Peringatan Keamanan

The most common adverse reactions reported for elvitegravir use during clinical trials include nausea, vomiting, and diarrhea. Less common side effects occurring in <2% of patients, include abdominal pain, dyspepsia, fatigue, insomnia, rash, depression, suicidal ideation, and suicidal attempt.

Elvitegravir

DB09101

small molecule approved

Deskripsi

Elvitegravir is a human immunodeficiency virus type 1 (HIV-1) integrase strand transfer inhibitor (INSTI) used for the treatment of HIV-1 infection in antiretroviral treatment-experienced adults. Because integrase is necessary for viral replication, inhibition prevents the integration of HIV-1 DNA into the host genome and thereby blocks the formation of the HIV-1 provirus and resulting propagation of the viral infection. Although available as a single dose tablet, elvitegravir must be used in combination with an HIV protease inhibitor coadministered with ritonavir and another antiretroviral drug.

Elvitegravir was first licensed from Japan Tobacco in 2008 and developed by Gilead Sciences. It was FDA approved on August 27, 2012. On September 24, 2014, the FDA approved the single pill form of elvitegravir.

Struktur Molekul 2D

Berat 447.884
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The median terminal plasma half-life following administration of elvitegravir and ritonavir was approximately 8.7 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Following oral administration of elvitegravir and ritonavir with food, in HIV-1 infected subjects, peak elvitegravir plasma concentrations were observed approximately 4 hours post-dose.

Metabolisme

Elvitegravir undergoes primarily oxidative metabolism via CYP3A, and is secondarily glucuronidated via UGT1A1/3 enzymes. Metabolites are found in the plasma at very low concentrations, displayed considerably lower anti-HIV activity, and did not contribute to the overall antiviral activity of elvitegravir.

Rute Eliminasi

Following oral administration of 14Celvitegravir/ritonavir, 94.8% of the dose was recovered in feces, while 6.7% was recovered in urine as metabolites.

Interaksi Makanan

3 Data
  • 1. Avoid St. John's Wort. This herb induces the CYP3A metabolism of elvitegravir. Therefore, it may reduce the serum concentration of elvitegravir and its effectiveness.
  • 2. Take separate from antacids. Take at least 2 hours before or after antacids.
  • 3. Take with food.

