Peringatan Keamanan

Data regarding the toxicity of cabotegravir is not readily available.L31188,L31193,L31203 In the event of overdose, patients should have their vital signs monitored, including an ECG to monitor the QT interval.L31188,L31193 Treat patients symptomatically and supportively.L31188,L31193 As cabotegravir is highly protein bound, dialysis is not expected to remove a significant amount of the drug from plasma.L31188,L31193

Cabotegravir

DB11751

small molecule approved investigational

Deskripsi

Cabotegravir, or GSK1265744, is an HIV-1 integrase inhibitor that is prescribed with the non-nucleoside reverse transcriptase inhibitor, rilpivirine.A227668,L31188,L31193 Early research into cabotegravir showed it had lower oral bioavailability than dolutegravir,A227668 which resulted in the development of long acting monthly intramuscular injection formulation for cabotegravir.A227668,L31193

Cabotegravir was granted FDA approval on 21 January 2021 in combination with rilpivirine to treat HIV-1 infection in virologically suppressed individuals.L31198 While previously administered once monthly only, this combination product was granted FDA approval for dosing every two months on February 01, 2022 L40084 and without the need for an oral lead-in period prior.L31193

Struktur Molekul 2D

Berat 405.358
Wujud liquid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean half life of oral cabotegravir is 41 hours.[L31188] The mean half life of intramuscular extended-release cabotegravir is 5.6-11.5 weeks.[L31193]
Volume Distribusi Data regarding the volume of distribution of cabotegravir is not readily available.[A227663,L31193,L31203]
Klirens (Clearance) Data regarding the clearance of cabotegravir is not readily available.[A227663,L31193,L31203] Clearance in dogs was 0.34 mL/min/kg and in cynomolgus monkeys was 0.32 mL/min/kg.[A227668]

Absorpsi

Oral cabotegravir has a Tmax of 3 hours, reaches a Cmax of 8.0 µg/mL, and has an AUC of 145 µg\*h/mL.L31188 Intramuscular extended-release cabotegravir has a Tmax of 7 days, reaches a Cmax of 8.0 µg/mL, and has an AUC of 1591 µg\*h/mL.L31193

Metabolisme

Cabotegravir is O-glucuronidated to the M1 and M2 metabolites, with 67% of glucuronidation performed by UGT1A1, and 33% by UGT1A9.A227653,A227658

Rute Eliminasi

An oral radiolabelled dose of cabotegravir is 58.5% recovered in the feces and 26.8% recovered in the urine.A227653,A227658,L31188

Interaksi Makanan

2 Data
  • 1. Take at the same time every day. Take the oral tablets at the same time every day.
  • 2. Take with food. Take the oral tablets with a meal.

