Peringatan Keamanan

A 40-70% increase in exposure was observed in subjects with severe renal impairment.

Selexipag

DB11362

small molecule approved

Deskripsi

Selexipag was approved by the United States FDA on December 22, 2015 for the treatment of pulmonary arterial hypertension (PAH) to delay disease progression and reduce risk of hospitalization. PAH is a relatively rare disease with usually a poor prognosis requiring more treatment options to prolong long-term outcomes. Marketed by Actelion Pharmaceuticals under brand name Uptravi, selexipag and its active metabolite, ACT-333679 (MRE-269), act as agonists of the prostacyclin receptor to increase vasodilation in the pulmonary circulation and decrease elevated pressure in the blood vessels supplying blood to the lungs.

Struktur Molekul 2D

Berat 496.63
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Selexipag's terminal half life is 0.8-2.5 hours. The active metabolite's terminal half life is 6.2-13.5 hours.
Volume Distribusi -
Klirens (Clearance) On average, 35 L/hour.

Absorpsi

After oral administration, maximum concentrations of selexipag and its metabolite were observed to be reached at 1-3 and 3-4 hours, respectively. Absorption was impaired in the presence of food, resulting in delayed time to maximum concentration as well as ~30% lower peak plasma concentration. However, exposure was not found to be significantly affected by food.

Metabolisme

Selexipag yields its active metabolite by hydrolysis of the acylsulfonamide by the enzyme hepatic carboxylesterase 1. Oxidative metabolism catalyzed by CYP3A4 and CYP2C8 results in hydroxylated and dealkylated products. UGT1A3 and UGT2B7 are involved in the glucuronidation of the active metabolite. Other than active metabolite, other metabolites in circulation do not exceed 3% of the total drug-related material.

Rute Eliminasi

93% in feces, 12% in urine.

