Peringatan Keamanan

Those with renal disease and creatinine clearance of <30 mL/min should not take bictegravir FDA LABEL.
Patients with hepatic disease should not take bictegravir.

Most common adverse reactions include diarrhea, nausea, and headache FDA LABEL.

Lactic acidosis/severe hepatomegaly with steatosis: Discontinue treatment in patients who develop symptoms/laboratory findings suggesting lactic acidosis or hepatotoxicity.

Bictegravir

DB11799

small molecule approved investigational

Deskripsi

Bictegravir is a recently approved investigational drug that has been used in trials studying the treatment of HIV-1 and HIV-2 infection. It has been approved for HIV-1 monotherapy combined with 2 other antiretrovirals in a single tablet.L43677

Struktur Molekul 2D

Berat 449.386
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Half-life is 17.3 hours.[L38944]
Volume Distribusi 0.2 L/Kg in humans [L1218]
Klirens (Clearance) Bictegravir is mainly cleared by the kidneys. Those with renal clearance <30 should not take bictegravir [FDA LABEL]

Absorpsi

Bictegravir is rapidly absorbed within the body. Tmax= 2.0-4.0h L1219

Metabolisme

In a 10-day dose-ranging study, monotherapy (5 mg to 100 mg) once daily in adults who were not previously treated with bictegravir, the median half-life of BIC ranged from 15.9 h - 20.9 h L1219. Bictegravir is metabolized in the liver and kidneys. CYP3A4 and UGT1A are the primary enzymes involved in the metabolism of bictegravir. Administration of bictegravir is not advised in patients with renal creatinine clearance of <30 mL/min and patients with hepatic disease FDA LABEL.

Rute Eliminasi

BIC is mainly eliminated through UGT1A1 glucuronidation and CYP3A4 oxidation, equally L1218. About 1% of the bictegravir dose is excreted in the urine, unchanged L1218,L1219.

Interaksi Makanan

5 Data
  • 1. Avoid St. John's Wort.
  • 2. Take at the same time every day.
  • 3. Take separate from antacids. Take bictegravir at least 2 hours before or 6 hours after taking antacids containing aluminum or magnesium.
  • 4. Take with food. When taking iron or calcium-containing products, bictegravir should be taken with food.
  • 5. Take with or without food.

