Aprepitant

DB00673

small molecule approved investigational

Deskripsi

Aprepitant, an antiemetic, is a substance P/neurokinin 1 (NK1) receptor antagonist which, in combination with other antiemetic agents, is indicated for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CI NV).

Struktur Molekul 2D

Berat 534.4267
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 9-13 hours
Volume Distribusi * 70 L
Klirens (Clearance) * Apparent plasma cl=62-90 mL/min

Absorpsi

The mean absolute oral bioavailability of aprepitant is approximately 60 to 65%.

Metabolisme

Aprepitant primarily undergoes CYP3A4-mediated metabolism, as well as minor metabolism mediated by CYP1A2 and CYP2C19. About seven metabolites of aprepitant have been identified in human plasma, which all retain weak pharmacological activity.

Rute Eliminasi

Aprepitant is eliminated primarily by metabolism; aprepitant is not renally excreted. Aprepitant is excreted in the milk of rats. It is not known whether this drug is excreted in human milk.

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

848 Data
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Aprepitant.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Aprepitant.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Aprepitant.
Everolimus The metabolism of Everolimus can be decreased when combined with Aprepitant.
Flibanserin The metabolism of Flibanserin can be decreased when combined with Aprepitant.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Aprepitant.
Ivabradine The metabolism of Ivabradine can be decreased when combined with Aprepitant.
Ivacaftor The metabolism of Ivacaftor can be decreased when combined with Aprepitant.
Lurasidone The metabolism of Lurasidone can be decreased when combined with Aprepitant.
Naloxegol The metabolism of Naloxegol can be decreased when combined with Aprepitant.
Olaparib The metabolism of Olaparib can be decreased when combined with Aprepitant.
Ranolazine The metabolism of Ranolazine can be decreased when combined with Aprepitant.
Sonidegib The metabolism of Sonidegib can be decreased when combined with Aprepitant.
Avanafil The metabolism of Avanafil can be decreased when combined with Aprepitant.
Eplerenone The metabolism of Eplerenone can be decreased when combined with Aprepitant.
Colchicine The metabolism of Colchicine can be decreased when combined with Aprepitant.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Aprepitant.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Aprepitant.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Aprepitant.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Aprepitant.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Aprepitant.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Aprepitant.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Aprepitant.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Aprepitant.
Octylphenoxy polyethoxyethanol The serum concentration of Octylphenoxy polyethoxyethanol can be decreased when it is combined with Aprepitant.
Trestolone The serum concentration of Trestolone can be decreased when it is combined with Aprepitant.
Nonoxynol-9 The serum concentration of Nonoxynol-9 can be decreased when it is combined with Aprepitant.
Cloprostenol The serum concentration of Cloprostenol can be decreased when it is combined with Aprepitant.
Gossypol The serum concentration of Gossypol can be decreased when it is combined with Aprepitant.
Ormeloxifene The serum concentration of Ormeloxifene can be decreased when it is combined with Aprepitant.
Norgestrienone The serum concentration of Norgestrienone can be decreased when it is combined with Aprepitant.
Norethindrone enanthate The serum concentration of Norethindrone enanthate can be decreased when it is combined with Aprepitant.
Segesterone acetate The serum concentration of Segesterone acetate can be decreased when it is combined with Aprepitant.
Etonogestrel The serum concentration of Etonogestrel can be decreased when it is combined with Aprepitant.
Megestrol acetate The serum concentration of Megestrol acetate can be decreased when it is combined with Aprepitant.
Ethynodiol diacetate The serum concentration of Ethynodiol diacetate can be decreased when it is combined with Aprepitant.
Ethinylestradiol The serum concentration of Ethinylestradiol can be decreased when it is combined with Aprepitant.
Norelgestromin The serum concentration of Norelgestromin can be decreased when it is combined with Aprepitant.
Ulipristal The serum concentration of Ulipristal can be decreased when it is combined with Aprepitant.
Dienogest The serum concentration of Dienogest can be decreased when it is combined with Aprepitant.
Norethynodrel The serum concentration of Norethynodrel can be decreased when it is combined with Aprepitant.
Norgestrel The serum concentration of Norgestrel can be decreased when it is combined with Aprepitant.
Gestrinone The serum concentration of Gestrinone can be decreased when it is combined with Aprepitant.
Nomegestrol The serum concentration of Nomegestrol can be decreased when it is combined with Aprepitant.
Chlormadinone The serum concentration of Chlormadinone can be decreased when it is combined with Aprepitant.
Quingestanol The serum concentration of Quingestanol can be decreased when it is combined with Aprepitant.
Demegestone The serum concentration of Demegestone can be decreased when it is combined with Aprepitant.
Etynodiol The serum concentration of Etynodiol can be decreased when it is combined with Aprepitant.
