site reactions, whereas 24.3% of patients reported injection site reactions as TEAEs from the iSRL group during the RCT phase. About the CHIASMA MPOWERED™ Trial The MPOWERED™ trial was a global, randomized, open-label and active-controlled, 15-month trial intended to support approval of MYCPASSA® (oral octreotide capsules) in the European Union. This non-inferiority clinical trial was designed to compare MYCAPSSA to long-acting injectable somatostatin analogs (SSAs) for maintenance of biochemical response in patients with acromegaly. The trial enrolled 146 adult acromegaly patients of which 92 patients who were responders to MYCAPSSA after a six-month run-in phase were randomized to a nine-month controlled phase with continued treatment on MYCAPSSA or on their prior injectable therapy. Patients were randomized to either MYCAPSSA (n=55) or injectable somatostatin receptor ligands (octreotide long-acting release or lanreotide autogel) (n=37), and then followed for an additional nine months. The primary endpoint of the trial was time-weighted average of IGF-1 <1.3 x upper limit of normal (ULN) during the nine-month randomized, controlled treatment (RCT) phase. As previously announced, MPOWERED met its primary endpoint of non-inferiority compared to long acting SSA injectables. About MYCAPSSA INDICATION AND IMPORTANT SAFETY INFORMATION INDICATION AND USAGE MYCAPSSA (octreotide) delayed-release capsules, for oral use, is a somatostatin analog indicated for long-term maintenance treatment in acromegaly patients who have responded to and tolerated treatment with octreotide or lanreotide. CONTRAINDICATIONS Hypersensitivity to octreotide or any of the components of MYCAPSSA. Anaphylactoid reactions, including anaphylactic shock, have been reported in patients receiving octreotide. IMPORTANT SAFETY INFORMATION WARNINGS AND PRECAUTIONS MYCAPSSA can cause problems with the gallbladder. Monitor patients periodically. Discontinue if complications of cholelithiasis are suspected. Blood sugar, thyroid levels, and vitamin B 12 levels should be monitored and treated accordingly. Bradycardia, arrhythmia, or conduction abnormalities may occur. Treatment with drugs that have bradycardia effects may need to be adjusted. ADVERSE REACTIONS The most common adverse reactions (incidence >10%) are nausea, diarrhea, headache, arthralgia, asthenia, hyperhidrosis, peripheral swelling, blood glucose increased, vomiting, abdominal discomfort, dyspepsia, sinusitis, and osteoarthritis. DRUG INTERACTIONS The following drugs require monitoring and possible dose adjustment when used with MYCAPSSA: cyclosporine, insulin, antidiabetic drugs, calcium channel blockers, beta blockers, lisinopril, digoxin, bromocriptine, and drugs mainly metabolized by CYP3A4. Counsel women to use an alternative non-hormonal method of contraception or a back-up method when MYCAPSSA is used with combined oral contraceptives. Patients taking proton pump inhibitors, H2-receptor antagonists, or antacids concomitantly with MYCAPSSA may require increased dosages of MYCAPSSA. PREGNANCY Advise premenopausal females of the potential for an unintended pregnancy. To report SUSPECTED ADVERSE REACTIONS, contact the product information department at 1-844-312-2462 or FDA at 1-800-FDA-1088 or The full Prescribing Information for MYCAPSSA is available at . About Acromegaly Acromegaly typically develops when a benign tumor of the pituitary gland produces too much growth hormone, ultimately leading to significant health problems. Common features of acromegaly are facial changes, intense headaches, joint pain, impaired vision and enlargement of the hands, feet, tongue and internal organs. Serious