Peringatan Keamanan

Ambrisentan is teratogenic and has a high risk of embryo-fetal toxicity. LD50 was found to be greater than or equal to 3160 mg/kg when studied in rats. There was no evidence of carcinogenic potential in 2 year oral daily dosing studies in rats and mice.

Ambrisentan

DB06403

small molecule approved investigational

Deskripsi

Ambrisentan is an orally active selective type A endothelin receptor antagonist indicated for the treatment of pulmonary arterial hypertension. It is approved in Europe, Canada and the United States for use as a single agent to improve exercise ability and delay clinical worsening. In addition, it is approved in the United States for use in combination with tadalafil to reduce the risks of disease progression, hospitalization and to improve exercise ability. Studies establishing the efficacy of Ambrisentan included patients with both idiopathic or heritable pulmonary arterial hypertension and those with pulmonary arterial hypertension associated with connective tissue diseases. Patients studied displayed symptoms and etiologies predominantly of WHO Functional Class II-III. As an endothelin receptor antagonist, Ambrisentan prevents endogenous endothelin peptide from constricting the muscles in blood vessels, allowing them to relax and permit a reduction in blood pressure.

Struktur Molekul 2D

Berat 378.428
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Ambrisentan has a terminal half-life of 15 hours. It is thought that steady state is achieved after around 4 days of repeat-dosing.
Volume Distribusi Ambrisentan has a low distribution into red blow cells, with a mean blood:plasma ratio of 0.57 and 0.61 in males and females, respectively.
Klirens (Clearance) The mean oral clearance of ambrisentan was found to be 38 mL/min in healthy subjects and 19 mL/min in patients with pulmonary artery hypertension.

Absorpsi

Ambrisentan is rapidly absorbed with peak plasma concentrations occuring around 2 hours after oral administration. Cmax and AUC increase proportionally with dose across the therapeutic dosing range. Absolute oral bioavailability of ambrisentan is unknown. Absorption is not affected by food.

Metabolisme

Ambrisentan is a metabolized primarily by uridine 5’-diphosphate glucuronosyltransferases (UGTs) 1A9S, 2B7S,1A3S to form ambrisentan glucuronide. Ambrisentan is also metabolized to a lesser extent by CYP3A4, CYP3A5 and CYP2C19 to form 4- hydroxymethyl ambrisentan which is further glucuronidated to 4-hydroxymethyl ambrisentan glucuronide.

Rute Eliminasi

Ambrisentan is primarily cleared by non-renal pathways. Along with its metabolites, ambrisentan is primarily found in the feces following hepatic and/or extra-hepatic metabolism. Approximately 22% of the administered dose is recovered in the urine following oral administration with 3.3% being unchanged ambrisentan.

