Peringatan Keamanan

Daily oral administration of netupitant in rats at doses up to 30 mg/kg (1.9 times the human AUC in male rats and 3.7 times the human AUC in female rats at the recommended human dose) had no effects on fertility or reproductive performance.

Netupitant

DB09048

small molecule approved investigational

Deskripsi

Netupitant is an antiemitic drug approved by the FDA in October 2014 for use in combination with palonosetron for the prevention of acute and delayed vomiting and nausea associated with cancer chemotherapy including highly emetogenic chemotherapy. Netupitant is a neurokinin 1 receptor antagonist. The combination drug is marketed by Eisai Inc. and Helsinn Therapeutics (U.S.) Inc. under the brand Akynzeo.

Struktur Molekul 2D

Berat 578.603
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 96 hours with CV% of 61.
Volume Distribusi In cancer patients, Vz/F: 1982 ± 906 L (mean ± SD).
Klirens (Clearance) Estimated systemic clearance of 20.3 ± 9.2 L/h (mean ± SD).

Absorpsi

Upon oral administration of a single dose of netupitant, netupitant started to be measurable in plasma between 15 minutes and 3 hours after dosing. Plasma concentrations reached Cmax in approximately 5 hours. There was a greater than dose-proportional increase in the systemic exposure with the dose increase from 10 mg to 300 mg and a dose-proportional increase in systemic exposure with a dose increase from 300 mg to 450 mg.

Metabolisme

Once absorbed, netupitant is extensively metabolized to form three major metabolites: desmethyl derivative, M1; N-oxide derivative, M2; and OH-methyl derivative, M3. Metabolism is mediated primarily by CYP3A4 and to a lesser extent by CYP2C9 and CYP2D6. Metabolites M1, M2 and M3 were shown to bind to the substance P/neurokinin 1 (NK1) receptor.

Rute Eliminasi

Primarily fecal.

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of netupitant, which may increase its serum concentration.
  • 2. Avoid St. John's Wort. This herb induces the CYP3A metabolism of netupitant and may reduce its serum concentration.
  • 3. Take with or without food.

