Macitentan
OPSUMIT
What it isEndothelin receptor antagonist; pulmonary arterial hypertension.
Why this oneCompared with bosentan, it penetrates tissue better and does not require routine monthly liver testing.
What limits itEmbryo-fetal toxicity requires restricted dispensing and pregnancy prevention. Anemia and peripheral edema can limit use.
FDA-approved for
- pulmonary arterial hypertension (2013)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Pulmonary arterial hypertension (PAH) | Adults | 10 mg QD | 10 mg QD | 10 mg QD |
Renal Undefined
Hepatic Undefined
Instructions
- Exclude pregnancy before starting; use effective contraception during and for 1 month after treatment.
- Obtain baseline liver enzymes and hemoglobin; monitor as clinically indicated.
Contraindications
- Pregnancy
Cautions
- Hepatotoxicity and liver failure — monitor liver enzymes
- Fluid retention/peripheral edema (may require diuretic; risk with LV dysfunction)
- Decreased hemoglobin/anemia — not recommended in severe anemia
- Pulmonary edema with pulmonary veno-occlusive disease — discontinue if confirmed
- Decreased sperm counts
Adverse reactions
- Anemia
- Nasopharyngitis/pharyngitis
- Bronchitis
- Headache
- Influenza
- Urinary tract infection
Pregnancy Contraindicated; teratogenic in animals at all doses; may cause fetal harm.
Lactation Advise not to breastfeed; no human data.
⚠ BOXED WARNING
- Embryo-fetal toxicity
Cost, est. cash$300–$2,500/month
Generic entry2021
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.
Mechanism of action: Macitentan ballicule
