Etravirine

DB06414

small molecule approved

Deskripsi

Etravirine is an antiretroviral agent more specifically classified as a Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI). Etraverine is used clinically for the treatment of human immunodeficiency virus type 1 (HIV-1) infection. On January 18, 2007, the FDA granted accelerated approved for the use of etravirine 100mg tablets in the treatment of adult HIV-1 infection documented to be resistant to therapy with other NNRTIs and antiretroviral agents. On March 26, 2012, approval was extended for use in treatment-experienced pediatric patients 6 to 18 years of age, weighing at least 16 kg. Etravarine must always be used in combination with other antiretroviral drugs.

Etravirine exerts its effects via direct inhibition of the reverse transcriptase enzyme of human immunodeficiency virus type 1 (HIV-1), and consequently blocks DNA-dependent and RNA-dependent polymerase activity. Etravirine does not inhibit human DNA polymerase alpha, beta or gamma.

Common side effects of use include mild to moderate rash within the first 6 weeks of therapy, nausea, diarrhea and peripheral neuropathy. Patients are advised to immediately contact their healthcare provider if a rash develops.

In 2009, postmarketing case reports of Stevens-Johnson Syndrome, toxic epidermal necrolysis, erythema multiforme, and other hypersensitivity reactions lead to a revision of etravirine's "Warnings and Precautions," as well as notification of health care providers.

In 2013, reports of Autoimmune disorders (such as Graves’ disease, polymyositis, and Guillain-Barré syndrome) in the setting of immune reconstitution, as well as more in depth information about the development of rashes in patients taking etravirine, lead to a modification of etravirine's monograph.

Struktur Molekul 2D

Berat 435.277
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Half life of 9.05-41 hours.
Volume Distribusi Distribution of etravirine into compartments other than plasma has not been evaluated in humans.
Klirens (Clearance) Renal clearance of etravirine is negligible (<1.2%), thus no dose adjustments are required in patients with renal impairment. Clearance is shown to be reduced in patients with Hepatitis B and/or co-infection, however, the safety profile of etravirine does not call for dosage adjustments.

Absorpsi

Maximum oral absorption is achieved in 2.5-4 hours. Absorption is unaffected by the concomitant use of oral ranitidine or omeprazole, which decrease gastric acidity. Administration under fasting conditions resulted in a near 50% decrease in systemic exposure (AUC) when compared to administration after a meal.

Metabolisme

Metabolized (in vitro) by the liver CYP450 enzymes: CYP3A4, CYP2C9, CYP2C19. The major metabolites formed by a methyl hydroxylation of the dimethylbenzonitrile moiety retained less than 90% of etravirine's activity.

Rute Eliminasi

After a 800mg dose of radio-labelled etraverine, 93.7% was found to undergo fecal elimination, with 81.2% - 86.4% eliminated unchanged. 1.2% of the dose was renally eliminated, changed. Etravirine is dialyzable (hemodialysis).

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits the CYP3A metabolism of etravirine, which may increase its serum concentration.
  • 2. Avoid St. John's Wort. This herb induces the CYP3A metabolism of etravirine and may reduce its serum concentration.
  • 3. Take after a meal. Take after meals. This increases the bioavailability of etravirine.