Interaksi Obat

1083 Data
Cyclosporine The serum concentration of Ambrisentan can be increased when it is combined with Cyclosporine.
Ranolazine The serum concentration of Ambrisentan can be increased when it is combined with Ranolazine.
Alfuzosin Alfuzosin may increase the hypotensive activities of Ambrisentan.
Amifostine Ambrisentan may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Ambrisentan.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Ambrisentan.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Ambrisentan.
Obinutuzumab Ambrisentan may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Ambrisentan.
Rituximab Ambrisentan may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Ambrisentan.
Midodrine Midodrine may decrease the antihypertensive activities of Ambrisentan.
Isoetharine Isoetharine may decrease the antihypertensive activities of Ambrisentan.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Ambrisentan.
Etomidate Etomidate may decrease the antihypertensive activities of Ambrisentan.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Ambrisentan.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Ambrisentan.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Ambrisentan.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Ambrisentan.
Droperidol Droperidol may decrease the antihypertensive activities of Ambrisentan.
Doxapram Doxapram may decrease the antihypertensive activities of Ambrisentan.
Atropine Atropine may decrease the antihypertensive activities of Ambrisentan.
Metaraminol Metaraminol may decrease the antihypertensive activities of Ambrisentan.
Nicergoline Nicergoline may decrease the antihypertensive activities of Ambrisentan.
Methoxamine Methoxamine may decrease the antihypertensive activities of Ambrisentan.
Propiomazine Propiomazine may decrease the antihypertensive activities of Ambrisentan.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Ambrisentan.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Ambrisentan.
Dobutamine Dobutamine may decrease the antihypertensive activities of Ambrisentan.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Ambrisentan.
Ritodrine Ritodrine may decrease the antihypertensive activities of Ambrisentan.
Terbutaline Terbutaline may decrease the antihypertensive activities of Ambrisentan.
Bitolterol Bitolterol may decrease the antihypertensive activities of Ambrisentan.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Ambrisentan.
Naratriptan Naratriptan may decrease the antihypertensive activities of Ambrisentan.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Ambrisentan.
Formoterol Formoterol may decrease the antihypertensive activities of Ambrisentan.
Dopamine Dopamine may decrease the antihypertensive activities of Ambrisentan.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Ambrisentan.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Ambrisentan.
Arbutamine Arbutamine may decrease the antihypertensive activities of Ambrisentan.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Ambrisentan.
Arformoterol Arformoterol may decrease the antihypertensive activities of Ambrisentan.
Fenoterol Fenoterol may decrease the antihypertensive activities of Ambrisentan.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Ambrisentan.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Ambrisentan.
Ephedrine Ephedrine may decrease the antihypertensive activities of Ambrisentan.
Mephentermine Mephentermine may decrease the antihypertensive activities of Ambrisentan.
Procaterol Procaterol may decrease the antihypertensive activities of Ambrisentan.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Ambrisentan.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Ambrisentan.
Bambuterol Bambuterol may decrease the antihypertensive activities of Ambrisentan.
MMDA MMDA may decrease the antihypertensive activities of Ambrisentan.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Ambrisentan.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Ambrisentan.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Ambrisentan.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Ambrisentan.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Ambrisentan.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Ambrisentan.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Ambrisentan.
Metamfetamine Metamfetamine may decrease the antihypertensive activities of Ambrisentan.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Ambrisentan.
Periciazine Periciazine may decrease the antihypertensive activities of Ambrisentan.
Acepromazine Acepromazine may decrease the antihypertensive activities of Ambrisentan.
Thioproperazine Thioproperazine may decrease the antihypertensive activities of Ambrisentan.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Ambrisentan.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Ambrisentan.
Amineptine Amineptine may decrease the antihypertensive activities of Ambrisentan.
Amibegron Amibegron may decrease the antihypertensive activities of Ambrisentan.
Naluzotan Naluzotan may decrease the antihypertensive activities of Ambrisentan.
Pizotifen Pizotifen may decrease the antihypertensive activities of Ambrisentan.
Solabegron Solabegron may decrease the antihypertensive activities of Ambrisentan.
Droxidopa Droxidopa may decrease the antihypertensive activities of Ambrisentan.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Ambrisentan.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Ambrisentan.
Xylometazoline Xylometazoline may decrease the antihypertensive activities of Ambrisentan.
Isometheptene Isometheptene may decrease the antihypertensive activities of Ambrisentan.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Ambrisentan.
Naphazoline Naphazoline may decrease the antihypertensive activities of Ambrisentan.
Saralasin Saralasin may decrease the antihypertensive activities of Ambrisentan.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Ambrisentan.
Cinitapride Cinitapride may decrease the antihypertensive activities of Ambrisentan.
Tyramine Tyramine may decrease the antihypertensive activities of Ambrisentan.
Adrafinil Adrafinil may decrease the antihypertensive activities of Ambrisentan.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Ambrisentan.
Hexoprenaline Hexoprenaline may decrease the antihypertensive activities of Ambrisentan.
Etilefrine Etilefrine may decrease the antihypertensive activities of Ambrisentan.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Ambrisentan.
Butriptyline Butriptyline may decrease the antihypertensive activities of Ambrisentan.
Olodaterol Olodaterol may decrease the antihypertensive activities of Ambrisentan.
Dosulepin Dosulepin may decrease the antihypertensive activities of Ambrisentan.
Cirazoline Cirazoline may decrease the antihypertensive activities of Ambrisentan.
Synephrine Synephrine may decrease the antihypertensive activities of Ambrisentan.
Moxisylyte Moxisylyte may decrease the antihypertensive activities of Ambrisentan.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Ambrisentan.
Iofetamine I-123 Iofetamine I-123 may decrease the antihypertensive activities of Ambrisentan.
Racepinephrine Racepinephrine may decrease the antihypertensive activities of Ambrisentan.
DL-Methylephedrine DL-Methylephedrine may decrease the antihypertensive activities of Ambrisentan.
Amitraz Amitraz may decrease the antihypertensive activities of Ambrisentan.
Medetomidine Medetomidine may decrease the antihypertensive activities of Ambrisentan.

