ambrisentan
Pharmaranks rates Ambrisentan 3.3/5 for recall safety — an independent score from its FDA recall history and its manufacturer's record. Ambrisentan is an endothelin receptor antagonist used to treat Pulmonary Hypertension.
Endothelin Receptor Antagonist · by Zydus Pharms USA Inc
Generic of Letairis
Based on 1 source · Recall-safety score from FDA recall history — this product's own recalls and its manufacturer's record. Not an efficacy or quality rating. methodology →
Key facts
- Active ingredient
- Ambrisentan
- Drug class
- Endothelin Receptor Antagonist
- Form
- Tablet
- Strength
- Ambrisentan 10MG · Ambrisentan 5MG
- Type
- Prescription (Rx)
- Brand or generic
- Generic
- May treat
- pulmonary hypertension
- Manufacturer
- Zydus Pharms USA Inc
- What the pharmacy pays
- ~$255.61 for 30 — not your price
- FDA application
- ANDA210058
- FDA boxed warning
- Yes — see the boxed warning
What is Ambrisentan?
From the FDA label: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
How to use
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 )].
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 Zydus Pharmaceuticals (USA) Inc. at 1-877-993-8779 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…
FDA Boxed Warning (the FDA’s most serious warning)
Boxed (black-box) warning — from the FDA 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 ).
Warnings
Important safety information
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.
Who should not take Ambrisentan
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 )].
Overdose — what happens if you take too much
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.
U.S. Poison Control: call or text 1-800-222-1222 (free, 24/7). In an emergency call 911. From the FDA label; not medical advice.
Interactions
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 ).
Storing Ambrisentan, and how long it keeps
Quoted from this product’s own FDA label. Storage belongs to the product and its device, not to the drug in general — a pen and a tablet of the same medicine are kept completely differently.
- “Store ambrisentan tablets in its original packaging.”
Drug class
How this class works, per Bosentan - StatPearls - NCBI Bookshelf.
May treat (source: NIH RxClass)
See how Ambrisentan ranks — best-rated endothelin receptor antagonist for:
Dosage forms
Tablet
The forms currently marketed in the U.S., per the FDA National Drug Code Directory.
Ways to save
Ask for the generic
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Request a 90-day supply
Bulk fills usually lower the per-dose price vs monthly refills.
Use copay cards
Manufacturer copay cards & patient-assistance programs — especially for brand drugs.
Compare alternatives
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Frequently asked questions
- What does Ambrisentan treat?
- Ambrisentan (Ambrisentan) may be used to treat pulmonary hypertension, based on NIH RxClass drug-classification data (conditions a drug may treat — not a verbatim copy of the FDA-approved label). This is general reference, not medical advice.
- How does Ambrisentan work?
- Ambrisentan is a endothelin receptor antagonist. Endothelin receptor antagonists block endothelin-1, a natural substance that powerfully tightens blood vessels. By stopping it from acting on its receptors, these drugs let vessels relax and widen, lowering pressure in the lung arteries in conditions like pulmonary arterial hypertension.
- How is Ambrisentan rated?
- pharmaranks gives Ambrisentan a composite score of 3.3 out of 5, currently based on 1 weighted source (FDA regulatory recall-safety data weighted highest). See our methodology at /how-we-rate.
- How much does Ambrisentan cost?
- Nobody can tell you what you will pay — your price is set by your insurer's formulary, your deductible and the pharmacy's markup, and none of those are published. What IS published is what the pharmacy paid to acquire it: about $255.61 for 30, per the CMS NADAC survey. Treat that as the floor, not the quote — ask the pharmacist for the cash price as well as your copay, because for cheap generics the cash price often wins.
- Is there a coupon or discount for Ambrisentan?
- pharmaranks is an independent ratings site, not a pharmacy — we don't issue coupons or sell Ambrisentan. To pay less, Ambrisentan is already a generic — usually the lowest-cost version — so the main levers are comparing cash prices between pharmacies and using a pharmacy discount-card service. Prices vary by pharmacy, insurance, and location, so always confirm at the counter. This is general reference, not medical or financial advice.
- Who makes Ambrisentan?
- Ambrisentan is marketed by Zydus Pharms USA Inc. You can see Zydus Pharms USA Inc's full profile, rating, and other products on pharmaranks.
- Is Ambrisentan a brand-name or generic drug?
- Ambrisentan is a generic medication; its active ingredient is Ambrisentan. Generics contain the same active ingredient as the brand-name original and are usually lower cost.
- Is Ambrisentan available over the counter?
- No. Ambrisentan is a prescription (Rx) medication in the US — you need a prescription from a licensed clinician (in person or via telehealth); it isn't sold over the counter. For some conditions there are OTC alternatives — ask your pharmacist.
- What forms does Ambrisentan come in?
- Ambrisentan is currently marketed as tablet, per the FDA's National Drug Code Directory.
- What class of drug is Ambrisentan?
- Ambrisentan is classified as endothelin receptor antagonist, per the FDA's Established Pharmacologic Class.
- Is Ambrisentan FDA-registered?
- Ambrisentan is on record with the U.S. FDA under application number ANDA210058. You can verify this on its official FDA label.
- Has Ambrisentan been recalled by the FDA?
- Ambrisentan has no FDA recalls recorded under its own application in the openFDA enforcement database. Its recall-safety score reflects its manufacturer's overall recall record. This is general reference, not medical advice — check the FDA recall database for the latest alerts.
- Is Ambrisentan safe?
- There's no single safe-or-not verdict. pharmaranks gives Ambrisentan a recall-safety score of 66/100, based on its FDA recall history (no recalls under its own FDA application) — not an efficacy or side-effect rating. Review its FDA-label side effects and warnings before use, and always consult a licensed professional.
- What are the side effects of Ambrisentan?
- Ambrisentan's side effects are taken directly from its FDA label. From the label: Clinically significant adverse reactions that appear in other sections of the labeling include: Embryo-fetal Toxicity [see Warnings and Precautions ( 5.1 ),… Both common and serious reactions are documented in full on this page. This is general reference from the FDA, not medical advice — always consult a professional.
Clinical content sourced from the FDA label via openFDA (U.S. FDA). View the FDA label on DailyMed → Provided for general reference only — not medical advice. Always consult a licensed professional and the current prescribing information.
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ambrisentan
66/100