Interaksi Obat

638 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Etravirine.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Etravirine.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Etravirine.
Dabrafenib The serum concentration of Etravirine can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Etravirine can be increased when it is combined with Luliconazole.
Brentuximab vedotin The metabolism of Brentuximab vedotin can be increased when combined with Etravirine.
Phenytoin The serum concentration of Etravirine can be decreased when it is combined with Phenytoin.
Fosphenytoin The serum concentration of Etravirine can be decreased when it is combined with Fosphenytoin.
Linagliptin The metabolism of Linagliptin can be increased when combined with Etravirine.
Daclatasvir The metabolism of Daclatasvir can be increased when combined with Etravirine.
Digoxin The serum concentration of Digoxin can be increased when it is combined with Etravirine.
Metildigoxin The serum concentration of Metildigoxin can be increased when it is combined with Etravirine.
Acetyldigoxin The serum concentration of Acetyldigoxin can be increased when it is combined with Etravirine.
Ritonavir The serum concentration of Etravirine can be decreased when it is combined with Ritonavir.
Rifabutin The serum concentration of Etravirine can be decreased when it is combined with Rifabutin.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Etravirine.
Perampanel The metabolism of Perampanel can be increased when combined with Etravirine.
Warfarin The metabolism of Warfarin can be increased when combined with Etravirine.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Etravirine.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Etravirine.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Etravirine.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Etravirine.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Etravirine.
Primidone The metabolism of Etravirine can be increased when combined with Primidone.
Methylphenobarbital The metabolism of Etravirine can be increased when combined with Methylphenobarbital.
Phenobarbital The metabolism of Etravirine can be increased when combined with Phenobarbital.
Diazepam The metabolism of Diazepam can be decreased when combined with Etravirine.
Tipranavir The serum concentration of Etravirine can be decreased when it is combined with Tipranavir.
Atazanavir The serum concentration of Etravirine can be increased when it is combined with Atazanavir.
Amprenavir The serum concentration of the active metabolites of Amprenavir can be increased when Amprenavir is used in combination with Etravirine.
Fosamprenavir The serum concentration of the active metabolites of Fosamprenavir can be increased when Fosamprenavir is used in combination with Etravirine.
Artemether The serum concentration of the active metabolites of Artemether can be reduced when Artemether is used in combination with Etravirine resulting in a loss in efficacy.
Dolutegravir The serum concentration of Dolutegravir can be decreased when it is combined with Etravirine.
Lumacaftor The serum concentration of Etravirine can be decreased when it is combined with Lumacaftor.
Doxorubicin The serum concentration of Doxorubicin can be decreased when it is combined with Etravirine.
Vincristine The metabolism of Vincristine can be increased when combined with Etravirine.
Rolapitant The metabolism of Rolapitant can be increased when combined with Etravirine.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Etravirine.
Diethylstilbestrol The metabolism of Diethylstilbestrol can be increased when combined with Etravirine.
Etonogestrel The metabolism of Etonogestrel can be increased when combined with Etravirine.
Desogestrel The metabolism of Desogestrel can be increased when combined with Etravirine.
Megestrol acetate The metabolism of Megestrol acetate can be increased when combined with Etravirine.
Levonorgestrel The metabolism of Levonorgestrel can be increased when combined with Etravirine.
Progesterone The metabolism of Progesterone can be increased when combined with Etravirine.
Medroxyprogesterone acetate The metabolism of Medroxyprogesterone acetate can be increased when combined with Etravirine.
Norethisterone The metabolism of Norethisterone can be increased when combined with Etravirine.
Estradiol The metabolism of Estradiol can be increased when combined with Etravirine.
Ethynodiol diacetate The metabolism of Ethynodiol diacetate can be increased when combined with Etravirine.
Mifepristone The metabolism of Mifepristone can be increased when combined with Etravirine.
Norgestimate The metabolism of Norgestimate can be increased when combined with Etravirine.
Ethinylestradiol The metabolism of Ethinylestradiol can be increased when combined with Etravirine.
Mestranol The metabolism of Mestranol can be increased when combined with Etravirine.
Drospirenone The metabolism of Drospirenone can be increased when combined with Etravirine.
Estrone sulfate The metabolism of Estrone sulfate can be increased when combined with Etravirine.
