Ambrisentan
Ambrisentan is an endothelin receptor antagonist used to treat pulmonary arterial hypertension (PAH). It works by blocking the action of endothelin, a substance that causes blood vessels to narrow. This medication helps improve exercise ability and slow disease progression in patients with PAH.
Ambrisentan is an oral medication used to treat pulmonary arterial hypertension by blocking endothelin receptors to help relax blood vessels.
Key facts at a glance
- ATC
- C02KX02
- RxNorm
- 358274
- Generic
- Ambrisentan
- Class
- atc-c02
- Brands
- Letairis
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 5mg once daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 5mg once daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 5mg once daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
8 groupspregnancy
first trimesteravoid completely
do not use during pregnancy due to known teratogenic effects - fetal abnormalities reported in animal studies
pregnancy testing required before and during treatment
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
second third trimesteravoid completely
discontinue therapy if pregnancy occurs
regular fetal ultrasound monitoring
Use of this medication in this population requires careful consideration of risks and benefits.
lactation
breastfeedingdiscontinue breastfeeding or avoid drug
do not breastfeed during treatment - unknown if excreted in human milk
monitor infant for adverse effects
Use of this medication in this population requires careful consideration of risks and benefits.
geriatric
elderly 65no specific dose adjustment required
use with caution due to increased susceptibility to adverse effects including fluid retention and anemia
regular monitoring of hemoglobin, liver function, and fluid status
Use with caution and monitor for adverse effects.
pediatric_age
children under 18not recommended
safety and efficacy not established in pediatric patients - avoid use in children
not applicable - avoid use
Use of this medication in this population requires careful consideration of risks and benefits.
renal_impairment
severe renal impairmentno initial dose adjustment needed
use with caution - increased exposure may occur; monitor for edema and anemia
regular monitoring of renal function, hemoglobin, and fluid status
Use with caution and monitor for adverse effects.
hepatic_impairment
moderate to severeavoid use
do not use in patients with moderate to severe hepatic impairment due to primarily hepatic metabolism
liver function tests before and during treatment
Use of this medication in this population requires careful consideration of risks and benefits.
hepatic_impairment
mildno specific adjustment
use with caution - monitor liver function closely
baseline and periodic liver function tests
Use with caution and monitor for adverse effects.
Statistics and clinical data
Drug class
Ambrisentan is classified as an endothelin receptor antagonist, specifically a selective ETA receptor blocker
FDA approval year
FDA approval date for Ambrisentan (brand name Letairis)
Primary indication
Primary therapeutic use for treatment of PAH to improve exercise capacity and delay clinical worsening
Mechanism of action
Blocks vasoconstriction and cell proliferation mediated by ETA receptors
Treatment of pulmonary arterial hypertension (PAH) to improve exercise capacity and delay clinical worsening. It may be used as monotherapy or in combination with other PAH medications.
Ambrisentan selectively blocks endothelin type A (ETA) receptors, preventing endothelin-1 from binding and causing vasoconstriction. This results in pulmonary vasodilation and reduced pulmonary vascular resistance.
Contraindicated in pregnancy due to teratogenic effects. Requires monthly liver function monitoring. Women of childbearing potential must use reliable contraception. May cause fluid retention or anemia. Only available through a restricted distribution program.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed August 24, 2026. · Read our editorial policy