Mediclarum
Medicine guide

Ambrisentan

10 mg · Tablet, Film Coated

  • Prescription only
  • Endothelin Receptor Antagonist
Active substance
Ambrisentan
Made by
Quallent Pharmaceuticals Health LLC

Quoted from the official source. Not yet reviewed by Mediclarum — the leaflet in your pack is authoritative.

At a glance

Quoted from the official label · 2026-01-05

What it is

Endothelin Receptor Antagonist

Used for
  • To improve exercise ability and delay clinical worsening.
The label’s usual adult dose

Initiate treatment at 5 mg once daily ( 2.1 ).

Full directions ↓
Serious 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…

All warnings ↓
Good to know
  • Prescription only
  • FDA enforcement reports list no ongoing recall, and none from the last two years, for this product code · checked 2026-10-02
25other products contain Ambrisentan — compare makers, forms and strengths

Every line above is selected, not written, from the official label. Nothing is reworded. DailyMed

What it is for

Ambrisentan tablets are indicated for the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1) in adult patients:

  • To improve exercise ability and delay clinical worsening.
  • Studies establishing effectiveness included predominantly patients with WHO Functional Class II–III symptoms and etiologies of idiopathic or heritable PAH (60%) or PAH associated with connective tissue diseases (34%).
  • Ambrisentan tablets are endothelin receptor antagonist indicated for the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1) in adult patients:
  • To improve exercise ability and delay clinical worsening.
  • Studies establishing effectiveness included trials predominantly in patients with WHO Functional Class II–III symptoms and etiologies of idiopathic or heritable PAH (60%) or PAH associated with connective tissue diseases (34%) ( 1 ).

From the official label · 2026-01-05 · DailyMed

How it works

From this product’s own US prescribing label.

Endothelin-1 (ET-1) is a potent autocrine and paracrine peptide.

Two receptor subtypes, ET A and ET B, mediate the effects of ET-1 in the vascular smooth muscle and endothelium.

Peak level after2 h
How the body breaks it down

Drug Interactions In Vitro Studies Studies with human liver tissue indicate that ambrisentan is metabolized by CYP3A, CYP2C19, and uridine 5'-diphosphate glucuronosyltransferases (UGTs) 1A9S, 2B7S, and 1A3S.

With food

Food does not affect its bioavailability.

Quoted from the prescribing label, sections “Mechanism of Action” and “Pharmacokinetics”. DailyMed · 2026-01-05

Serious warning

The strongest warning the FDA requires. It is printed in a box at the top of the label.

  • EMBRYO-FETAL TOXICITY 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 ).

Quoted from the official label, section “Boxed Warning”.

Do not take it if

  • Pregnancy ( 4.1 ) Idiopathic Pulmonary Fibrosis ( 4.2 )
  • 4.1 Pregnancy Ambrisentan may cause fetal harm when administered to a pregnant female.
  • Ambrisentan is contraindicated in females who are pregnant.
  • Ambrisentan was 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 is contraindicated in patients with Idiopathic Pulmonary Fibrosis (IPF), including IPF patients with pulmonary hypertension (WHO Group 3) [see Clinical Studies ( 14.4 )].

Quoted from the official label, section “Contraindications”.

How to take it

These directions are for this exact strength and form. Another one is different.

  • Initiate treatment at 5 mg once daily ( 2.1 ).
  • Titrate at 4-week intervals as needed and tolerated ( 2.1 ).
  • Do not split, crush, or chew tablets ( 2.1 ).
  • 2.1 Adult Dosage Initiate treatment at 5 mg once daily.
  • At 4-week intervals, the dose of ambrisentan can be increased, as needed and tolerated to 10 mg.
  • Do not split, crush, or chew tablets.
  • 2.2 Pregnancy Testing in Females of Reproductive Potential Exclude pregnancy before initiating treatment with ambrisentan tablets in females of reproductive potential [see Warnings and Precautions ( 5.1 ), Use in Specific Populations ( 8.1 , 8.3 )].

Quoted from the official label, section “Dosage & Administration”.