Interaksi Obat

172 Data
Desogestrel The metabolism of Bictegravir can be increased when combined with Desogestrel.
Zidovudine The metabolism of Bictegravir can be increased when combined with Zidovudine.
Lamotrigine The metabolism of Bictegravir can be increased when combined with Lamotrigine.
Ethinylestradiol The metabolism of Bictegravir can be increased when combined with Ethinylestradiol.
Testosterone propionate The metabolism of Bictegravir can be increased when combined with Testosterone propionate.
Pitolisant The serum concentration of Bictegravir can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Bictegravir can be increased when combined with Metreleptin.
Adenine The metabolism of Bictegravir can be decreased when combined with Adenine.
Valproic acid The metabolism of Bictegravir can be decreased when combined with Valproic acid.
Indomethacin The metabolism of Bictegravir can be decreased when combined with Indomethacin.
Sorafenib The metabolism of Bictegravir can be decreased when combined with Sorafenib.
Erlotinib The metabolism of Bictegravir can be decreased when combined with Erlotinib.
Flurbiprofen The metabolism of Bictegravir can be decreased when combined with Flurbiprofen.
Propofol The metabolism of Bictegravir can be decreased when combined with Propofol.
Probenecid The metabolism of Bictegravir can be decreased when combined with Probenecid.
Gemfibrozil The metabolism of Bictegravir can be decreased when combined with Gemfibrozil.
Flunitrazepam The metabolism of Bictegravir can be decreased when combined with Flunitrazepam.
Deferasirox The metabolism of Bictegravir can be decreased when combined with Deferasirox.
Eltrombopag The metabolism of Bictegravir can be decreased when combined with Eltrombopag.
Pazopanib The metabolism of Bictegravir can be decreased when combined with Pazopanib.
Regorafenib The metabolism of Bictegravir can be decreased when combined with Regorafenib.
Dasabuvir The metabolism of Bictegravir can be decreased when combined with Dasabuvir.
Sodium aurothiomalate The metabolism of Bictegravir can be decreased when combined with Sodium aurothiomalate.
Ombitasvir The metabolism of Bictegravir can be decreased when combined with Ombitasvir.
Paritaprevir The metabolism of Bictegravir can be decreased when combined with Paritaprevir.
Silibinin The metabolism of Bictegravir can be decreased when combined with Silibinin.
Dacomitinib The metabolism of Bictegravir can be decreased when combined with Dacomitinib.
Fostamatinib The metabolism of Bictegravir can be decreased when combined with Fostamatinib.
Enasidenib The metabolism of Bictegravir can be decreased when combined with Enasidenib.
Pibrentasvir The metabolism of Bictegravir can be decreased when combined with Pibrentasvir.
Glecaprevir The metabolism of Bictegravir can be decreased when combined with Glecaprevir.
Pexidartinib The metabolism of Bictegravir can be decreased when combined with Pexidartinib.
Amitriptyline The metabolism of Bictegravir can be decreased when combined with Amitriptyline.
Topotecan The excretion of Topotecan can be decreased when combined with Bictegravir.
Procainamide The excretion of Procainamide can be decreased when combined with Bictegravir.
Abemaciclib The excretion of Abemaciclib can be decreased when combined with Bictegravir.
Metformin The excretion of Metformin can be decreased when combined with Bictegravir.
Ciprofloxacin The metabolism of Bictegravir can be decreased when combined with Ciprofloxacin.
Cephalexin The excretion of Cephalexin can be decreased when combined with Bictegravir.
Acyclovir The excretion of Acyclovir can be decreased when combined with Bictegravir.
Ganciclovir The excretion of Ganciclovir can be decreased when combined with Bictegravir.
Levofloxacin The excretion of Levofloxacin can be decreased when combined with Bictegravir.
Cefradine The excretion of Cefradine can be decreased when combined with Bictegravir.
Estrone sulfate The excretion of Estrone sulfate can be decreased when combined with Bictegravir.
N-methylnicotinamide The excretion of N-methylnicotinamide can be decreased when combined with Bictegravir.
Relebactam The excretion of Relebactam can be decreased when combined with Bictegravir.
Solriamfetol The excretion of Solriamfetol can be decreased when combined with Bictegravir.
Nadolol The excretion of Nadolol can be decreased when combined with Bictegravir.
Flecainide The excretion of Flecainide can be decreased when combined with Bictegravir.
Guanidine The excretion of Guanidine can be decreased when combined with Bictegravir.
Rubella virus vaccine The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Bictegravir.
Bacillus calmette-guerin substrain tice live antigen The therapeutic efficacy of Bacillus calmette-guerin substrain tice live antigen can be decreased when used in combination with Bictegravir.
Bacillus calmette-guerin substrain connaught live antigen The therapeutic efficacy of Bacillus calmette-guerin substrain connaught live antigen can be decreased when used in combination with Bictegravir.