health conditions associated with the progression of acromegaly include type 2 diabetes, hypertension, respiratory disorders, and cardiac and cerebrovascular disease. Chiasma estimates that approximately 8,000 adult acromegaly patients are chronically treated with somatostatin analog injections in the United States. About Chiasma Chiasma is a commercial-stage biopharmaceutical company focused on developing and commercializing oral therapies to improve the lives of patients who face challenges associated with their existing treatments for rare and serious chronic diseases. Employing its Transient Permeability Enhancer (TPE®) technology platform, Chiasma seeks to develop oral medications that are currently available only as injections. In June 2020, Chiasma received FDA approval of MYCAPSSA for long-term maintenance therapy in acromegaly patients who have responded to and tolerated treatment with octreotide or lanreotide. MYCAPSSA, the first and only oral somatostatin analog approved by the FDA, is available for commercial sale. Chiasma is headquartered in Needham, MA with a wholly owned subsidiary in Israel. MYCAPSSA, TPE and CHIASMA are registered trademarks of Chiasma. For more information, please visit the company’s website at . Forward-Looking Statements This release contains “forward-looking statements” within the meaning of the Private Securities Litigation Reform Act of 1995, including, but not limited to, statements regarding the data from the MPOWERED trial and whether the data will support the submission of a marketing authorization application (MAA) to the European Medicines Agency (EMA) for MYCAPSSA in the European Union and ultimately regulatory approval, statements regarding the timing of an MAA submission and regulatory review, statements regarding the company’s expectations relating to MYCAPSSA for the long-term maintenance therapy in acromegaly patients who have responded to and tolerated treatment with octreotide or lanreotide, and statements concerning the therapeutic potential of MYCAPSSA, including its ability to become a standard of care. Such statements are subject to numerous important factors, risks and uncertainties, many of which are beyond the company’s control, that may cause actual events or results to differ materially from the company’s current expectations. Management’s expectations and, therefore, any forward-looking statements in this press release could be affected by risks and uncertainties relating to a number of factors, including the following: the content and timing of decisions made by the EMA, the sufficiency of the data collected from the company’s clinical trials to obtain regulatory approval in the European Union or elsewhere, and the impact the ongoing COVID-19 pandemic may have on the company’s business, including its expected development, manufacturing, regulatory and commercialization timelines for MYCAPSSA. For a discussion of these and other risks and uncertainties, and other important factors, any of which could cause the company’s actual results to differ from those contained in the forward-looking statements, see the section entitled “Risk Factors” in Chiasma’s Annual Report on Form 10-K for the year ended December 31, 2020, and in subsequent filings with the Securities and Exchange Commission. All information in this press release is as of the date of the release, and Chiasma undertakes no duty to update this information unless required by law. Investor Relations and Corporate Communications: Ashley Robinson LifeSci Advisors, LLC 617-430-7577 arr@lifesciadvisors.com Media Relations: Patrick Bursey LifeSci Communications 646-876-4932 pbursey@lifescicomms.com