Other warnings

  • Fluid retention may require intervention ( 5.2 ).
  • If patients develop acute pulmonary edema during initiation of therapy with ambrisentan, consider underlying pulmonary venoocclusive disease and discontinue treatment if necessary ( 5.3 ).
  • Decreases in sperm count have been observed in patients taking endothelin receptor antagonists ( 5.4 ).
  • Decreases in hemoglobin have been observed within the first few weeks; measure hemoglobin at initiation, at 1 month, and periodically thereafter ( 5.5 ).
  • 5.1 Embryo-fetal Toxicity Based on data from animal reproduction studies, ambrisentan may cause fetal harm when administered during pregnancy and is contraindicated during pregnancy.
  • The available human data for endothelin receptor antagonists do not establish the presence or absence of major birth defects related to the use of ambrisentan.
  • Advise patients who can become pregnant of the potential risk to a fetus.
  • Obtain a pregnancy test prior to initiation of treatment with ambrisentan.
  • Advise patients who can become pregnant to use effective contraception prior to initiation of treatment, during treatment, and for one month after discontinuation of treatment with ambrisentan.
  • When pregnancy is detected, discontinue use as soon as possible [see Dosage and Administration ( 2.2 ), and Use in Specific Populations ( 8.1 , 8.3 )] .
  • 5.2 Fluid Retention Peripheral edema is a known class effect of endothelin receptor antagonists, and is also a clinical consequence of PAH and worsening PAH.
  • In the placebo-controlled studies, there was an increased incidence of peripheral edema in patients treated with doses of 5 or 10 mg ambrisentan compared to placebo [see Adverse Reactions ( 6.1 )].
  • Most edema was mild to moderate in severity.
  • In addition, there have been postmarketing reports of fluid retention in patients with pulmonary hypertension, occurring within weeks after starting ambrisentan.
  • Patients required intervention with a diuretic, fluid management, or, in some cases, hospitalization for decompensating heart failure.
  • If clinically significant fluid retention develops, with or without associated weight gain, further evaluation should be undertaken to determine the cause, such as ambrisentan or underlying heart failure, and the possible need for specific treatment or discontinuation of ambrisentan therapy.
  • 5.3 Pulmonary Edema with Pulmonary Veno-occlusive Disease (PVOD) If patients develop acute pulmonary edema during initiation of therapy with vasodilating agents such as ambrisentan, the possibility of PVOD should be considered, and if confirmed ambrisentan tablets should be discontinued.
  • 5.4 Decreased Sperm Counts Decreased sperm counts have been observed in human and animal studies with another endothelin receptor antagonist and in animal fertility studies with ambrisentan.
  • Ambrisentan may have an adverse effect on spermatogenesis. [see Use in Specific Populations ( 8.6 ) and Nonclinical Toxicology ( 13.1 )].
  • 5.5 Hematological Changes Decreases in hemoglobin concentration and hematocrit have followed administration of other endothelin receptor antagonists and were observed in clinical studies with ambrisentan.
  • These decreases were observed within the first few weeks of treatment with ambrisentan, and stabilized thereafter.
  • The mean decrease in hemoglobin from baseline to end of treatment for those patients receiving ambrisentan in the 12-week placebo-controlled studies was 0.8 g/dL.
  • Marked decreases in hemoglobin (>15% decrease from baseline resulting in a value below the lower limit of normal) were observed in 7% of all patients receiving ambrisentan (and 10% of patients receiving 10 mg) compared to 4% of patients receiving placebo.
  • The cause of the decrease in hemoglobin is unknown, but it does not appear to result from hemorrhage or hemolysis.
  • In the long-term open-label extension of the two pivotal clinical studies, mean decreases from baseline (ranging from 0.9 to 1.2 g/dL) in hemoglobin concentrations persisted for up to 4 years of treatment.
  • There have been postmarketing reports of decreases in hemoglobin concentration and hematocrit that have resulted in anemia requiring transfusion.
  • Measure hemoglobin prior to initiation of ambrisentan, at one month, and periodically thereafter.
  • Initiation of ambrisentan therapy is not recommended for patients with clinically significant anemia.
  • If a clinically significant decrease in hemoglobin is observed and other causes have been excluded, consider discontinuing ambrisentan.

Quoted from the official label, section “Warnings”.

Pregnancy and breastfeeding

  • Ambrisentan may cause fetal harm when administered to a pregnant female.
  • Ambrisentan is contraindicated in females who are pregnant.
  • Ambrisentan was 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 )] .
  • 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) based on AUC. In both species, there were abnormalities of the lower jaw and hard and soft palate, malformation of the heart and great vessels, and failure of formation of the thymus and thyroid. A preclinical study in rats has shown decreased survival of newborn pups (mid and high dosages) and effects on testicle size and fertility of pups (high dosage) following maternal treatment with ambrisentan from late gestation through weaning. The mid and high dosages were 51 x, and 170 x (on a mg/m 2 body surface area basis) the maximum oral human dose of 10 mg and an average adult body weight of 70 kg. These effects were absent at a maternal dosage 17 x the human dose based on mg/m 2 .
  • IN SPECIFIC POPULATIONS Breastfeeding:
  • Choose ambrisentan tablets or breastfeeding ( 8.2 ). Not recommended in patients with moderate or severe hepatic impairment ( 8.7 ). 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) based on AUC. In both species, there were abnormalities of the lower jaw and hard and soft palate, malformation of the heart and great vessels, and failure of formation of the thymus and thyroid. A preclinical study in rats has shown decreased survival of newborn pups (mid and high dosages) and effects on testicle size and fertility of pups (high dosage) following maternal treatment with ambrisentan from late gestation through weaning. The mid and high dosages were 51 x, and 170 x (on a mg/m 2 body surface area basis) the maximum oral human dose of 10 mg and an average adult body weight of 70 kg. These effects were absent at a maternal dosage 17 x the human dose based on mg/m 2 . 8.2 Lactation Risk Summary It is not known whether ambrisentan is present in human milk. Because many drugs are present in human milk and because of the potential for serious adverse reactions in breastfed infants from ambrisentan, a decision should be made whether to discontinue breastfeeding or discontinue ambrisentan, taking into account the importance of the drug to the mother. 8.3 Females and Males of Reproductive Potential Based on data from animal reproductive toxicity studies, ambrisentan may cause fetal harm, including birth defects and fetal death, when administered to a pregnant patient and is contraindicated during pregnancy [see Contraindications ( 4.1 ), Use in Specific Populations ( 8.1 )]. Pregnancy Testing Verify that patients who can become pregnant are not pregnant prior to initiating ambrisentan. The patient should contact their physician immediately for pregnancy testing if onset of menses is delayed or pregnancy is suspected. If the pregnancy test is positive, the physician and patient should discuss the risks to the pregnancy and the fetus. Contraception Patients who can become pregnant who are using ambrisentan should use effective contraception prior to initiation of treatment, during treatment, and for one month after discontinuation of treatment with ambrisentan to prevent pregnancy [see Warnings and Precautions ( 5.1 )]. Infertility Males In a 6-month study of another endothelin receptor antagonist, bosentan, 25 male patients with WHO functional class III and IV PAH and normal baseline sperm count were evaluated for effects on testicular function. There was a decline in sperm count of at least 50% in 25% of the patients after 3 or 6 months of treatment with bosentan. One patient developed marked oligospermia at 3 months, and the sperm count remained low with 2 follow-up measurements over the subsequent 6 weeks. Bosentan was discontinued and after 2 months the sperm count had returned to baseline levels. In 22 patients who completed 6 months of treatment, sperm count remained within the normal range and no changes in sperm morphology, sperm motility, or hormone levels were observed. Based on these findings and preclinical data [see Nonclinical Toxicology ( 13.1 )] from endothelin receptor antagonists, it cannot be excluded that endothelin receptor antagonists such as ambrisentan have an adverse effect on spermatogenesis. Counsel patients about the potential effects on fertility [see Warnings and Precautions ( 5.5 )] . 8.4 Pediatric Use Safety and effectiveness of ambrisentan in pediatric patients have not been established. Juvenile Animal Data In juvenile rats administered ambrisentan orally once daily during postnatal day 7 to 26, 36, or 62, a decrease in brain weight (−3% to −8%) with no morphologic or neurobehavioral changes occurred after breathing sounds, apnea, and hypoxia were observed, at exposures approximately 1.8 to 7 times human pediatric exposures at 10 mg, based on AUC. 8.5 Geriatric Use In the two placebo-controlled clinical studies of ambrisentan, 21% of patients were ≥65 years old and 5% were ≥75 years old. The elderly (age ≥65 years) showed less improvement in walk distances with ambrisentan than younger patients did, but the results of such subgroup analyses must be interpreted cautiously. Peripheral edema was more common in the elderly than in younger patients. 8.6 Renal Impairment The impact of renal impairment on the pharmacokinetics of ambrisentan has been examined using a population pharmacokinetic approach in PAH patients with creatinine clearances ranging between 20 and 150 mL/min. There was no significant impact of mild or moderate renal impairment on exposure to ambrisentan [see Clinical Pharmacology ( 12.3 )] . Dose adjustment of ambrisentan in patients with mild or moderate renal impairment is therefore not required. There is no information on the exposure to ambrisentan in patients with severe renal impairment. The impact of hemodialysis on the disposition of ambrisentan has not been investigated. 8.7 Hepatic Impairment Pre-existing Hepatic Impairment The influence of pre-existing hepatic impairment on the pharmacokinetics of ambrisentan has not been evaluated. Because there is in vitro and in vivo evidence of significant metabolic and biliary contribution to the elimination of ambrisentan, hepatic impairment might be expected to have significant effects on the pharmacokinetics of ambrisentan [see Clinical Pharmacology ( 12.3 )] . Ambrisentan is not recommended in patients with moderate or severe hepatic impairment. There is no information on the use of ambrisentan in patients with mild pre-existing impaired liver function; however, exposure to ambrisentan may be increased in these patients. Elevation of Liver Transaminases Other endothelin receptor antagonists (ERAs) have been associated with aminotransferase (AST, ALT) elevations, hepatotoxicity, and cases of liver failure [see Adverse Reactions ( 6.1 , 6.2 )]. In patients who develop hepatic impairment after ambrisentan initiation, the cause of liver injury should be fully investigated. Discontinue ambrisentan if elevations of liver aminotransferases are >5 x ULN or if elevations are accompanied by bilirubin >2 x ULN, or by signs or symptoms of liver dysfunction and other causes are excluded.

