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Ambrisentan

Also known as: Letairis

Endothelin Receptor AntagonistEndothelin Receptor Antagonists

Route: Oral

1 interaction on record⛔ Black Box Warning

Ambrisentan has 1 known drug interaction based on U.S. FDA drug labeling data. Notable interactions include combinations with Cyclosporine. Patients taking Ambrisentan should inform their healthcare provider of all current medications — including over-the-counter drugs and supplements — to avoid potentially harmful combinations. Data sourced from OpenFDA and the NIH National Library of Medicine.

Total: 1
Moderate: 1

Moderate (1)

Ambrisentan + Cyclosporine— Cyclosporine increases ambrisentan exposure approximately 2-fold. Limit ambrisentan dose to 5 mg once daily when coadmin…

Ambrisentan + Cyclosporine🟡Moderate

Cyclosporine increases ambrisentan exposure approximately 2-fold. Limit ambrisentan dose to 5 mg once daily when coadministered with cyclosporine.

⛔ FDA Black Box Warning

WARNING: EMBRYO-FETAL TOXICITY Ambrisentan is contraindicated for use during pregnancy because it may cause major birth defects if used by pregnant patients, based on studies in animals [see Contraindications (4.1) , Warnings and Precautions (5.1) , and Use in Specific Populations (8.1) ]. Therefore, for females of reproductive potential, exclude pregnancy before the initiation of treatment with ambrisentan. Advise use of effective contraception before initiation, during treatment, and for one month after treatment with ambrisentan [see Dosage and Administration (2.2) Contraindications (4.1) , Warnings and Precautions (5.1) , and Use in Specific Populations (8.1 , 8.3) ]. When pregnancy is detected, discontinue ambrisentan as soon as possible ( 5.1 ). WARNING: EMBRYO-FETAL TOXICITY See full prescribing information for complete boxed warning. Based on animal data ambrisentan may cause fetal harm if used during pregnancy ( 4.1 , 5.1 , 8.1 ). Females of reproductive potential: Exclude pregnancy before the start of treatment. Use effective contraception prior to initiation of treatment, during treatment, and for one month after treatment with ambrisentan ( 2.2 , 4.1 , 5.1 , 8.1 , 8.3 ) When pregnancy is detected, discontinue ambrisentan as soon as possible ( 5.1 ).

Contraindications

4 CONTRAINDICATIONS Pregnancy ( 4.1 ) Idiopathic Pulmonary Fibrosis ( 4.2 ) 4.1 Pregnancy Ambrisentan tablets may cause fetal harm when administered to a pregnant female. Ambrisentan tablets are contraindicated in females who are pregnant. Ambrisentan tablets were consistently shown to have teratogenic effects when administered to animals. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to a fetus [see Dosage and Administration (2.2) , Warnings and Precautions (5.1) , and Use in Specific Populations (8.1) ]. 4.2 Idiopathic Pulmonary Fibrosis Ambrisentan tablets are contraindicated in patients with Idiopathic Pulmonary Fibrosis (IPF), including IPF patients with pulmonary hypertension (WHO Group 3) [see Clinical Studies (14.4) ] .

Pregnancy & Breastfeeding

8.1 Pregnancy Risk Summary Based on data from animal reproduction studies, ambrisentan may cause fetal harm, including birth defects and fetal death, when administered to a pregnant woman and is contraindicated during pregnancy. There are limited data on ambrisentan use in pregnant women. Available data from postmarketing reports and published literature over decades of use with endothelin receptor antagonists in the same class as ambrisentan have not identified an increased risk of major birth defects; however, these data are limited. Methodological limitations of these postmarketing reports and published literature include lack of a control group; limited information regarding dose, duration, and timing of drug exposure; and missing data. These limitations preclude establishing a reliable estimate of the risk of adverse fetal and neonatal outcomes with maternal endothelin receptor antagonist use. In animal reproduction studies, ambrisentan was teratogenic in rats and rabbits at doses which resulted in exposures of 3.5 and 1.7 times, respectively, the human dose of 10 mg per day [see Animal Data] . If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, advise the patient of the potential hazard to a fetus [see Contraindications (4.1) , Warnings and Precautions (5.1) ] . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data Ambrisentan was teratogenic at oral dosages of ≥15 mg/kg/day (AUC 51.7 h•mcg/mL) in rats and ≥7 mg/kg/day (24.7 h•mcg/mL) in rabbits; it was not studied at lower dosages. These dosages are of 3.5 and 1.7 times, respectively, the human dose of 10 mg per day (14.8 h•mcg/mL

Data sourced from U.S. FDA drug labeling via openFDA and the NIH National Library of Medicine, supplemented with a small number of well-established interactions from curated clinical references. For informational purposes only. Always consult your pharmacist or physician.