Fosamprenavir

DB01319

small molecule approved

Deskripsi

Fosamprenavir is a prodrug of amprenavir, an inhibitor of human immunodeficiency virus (HIV) protease.

Struktur Molekul 2D

Berat 585.607
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The plasma elimination half-life of amprenavir (the active metabolite) is approximately 7.7 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

The absolute oral bioavailability of amprenavir after administration of fosamprenavir in humans has not been established. After administration of a single 1,400 mg dose in the fasted state, fosamprenavir oral suspension (50 mg/mL) and fosamprenavir tablets (700 mg) provided similar amprenavir exposures (AUC), however, the Cmax of amprenavir after administration of the suspension formulation was 14.5 % higher compared with the tablet.

Metabolisme

In the gut epithelium during absorption, fosamprenavir is rapidly and almost completely hydrolyzed to amprenavir and inorganic phosphate prior to reaching the systemic circulation. Amprenavir is metabolized in the liver by the cytochrome P450 3A4 (CYP3A4) enzyme system.

Rute Eliminasi

Excretion of unchanged amprenavir in urine and feces is minimal. The renal elimination of unchanged amprenavir represents approximately 1% of the administered dose; therefore, renal impairment is not expected to significantly impact the elimination of amprenavir. Amprenavir, the active metabolite of fosamprenavir, is metabolized in the liver by the cytochrome P450 enzyme system.

Interaksi Makanan

3 Data
  • 1. Avoid alcohol. Drug impairs alcohol metabolism.
  • 2. Avoid fatty foods.
  • 3. Take with or without food.