Interaksi Obat

1152 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Netupitant.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Netupitant.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Netupitant.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Netupitant.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Netupitant.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Netupitant.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Netupitant.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Netupitant.
Silodosin The excretion of Silodosin can be decreased when combined with Netupitant.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Netupitant.
Phenytoin The metabolism of Netupitant can be increased when combined with Phenytoin.
Fosphenytoin The metabolism of Netupitant can be increased when combined with Fosphenytoin.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Netupitant.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Netupitant.
Everolimus The metabolism of Everolimus can be decreased when combined with Netupitant.
Flibanserin The metabolism of Flibanserin can be decreased when combined with Netupitant.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Netupitant.
Ivabradine The metabolism of Ivabradine can be decreased when combined with Netupitant.
Ivacaftor The metabolism of Ivacaftor can be decreased when combined with Netupitant.
Lurasidone The metabolism of Lurasidone can be decreased when combined with Netupitant.
Olaparib The metabolism of Olaparib can be decreased when combined with Netupitant.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Netupitant.
Sonidegib The metabolism of Sonidegib can be decreased when combined with Netupitant.
Avanafil The metabolism of Avanafil can be decreased when combined with Netupitant.
Eplerenone The metabolism of Eplerenone can be decreased when combined with Netupitant.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Netupitant.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Netupitant.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Netupitant.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Netupitant.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Netupitant.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Netupitant.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Netupitant.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Netupitant.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Netupitant.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Netupitant.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Netupitant.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Netupitant.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Netupitant.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Netupitant.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Netupitant.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Netupitant.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Netupitant.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Netupitant.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Netupitant.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Netupitant.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Netupitant.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Netupitant.
Mirabegron The serum concentration of Netupitant can be increased when it is combined with Mirabegron.
Dexamethasone The metabolism of Dexamethasone can be decreased when combined with Netupitant.
Vincristine The excretion of Vincristine can be decreased when combined with Netupitant.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Netupitant.
Bexarotene The metabolism of Netupitant can be increased when combined with Bexarotene.
Nafcillin The metabolism of Netupitant can be increased when combined with Nafcillin.
Modafinil The metabolism of Netupitant can be increased when combined with Modafinil.
Etravirine The metabolism of Netupitant can be increased when combined with Etravirine.
Echinacea The metabolism of Netupitant can be increased when combined with Echinacea.
Dexamethasone acetate The metabolism of Netupitant can be increased when combined with Dexamethasone acetate.
Cyclosporine The metabolism of Netupitant can be decreased when combined with Cyclosporine.
Imipramine The metabolism of Netupitant can be decreased when combined with Imipramine.
Metoprolol The metabolism of Netupitant can be decreased when combined with Metoprolol.
Venlafaxine The metabolism of Venlafaxine can be decreased when combined with Netupitant.
Clozapine The serum concentration of Clozapine can be increased when it is combined with Netupitant.
Quinine The metabolism of Netupitant can be decreased when combined with Quinine.
Cimetidine The metabolism of Netupitant can be decreased when combined with Cimetidine.
Fluvoxamine The metabolism of Netupitant can be decreased when combined with Fluvoxamine.
Abiraterone The metabolism of Netupitant can be decreased when combined with Abiraterone.
Nicardipine The metabolism of Netupitant can be decreased when combined with Nicardipine.
Sulfaphenazole The metabolism of Netupitant can be decreased when combined with Sulfaphenazole.
Tranylcypromine The metabolism of Netupitant can be decreased when combined with Tranylcypromine.
Manidipine The metabolism of Netupitant can be decreased when combined with Manidipine.
Rucaparib The metabolism of Netupitant can be decreased when combined with Rucaparib.
Clobazam The serum concentration of Netupitant can be increased when it is combined with Clobazam.
Primaquine The metabolism of Netupitant can be decreased when combined with Primaquine.
Fusidic acid The metabolism of Netupitant can be decreased when combined with Fusidic acid.
Cholecalciferol The metabolism of Netupitant can be decreased when combined with Cholecalciferol.
Duloxetine The metabolism of Netupitant can be decreased when combined with Duloxetine.
Chlorpromazine The metabolism of Netupitant can be decreased when combined with Chlorpromazine.
Celecoxib The metabolism of Netupitant can be decreased when combined with Celecoxib.
Chloroquine The metabolism of Netupitant can be decreased when combined with Chloroquine.
Perhexiline The metabolism of Netupitant can be decreased when combined with Perhexiline.
Lorcaserin The metabolism of Netupitant can be decreased when combined with Lorcaserin.
Panobinostat The metabolism of Netupitant can be decreased when combined with Panobinostat.
Vilazodone The metabolism of Netupitant can be decreased when combined with Vilazodone.
Rolapitant The metabolism of Netupitant can be decreased when combined with Rolapitant.
Asunaprevir The metabolism of Netupitant can be decreased when combined with Asunaprevir.
Tegaserod The metabolism of Netupitant can be decreased when combined with Tegaserod.
Phenylbutyric acid The metabolism of Netupitant can be decreased when combined with Phenylbutyric acid.
Ritanserin The metabolism of Netupitant can be decreased when combined with Ritanserin.
Rhein The metabolism of Netupitant can be decreased when combined with Rhein.
Terbinafine The metabolism of Netupitant can be decreased when combined with Terbinafine.
Lumefantrine The metabolism of Netupitant can be decreased when combined with Lumefantrine.
Darifenacin The metabolism of Netupitant can be decreased when combined with Darifenacin.
Desipramine The metabolism of Netupitant can be decreased when combined with Desipramine.
Dosulepin The metabolism of Netupitant can be decreased when combined with Dosulepin.
Thioridazine The metabolism of Netupitant can be decreased when combined with Thioridazine.
Paroxetine The metabolism of Netupitant can be decreased when combined with Paroxetine.
Cinacalcet The metabolism of Netupitant can be decreased when combined with Cinacalcet.
Bupropion The metabolism of Netupitant can be decreased when combined with Bupropion.
Orphenadrine The metabolism of Netupitant can be decreased when combined with Orphenadrine.
Propafenone The metabolism of Netupitant can be decreased when combined with Propafenone.

Target Protein

Substance-P receptor TACR1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25687374
    Darmani NA, Zhong W, Chebolu S, Mercadante F: Differential and additive suppressive effects of 5-HT3 (palonosetron)- and NK1 (netupitant)-receptor antagonists on cisplatin-induced vomiting and ERK1/2, PKA and PKC activation. Pharmacol Biochem Behav. 2015 Apr;131:104-11. doi: 10.1016/j.pbb.2015.02.010. Epub 2015 Feb 14.

Contoh Produk & Brand

Produk: 7 • International brands: 0
Produk
  • Akynzeo
    Capsule • - • Oral • US • Approved
  • Akynzeo
    Capsule • - • Oral • US • Approved
  • Akynzeo
    Capsule • - • Oral • Canada • Approved
  • Akynzeo
    Capsule • - • Oral • EU • Approved
  • Akynzeo
    Capsule • - • Oral • EU • Approved
  • Akynzeo
    Injection, powder, for solution • - • Intravenous • EU • Approved
  • Akynzeo
    Injection, solution, concentrate • - • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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