Interaksi Obat

1056 Data
Ranolazine The serum concentration of Selexipag can be increased when it is combined with Ranolazine.
Alfuzosin Alfuzosin may increase the hypotensive activities of Selexipag.
Amifostine Selexipag may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Selexipag.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Selexipag.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Selexipag.
Obinutuzumab Selexipag may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Selexipag.
Rituximab Selexipag may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Selexipag.
Midodrine Midodrine may decrease the antihypertensive activities of Selexipag.
Isoetharine Isoetharine may decrease the antihypertensive activities of Selexipag.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Selexipag.
Etomidate Etomidate may decrease the antihypertensive activities of Selexipag.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Selexipag.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Selexipag.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Selexipag.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Selexipag.
Droperidol Droperidol may decrease the antihypertensive activities of Selexipag.
Doxapram Doxapram may decrease the antihypertensive activities of Selexipag.
Atropine Atropine may decrease the antihypertensive activities of Selexipag.
Metaraminol Metaraminol may decrease the antihypertensive activities of Selexipag.
Nicergoline Nicergoline may decrease the antihypertensive activities of Selexipag.
Methoxamine Methoxamine may decrease the antihypertensive activities of Selexipag.
Propiomazine Propiomazine may decrease the antihypertensive activities of Selexipag.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Selexipag.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Selexipag.
Dobutamine Dobutamine may decrease the antihypertensive activities of Selexipag.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Selexipag.
Ritodrine Ritodrine may decrease the antihypertensive activities of Selexipag.
Terbutaline Terbutaline may decrease the antihypertensive activities of Selexipag.
Bitolterol Bitolterol may decrease the antihypertensive activities of Selexipag.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Selexipag.
Naratriptan Naratriptan may decrease the antihypertensive activities of Selexipag.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Selexipag.
Formoterol Formoterol may decrease the antihypertensive activities of Selexipag.
Dopamine Dopamine may decrease the antihypertensive activities of Selexipag.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Selexipag.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Selexipag.
Arbutamine Arbutamine may decrease the antihypertensive activities of Selexipag.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Selexipag.
Arformoterol Arformoterol may decrease the antihypertensive activities of Selexipag.
Fenoterol Fenoterol may decrease the antihypertensive activities of Selexipag.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Selexipag.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Selexipag.
Ephedrine Ephedrine may decrease the antihypertensive activities of Selexipag.
Mephentermine Mephentermine may decrease the antihypertensive activities of Selexipag.
Procaterol Procaterol may decrease the antihypertensive activities of Selexipag.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Selexipag.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Selexipag.
Bambuterol Bambuterol may decrease the antihypertensive activities of Selexipag.
MMDA MMDA may decrease the antihypertensive activities of Selexipag.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Selexipag.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Selexipag.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Selexipag.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Selexipag.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Selexipag.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Selexipag.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Selexipag.
Metamfetamine Metamfetamine may decrease the antihypertensive activities of Selexipag.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Selexipag.
Periciazine Periciazine may decrease the antihypertensive activities of Selexipag.
Acepromazine Acepromazine may decrease the antihypertensive activities of Selexipag.
Thioproperazine Thioproperazine may decrease the antihypertensive activities of Selexipag.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Selexipag.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Selexipag.
Amineptine Amineptine may decrease the antihypertensive activities of Selexipag.
Amibegron Amibegron may decrease the antihypertensive activities of Selexipag.
Naluzotan Naluzotan may decrease the antihypertensive activities of Selexipag.
Pizotifen Pizotifen may decrease the antihypertensive activities of Selexipag.
Solabegron Solabegron may decrease the antihypertensive activities of Selexipag.
Droxidopa Droxidopa may decrease the antihypertensive activities of Selexipag.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Selexipag.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Selexipag.
Xylometazoline Xylometazoline may decrease the antihypertensive activities of Selexipag.
Isometheptene Isometheptene may decrease the antihypertensive activities of Selexipag.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Selexipag.
Naphazoline Naphazoline may decrease the antihypertensive activities of Selexipag.
Saralasin Saralasin may decrease the antihypertensive activities of Selexipag.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Selexipag.
Cinitapride Cinitapride may decrease the antihypertensive activities of Selexipag.
Tyramine Tyramine may decrease the antihypertensive activities of Selexipag.
Adrafinil Adrafinil may decrease the antihypertensive activities of Selexipag.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Selexipag.
Hexoprenaline Hexoprenaline may decrease the antihypertensive activities of Selexipag.
Etilefrine Etilefrine may decrease the antihypertensive activities of Selexipag.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Selexipag.
Butriptyline Butriptyline may decrease the antihypertensive activities of Selexipag.
Dosulepin Dosulepin may decrease the antihypertensive activities of Selexipag.
Cirazoline Cirazoline may decrease the antihypertensive activities of Selexipag.
Synephrine Synephrine may decrease the antihypertensive activities of Selexipag.
Moxisylyte Moxisylyte may decrease the antihypertensive activities of Selexipag.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Selexipag.
Iofetamine I-123 Iofetamine I-123 may decrease the antihypertensive activities of Selexipag.
Racepinephrine Racepinephrine may decrease the antihypertensive activities of Selexipag.
DL-Methylephedrine DL-Methylephedrine may decrease the antihypertensive activities of Selexipag.
Amitraz Amitraz may decrease the antihypertensive activities of Selexipag.
Medetomidine Medetomidine may decrease the antihypertensive activities of Selexipag.
Xylazine Xylazine may decrease the antihypertensive activities of Selexipag.
Atipamezole Atipamezole may decrease the antihypertensive activities of Selexipag.

Target Protein

Prostacyclin receptor PTGIR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 26567613
    Sharma K: Selexipag for the treatment of pulmonary arterial hypertension. Expert Rev Respir Med. 2016 Jan;10(1):1-3. doi: 10.1586/17476348.2016.1121103. Epub 2015 Dec 7.
  • PMID: 25850750
    Kaufmann P, Okubo K, Bruderer S, Mant T, Yamada T, Dingemanse J, Mukai H: Pharmacokinetics and Tolerability of the Novel Oral Prostacyclin IP Receptor Agonist Selexipag. Am J Cardiovasc Drugs. 2015 Jun;15(3):195-203. doi: 10.1007/s40256-015-0117-4.

Contoh Produk & Brand

Produk: 33 • International brands: 0
Produk
  • Uptravi
    Tablet, coated • 200 ug/1 • Oral • US • Approved
  • Uptravi
    Tablet, coated • 400 ug/1 • Oral • US • Approved
  • Uptravi
    Tablet, coated • 600 ug/1 • Oral • US • Approved
  • Uptravi
    Tablet, coated • 800 ug/1 • Oral • US • Approved
  • Uptravi
    Tablet, coated • 1000 ug/1 • Oral • US • Approved
  • Uptravi
    Tablet, coated • 1200 ug/1 • Oral • US • Approved
  • Uptravi
    Tablet, coated • 1400 ug/1 • Oral • US • Approved
  • Uptravi
    Tablet, coated • 1600 ug/1 • Oral • US • Approved
Menampilkan 8 dari 33 produk.

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