Interaksi Obat

399 Data
Alprazolam The serum concentration of Alprazolam can be increased when it is combined with Fosamprenavir.
Cisapride The serum concentration of Cisapride can be increased when it is combined with Fosamprenavir.
Clarithromycin The serum concentration of Clarithromycin can be increased when it is combined with Fosamprenavir.
Cyclophosphamide The serum concentration of the active metabolites of Cyclophosphamide can be increased when Cyclophosphamide is used in combination with Fosamprenavir.
Methadone The serum concentration of the active metabolites of Fosamprenavir can be reduced when Fosamprenavir is used in combination with Methadone resulting in a loss in efficacy.
Olanzapine Olanzapine can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cimetidine Cimetidine can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Nizatidine Nizatidine can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ranitidine Ranitidine can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Famotidine Famotidine can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methantheline Methantheline can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Promethazine Promethazine can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Asenapine Asenapine can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Metiamide Metiamide can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Roxatidine acetate Roxatidine acetate can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lafutidine Lafutidine can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lavoltidine Lavoltidine can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Niperotidine Niperotidine can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Doxepin Doxepin can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Epinastine Epinastine can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Voriconazole The serum concentration of Voriconazole can be increased when it is combined with Fosamprenavir.
Rifabutin The serum concentration of 25-O-Desacetylrifabutin, an active metabolite of Rifabutin, can be increased when used in combination with Fosamprenavir.
Efavirenz The serum concentration of the active metabolites of Fosamprenavir can be reduced when Fosamprenavir is used in combination with Efavirenz resulting in a loss in efficacy.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Fosamprenavir.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Fosamprenavir.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Fosamprenavir.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Fosamprenavir.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Fosamprenavir.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Fosamprenavir.
Delavirdine The serum concentration of Delavirdine can be decreased when it is combined with Fosamprenavir.
Paroxetine The serum concentration of Paroxetine can be decreased when it is combined with Fosamprenavir.
Ketoconazole The serum concentration of Ketoconazole can be increased when it is combined with Fosamprenavir.
Itraconazole The serum concentration of Itraconazole can be increased when it is combined with Fosamprenavir.
Propafenone The serum concentration of Propafenone can be increased when it is combined with Fosamprenavir.
Flecainide The serum concentration of Flecainide can be increased when it is combined with Fosamprenavir.
Dolutegravir The serum concentration of Dolutegravir can be decreased when it is combined with Fosamprenavir.
Etravirine The serum concentration of the active metabolites of Fosamprenavir can be increased when Fosamprenavir is used in combination with Etravirine.
Lopinavir The serum concentration of Lopinavir can be decreased when it is combined with Fosamprenavir.
Raltegravir The serum concentration of Raltegravir can be decreased when it is combined with Fosamprenavir.
Telaprevir The serum concentration of Telaprevir can be decreased when it is combined with Fosamprenavir.
Garlic Garlic can cause a decrease in the absorption of Fosamprenavir 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 Fosamprenavir.
Insulin lispro The therapeutic efficacy of Insulin lispro can be decreased when used in combination with Fosamprenavir.
Insulin glargine The therapeutic efficacy of Insulin glargine can be decreased when used in combination with Fosamprenavir.
Insulin pork The therapeutic efficacy of Insulin pork can be decreased when used in combination with Fosamprenavir.
Troglitazone The therapeutic efficacy of Troglitazone can be decreased when used in combination with Fosamprenavir.
Glimepiride The therapeutic efficacy of Glimepiride can be decreased when used in combination with Fosamprenavir.
Sulfisoxazole The therapeutic efficacy of Sulfisoxazole can be decreased when used in combination with Fosamprenavir.
Disopyramide The therapeutic efficacy of Disopyramide can be decreased when used in combination with Fosamprenavir.
Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Fosamprenavir.
Sulfadiazine The therapeutic efficacy of Sulfadiazine can be decreased when used in combination with Fosamprenavir.
Rosiglitazone The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Fosamprenavir.
Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Fosamprenavir.
Miglitol The therapeutic efficacy of Miglitol can be decreased when used in combination with Fosamprenavir.
Chlorpropamide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Fosamprenavir.
Nateglinide The therapeutic efficacy of Nateglinide can be decreased when used in combination with Fosamprenavir.
Pentamidine The therapeutic efficacy of Pentamidine can be decreased when used in combination with Fosamprenavir.
Mifepristone The therapeutic efficacy of Mifepristone can be decreased when used in combination with Fosamprenavir.
Tolazamide The therapeutic efficacy of Tolazamide can be decreased when used in combination with Fosamprenavir.
Repaglinide The therapeutic efficacy of Repaglinide can be decreased when used in combination with Fosamprenavir.
Phenformin The therapeutic efficacy of Phenformin can be decreased when used in combination with Fosamprenavir.
Sulfamethoxazole The therapeutic efficacy of Sulfamethoxazole can be decreased when used in combination with Fosamprenavir.
Glyburide The therapeutic efficacy of Glyburide can be decreased when used in combination with Fosamprenavir.
Glipizide The therapeutic efficacy of Glipizide can be decreased when used in combination with Fosamprenavir.
Gliclazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Fosamprenavir.
Tolbutamide The therapeutic efficacy of Tolbutamide can be decreased when used in combination with Fosamprenavir.
Pioglitazone The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Fosamprenavir.
Gliquidone The therapeutic efficacy of Gliquidone can be decreased when used in combination with Fosamprenavir.
Mitiglinide The therapeutic efficacy of Mitiglinide can be decreased when used in combination with Fosamprenavir.
Exenatide The therapeutic efficacy of Exenatide can be decreased when used in combination with Fosamprenavir.
Mecasermin The therapeutic efficacy of Mecasermin can be decreased when used in combination with Fosamprenavir.
Pramlintide The therapeutic efficacy of Pramlintide can be decreased when used in combination with Fosamprenavir.
Glisoxepide The therapeutic efficacy of Glisoxepide can be decreased when used in combination with Fosamprenavir.
Insulin aspart The therapeutic efficacy of Insulin aspart can be decreased when used in combination with Fosamprenavir.
Insulin detemir The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Fosamprenavir.
Insulin glulisine The therapeutic efficacy of Insulin glulisine can be decreased when used in combination with Fosamprenavir.
Glymidine The therapeutic efficacy of Glymidine can be decreased when used in combination with Fosamprenavir.
AICA ribonucleotide The therapeutic efficacy of AICA ribonucleotide can be decreased when used in combination with Fosamprenavir.
Buformin The therapeutic efficacy of Buformin can be decreased when used in combination with Fosamprenavir.
Vildagliptin The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Fosamprenavir.
Voglibose The therapeutic efficacy of Voglibose can be decreased when used in combination with Fosamprenavir.
NN344 The therapeutic efficacy of NN344 can be decreased when used in combination with Fosamprenavir.
AMG-222 The therapeutic efficacy of AMG-222 can be decreased when used in combination with Fosamprenavir.
Bisegliptin The therapeutic efficacy of Bisegliptin can be decreased when used in combination with Fosamprenavir.
Alogliptin The therapeutic efficacy of Alogliptin can be decreased when used in combination with Fosamprenavir.
Saxagliptin The therapeutic efficacy of Saxagliptin can be decreased when used in combination with Fosamprenavir.
Liraglutide The therapeutic efficacy of Liraglutide can be decreased when used in combination with Fosamprenavir.
Gosogliptin The therapeutic efficacy of Gosogliptin can be decreased when used in combination with Fosamprenavir.
Glibornuride The therapeutic efficacy of Glibornuride can be decreased when used in combination with Fosamprenavir.
Benfluorex The therapeutic efficacy of Benfluorex can be decreased when used in combination with Fosamprenavir.
Empagliflozin The therapeutic efficacy of Empagliflozin can be decreased when used in combination with Fosamprenavir.
Albiglutide The therapeutic efficacy of Albiglutide can be decreased when used in combination with Fosamprenavir.
Dulaglutide The therapeutic efficacy of Dulaglutide can be decreased when used in combination with Fosamprenavir.
Lobeglitazone The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Fosamprenavir.
Netoglitazone The therapeutic efficacy of Netoglitazone can be decreased when used in combination with Fosamprenavir.
Rivoglitazone The therapeutic efficacy of Rivoglitazone can be decreased when used in combination with Fosamprenavir.
Ciglitazone The therapeutic efficacy of Ciglitazone can be decreased when used in combination with Fosamprenavir.
Lixisenatide The therapeutic efficacy of Lixisenatide can be decreased when used in combination with Fosamprenavir.
Insulin beef The therapeutic efficacy of Insulin beef can be decreased when used in combination with Fosamprenavir.
Insulin degludec The therapeutic efficacy of Insulin degludec can be decreased when used in combination with Fosamprenavir.

