Generic Name and Formulations:
Macitentan 10mg; tabs.
Indications for OPSUMIT:
Treatment of pulmonary arterial hypertension (PAH, WHO Group I) to delay disease progression and to reduce hospitalization for PAH.
10mg once daily. Doses >10mg once daily: not recommended.
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 >2xULN, 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.
Endothelin receptor antagonist.
Potentiated by strong CYP3A4 inhibitors (eg, ketoconazole, ritonavir); avoid concomitant use. Antagonized by strong CYP3A4 inducers (eg, rifampin); avoid concomitant use.
Anemia, nasopharyngitis/pharyngitis, bronchitis, headache, influenza, urinary tract infection; hepatotoxicity, decreased hemoglobin.
For all female patients: available only through the Opsumit REMS program. To enroll call (866) 228-3546 or www.OpsumitREMS.com.