Peringatan Keamanan

The most common adverse reactions reported during clinical trials were jaundice (13%), ocular icterus (15%), and nausea (12%).

Cobicistat

DB09065

small molecule approved

Deskripsi

Cobicistat, marketed under the name Tybost (formerly GS-9350), indicated for treating infection with human immunodeficiency virus (HIV). Although it does not have any anti-HIV activity, cobicistat acts as a pharmacokinetic enhancer by inhibiting cytochrome P450 3A isoforms (CYP3A) and therefore increases the systemic exposure of coadministered agents that are metabolized by CYP3A enzymes. More specifically, cobicistat is indicated to increase systemic exposure of atazanavir or darunavir (once daily dosing regimen) in combination with other antiretroviral agents in the treatment of HIV-1 infection. Increasing systemic exposure of anti-retrovirals (ARVs) without increasing dosage allows for better treatment outcomes and a decreased side effect profile.

Struktur Molekul 2D

Berat 776.03
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal plasma half-life of cobicistat is approximately 3 to 4 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Median peak plasma concentrations were observed at 3.5 hours post-dose.

Metabolisme

Cobicistat is metabolized by CYP3A and to a minor extent by CYP2D6 enzymes and does not undergo glucuronidation.

Rute Eliminasi

With single dose administration of 14C cobicistat after multiple dosing of cobicistat for six days, the mean percent of the administered dose excreted in feces and urine was 86.2% and 8.2%, respectively.

Interaksi Makanan

3 Data
  • 1. Avoid St. John's Wort. St. John's Wort is contraindicated as it induces the CYP3A metabolism of cobicistat and may reduce its serum concentration.
  • 2. Take at the same time every day.
  • 3. Take with food.