Target Protein

Pol polyprotein pol
Gag-Pol polyprotein gag-pol

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18373851
    Smith KY, Weinberg WG, Dejesus E, Fischl MA, Liao Q, Ross LL, Pakes GE, Pappa KA, Lancaster CT: Fosamprenavir or atazanavir once daily boosted with ritonavir 100 mg, plus tenofovir/emtricitabine, for the initial treatment of HIV infection: 48-week results of ALERT. AIDS Res Ther. 2008 Mar 28;5:5. doi: 10.1186/1742-6405-5-5.
  • PMID: 18042502
    Hoffman RM, Umeh OC, Garris C, Givens N, Currier JS: Evaluation of sex differences of fosamprenavir (with and without ritonavir) in HIV-infected men and women. HIV Clin Trials. 2007 Nov-Dec;8(6):371-80.
  • PMID: 15341507
    Chapman TM, Plosker GL, Perry CM: Fosamprenavir: a review of its use in the management of antiretroviral therapy-naive patients with HIV infection. Drugs. 2004;64(18):2101-24.
  • PMID: 14982766
    Furfine ES, Baker CT, Hale MR, Reynolds DJ, Salisbury JA, Searle AD, Studenberg SD, Todd D, Tung RD, Spaltenstein A: Preclinical pharmacology and pharmacokinetics of GW433908, a water-soluble prodrug of the human immunodeficiency virus protease inhibitor amprenavir. Antimicrob Agents Chemother. 2004 Mar;48(3):791-8.
  • PMID: 15116286
    Sension M: Initial therapy for human immunodeficiency virus: broadening the options. HIV Clin Trials. 2004 Mar-Apr;5(2):99-111.
  • PMID: 14693528
    Wood R, Arasteh K, Stellbrink HJ, Teofilo E, Raffi F, Pollard RB, Eron J, Yeo J, Millard J, Wire MB, Naderer OJ: Six-week randomized controlled trial to compare the tolerabilities, pharmacokinetics, and antiviral activities of GW433908 and amprenavir in human immunodeficiency virus type 1-infected patients. Antimicrob Agents Chemother. 2004 Jan;48(1):116-23.
  • PMID: 12162471
    Falcoz C, Jenkins JM, Bye C, Hardman TC, Kenney KB, Studenberg S, Fuder H, Prince WT: Pharmacokinetics of GW433908, a prodrug of amprenavir, in healthy male volunteers. J Clin Pharmacol. 2002 Aug;42(8):887-98.
  • PMID: 16485915
    Wire MB, Shelton MJ, Studenberg S: Fosamprenavir : clinical pharmacokinetics and drug interactions of the amprenavir prodrug. Clin Pharmacokinet. 2006;45(2):137-68. doi: 10.2165/00003088-200645020-00002.

Contoh Produk & Brand

Produk: 15 • International brands: 0
Produk
  • Fosamprenavir Calcium
    Tablet, film coated • 700 mg/1 • Oral • US • Generic • Approved
  • Fosamprenavir Calcium
    Tablet, coated • 700 mg/1 • Oral • US • Generic • Approved
  • Lexiva
    Tablet, film coated • 700 mg/1 • Oral • US • Approved
  • Lexiva
    Tablet, film coated • 700 mg/1 • Oral • US • Approved
  • Lexiva
    Suspension • 50 mg/1mL • Oral • US • Approved
  • Lexiva
    Tablet, film coated • 700 mg/1 • Oral • US • Approved
  • Lexiva
    Tablet, film coated • 700 mg/1 • Oral • US • Approved
  • Lexiva
    Tablet, film coated • 700 mg/1 • Oral • US • Approved
Menampilkan 8 dari 15 produk.

Sekuens Gen/Protein (FASTA)

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