REMS restricted

Ambrisentan

LETAIRIS

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Pronunciation: am-bri-SEN-tan (le-TAIR-is)

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

What it isSelective endothelin A receptor antagonist; pulmonary arterial hypertension.

Why this oneOnce daily, and combined with tadalafil up front it improves outcomes more than either alone.

What limits itEmbryo-fetal toxicity under a REMS. Peripheral edema and anemia; it is contraindicated in idiopathic pulmonary fibrosis.

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

FDA-approved for

pulmonary arterial hypertension (2007)

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—may cause major birth defects; 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 (WHO Group 1)	Adult	5 mg QD	5–10 mg QD	10 mg QD

Titration May increase at 4-week intervals as needed and tolerated.

Renal No adjustment for mild–moderate impairment; no data in severe impairment.

Hepatic Not recommended in moderate or severe impairment; no data in mild.

Instructions

Do not split, crush, or chew tablets.
Obtain pregnancy test before initiation; use effective contraception.
Measure hemoglobin at baseline, at 1 month, then periodically.

Available strengths

tab 5, 10 mg

Contraindications

Pregnancy
Idiopathic pulmonary fibrosis (including IPF with pulmonary hypertension, WHO Group 3)

Cautions

Fluid retention/peripheral edema (may need intervention)
Pulmonary edema—consider pulmonary veno-occlusive disease
Decreased sperm counts
Decreases in hemoglobin/hematocrit; anemia can require transfusion

Adverse reactions

Peripheral edema
Nasal congestion
Sinusitis
Flushing

Pregnancy Contraindicated—may cause fetal harm, including birth defects and fetal death (teratogenic in animals).

Lactation Unknown whether present in human milk; decide whether to discontinue breastfeeding or the drug.

Cost

Ambrisentan (LETAIRIS)

What pharmacies pay · NADAC 9/30/26

Strength		#/mo	generic $/mo	CostPlus
5 mg	tab	30 qd		not offered
10 mg	tab	30 qd	$240.74	not offered

Generic entry2019

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Self-check

In which pulmonary disease is ambrisentan contraindicated?
Idiopathic pulmonary fibrosis.
Which drug improves outcomes when combined up front with ambrisentan?
Tadalafil.