Share on Facebook
Share on Twitter
Share on LinkedIn
Share by Email
Print
Opsumit Generic Name & Formulations
Legal Class
Rx
General Description
Macitentan 10mg; tabs.
Pharmacological Class
Endothelin receptor antagonist.
How Supplied
Tabs—15, 30
Manufacturer
Generic Availability
NO
Mechanism of Action
Macitentan inhibits the binding of endothelin (ET)-1 to both ETA and ETB receptors. Macitentan displays high affinity and sustained occupancy of the ET receptors in human pulmonary arterial smooth muscle cells. One of the metabolites of macitentan is also pharmacologically active at the ET receptors and is estimated to be about 20% as potent as the parent drug in vitro. The clinical impact of dual endothelin blockage is unknown.
Opsumit Indications
Indications
Treatment of pulmonary arterial hypertension (PAH, WHO Group I) to reduce disease progression risks and hospitalization for PAH.
Opsumit Dosage and Administration
Adult
10mg once daily. Doses >10mg once daily: not recommended.
Children
Not established.
Opsumit Contraindications
Contraindications
Pregnancy.
Opsumit Boxed Warnings
Boxed Warning
Embryo-fetal toxicity.
Opsumit Warnings/Precautions
Warnings/Precautions
Embryo-fetal toxicity: in females of reproductive potential, exclude pregnancy prior to initiation, monthly during, and for 1 month after treatment discontinuation; must use acceptable methods of contraception. Obtain LFTs prior to initiation and repeat during treatment as clinically indicated. Discontinue if clinically relevant ALT/AST elevations or if elevations accompanied by bilirubin >2×ULN, or by symptoms of hepatotoxicity occur. Underlying left ventricular dysfunction: monitor for fluid retention; evaluate if develops. Severe anemia: not recommended. Measure Hgb prior to initiation and repeat during treatment as clinically indicated. Consider pulmonary veno-occlusive disease if signs of pulmonary edema occur; discontinue if confirmed. Potential decrease in sperm count; counsel men on fertility effects. Nursing mothers: not recommended.
REMS
Opsumit Pharmacokinetics
Absorption
Maximum plasma concentration: ~8 hours after oral administration.
Distribution
Apparent volume of distribution: ~50 L. Plasma protein bound: >99%.
Elimination
Renal (50%), fecal (24%). Half-life: ~16 hours.
Opsumit Interactions
Interactions
Potentiated by strong CYP3A4 inhibitors (eg, ketoconazole, ritonavir); avoid concomitant use. May be potentiated by moderate dual or combined CYP3A4 and CYP2C9 inhibitors (eg, fluconazole, amiodarone); avoid concomitant use. Antagonized by strong CYP3A4 inducers (eg, rifampin); avoid concomitant use.
Opsumit Adverse Reactions
Adverse Reactions
Anemia, nasopharyngitis/pharyngitis, bronchitis, headache, influenza, urinary tract infection; hepatotoxicity, decreased hemoglobin.
Opsumit Clinical Trials
See Literature
Opsumit Note
Notes
For all female patients: available only through the Opsumit REMS program. To enroll call (866) 228-3546 or www.OpsumitREMS.com.
Opsumit Patient Counseling
See Literature
Images