Quoted from the official label, section “OTC — Pregnancy or Breast Feeding”.

Other medicines

  • Multiple dose coadministration of ambrisentan and cyclosporine resulted in an approximately 2-fold increase in ambrisentan exposure in healthy volunteers; therefore, limit the dose of ambrisentan to 5 mg once daily when coadministered with cyclosporine [see Clinical Pharmacology ( 12.3 )] .
  • Cyclosporine increases ambrisentan exposure; limit ambrisentan dose to 5 mg once daily ( 7 ).

Quoted from the official label, section “Drug Interactions”.

If you take too much

In an emergency, call your local emergency number or a poison control centre.

  • There is no experience with overdosage of ambrisentan.
  • The highest single dose of ambrisentan administered to healthy volunteers was 100 mg, and the highest daily dose administered to patients with PAH was 10 mg once daily.
  • In healthy volunteers, single doses of 50 mg and 100 mg (5 to 10 times the maximum recommended dose) were associated with headache, flushing, dizziness, nausea, and nasal congestion.
  • Massive overdosage could potentially result in hypotension that may require intervention.

Quoted from the official label, section “Overdosage”.

Use in children

  • Safety and effectiveness of ambrisentan in pediatric patients have not been established.
  • Juvenile Animal Data In juvenile rats administered ambrisentan orally once daily during postnatal day 7 to 26, 36, or 62, a decrease in brain weight (−3% to −8%) with no morphologic or neurobehavioral changes occurred after breathing sounds, apnea, and hypoxia were observed, at exposures approximately 1.8 to 7 times human pediatric exposures at 10 mg, based on AUC.

Quoted from the official label, section “Pediatric Use”.

Use in older people

  • In the two placebo-controlled clinical studies of ambrisentan, 21% of patients were ≥65 years old and 5% were ≥75 years old.
  • The elderly (age ≥65 years) showed less improvement in walk distances with ambrisentan than younger patients did, but the results of such subgroup analyses must be interpreted cautiously.
  • Peripheral edema was more common in the elderly than in younger patients.