Interaksi Obat

859 Data
Eliglustat The metabolism of Eliglustat can be decreased when combined with Elvitegravir.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Elvitegravir.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Elvitegravir.
Colchicine The metabolism of Colchicine can be decreased when combined with Elvitegravir.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Elvitegravir.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Elvitegravir.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Elvitegravir.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Elvitegravir.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Elvitegravir.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Elvitegravir.
Carbamazepine The metabolism of Elvitegravir can be increased when combined with Carbamazepine.
Rifabutin The serum concentration of Rifabutin can be increased when it is combined with Elvitegravir.
Warfarin The serum concentration of Warfarin can be decreased when it is combined with Elvitegravir.
Acenocoumarol The serum concentration of Acenocoumarol can be decreased when it is combined with Elvitegravir.
(R)-warfarin The serum concentration of (R)-warfarin can be decreased when it is combined with Elvitegravir.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be decreased when it is combined with Elvitegravir.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be decreased when it is combined with Elvitegravir.
(S)-Warfarin The serum concentration of (S)-Warfarin can be decreased when it is combined with Elvitegravir.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Elvitegravir.
Lamotrigine The metabolism of Elvitegravir can be increased when combined with Lamotrigine.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Elvitegravir.
Ketoconazole The serum concentration of Elvitegravir can be increased when it is combined with Ketoconazole.
Atazanavir The serum concentration of Elvitegravir can be increased when it is combined with Atazanavir.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Elvitegravir.
Itraconazole The metabolism of Elvitegravir can be decreased when combined with Itraconazole.
Dexamethasone The serum concentration of Elvitegravir can be decreased when it is combined with Dexamethasone.
Magnesium oxide Magnesium oxide can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sodium bicarbonate Sodium bicarbonate can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum hydroxide Aluminum hydroxide can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium carbonate Calcium carbonate can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magaldrate Magaldrate can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium hydroxide Magnesium hydroxide can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium trisilicate Magnesium trisilicate can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium carbonate Magnesium carbonate can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bismuth subnitrate Bismuth subnitrate can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium silicate Magnesium silicate can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium acetoacetate Aluminium acetoacetate can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Hydrotalcite Hydrotalcite can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium peroxide Magnesium peroxide can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Almasilate Almasilate can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium glycinate Aluminium glycinate can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aloglutamol Aloglutamol can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium silicate Calcium silicate can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium phosphate Aluminium phosphate can cause a decrease in the absorption of Elvitegravir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Diethylstilbestrol The serum concentration of Diethylstilbestrol can be decreased when it is combined with Elvitegravir.
Etonogestrel The serum concentration of Etonogestrel can be decreased when it is combined with Elvitegravir.
Desogestrel The serum concentration of Desogestrel can be decreased when it is combined with Elvitegravir.
Megestrol acetate The serum concentration of Megestrol acetate can be decreased when it is combined with Elvitegravir.
Levonorgestrel The serum concentration of Levonorgestrel can be decreased when it is combined with Elvitegravir.
Progesterone The serum concentration of Progesterone can be decreased when it is combined with Elvitegravir.
Medroxyprogesterone acetate The serum concentration of Medroxyprogesterone acetate can be decreased when it is combined with Elvitegravir.
Norethisterone The serum concentration of Norethisterone can be decreased when it is combined with Elvitegravir.
Estradiol The serum concentration of Estradiol can be decreased when it is combined with Elvitegravir.
Ethynodiol diacetate The serum concentration of Ethynodiol diacetate can be decreased when it is combined with Elvitegravir.
Norgestimate The serum concentration of Norgestimate can be decreased when it is combined with Elvitegravir.
Ethinylestradiol The serum concentration of Ethinylestradiol can be decreased when it is combined with Elvitegravir.
Mestranol The serum concentration of Mestranol can be decreased when it is combined with Elvitegravir.
Drospirenone The serum concentration of Drospirenone can be decreased when it is combined with Elvitegravir.
Estrone sulfate The serum concentration of Estrone sulfate can be decreased when it is combined with Elvitegravir.
Octylphenoxy polyethoxyethanol The serum concentration of Octylphenoxy polyethoxyethanol can be decreased when it is combined with Elvitegravir.
Cyproterone acetate The serum concentration of Cyproterone acetate can be decreased when it is combined with Elvitegravir.
Trestolone The serum concentration of Trestolone can be decreased when it is combined with Elvitegravir.
Norelgestromin The serum concentration of Norelgestromin can be decreased when it is combined with Elvitegravir.
Gestodene The serum concentration of Gestodene can be decreased when it is combined with Elvitegravir.
Hydroxyprogesterone caproate The serum concentration of Hydroxyprogesterone caproate can be decreased when it is combined with Elvitegravir.
Ulipristal The serum concentration of Ulipristal can be decreased when it is combined with Elvitegravir.
Dienogest The serum concentration of Dienogest can be decreased when it is combined with Elvitegravir.
Norethynodrel The serum concentration of Norethynodrel can be decreased when it is combined with Elvitegravir.
Norgestrel The serum concentration of Norgestrel can be decreased when it is combined with Elvitegravir.
Cloprostenol The serum concentration of Cloprostenol can be decreased when it is combined with Elvitegravir.
Gestrinone The serum concentration of Gestrinone can be decreased when it is combined with Elvitegravir.
Nomegestrol The serum concentration of Nomegestrol can be decreased when it is combined with Elvitegravir.
Lynestrenol The serum concentration of Lynestrenol can be decreased when it is combined with Elvitegravir.
Gossypol The serum concentration of Gossypol can be decreased when it is combined with Elvitegravir.
Ormeloxifene The serum concentration of Ormeloxifene can be decreased when it is combined with Elvitegravir.
Chlormadinone The serum concentration of Chlormadinone can be decreased when it is combined with Elvitegravir.
Norgestrienone The serum concentration of Norgestrienone can be decreased when it is combined with Elvitegravir.
Quingestanol The serum concentration of Quingestanol can be decreased when it is combined with Elvitegravir.
Demegestone The serum concentration of Demegestone can be decreased when it is combined with Elvitegravir.
Etynodiol The serum concentration of Etynodiol can be decreased when it is combined with Elvitegravir.
Testosterone enanthate The serum concentration of Testosterone enanthate can be decreased when it is combined with Elvitegravir.
Estradiol benzoate The serum concentration of Estradiol benzoate can be decreased when it is combined with Elvitegravir.
Estradiol cypionate The serum concentration of Estradiol cypionate can be decreased when it is combined with Elvitegravir.
Estradiol valerate The serum concentration of Estradiol valerate can be decreased when it is combined with Elvitegravir.
Nomegestrol acetate The serum concentration of Nomegestrol acetate can be decreased when it is combined with Elvitegravir.
Norethindrone enanthate The serum concentration of Norethindrone enanthate can be decreased when it is combined with Elvitegravir.
Pitolisant The serum concentration of Elvitegravir can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Elvitegravir can be increased when combined with Metreleptin.
Adenine The metabolism of Elvitegravir can be decreased when combined with Adenine.
Valproic acid The metabolism of Elvitegravir can be decreased when combined with Valproic acid.
Indomethacin The metabolism of Elvitegravir can be decreased when combined with Indomethacin.
Flurbiprofen The metabolism of Elvitegravir can be decreased when combined with Flurbiprofen.
Propofol The metabolism of Elvitegravir can be decreased when combined with Propofol.
Probenecid The metabolism of Elvitegravir can be decreased when combined with Probenecid.
Deferasirox The metabolism of Elvitegravir can be decreased when combined with Deferasirox.
Eltrombopag The metabolism of Elvitegravir can be decreased when combined with Eltrombopag.
Sodium aurothiomalate The metabolism of Elvitegravir can be decreased when combined with Sodium aurothiomalate.
Ombitasvir The metabolism of Elvitegravir can be decreased when combined with Ombitasvir.
Silibinin The metabolism of Elvitegravir can be decreased when combined with Silibinin.
Pibrentasvir The metabolism of Elvitegravir can be decreased when combined with Pibrentasvir.