Target Protein

Endothelin-1 receptor EDNRA
Endothelin receptor type B EDNRB

Referensi & Sumber

Synthesis reference: - Riechers H, Albrecht HP, Amberg W, Baumann E, Bernard H, Bohm HJ, Klinge D, Kling A, Muller S, Raschack M, Unger L, Walker N, Wernet W: Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists. J Med Chem. 1996 May 24;39(11):2123-8. Pubmed(http://www.ncbi.nlm.nih.gov/pubmed/8667356). - Peng X, Li P, Shi Y: Synthesis of (+)-ambrisentan via chiral ketone-catalyzed asymmetric epoxidation. J Org Chem. 2012 Jan 6;77(1):701-3. doi: 10.1021/jo201927m. Epub 2011 Nov 29. Pubmed(http://www.ncbi.nlm.nih.gov/pubmed/22098088).
Artikel (PubMed)
  • PMID: 26779523
    Said K: AMBITION: An important piece in the therapeutic puzzle of pulmonary arterial hypertension. Glob Cardiol Sci Pract. 2015 Nov 13;2015(4):48. doi: 10.5339/gcsp.2015.48. eCollection 2015.
  • PMID: 25207548
    Markert C, Wirsching T, Hellwig R, Burhenne J, Weiss J, Riedel KD, Mikus G, Haefeli WE: Lack of a clinically significant interaction of grapefruit juice with ambrisentan and bosentan in healthy adults. Int J Clin Pharmacol Ther. 2014 Nov;52(11):957-64. doi: 10.5414/CP202164.
  • PMID: 18506008
    Galie N, Olschewski H, Oudiz RJ, Torres F, Frost A, Ghofrani HA, Badesch DB, McGoon MD, McLaughlin VV, Roecker EB, Gerber MJ, Dufton C, Wiens BL, Rubin LJ: Ambrisentan for the treatment of pulmonary arterial hypertension: results of the ambrisentan in pulmonary arterial hypertension, randomized, double-blind, placebo-controlled, multicenter, efficacy (ARIES) study 1 and 2. Circulation. 2008 Jun 10;117(23):3010-9. doi: 10.1161/CIRCULATIONAHA.107.742510. Epub 2008 May 27.
  • PMID: 22205719
    Venitz J, Zack J, Gillies H, Allard M, Regnault J, Dufton C: Clinical pharmacokinetics and drug-drug interactions of endothelin receptor antagonists in pulmonary arterial hypertension. J Clin Pharmacol. 2012 Dec;52(12):1784-805. doi: 10.1177/0091270011423662. Epub 2011 Dec 28.
  • PMID: 26196225
    Peacock AJ, Zamboni W, Vizza CD: Ambrisentan for the treatment of adults with pulmonary arterial hypertension: a review. Curr Med Res Opin. 2015;31(9):1793-807. doi: 10.1185/03007995.2015.1074890. Epub 2015 Aug 27.
  • PMID: 19920913
    Casserly B, Klinger JR: Ambrisentan for the treatment of pulmonary arterial hypertension. Drug Des Devel Ther. 2009 Feb 6;2:265-80.
  • PMID: 19601701
    Kingman M, Ruggiero R, Torres F: Ambrisentan, an endothelin receptor type A-selective endothelin receptor antagonist, for the treatment of pulmonary arterial hypertension. Expert Opin Pharmacother. 2009 Aug;10(11):1847-58. doi: 10.1517/14656560903061275.
  • PMID: 21299444
    Buckley MS, Wicks LM, Staib RL, Kirejczyk AK, Varker AS, Gibson JJ, Feldman JP: Pharmacokinetic evaluation of ambrisentan. Expert Opin Drug Metab Toxicol. 2011 Mar;7(3):371-80. doi: 10.1517/17425255.2011.557181. Epub 2011 Feb 8.

Contoh Produk & Brand

Produk: 54 • International brands: 4
Produk
  • Ambrisentan
    Tablet, film coated • 10 mg/1 • Oral • US • Generic • Approved
  • Ambrisentan
    Tablet, film coated • 5 mg/1 • Oral • US • Generic • Approved
  • Ambrisentan
    Tablet, film coated • 10 mg/1 • Oral • US • Generic • Approved
  • Ambrisentan
    Tablet, film coated • 5 mg/1 • Oral • US • Generic • Approved
  • Ambrisentan
    Tablet, film coated • 10 mg/1 • Oral • US • Generic • Approved
  • Ambrisentan
    Tablet, film coated • 5 mg/1 • Oral • US • Generic • Approved
  • Ambrisentan
    Tablet, film coated • 10 mg/1 • Oral • US • Generic • Approved
  • Ambrisentan
    Tablet, film coated • 5 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 54 produk.
International Brands
  • Ambrican — Lupin
  • Endobloc — Cipla Ltd.
  • Pulmonext — MSN Labs
  • Zambri — German Remedies Ltd.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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