Quoted from the official label, section “Geriatric Use”.

Side effects

  • Clinically significant adverse reactions that appear in other sections of the labeling include:
  • Embryo-fetal Toxicity [see Warnings and Precautions ( 5.1 ), Use in Specific Populations ( 8.1 )] Fluid Retention [see Warnings and Precautions ( 5.2 )] Pulmonary Edema with PVOD [see Warnings and Precautions ( 5.3 )] Decreased Sperm Count [see Warnings and Precautions ( 5.4 )] Hematologic Changes [see Warnings and Precautions ( 5.5 )] Most common adverse reactions (>3% compared to placebo) are peripheral edema, nasal congestion, sinusitis, and flushing ( 6.1 ).
  • To report SUSPECTED ADVERSE REACTIONS, contact Quallent Pharmaceuticals Health LLC at 1-877-605-7243 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
  • 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
  • Safety data for ambrisentan are presented from two 12-week, placebo-controlled studies (ARIES-1 and ARIES-2) in patients with pulmonary arterial hypertension (PAH).
  • The exposure to ambrisentan in these studies ranged from 6 days to 100 days.
  • In ARIES-1 and ARIES-2, a total of 261 patients received ambrisentan at doses of 2.5, 5, or 10 mg once daily and 132 patients received placebo.
  • The adverse reactions that occurred in >3% more patients receiving ambrisentan than receiving placebo are shown in Table 1.
  • Table 1 Adverse Reactions with Placebo-Adjusted Rates >3% in ARIES-1 and ARIES-2 Placebo ( N = 132 ) Ambrisentan ( N = 261 ) Adverse Reaction n (%) n (%) Placebo - adjusted (%) Peripheral edema 14 (11) 45 (17) 6 Nasal congestion 2 (2) 15 (6) 4 Sinusitis 0 (0) 8 (3) 3 Flushing 1 (1) 10 (4) 3 Most adverse drug reactions were mild to moderate and only nasal congestion was dose-dependent.
  • Few notable differences in the incidence of adverse reactions were observed for patients by age or sex.
  • Peripheral edema was similar in younger patients (<65 years) receiving ambrisentan (14%; 29/205) or placebo (13%; 13/104), and was greater in elderly patients (≥65 years) receiving ambrisentan (29%; 16/56) compared to placebo (4%; 1/28).
  • The results of such subgroup analyses must be interpreted cautiously.
  • The incidence of treatment discontinuations due to adverse events other than those related to PAH during the clinical trials in patients with PAH was similar for ambrisentan (2%; 5/261 patients) and placebo (2%; 3/132 patients).
  • The incidence of patients with serious adverse events other than those related to PAH during the clinical trials in patients with PAH was similar for placebo (7%; 9/132 patients) and for ambrisentan (5%; 13/261 patients).
  • During 12-week controlled clinical trials, the incidence of aminotransferase elevations >3 x upper limit of normal (ULN) were 0% on ambrisentan and 2.3% on placebo.
  • In practice, cases of hepatic injury should be carefully evaluated for cause.
  • Use in Patients with Prior Endothelin Receptor Antagonist (ERA) Related Serum Liver Enzyme Abnormalities In an uncontrolled, open - label study, 36 patients who had previously discontinued endothelin receptor antagonists (ERAs:
  • bosentan, an investigational drug, or both) due to aminotransferase elevations >3 x ULN were treated with ambrisentan.
  • Prior elevations were predominantly moderate, with 64% of the ALT elevations <5 x ULN, but 9 patients had elevations >8 x ULN.
  • Eight patients had been re-challenged with bosentan and/or the investigational ERA and all eight had a recurrence of aminotransferase abnormalities that required discontinuation of ERA therapy.
  • All patients had to have normal aminotransferase levels on entry to this study.
  • Twenty-five of the 36 patients were also receiving prostanoid and/or phosphodiesterase type 5 (PDE5) inhibitor therapy.
  • Two patients discontinued early (including one of the patients with a prior 8 x ULN elevation).
  • Of the remaining 34 patients, one patient experienced a mild aminotransferase elevation at 12 weeks on ambrisentan 5 mg that resolved with decreasing the dosage to 2.5 mg, and that did not recur with later escalations to 10 mg.
  • With a median follow-up of 13 months and with 50% of patients increasing the dose of ambrisentan to 10 mg, no patients were discontinued for aminotransferase elevations.
  • While the uncontrolled study design does not provide information about what would have occurred with re - administration of previously used ERAs or show that ambrisentan led to fewer aminotransferase elevations than would have been seen with those drugs, the study indicates that ambrisentan may be tried in patients who have experienced asymptomatic aminotransferase elevations on other ERAs after aminotransferase levels have returned to normal.
  • 6.2 Postmarketing Experience The following adverse reactions were identified during post-approval use of ambrisentan.
  • Because these reactions were reported voluntarily from a population of uncertain size, it is not possible to estimate reliably the frequency or to establish a causal relationship to drug exposure:
  • anemia requiring transfusion [see Warnings and Precautions ( 5.5 )] heart failure (associated with fluid retention), symptomatic hypotension, and hypersensitivity (e.g., angioedema, rash).
  • Elevations of liver aminotransferases (ALT, AST) have been reported with ambrisentan use; in most cases alternative causes of the liver injury could be identified (heart failure, hepatic congestion, hepatitis, alcohol use, hepatotoxic medications).
  • Other endothelin receptor antagonists have been associated with elevations of aminotransferases, hepatotoxicity, and cases of liver failure [see Adverse Reactions ( 6.1 )].

