Peringatan Keamanan

Carcinogenicity studies in mice and rats were conducted with nelfinavir at oral doses up to 1000 mg/kg/day. No evidence of a
tumorigenic effect was noted in mice at systemic exposures (Cmax) up to 9-fold those measured in humans at the recommended
therapeutic dose (750 mg TID or 1250 mg BID). In rats, thyroid follicular cell adenomas and carcinomas were increased in males at
300 mg/kg/day and higher and in females at 1000 mg/kg/day. Systemic exposures (Cmax) at 300 and 1000 mg/kg/day were 1- to 3-fold, respectively, those measured in humans at the recommended therapeutic dose. Repeated administration of nelfinavir to rats produced
effects consistent with hepatic microsomal enzyme induction and increased thyroid hormone deposition; these effects predispose rats, but not humans, to thyroid follicular cell neoplasms. Nelfinavir showed no evidence of mutagenic or clastogenic activity in a battery of in vitro and in vivo genetic toxicology assays. These studies included bacterial mutation assays in S. typhimurium and E. coli, a mouse lymphoma tyrosine kinase assay, a chromosomal aberration assay in human lymphocytes, and an in vivo mouse bone marrow micronucleus assay.L36485

Nelfinavir produced no effects on either male or female mating and fertility or embryo survival in rats at systemic exposures
comparable to the human therapeutic exposure.L36485

Human experience of acute overdose with nelfinavir is limited. There is no specific antidote for overdose with VIRACEPT. If
indicated, elimination of unabsorbed drug should be achieved by emesis or gastric lavage. Administration of activated charcoal may
also be used to aid the removal of unabsorbed drug. Since nelfinavir is highly protein-bound, dialysis is unlikely to significantly remove the drug from blood.L36485

Nelfinavir

DB00220

small molecule approved

Deskripsi

Nelfinavir is a potent HIV-1 protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children. Nelfinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.L36485

Struktur Molekul 2D

Berat 567.782
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 half-life in plasma was typically 3.5 to 5 hours.[L36485]
Volume Distribusi The apparent volume of distribution following oral administration of nelfinavir was 2-7 L/kg.[L36485]
Klirens (Clearance) Oral clearance estimates after single doses (24-33 L/h) and multiple doses (26-61 L/h) indicate that nelfinavir is a drug with medium to high hepatic bioavailability.[L41608]

Absorpsi

Well absorbed following oral administration.

Metabolisme

Unchanged nelfinavir comprised 82-86% of the total plasma radioactivity after a single oral 750 mg dose of 14C-nelfinavir. In vitro, multiple cytochrome P-450 enzymes including CYP3A and CYP2C19 are responsible for the metabolism of nelfinavir. One major and several minor oxidative metabolites were found in plasma. The major oxidative metabolite has in vitro antiviral activity comparable to the parent drug.L36485

Rute Eliminasi

The majority (87%) of an oral 750 mg dose containing 14C-nelfinavir was recovered in the feces; fecal radioactivity consisted of numerous oxidative metabolites (78%) and unchanged nelfinavir (22%). Only 1–2% of the dose was recovered in urine, of which unchanged nelfinavir was the major component.L36485