Yellow fever vaccine The therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Bictegravir.
Anthrax vaccine The therapeutic efficacy of Anthrax vaccine can be decreased when used in combination with Bictegravir.
Typhoid Vaccine Live The therapeutic efficacy of Typhoid Vaccine Live can be decreased when used in combination with Bictegravir.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Bictegravir.
Human adenovirus e serotype 4 strain cl-68578 antigen The therapeutic efficacy of Human adenovirus e serotype 4 strain cl-68578 antigen can be decreased when used in combination with Bictegravir.
Vibrio cholerae CVD 103-HgR strain live antigen The therapeutic efficacy of Vibrio cholerae CVD 103-HgR strain live antigen can be decreased when used in combination with Bictegravir.
Adenovirus type 7 vaccine live The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Bictegravir.
Varicella zoster vaccine (live/attenuated) The therapeutic efficacy of Varicella zoster vaccine (live/attenuated) can be decreased when used in combination with Bictegravir.
Bacillus calmette-guerin substrain russian BCG-I live antigen The therapeutic efficacy of Bacillus calmette-guerin substrain russian BCG-I live antigen can be decreased when used in combination with Bictegravir.
Cenobamate The serum concentration of Bictegravir can be decreased when it is combined with Cenobamate.
Ritonavir The serum concentration of Bictegravir can be increased when it is combined with Ritonavir.
Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Bictegravir.
Tucatinib The metabolism of Tucatinib can be decreased when combined with Bictegravir.
Abametapir The serum concentration of Bictegravir can be increased when it is combined with Abametapir.
Satralizumab The serum concentration of Bictegravir can be decreased when it is combined with Satralizumab.
Sotorasib The serum concentration of Bictegravir can be decreased when it is combined with Sotorasib.
Cyclosporine The metabolism of Bictegravir can be decreased when combined with Cyclosporine.
Fluvoxamine The metabolism of Bictegravir can be decreased when combined with Fluvoxamine.
Fluconazole The metabolism of Bictegravir can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Bictegravir can be increased when it is combined with Erythromycin.
Ziprasidone The metabolism of Bictegravir can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Bictegravir can be decreased when combined with Isradipine.
Diltiazem The metabolism of Bictegravir can be decreased when combined with Diltiazem.
Clozapine The metabolism of Bictegravir can be decreased when combined with Clozapine.
Nicardipine The metabolism of Bictegravir can be decreased when combined with Nicardipine.
Verapamil The metabolism of Bictegravir can be decreased when combined with Verapamil.
Aprepitant The metabolism of Bictegravir can be decreased when combined with Aprepitant.
Isoniazid The metabolism of Bictegravir can be decreased when combined with Isoniazid.
Primaquine The metabolism of Bictegravir can be decreased when combined with Primaquine.
Miconazole The metabolism of Bictegravir can be decreased when combined with Miconazole.
Fusidic acid The metabolism of Bictegravir can be decreased when combined with Fusidic acid.
Zimelidine The metabolism of Bictegravir can be decreased when combined with Zimelidine.
Dronedarone The metabolism of Bictegravir can be decreased when combined with Dronedarone.
Milnacipran The metabolism of Bictegravir can be decreased when combined with Milnacipran.
Simeprevir The metabolism of Bictegravir can be decreased when combined with Simeprevir.
Isavuconazonium The metabolism of Bictegravir can be decreased when combined with Isavuconazonium.
Desvenlafaxine The metabolism of Bictegravir can be decreased when combined with Desvenlafaxine.
Nilvadipine The metabolism of Bictegravir can be decreased when combined with Nilvadipine.
Seproxetine The metabolism of Bictegravir can be decreased when combined with Seproxetine.
Linagliptin The metabolism of Bictegravir can be decreased when combined with Linagliptin.
Indalpine The metabolism of Bictegravir can be decreased when combined with Indalpine.
Netupitant The metabolism of Bictegravir can be decreased when combined with Netupitant.
Barnidipine The metabolism of Bictegravir can be decreased when combined with Barnidipine.
Benidipine The metabolism of Bictegravir can be decreased when combined with Benidipine.
Venetoclax The metabolism of Bictegravir can be decreased when combined with Venetoclax.
Isavuconazole The metabolism of Bictegravir can be decreased when combined with Isavuconazole.
Fosnetupitant The metabolism of Bictegravir can be decreased when combined with Fosnetupitant.

Target Protein

Reverse transcriptase/RNaseH pol
Integrase pol

Referensi & Sumber

Artikel (PubMed)
  • PMID: 5118987
    Chase SP, Freimanis AK: Abdominal echography. Ohio State Med J. 1971 Oct;67(10):901-6.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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