Target Protein

Integrase pol
Gag-Pol polyprotein gag-pol

Referensi & Sumber

Artikel (PubMed)
  • PMID: 15729361
    Pommier Y, Johnson AA, Marchand C: Integrase inhibitors to treat HIV/AIDS. Nat Rev Drug Discov. 2005 Mar;4(3):236-48.
  • PMID: 20040702
    Schafer JJ, Squires KE: Integrase inhibitors: a novel class of antiretroviral agents. Ann Pharmacother. 2010 Jan;44(1):145-56. doi: 10.1345/aph.1M309. Epub 2009 Dec 29.
  • PMID: 10649997
    Hazuda DJ, Felock P, Witmer M, Wolfe A, Stillmock K, Grobler JA, Espeseth A, Gabryelski L, Schleif W, Blau C, Miller MD: Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells. Science. 2000 Jan 28;287(5453):646-50.
  • PMID: 21044030
    Luo ZG, Tan JJ, Zeng Y, Wang CX, Hu LM: Development of integrase inhibitors of quinolone acid derivatives for treatment of AIDS: an overview. Mini Rev Med Chem. 2010 Oct;10(11):1046-57.
  • PMID: 21505303
    Metifiot M, Vandegraaff N, Maddali K, Naumova A, Zhang X, Rhodes D, Marchand C, Pommier Y: Elvitegravir overcomes resistance to raltegravir induced by integrase mutation Y143. AIDS. 2011 Jun 1;25(9):1175-8. doi: 10.1097/QAD.0b013e3283473599.
  • PMID: 22347806
    Lee JS, Calmy A, Andrieux-Meyer I, Ford N: Review of the safety, efficacy, and pharmacokinetics of elvitegravir with an emphasis on resource-limited settings. HIV AIDS (Auckl). 2012;4:5-15. doi: 10.2147/HIV.S20993. Epub 2012 Jan 12.
  • PMID: 22321026
    Wills T, Vega V: Elvitegravir: a once-daily inhibitor of HIV-1 integrase. Expert Opin Investig Drugs. 2012 Mar;21(3):395-401. doi: 10.1517/13543784.2012.658914. Epub 2012 Feb 10.
  • PMID: 22789987
    Adams JL, Greener BN, Kashuba AD: Pharmacology of HIV integrase inhibitors. Curr Opin HIV AIDS. 2012 Sep;7(5):390-400. doi: 10.1097/COH.0b013e328356e91c.
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