Nomegestrol acetate The serum concentration of Nomegestrol acetate can be decreased when it is combined with Aprepitant.
Diethylstilbestrol The serum concentration of Diethylstilbestrol can be decreased when it is combined with Aprepitant.
Medroxyprogesterone acetate The serum concentration of Medroxyprogesterone acetate can be decreased when it is combined with Aprepitant.
Norgestimate The serum concentration of Norgestimate can be decreased when it is combined with Aprepitant.
Cyproterone acetate The serum concentration of Cyproterone acetate can be decreased when it is combined with Aprepitant.
Desogestrel The serum concentration of Desogestrel can be decreased when it is combined with Aprepitant.
Mestranol The serum concentration of Mestranol can be decreased when it is combined with Aprepitant.
Estrone sulfate The serum concentration of Estrone sulfate can be decreased when it is combined with Aprepitant.
Lynestrenol The serum concentration of Lynestrenol can be decreased when it is combined with Aprepitant.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Aprepitant.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Aprepitant.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Aprepitant.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Aprepitant.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Aprepitant.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Aprepitant.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Aprepitant.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Aprepitant.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Aprepitant.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Aprepitant.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Aprepitant.
Cobimetinib The metabolism of Cobimetinib can be decreased when combined with Aprepitant.
Pitolisant The serum concentration of Aprepitant can be decreased when it is combined with Pitolisant.
Aripiprazole The metabolism of Aripiprazole can be decreased when combined with Aprepitant.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be decreased when combined with Aprepitant.
Metreleptin The metabolism of Aprepitant can be increased when combined with Metreleptin.
Tezacaftor The metabolism of Tezacaftor can be decreased when combined with Aprepitant.
Vincristine The metabolism of Vincristine can be decreased when combined with Aprepitant.
Irinotecan The metabolism of Irinotecan can be decreased when combined with Aprepitant.
Dasatinib The metabolism of Dasatinib can be decreased when combined with Aprepitant.
Romidepsin The metabolism of Romidepsin can be decreased when combined with Aprepitant.
Axitinib The metabolism of Axitinib can be decreased when combined with Aprepitant.
Cabazitaxel The metabolism of Cabazitaxel can be decreased when combined with Aprepitant.
Ponatinib The metabolism of Ponatinib can be decreased when combined with Aprepitant.
Copanlisib The metabolism of Copanlisib can be decreased when combined with Aprepitant.
Bortezomib The metabolism of Bortezomib can be decreased when combined with Aprepitant.
Trabectedin The metabolism of Trabectedin can be decreased when combined with Aprepitant.
Erdafitinib The metabolism of Erdafitinib can be decreased when combined with Aprepitant.
Dofetilide The metabolism of Dofetilide can be decreased when combined with Aprepitant.
Theophylline The metabolism of Theophylline can be decreased when combined with Aprepitant.
Busulfan The metabolism of Busulfan can be decreased when combined with Aprepitant.
Aminophylline The metabolism of Aminophylline can be decreased when combined with Aprepitant.
Digitoxin The metabolism of Digitoxin can be decreased when combined with Aprepitant.
Tianeptine The metabolism of Tianeptine can be decreased when combined with Aprepitant.
Carbamazepine The metabolism of Carbamazepine can be decreased when combined with Aprepitant.
Paclitaxel The metabolism of Paclitaxel can be decreased when combined with Aprepitant.
Sorafenib The metabolism of Sorafenib can be decreased when combined with Aprepitant.
Teniposide The metabolism of Teniposide can be decreased when combined with Aprepitant.
Erlotinib The metabolism of Erlotinib can be decreased when combined with Aprepitant.
Cyclophosphamide The metabolism of Cyclophosphamide can be decreased when combined with Aprepitant.
Tamoxifen The metabolism of Tamoxifen can be decreased when combined with Aprepitant.
Etoposide The metabolism of Etoposide can be decreased when combined with Aprepitant.
Ifosfamide The metabolism of Ifosfamide can be decreased when combined with Aprepitant.

Target Protein

Substance-P receptor TACR1

Referensi & Sumber

Synthesis reference: Mangesh Shivram Sawant, Girish Dixit, Nitin Sharad Chandra Pradhan, Mubeen Ahmad Khan, Sukumar Sinha, "Amorphous and Crystalline Forms of Aprepitant and Processes for the Preparation Thereof." U.S. Patent US20090192161, issued July 30, 2009.

Contoh Produk & Brand

Produk: 42 • International brands: 1
Produk
  • Aponvie
    Emulsion • 32 mg/4.4mL • Intravenous • US • Approved
  • Aprepitant
    Powder • 1 kg/1kg • Not applicable • US
  • Aprepitant
    Capsule • 40 mg/1 • Oral • US • Generic • Approved
  • Aprepitant
    Capsule • 80 mg/1 • Oral • US • Generic • Approved
  • Aprepitant
    Capsule; Kit • - • Oral • US • Generic • Approved
  • Aprepitant
    Capsule; Kit • - • Oral • US • Generic • Approved
  • Aprepitant
    Capsule • 125 mg/1 • Oral • US • Generic • Approved
  • Aprepitant
    Capsule • 40 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 42 produk.
International Brands
  • Aprecap — Glenmark

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul