Brand Name
Opsumit
Generic Name
Macitentan
View Brand Information FDA approval date: November 04, 2013
Classification: Endothelin Receptor Antagonist
Form: Tablet
What is Opsumit (Macitentan)?
OPSUMIT is an endothelin receptor antagonist indicated for the treatment of pulmonary arterial hypertension to reduce the risks of disease progression and hospitalization for PAH.
Approved To Treat
Top Global Experts
Save this treatment for later
Not sure about your diagnosis?
Related Clinical Trials
A Prospective, Open-label, Platform Study for Long-term Follow-up of Participants Using Study Intervention in Pulmonary Hypertension Parent Studies
Summary: The purpose of the study is to enable participants with pulmonary hypertension (PH) currently treated with study intervention(s) in a clinical study (parent studies \[NCT03422328, NCT03904693,NCT04565990, NCT02932410, NCT03492177, and NCT04175600\]), to continue to benefit from the intervention after closure of the parent study in case they have no alternative means of access to the study interven...
A Multicenter, Randomized, Double-Blind, Exploratory Clinical Trial to Evaluate the Efficacy and Safety in Concomitant Administration of Macitentan and Dapagliflozin in Patients With Heart Failure With Mildly Reduced and Preserved Ejection Fraction (HFmrEF and HFpEF) and Combined Pre- and Post-capillary Pulmonary Hypertension (CpcPH)
Summary: This clinical trial will evaluate whether combination therapy with Dapagliflozin + Macitentan improves outcomes compared to Dapagliflozin + placebo in patients with combined pre- and post-capillary pulmonary hypertension (CpcPH). The study will measure changes in pulmonary vascular resistance, NT-proBNP, 6-minute walk distance, and quality of life (KCCQ scores) over 24 weeks. Participants will be ...
Efficacy and Mechanisms of Macitentan for Non-Coronary Obstructive Angina
Summary: Angina with non-obstructive coronary arteries (ANOCA) is highly prevalent, impairing quality of life and independently associated with cardiovascular events, yet effective treatments are lacking. The endothelin-1 (ET-1)-endothelin receptor (ETR) system is pivotal in ANOCA pathogenesis. Preclinical studies show that ETR blockade or pericyte-specific knockout of ETA receptor improves coronary microc...
Related Latest Advances
Brand Information
OPSUMIT (macitentan)
WARNING: EMBRYO-FETAL TOXICITY
OPSUMIT is contraindicated for use during pregnancy because it may cause fetal harm based on animal data
Therefore, for females of reproductive potential, exclude pregnancy before the start of treatment with OPSUMIT. Advise use of effective contraception before the initiation of treatment, during treatment, and for one month after stopping treatment with OPSUMIT
1DOSAGE FORMS AND STRENGTHS
Tablets: 10 mg, bi-convex film-coated, round, white, and debossed with "10" on both sides.
2ADVERSE REACTIONS
Clinically significant adverse reactions that appear in other sections of the labeling include:
- Embryo-fetal Toxicity
- Hepatotoxicity
- Fluid Retention
- Decrease in Hemoglobin
2.1Clinical Trial Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.
Safety data for OPSUMIT were obtained primarily from one placebo-controlled clinical study in 742 patients with PAH (SERAPHIN study)
The exposure to OPSUMIT in this trial was up to 3.6 years with a median exposure of about 2 years (N=542 for 1 year; N=429 for 2 years; and N=98 for more than 3 years). The overall incidence of treatment discontinuations because of adverse events was similar across OPSUMIT 10 mg and placebo treatment groups (approximately 11%).
Table 2 presents adverse reactions more frequent on OPSUMIT than on placebo by ≥3%.
2.2Postmarketing Experience
The following adverse reactions have been identified during post-approval use of OPSUMIT. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Immune system disorders:hypersensitivity reactions (angioedema, pruritus and rash)
Vascular disorders: flushing
Respiratory, thoracic and mediastinal disorders: nasal congestion
Gastrointestinal disorders: Elevations of liver aminotransferases (ALT, AST) and liver injury have been reported with OPSUMIT use; in most cases alternative causes could be identified (heart failure, hepatic congestion, autoimmune hepatitis). Endothelin receptor antagonists have been associated with elevations of aminotransferases, hepatotoxicity, and cases of liver failure [see .
General disorders and administration site conditions:edema/fluid retention. Cases of edema and fluid retention occurred within weeks of starting OPSUMIT, some requiring intervention with a diuretic, fluid management or hospitalization for decompensated heart failure [see
Cardiac disorders: symptomatic hypotension
3OVERDOSAGE
OPSUMIT has been administered as a single dose of up to and including 600 mg to healthy subjects (60 times the approved dosage). Adverse reactions of headache, nausea and vomiting were observed. In the event of an overdose, standard supportive measures should be taken, as required. Dialysis is unlikely to be effective because macitentan is highly protein-bound.
4DESCRIPTION
OPSUMIT
Macitentan is a crystalline powder that is insoluble in water. In the solid state macitentan is very stable, is not hygroscopic, and is not light sensitive.
OPSUMIT is available as a 10 mg film-coated tablet for once daily oral administration. The tablets include the following inactive ingredients: lactose monohydrate, magnesium stearate, microcrystalline cellulose, polysorbate 80, povidone, and sodium starch glycolate Type A. The tablets are film-coated with a coating material containing polyvinyl alcohol, soya lecithin, talc, titanium dioxide, and xanthan gum.
5HOW SUPPLIED/STORAGE AND HANDLING
OPSUMIT
15 count /PVC/ PE/PVDC aluminum foil blisters in carton (NDC 66215-501-15)
30 count white high-density polyethylene bottle in carton (NDC 66215-501-30)
6PATIENT COUNSELING INFORMATION
Advise patient to read FDA-approved patient labeling (Medication Guide).
7PRINCIPAL DISPLAY PANEL - 10 mg Tablet Bottle Carton
NDC 66215-501-30
Opsumit
10 mg
Dispense the
Rx only
janssen