100 Deals associated with Cabergoline

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KEGG	Wiki	ATC	Drug Bank
D00987	Cabergoline	N04BC06 G02CB03	DB00248

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Indication	Country/Location	Organization	Date
Lactation Disorders	JP	Pfizer Japan, Inc.	16 Apr 2003
Parkinson Disease	JP	Pfizer Japan, Inc.	16 Jun 1999
Hyperprolactinemia	AU	Pfizer Inc.	21 Apr 1995

Developing

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Indication	Highest Phase	Country/Location	Organization	Date
Restless Legs Syndrome	Discovery	-	Pfizer Inc.	01 Nov 2002

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01794793 (B2412, CTgov)	Phase 4	Pituitary ACTH Hypersecretion \| Dumping Syndrome \| Pituitary Neoplasms \| Acromegaly \| Melanoma \| Prostatic Cancer \| Ectopic ACTH Syndrome	337	Cabergoline+Pasireotide (Pasireotide Subcutaneous)	quznkkzjvk(dpmzxscvjj) = osylyeyscr ujwsghaeew (ntbftlgxns, plsrwwgqor - ljfzlevyuo) View more	-	28 Aug 2024
				Pasireotide LAR (Pasireotide Long Acting Release (LAR))	quznkkzjvk(dpmzxscvjj) = zdyyqpmcyu ujwsghaeew (ntbftlgxns, ayawnyyfxl - bfvijgdavk) View more
ENDO2024	Not Applicable	-	-	Cabergoline 0.5 mg	khjtrtwvqe(sdrtvttujl) = cmbxhldudj ehbixrqjzc (hdhpbfklmy, 7.2 - 63.3) View more	-	01 Jun 2024
NCT05024422 (Pubmed \| Am J Obstet Gynecol)	Phase 3	Breast Feeding	-	Cabergoline	tublyosnom(ddqomaonck) = dipgjitsuo aaywyochtg (slcaijlovn ) View more	Positive	01 May 2024
				Pyridoxine	tublyosnom(ddqomaonck) = wuncarhcqw aaywyochtg (slcaijlovn ) View more
FRI248 (ENDO2023)	Not Applicable	Pituitary ACTH Hypersecretion	1	Desmopressin	(vjquktxjak) = xyysrfdqcu lviuqzdoch (flkhibxttj ) View more	-	05 Oct 2023
				Cabergoline	(vjquktxjak) = cewkispvip lviuqzdoch (flkhibxttj ) View more
FRI323 (ENDO2023)	Not Applicable	Prolactinoma testosterone \| estradiol \| PRL	-	Cabergoline	vhbitkwtjg(lgjhqthkkt) = dbetqkknau uznwvhybfx (lbmaezqlnk )	-	05 Oct 2023
				Testosterone cypionate 60 mg weekly	vhbitkwtjg(lgjhqthkkt) = mqxjxsbknw uznwvhybfx (lbmaezqlnk )
FRI474 (ENDO2023)	Not Applicable	Combined Pituitary Hormone Deficiency \| Hypothyroidism	-	Levothyroxine	pagndvkviu(rogfqaitki) = significantly improved after initiating the hormone replacement with levothyroxine and a stress hydrocortisone dose, gradually tapered to a physiological dose, and cabergoline fhzinoqych (uuymlsfcue )	-	05 Oct 2023
				Stress hydrocortisone
NCT01794793 (B2412, ENDO2023)	Phase 4	-	341	Pasireotide LAR	pmfxmhasyh(elwjprmiqj) = hpromlfprg eruugnazkj (upwohgvbsi )	Positive	05 Oct 2023
				Pasireotide sc	pmfxmhasyh(elwjprmiqj) = tjxvmwowxm eruugnazkj (upwohgvbsi )
THU028 (ENDO2023)	Not Applicable	Acromegaly	2	Oral Octreotide	oidaarzkcj(pqaytbtdfu) = xcelleeazc qspxfwwuuy (zpsgnregny ) View more	Positive	05 Oct 2023
				Cabergoline	oidaarzkcj(pqaytbtdfu) = ibtsmaulot qspxfwwuuy (zpsgnregny ) View more
NCT04701333 (Pubmed \| Obstet Gynecol)	Phase 2	Abortion	73	Cabergoline 1 mg	tyjonfdffq(djckfzehgi) = jqmsyqfzbj xaliavxngc (mivzmlowpb )	Positive	01 Jun 2023
				Placebo	tyjonfdffq(djckfzehgi) = yqjfiuxzoy xaliavxngc (mivzmlowpb )
NCT04701333 (LISTA, CTgov)	Phase 2	Breast Feeding \| second trimester abortion	73	Cabergoline 1 MG (Cabergoline)	qxcrjqkehg(hbnvqniczi) = ckctkfojfy xjbzfmynot (rhlahqcluu, szefrilzbd - uorxryseym) View more	-	05 Apr 2023
				Placebo (Placebo)	qxcrjqkehg(hbnvqniczi) = shboxtbhje xjbzfmynot (rhlahqcluu, bngtbdyenf - pekqtegvmb) View more

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