REMS restricted

Macitentan

OPSUMIT

Open Macitentan in the interactive console ↗

Pronunciation: ma-si-TEN-tan (OP-sum-it)

Macitentan ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Macitentan ballicule

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.

Macitentan molecular structure (skeletal formula) — Molecular structure: Macitentan

FDA-approved for

pulmonary arterial hypertension (2013)

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk4 / 4

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.

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Embryo-fetal toxicity — contraindicated in pregnancy; exclude pregnancy before starting and use effective contraception during and for 1 month after treatment.

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.

Available strengths

tab 10 mg

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.

Cost

Macitentan (OPSUMIT)

Strength		#/mo	generic $/mo	CostPlus
10 mg	tab	30 qd		offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Macitentan is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2021

Open Macitentan in the interactive console ↗

Self-check

Unlike bosentan, does macitentan require routine monthly liver testing?
No.
What reproductive risk requires macitentan pregnancy prevention?
Embryo-fetal toxicity.