Interaksi Obat

161 Data
Succinic acid The excretion of Succinic acid can be decreased when combined with Cabotegravir.
Citrulline The excretion of Citrulline can be decreased when combined with Cabotegravir.
Pravastatin The excretion of Pravastatin can be decreased when combined with Cabotegravir.
Oseltamivir The excretion of Oseltamivir can be decreased when combined with Cabotegravir.
Cefotiam The excretion of Cefotiam can be decreased when combined with Cabotegravir.
Conjugated estrogens The excretion of Conjugated estrogens can be decreased when combined with Cabotegravir.
Tenofovir disoproxil The excretion of Tenofovir disoproxil can be decreased when combined with Cabotegravir.
Piperacillin The excretion of Piperacillin can be decreased when combined with Cabotegravir.
Indomethacin The excretion of Indomethacin can be decreased when combined with Cabotegravir.
Aminohippuric acid The excretion of Aminohippuric acid can be decreased when combined with Cabotegravir.
Trifluridine The excretion of Trifluridine can be decreased when combined with Cabotegravir.
Allopurinol The excretion of Allopurinol can be decreased when combined with Cabotegravir.
Zidovudine The excretion of Zidovudine can be decreased when combined with Cabotegravir.
Cimetidine The excretion of Cimetidine can be decreased when combined with Cabotegravir.
Cefdinir The excretion of Cefdinir can be decreased when combined with Cabotegravir.
Methotrexate The excretion of Methotrexate can be decreased when combined with Cabotegravir.
Cephalexin The excretion of Cephalexin can be decreased when combined with Cabotegravir.
Valaciclovir The excretion of Valaciclovir can be decreased when combined with Cabotegravir.
Levocarnitine The excretion of Levocarnitine can be decreased when combined with Cabotegravir.
Leucovorin The excretion of Leucovorin can be decreased when combined with Cabotegravir.
Fluorescein The excretion of Fluorescein can be decreased when combined with Cabotegravir.
Hydrocortisone The excretion of Hydrocortisone can be decreased when combined with Cabotegravir.
Tetracycline The excretion of Tetracycline can be decreased when combined with Cabotegravir.
Estradiol The excretion of Estradiol can be decreased when combined with Cabotegravir.
Acyclovir The excretion of Acyclovir can be decreased when combined with Cabotegravir.
Cefaclor The excretion of Cefaclor can be decreased when combined with Cabotegravir.
Ranitidine The excretion of Ranitidine can be decreased when combined with Cabotegravir.
Quinapril The excretion of Quinapril can be decreased when combined with Cabotegravir.
Bumetanide The excretion of Bumetanide can be decreased when combined with Cabotegravir.
Dinoprostone The excretion of Dinoprostone can be decreased when combined with Cabotegravir.
Famotidine The excretion of Famotidine can be decreased when combined with Cabotegravir.
Fexofenadine The excretion of Fexofenadine can be decreased when combined with Cabotegravir.
Benzylpenicillin The excretion of Benzylpenicillin can be decreased when combined with Cabotegravir.
Rosuvastatin The excretion of Rosuvastatin can be decreased when combined with Cabotegravir.
Captopril The excretion of Captopril can be decreased when combined with Cabotegravir.
Sitagliptin The excretion of Sitagliptin can be decreased when combined with Cabotegravir.
Cefazolin The excretion of Cefazolin can be decreased when combined with Cabotegravir.
Ceftizoxime The excretion of Ceftizoxime can be decreased when combined with Cabotegravir.
Cefacetrile The excretion of Cefacetrile can be decreased when combined with Cabotegravir.
Ceftibuten The excretion of Ceftibuten can be decreased when combined with Cabotegravir.
Tazobactam The excretion of Tazobactam can be decreased when combined with Cabotegravir.
Cyclic adenosine monophosphate The excretion of Cyclic adenosine monophosphate can be decreased when combined with Cabotegravir.
Cholic Acid The excretion of Cholic Acid can be decreased when combined with Cabotegravir.
Glutaric Acid The excretion of Glutaric Acid can be decreased when combined with Cabotegravir.
Oxalic Acid The excretion of Oxalic Acid can be decreased when combined with Cabotegravir.
Taurocholic acid The excretion of Taurocholic acid can be decreased when combined with Cabotegravir.
Doripenem The excretion of Doripenem can be decreased when combined with Cabotegravir.
Saxagliptin The excretion of Saxagliptin can be decreased when combined with Cabotegravir.
Ellagic acid The excretion of Ellagic acid can be decreased when combined with Cabotegravir.
Cefaloridine The excretion of Cefaloridine can be decreased when combined with Cabotegravir.