Interaksi Makanan

1 Data
  • 1. Take with food. Food increases exposure and decreases pharmacokinetic variability.

Interaksi Obat

1286 Data
Reserpine Reserpine may decrease the excretion rate of Nelfinavir which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Nelfinavir which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Nelfinavir which could result in a higher serum level.
Valinomycin Valinomycin may decrease the excretion rate of Nelfinavir which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Nelfinavir which could result in a higher serum level.
Pravastatin The serum concentration of Pravastatin can be decreased when it is combined with Nelfinavir.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Nelfinavir.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Nelfinavir.
Azithromycin The serum concentration of Azithromycin can be increased when it is combined with Nelfinavir.
Omeprazole The serum concentration of Nelfinavir can be decreased when it is combined with Omeprazole.
Lansoprazole The serum concentration of Nelfinavir can be decreased when it is combined with Lansoprazole.
Esomeprazole The serum concentration of Nelfinavir can be decreased when it is combined with Esomeprazole.
Rabeprazole The serum concentration of Nelfinavir can be decreased when it is combined with Rabeprazole.
Dexlansoprazole The serum concentration of Nelfinavir can be decreased when it is combined with Dexlansoprazole.
Dexrabeprazole The serum concentration of Nelfinavir can be decreased when it is combined with Dexrabeprazole.
Ilaprazole The serum concentration of Nelfinavir can be decreased when it is combined with Ilaprazole.
Vonoprazan The absorption of Nelfinavir can be decreased when combined with Vonoprazan.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Nelfinavir.
Cisapride The serum concentration of Cisapride can be increased when it is combined with Nelfinavir.
Clarithromycin The serum concentration of Clarithromycin can be increased when it is combined with Nelfinavir.
Cyclophosphamide The serum concentration of the active metabolites of Cyclophosphamide can be increased when Cyclophosphamide is used in combination with Nelfinavir.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Nelfinavir.
Phenytoin The serum concentration of Nelfinavir can be decreased when it is combined with Phenytoin.
Fosphenytoin The serum concentration of Nelfinavir can be decreased when it is combined with Fosphenytoin.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Nelfinavir.
Lopinavir The serum concentration of Lopinavir can be decreased when it is combined with Nelfinavir.
Methadone The serum concentration of Methadone can be decreased when it is combined with Nelfinavir.
Quinine The metabolism of Quinine can be decreased when combined with Nelfinavir.
Quinidine The metabolism of Quinidine can be decreased when combined with Nelfinavir.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Nelfinavir.
Rifabutin The serum concentration of the active metabolites of Rifabutin can be increased when Rifabutin is used in combination with Nelfinavir.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Nelfinavir.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Nelfinavir.
Alprazolam The serum concentration of Alprazolam can be increased when it is combined with Nelfinavir.
Olanzapine Olanzapine can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cimetidine Cimetidine can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Nizatidine Nizatidine can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ranitidine Ranitidine can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Famotidine Famotidine can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methantheline Methantheline can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Promethazine Promethazine can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Doxepin Doxepin can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Asenapine Asenapine can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Metiamide Metiamide can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Roxatidine acetate Roxatidine acetate can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lafutidine Lafutidine can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lavoltidine Lavoltidine can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Niperotidine Niperotidine can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Epinastine Epinastine can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Deferasirox The metabolism of Deferasirox can be increased when combined with Nelfinavir.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Nelfinavir.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Nelfinavir.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Nelfinavir.
Troglitazone Troglitazone may decrease the excretion rate of Nelfinavir which could result in a higher serum level.
Liothyronine The metabolism of Liothyronine can be increased when combined with Nelfinavir.
Indomethacin The metabolism of Indomethacin can be increased when combined with Nelfinavir.
Minoxidil The metabolism of Minoxidil can be increased when combined with Nelfinavir.
Raloxifene The metabolism of Raloxifene can be increased when combined with Nelfinavir.
Lamotrigine The metabolism of Lamotrigine can be increased when combined with Nelfinavir.
Labetalol The metabolism of Labetalol can be increased when combined with Nelfinavir.
Furosemide The metabolism of Furosemide can be increased when combined with Nelfinavir.
Naltrexone The metabolism of Naltrexone can be increased when combined with Nelfinavir.
Flurbiprofen The metabolism of Flurbiprofen can be increased when combined with Nelfinavir.
Naproxen The metabolism of Naproxen can be increased when combined with Nelfinavir.
Propofol The metabolism of Propofol can be increased when combined with Nelfinavir.
Ezetimibe The metabolism of Ezetimibe can be increased when combined with Nelfinavir.
Ketoprofen The metabolism of Ketoprofen can be increased when combined with Nelfinavir.
Abacavir The metabolism of Abacavir can be increased when combined with Nelfinavir.
Alvocidib The metabolism of Alvocidib can be increased when combined with Nelfinavir.
Ezogabine The metabolism of Ezogabine can be increased when combined with Nelfinavir.
Eltrombopag The metabolism of Eltrombopag can be increased when combined with Nelfinavir.
Bazedoxifene The metabolism of Bazedoxifene can be increased when combined with Nelfinavir.
Muraglitazar The metabolism of Muraglitazar can be increased when combined with Nelfinavir.
Gavestinel The metabolism of Gavestinel can be increased when combined with Nelfinavir.
Raltegravir The metabolism of Raltegravir can be increased when combined with Nelfinavir.
Dolutegravir The metabolism of Dolutegravir can be increased when combined with Nelfinavir.
Eslicarbazepine acetate The metabolism of Eslicarbazepine acetate can be increased when combined with Nelfinavir.
Delafloxacin The metabolism of Delafloxacin can be increased when combined with Nelfinavir.
Eslicarbazepine The metabolism of Eslicarbazepine can be increased when combined with Nelfinavir.
Fulvestrant The metabolism of Fulvestrant can be increased when combined with Nelfinavir.
Glipizide The metabolism of Glipizide can be increased when combined with Nelfinavir.
Dexibuprofen The metabolism of Dexibuprofen can be increased when combined with Nelfinavir.
Elagolix The excretion of Elagolix can be decreased when combined with Nelfinavir.
Letermovir The metabolism of Letermovir can be increased when combined with Nelfinavir.
Cabotegravir The metabolism of Cabotegravir can be increased when combined with Nelfinavir.
Febuxostat The metabolism of Febuxostat can be increased when combined with Nelfinavir.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Nelfinavir.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Nelfinavir.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Nelfinavir.
Garlic Garlic can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Insulin human The therapeutic efficacy of Insulin human can be decreased when used in combination with Nelfinavir.
Insulin lispro The therapeutic efficacy of Insulin lispro can be decreased when used in combination with Nelfinavir.
Insulin glargine The therapeutic efficacy of Insulin glargine can be decreased when used in combination with Nelfinavir.
Insulin pork The therapeutic efficacy of Insulin pork can be decreased when used in combination with Nelfinavir.
Glimepiride The therapeutic efficacy of Glimepiride can be decreased when used in combination with Nelfinavir.
Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Nelfinavir.
Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Nelfinavir.
Miglitol The therapeutic efficacy of Miglitol can be decreased when used in combination with Nelfinavir.
Chlorpropamide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Nelfinavir.
Tolazamide The therapeutic efficacy of Tolazamide can be decreased when used in combination with Nelfinavir.