Quoted from the official label, section “Adverse Reactions”.

What to discuss with your doctor

  • Advise patients to read the FDA-approved patient labeling (Medication Guide).
  • Embryo-fetal Toxicity Instruct patients on the risk of fetal harm when ambrisentan is used in pregnancy [see Warnings and Precautions ( 5.1 ) and Use in Specific Populations ( 8.1 )] .
  • Instruct females of reproductive potential to immediately contact their physician if they suspect they may be pregnant.
  • Educate and counsel patients who can become pregnant about the need to use effective contraception prior to treatment with ambrisentan, during treatment, and for one month after treatment discontinuation [see Warnings and Precautions ( 5.1 ) and Use in Specific Populations ( 8.1 , 8.3 )].
  • Patients who can become pregnant should have a negative pregnancy test prior to treatment with ambrisentan [see Dosage and Administration ( 2.2 ), Contraindications ( 4.1 ), Warnings and Precautions ( 5.1 ), Use in Specific Populations ( 8.1 , 8.3 )].
  • Counsel patients who can become pregnant about pregnancy planning and prevention, including emergency contraception, or designate counseling by another healthcare provider trained in contraceptive counseling [see Boxed Warning].
  • Hepatic Effects Advise patients of the symptoms of potential liver injury and instruct them to report any of these symptoms to their physician.
  • Hematological Change Advise patients of the importance of hemoglobin testing.
  • Other Risks Associated with ambrisentan tablets Instruct patients that the risks associated with ambrisentan tablets also include the following:
  • Decreases in sperm count Fluid overload Administration Advise patients not to split, crush, or chew tablets.
  • Medication Guide available at www.zydususa.com/medguides or call 1-877-993-8779.

Quoted from the official label, section “Patient Counseling Information”.

Strengths and forms

  • FORMS AND STRENGTHS Ambrisentan Tablets, 5 mg are pink-colored, round shaped, film coated tablets debossed with "1179" on one side and plain on the other side.
  • Ambrisentan Tablets, 10 mg are white to off-white, oval shaped, film coated tablets debossed with "1180" on one side and plain on the other side.
  • Tablet: 5 mg and 10 mg ( 3 )

Quoted from the official label, section “Dosage Forms & Strengths”.

What it looks like and how it is packed

  • Ambrisentan Tablets, 5 mg are pink-colored, round shaped, film-coated tablets debossed with "1179" on one side and plain on the other side and are supplied as follows:
  • NDC 82009-141-30 in bottle of 30 tablets with child-resistant closure Ambrisentan Tablets, 10 mg are white to off-white, oval shaped, film-coated tablets debossed with "1180" on one side and plain on the other side and are supplied as follows:
  • NDC 82009-142-30 in bottle of 30 tablets with child-resistant closure
  • Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].
  • Store ambrisentan tablets in its original packaging.