Avibactam The excretion of Avibactam can be decreased when combined with Cabotegravir.
Eluxadoline The excretion of Eluxadoline can be decreased when combined with Cabotegravir.
Silibinin The excretion of Silibinin can be decreased when combined with Cabotegravir.
Tenofovir alafenamide The excretion of Tenofovir alafenamide can be decreased when combined with Cabotegravir.
Baricitinib The serum concentration of Baricitinib can be increased when it is combined with Cabotegravir.
Relebactam The excretion of Relebactam can be decreased when combined with Cabotegravir.
Tenofovir The excretion of Tenofovir can be decreased when combined with Cabotegravir.
Hydrochlorothiazide The excretion of Hydrochlorothiazide can be decreased when combined with Cabotegravir.
Dexamethasone The excretion of Dexamethasone can be decreased when combined with Cabotegravir.
Oxytetracycline The excretion of Oxytetracycline can be decreased when combined with Cabotegravir.
Polythiazide The excretion of Polythiazide can be decreased when combined with Cabotegravir.
Prednisolone phosphate The excretion of Prednisolone phosphate can be decreased when combined with Cabotegravir.
Dexamethasone acetate The excretion of Dexamethasone acetate can be decreased when combined with Cabotegravir.
Acamprosate The excretion of Acamprosate can be decreased when combined with Cabotegravir.
Nelfinavir The metabolism of Cabotegravir can be increased when combined with Nelfinavir.
Desogestrel The metabolism of Cabotegravir can be increased when combined with Desogestrel.
Ritonavir The metabolism of Cabotegravir can be increased when combined with Ritonavir.
Lamotrigine The metabolism of Cabotegravir can be increased when combined with Lamotrigine.
Efavirenz The metabolism of Cabotegravir can be increased when combined with Efavirenz.
Primidone The metabolism of Cabotegravir can be increased when combined with Primidone.
Tipranavir The metabolism of Cabotegravir can be increased when combined with Tipranavir.
Ethinylestradiol The metabolism of Cabotegravir can be increased when combined with Ethinylestradiol.
Testosterone propionate The metabolism of Cabotegravir can be increased when combined with Testosterone propionate.
Pemetrexed Cabotegravir may decrease the excretion rate of Pemetrexed which could result in a higher serum level.
Mercaptopurine The excretion of Mercaptopurine can be decreased when combined with Cabotegravir.
Valproic acid The excretion of Valproic acid can be decreased when combined with Cabotegravir.
Clofarabine The excretion of Clofarabine can be decreased when combined with Cabotegravir.
Grepafloxacin The excretion of Grepafloxacin can be decreased when combined with Cabotegravir.
Cidofovir The excretion of Cidofovir can be decreased when combined with Cabotegravir.
Stavudine The excretion of Stavudine can be decreased when combined with Cabotegravir.
Lamivudine The excretion of Lamivudine can be decreased when combined with Cabotegravir.
Adefovir dipivoxil The excretion of Adefovir dipivoxil can be decreased when combined with Cabotegravir.
Didanosine The excretion of Didanosine can be decreased when combined with Cabotegravir.
Zalcitabine The excretion of Zalcitabine can be decreased when combined with Cabotegravir.
Levofloxacin The excretion of Levofloxacin can be decreased when combined with Cabotegravir.
Adenine The metabolism of Cabotegravir can be decreased when combined with Adenine.
Indinavir The metabolism of Cabotegravir can be decreased when combined with Indinavir.
Amitriptyline The metabolism of Cabotegravir can be decreased when combined with Amitriptyline.
Sorafenib The metabolism of Cabotegravir can be decreased when combined with Sorafenib.
Erlotinib The metabolism of Cabotegravir can be decreased when combined with Erlotinib.
Flurbiprofen The metabolism of Cabotegravir can be decreased when combined with Flurbiprofen.
Propofol The metabolism of Cabotegravir can be decreased when combined with Propofol.
Ketoconazole The metabolism of Cabotegravir can be decreased when combined with Ketoconazole.
Probenecid The metabolism of Cabotegravir can be decreased when combined with Probenecid.
Atazanavir The metabolism of Cabotegravir can be decreased when combined with Atazanavir.
Gemfibrozil The metabolism of Cabotegravir can be decreased when combined with Gemfibrozil.
Flunitrazepam The metabolism of Cabotegravir can be decreased when combined with Flunitrazepam.
Deferasirox The metabolism of Cabotegravir can be decreased when combined with Deferasirox.
Nilotinib The metabolism of Cabotegravir can be decreased when combined with Nilotinib.
Eltrombopag The metabolism of Cabotegravir can be decreased when combined with Eltrombopag.