Interaksi Obat

774 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Cobicistat.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Cobicistat.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Cobicistat.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Cobicistat.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Cobicistat.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Cobicistat.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Cobicistat.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Cobicistat.
Silodosin The excretion of Silodosin can be decreased when combined with Cobicistat.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Cobicistat.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Cobicistat.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Cobicistat.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Cobicistat.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Cobicistat.
Dofetilide The serum concentration of Dofetilide can be increased when it is combined with Cobicistat.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Cobicistat.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Cobicistat.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Cobicistat.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Cobicistat.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Cobicistat.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Cobicistat.
Vardenafil The serum concentration of Vardenafil can be increased when it is combined with Cobicistat.
Tenofovir The serum concentration of Tenofovir can be increased when it is combined with Cobicistat.
Methadone The serum concentration of Methadone can be increased when it is combined with Cobicistat.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Cobicistat.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Cobicistat.
Bosentan The serum concentration of Bosentan can be increased when it is combined with Cobicistat.
Carbamazepine The metabolism of Cobicistat can be increased when combined with Carbamazepine.
Cisapride The risk or severity of QTc prolongation and Cardiac Arrhythmia can be increased when Cobicistat is combined with Cisapride.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Cobicistat.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Cobicistat.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Cobicistat.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Cobicistat.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Cobicistat.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Cobicistat.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Cobicistat.
Oxcarbazepine The metabolism of Cobicistat can be increased when combined with Oxcarbazepine.
Primidone The serum concentration of Cobicistat can be decreased when it is combined with Primidone.
Methylphenobarbital The serum concentration of Cobicistat can be decreased when it is combined with Methylphenobarbital.
Phenobarbital The serum concentration of Cobicistat can be decreased when it is combined with Phenobarbital.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Cobicistat.
Buprenorphine The serum concentration of Buprenorphine can be increased when it is combined with Cobicistat.
Ketoconazole The serum concentration of Cobicistat can be increased when it is combined with Ketoconazole.
Atorvastatin The serum concentration of Atorvastatin can be increased when it is combined with Cobicistat.
Itraconazole The metabolism of Cobicistat can be decreased when combined with Itraconazole.
Dexamethasone The serum concentration of Cobicistat can be decreased when it is combined with Dexamethasone.
Methysergide The serum concentration of Methysergide can be increased when it is combined with Cobicistat.
Cabergoline The serum concentration of Cabergoline can be increased when it is combined with Cobicistat.
Dihydroergotamine The serum concentration of Dihydroergotamine can be increased when it is combined with Cobicistat.
Methylergometrine The serum concentration of Methylergometrine can be increased when it is combined with Cobicistat.
Lisuride The serum concentration of Lisuride can be increased when it is combined with Cobicistat.
Ergotamine The serum concentration of Ergotamine can be increased when it is combined with Cobicistat.
Nicergoline The serum concentration of Nicergoline can be increased when it is combined with Cobicistat.
Ergoloid mesylate The serum concentration of Ergoloid mesylate can be increased when it is combined with Cobicistat.
Pergolide The serum concentration of Pergolide can be increased when it is combined with Cobicistat.
Bromocriptine The serum concentration of Bromocriptine can be increased when it is combined with Cobicistat.
Ergometrine The serum concentration of Ergometrine can be increased when it is combined with Cobicistat.
Lysergic acid diethylamide The serum concentration of Lysergic acid diethylamide can be increased when it is combined with Cobicistat.
Dihydroergocornine The serum concentration of Dihydroergocornine can be increased when it is combined with Cobicistat.
Dihydroergocristine The serum concentration of Dihydroergocristine can be increased when it is combined with Cobicistat.
Dihydroergocryptine The serum concentration of Dihydroergocryptine can be increased when it is combined with Cobicistat.
Terguride The serum concentration of Terguride can be increased when it is combined with Cobicistat.
Metergoline The serum concentration of Metergoline can be increased when it is combined with Cobicistat.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Cobicistat.
Vincristine The serum concentration of Vincristine can be increased when it is combined with Cobicistat.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Cobicistat.
Diethylstilbestrol The serum concentration of Diethylstilbestrol can be decreased when it is combined with Cobicistat.
Etonogestrel The serum concentration of Etonogestrel can be decreased when it is combined with Cobicistat.
Desogestrel The serum concentration of Desogestrel can be decreased when it is combined with Cobicistat.
Megestrol acetate The serum concentration of Megestrol acetate can be decreased when it is combined with Cobicistat.
Levonorgestrel The serum concentration of Levonorgestrel can be decreased when it is combined with Cobicistat.
Progesterone The serum concentration of Progesterone can be decreased when it is combined with Cobicistat.
Medroxyprogesterone acetate The serum concentration of Medroxyprogesterone acetate can be decreased when it is combined with Cobicistat.
Norethisterone The serum concentration of Norethisterone can be decreased when it is combined with Cobicistat.
Estradiol The serum concentration of Estradiol can be decreased when it is combined with Cobicistat.
Ethynodiol diacetate The serum concentration of Ethynodiol diacetate can be decreased when it is combined with Cobicistat.
Norgestimate The serum concentration of Norgestimate can be decreased when it is combined with Cobicistat.
Ethinylestradiol The serum concentration of Ethinylestradiol can be decreased when it is combined with Cobicistat.
Mestranol The serum concentration of Mestranol can be decreased when it is combined with Cobicistat.
Drospirenone The serum concentration of Drospirenone can be decreased when it is combined with Cobicistat.
Estrone sulfate The serum concentration of Estrone sulfate can be decreased when it is combined with Cobicistat.
Octylphenoxy polyethoxyethanol The serum concentration of Octylphenoxy polyethoxyethanol can be decreased when it is combined with Cobicistat.
Cyproterone acetate The serum concentration of Cyproterone acetate can be decreased when it is combined with Cobicistat.
Trestolone The serum concentration of Trestolone can be decreased when it is combined with Cobicistat.
Norelgestromin The serum concentration of Norelgestromin can be decreased when it is combined with Cobicistat.
Gestodene The serum concentration of Gestodene can be decreased when it is combined with Cobicistat.
Hydroxyprogesterone caproate The serum concentration of Hydroxyprogesterone caproate can be decreased when it is combined with Cobicistat.
Ulipristal The serum concentration of Ulipristal can be decreased when it is combined with Cobicistat.
Dienogest The serum concentration of Dienogest can be decreased when it is combined with Cobicistat.
Norethynodrel The serum concentration of Norethynodrel can be decreased when it is combined with Cobicistat.
Norgestrel The serum concentration of Norgestrel can be decreased when it is combined with Cobicistat.
Cloprostenol The serum concentration of Cloprostenol can be decreased when it is combined with Cobicistat.
Gestrinone The serum concentration of Gestrinone can be decreased when it is combined with Cobicistat.
Nomegestrol The serum concentration of Nomegestrol can be decreased when it is combined with Cobicistat.
Lynestrenol The serum concentration of Lynestrenol can be decreased when it is combined with Cobicistat.
Gossypol The serum concentration of Gossypol can be decreased when it is combined with Cobicistat.
Ormeloxifene The serum concentration of Ormeloxifene can be decreased when it is combined with Cobicistat.
Chlormadinone The serum concentration of Chlormadinone can be decreased when it is combined with Cobicistat.
Norgestrienone The serum concentration of Norgestrienone can be decreased when it is combined with Cobicistat.
Quingestanol The serum concentration of Quingestanol can be decreased when it is combined with Cobicistat.

Target Protein

Cytochrome P450 3A4 CYP3A4
Cytochrome P450 3A5 CYP3A5
Cytochrome P450 3A7 CYP3A7

Referensi & Sumber

Artikel (PubMed)
  • PMID: 20683270
    German P, Warren D, West S, Hui J, Kearney BP: Pharmacokinetics and bioavailability of an integrase and novel pharmacoenhancer-containing single-tablet fixed-dose combination regimen for the treatment of HIV. J Acquir Immune Defic Syndr. 2010 Nov;55(3):323-9. doi: 10.1097/QAI.0b013e3181eb376b.
  • PMID: 20043009
    Mathias AA, German P, Murray BP, Wei L, Jain A, West S, Warren D, Hui J, Kearney BP: Pharmacokinetics and pharmacodynamics of GS-9350: a novel pharmacokinetic enhancer without anti-HIV activity. Clin Pharmacol Ther. 2010 Mar;87(3):322-9. doi: 10.1038/clpt.2009.228. Epub 2009 Dec 30.
  • PMID: 25164142
    Larson KB, Wang K, Delille C, Otofokun I, Acosta EP: Pharmacokinetic enhancers in HIV therapeutics. Clin Pharmacokinet. 2014 Oct;53(10):865-72. doi: 10.1007/s40262-014-0167-9.
  • PMID: 22850510
    Lepist EI, Phan TK, Roy A, Tong L, Maclennan K, Murray B, Ray AS: Cobicistat boosts the intestinal absorption of transport substrates, including HIV protease inhibitors and GS-7340, in vitro. Antimicrob Agents Chemother. 2012 Oct;56(10):5409-13. doi: 10.1128/AAC.01089-12. Epub 2012 Jul 30.

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