Quoted from the official label, section “How Supplied”.

What is in it

  • Ambrisentan is an endothelin receptor antagonist.
  • The chemical name of ambrisentan is (+)-(2 S )-2-[(4, 6-dimethylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid.
  • It has a molecular formula of C 22 H 22 N 2 O 4 and a molecular weight of 378.42.
  • It contains a single chiral center determined to be the ( S ) configuration and has the following structural formula:
  • Figure 1 Ambrisentan Structural Formula Ambrisentan is a white to light yellow crystalline powder.
  • It is a carboxylic acid with a pKa of 4.0.
  • It is freely soluble in tetrahydrofuran, sparingly soluble in ethyl acetate, slightly soluble in ethanol, practically insoluble in n-hexane, water and in aqueous solutions at low pH.
  • Solubility increases in aqueous solutions at higher pH.
  • In the solid state ambrisentan is very stable, is not hygroscopic, and is not light sensitive.
  • Ambrisentan tablets are available as 5 mg and 10 mg film-coated tablets for once daily oral administration and contain the following inactive ingredients:
  • croscarmellose sodium, lactose monohydrate, lecithin, magnesium stearate, microcrystalline cellulose, partially hydrolyzed polyvinyl alcohol, polyethylene glycol, povidone, talc and titanium dioxide.
  • Additionally, 5 mg tablet contains: FD&C red#40 aluminum lake. image

Quoted from the official label, section “Description”.

Ingredients people check for

Lactose, gluten, dyes, sugars and other ingredients that matter with an allergy, intolerance or diet — as this product’s FDA label lists them.

  • Lactoselactose monohydrateMilk sugar: matters with lactose intolerance or a milk allergy.
  • Colour dyes5 mg tablet contains: FD&C red#40 aluminum lakeSome people react to dyes such as tartrazine (Yellow 5) or carmine.
  • SoylecithinMatters with a soy allergy.
  • Titanium dioxidetitanium dioxideA whitening agent no longer allowed in food in the EU (E171).

Quoted from the FDA label. A label that does not name an ingredient is not a guarantee that the product is free of it, and formulations change. With an allergy, check the pack and ask a pharmacist.

Every version of this medicine (13)

The same active substance, strength and kind of form, from every company that sells it — with what each label lists.

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Same active substance, strength and form in other countries

Matched on active substance, strength and kind of form only. This is not a statement that the products are equivalent or interchangeable: other ingredients, release and approved uses can differ — ask a pharmacist before swapping.

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European UnionNo exact match for this strength and form

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France6 matching products

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Canada5 matching products

Every strength and form (10)

Netherlands8 matching products

Every strength and form (17)

Details

Made byQuallent Pharmaceuticals Health LLC
Active substanceAmbrisentan
Strength10 mg
FormTablet, Film Coated
RouteOral
Packs30 TABLET, FILM COATED in 1 BOTTLE
NDC82009-142

Source: NDC Directory · 2026-09-13 · not reviewed by a clinician

Source: US Food and Drug Administration, NDC Directory. Reuse terms: US government work (FDA).

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Other strengths and forms

24 products are sold under this name. Grouped by form; a number on a strength means several companies make it.

Same active substance

These contain the same substance. That does not mean one can replace another — ask a pharmacist.

Ambrisentan5 mgPrescription onlyTablet, Film Coated Mylan Pharmaceuticals Inc. · AmbrisentanAmbrisentan10 mgPrescription onlyTablet, Film Coated Mylan Pharmaceuticals Inc. · AmbrisentanAmbrisentan5 mgPrescription onlyTablet, Film Coated Actavis Pharma, Inc. · AmbrisentanAmbrisentan10 mgPrescription onlyTablet, Film Coated Actavis Pharma, Inc. · AmbrisentanAmbrisentan5 mgPrescription onlyTablet, Film Coated Sigmapharm Laboratories, LLC · AmbrisentanAmbrisentan10 mgPrescription onlyTablet, Film Coated Sigmapharm Laboratories, LLC · Ambrisentan

See every product with Ambrisentan