Target Protein

HIV-1 protease HIV-1 protease

Referensi & Sumber

Artikel (PubMed)
  • PMID: 9397180
    Kaldor SW, Kalish VJ, Davies JF 2nd, Shetty BV, Fritz JE, Appelt K, Burgess JA, Campanale KM, Chirgadze NY, Clawson DK, Dressman BA, Hatch SD, Khalil DA, Kosa MB, Lubbehusen PP, Muesing MA, Patick AK, Reich SH, Su KS, Tatlock JH: Viracept (nelfinavir mesylate, AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease. J Med Chem. 1997 Nov 21;40(24):3979-85.
  • PMID: 23754941
    Konnyu B, Sadiq SK, Turanyi T, Hirmondo R, Muller B, Krausslich HG, Coveney PV, Muller V: Gag-Pol processing during HIV-1 virion maturation: a systems biology approach. PLoS Comput Biol. 2013;9(6):e1003103. doi: 10.1371/journal.pcbi.1003103. Epub 2013 Jun 6.
  • PMID: 29123989
    Takagi S, Momose F, Morikawa Y: FRET analysis of HIV-1 Gag and GagPol interactions. FEBS Open Bio. 2017 Oct 19;7(11):1815-1825. doi: 10.1002/2211-5463.12328. eCollection 2017 Nov.
  • PMID: 26296708
    McDonald MG, Au NT, Rettie AE: P450-Based Drug-Drug Interactions of Amiodarone and its Metabolites: Diversity of Inhibitory Mechanisms. Drug Metab Dispos. 2015 Nov;43(11):1661-9. doi: 10.1124/dmd.115.065623. Epub 2015 Aug 21.

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