Target Protein

Integrase pol
Gag-Pol polyprotein gag-pol

Referensi & Sumber

Artikel (PubMed)
  • PMID: 26134155
    Bowers GD, Culp A, Reese MJ, Tabolt G, Moss L, Piscitelli S, Huynh P, Wagner D, Ford SL, Gould EP, Pan R, Lou Y, Margolis DA, Spreen WR: Disposition and metabolism of cabotegravir: a comparison of biotransformation and excretion between different species and routes of administration in humans. Xenobiotica. 2016;46(2):147-62. doi: 10.3109/00498254.2015.1060372. Epub 2015 Jul 1.
  • PMID: 31175220
    Patel M, Eberl HC, Wolf A, Pierre E, Polli JW, Zamek-Gliszczynski MJ: Mechanistic Basis of Cabotegravir-Glucuronide Disposition in Humans. J Pharmacol Exp Ther. 2019 Aug;370(2):269-277. doi: 10.1124/jpet.119.258384. Epub 2019 Jun 7.
  • PMID: 24144896
    Spreen W, Min S, Ford SL, Chen S, Lou Y, Bomar M, St Clair M, Piscitelli S, Fujiwara T: Pharmacokinetics, safety, and monotherapy antiviral activity of GSK1265744, an HIV integrase strand transfer inhibitor. HIV Clin Trials. 2013 Sep-Oct;14(5):192-203. doi: 10.1310/hct1405-192.
  • PMID: 23845180
    Johns BA, Kawasuji T, Weatherhead JG, Taishi T, Temelkoff DP, Yoshida H, Akiyama T, Taoda Y, Murai H, Kiyama R, Fuji M, Tanimoto N, Jeffrey J, Foster SA, Yoshinaga T, Seki T, Kobayashi M, Sato A, Johnson MN, Garvey EP, Fujiwara T: Carbamoyl pyridone HIV-1 integrase inhibitors 3. A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744). J Med Chem. 2013 Jul 25;56(14):5901-16. doi: 10.1021/jm400645w. Epub 2013 Jul 11.
  • PMID: 30811880
    Shaik JSB, Ford SL, Lou Y, Zhang Z, Bakshi KK, Tenorio AR, Trezza C, Spreen WR, Patel P: A Phase 1 Study to Evaluate the Pharmacokinetics and Safety of Cabotegravir in Patients With Hepatic Impairment and Healthy Matched Controls. Clin Pharmacol Drug Dev. 2019 Jul;8(5):664-673. doi: 10.1002/cpdd.655. Epub 2019 Feb 27.

Contoh Produk & Brand

Produk: 16 • International brands: 1
Produk
  • Apretude
    Injection, suspension, extended release; Kit • 200 mg/1mL • Intramuscular • US • Approved
  • Apretude
    Tablet, film coated • 30 mg • Oral • EU • Approved
  • Apretude
    - • 600 mg • Intramuscular • EU • Approved
  • Apretude
    - • 600 mg • Intramuscular • EU • Approved
  • Apretude
    Tablet • 30 mg • Oral • Canada • Approved
  • Apretude
    Injection, suspension, extended release; Kit • 200 mg/1mL • Intramuscular • US • Approved
  • Apretude
    Suspension, extended release • 200 mg / mL • Intramuscular • Canada • Approved
  • Cabenuva
    Injection, suspension, extended release; Kit • - • Intramuscular • US • Approved
Menampilkan 8 dari 16 produk.
International Brands
  • Vocabria — ViiV Healthcare

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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