Octylphenoxy polyethoxyethanol The metabolism of Octylphenoxy polyethoxyethanol can be increased when combined with Etravirine.
Cyproterone acetate The metabolism of Cyproterone acetate can be increased when combined with Etravirine.
Trestolone The metabolism of Trestolone can be increased when combined with Etravirine.
Norelgestromin The metabolism of Norelgestromin can be increased when combined with Etravirine.
Gestodene The metabolism of Gestodene can be increased when combined with Etravirine.
Hydroxyprogesterone caproate The metabolism of Hydroxyprogesterone caproate can be increased when combined with Etravirine.
Dienogest The metabolism of Dienogest can be increased when combined with Etravirine.
Norethynodrel The metabolism of Norethynodrel can be increased when combined with Etravirine.
Norgestrel The metabolism of Norgestrel can be increased when combined with Etravirine.
Cloprostenol The metabolism of Cloprostenol can be increased when combined with Etravirine.
Gestrinone The metabolism of Gestrinone can be increased when combined with Etravirine.
Nomegestrol The metabolism of Nomegestrol can be increased when combined with Etravirine.
Gossypol The metabolism of Gossypol can be increased when combined with Etravirine.
Ormeloxifene The metabolism of Ormeloxifene can be increased when combined with Etravirine.
Chlormadinone The metabolism of Chlormadinone can be increased when combined with Etravirine.
Norgestrienone The metabolism of Norgestrienone can be increased when combined with Etravirine.
Quingestanol The metabolism of Quingestanol can be increased when combined with Etravirine.
Demegestone The metabolism of Demegestone can be increased when combined with Etravirine.
Etynodiol The metabolism of Etynodiol can be increased when combined with Etravirine.
Testosterone enanthate The metabolism of Testosterone enanthate can be increased when combined with Etravirine.
Estradiol benzoate The metabolism of Estradiol benzoate can be increased when combined with Etravirine.
Estradiol cypionate The metabolism of Estradiol cypionate can be increased when combined with Etravirine.
Estradiol valerate The metabolism of Estradiol valerate can be increased when combined with Etravirine.
Nomegestrol acetate The metabolism of Nomegestrol acetate can be increased when combined with Etravirine.
Norethindrone enanthate The metabolism of Norethindrone enanthate can be increased when combined with Etravirine.
Ulipristal The metabolism of Ulipristal can be increased when combined with Etravirine.
Azithromycin The metabolism of Azithromycin can be increased when combined with Etravirine.
Ziprasidone The metabolism of Ziprasidone can be increased when combined with Etravirine.
Chlorpromazine The metabolism of Chlorpromazine can be increased when combined with Etravirine.
Cephalexin The metabolism of Cephalexin can be increased when combined with Etravirine.
Doxazosin The metabolism of Doxazosin can be increased when combined with Etravirine.
Rosuvastatin The metabolism of Rosuvastatin can be increased when combined with Etravirine.
Allylestrenol The metabolism of Allylestrenol can be increased when combined with Etravirine.
Zuclopenthixol The metabolism of Zuclopenthixol can be increased when combined with Etravirine.
Roflumilast The metabolism of Roflumilast can be increased when combined with Etravirine.
Vorapaxar The metabolism of Vorapaxar can be increased when combined with Etravirine.
Suvorexant The metabolism of Suvorexant can be increased when combined with Etravirine.
Netupitant The metabolism of Netupitant can be increased when combined with Etravirine.
Tasimelteon The metabolism of Tasimelteon can be increased when combined with Etravirine.
Nintedanib The metabolism of Nintedanib can be increased when combined with Etravirine.
Tenofovir alafenamide The metabolism of Tenofovir alafenamide can be increased when combined with Etravirine.
Dihydroergocornine The metabolism of Dihydroergocornine can be increased when combined with Etravirine.
Duvelisib The metabolism of Duvelisib can be increased when combined with Etravirine.
Gilteritinib The metabolism of Gilteritinib can be increased when combined with Etravirine.
9-aminocamptothecin The metabolism of 9-aminocamptothecin can be increased when combined with Etravirine.
Methylprednisone The metabolism of Methylprednisone can be increased when combined with Etravirine.

Target Protein

Gag-Pol polyprotein gag-pol
Gag-Pol polyprotein gag-pol
Reverse transcriptase/RNaseH pol

Contoh Produk & Brand

Produk: 27 • International brands: 0
Produk
  • Etravirine
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Etravirine
    Tablet • 200 mg/1 • Oral • US • Generic • Approved
  • Etravirine
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Etravirine
    Tablet • 200 mg/1 • Oral • US • Generic • Approved
  • Etravirine
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Etravirine
    Tablet • 25 mg/1 • Oral • US • Generic • Approved
  • Etravirine
    Tablet • 200 mg/1 • Oral • US • Generic • Approved
  • Etravirine
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 27 produk.

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