Bictegravir/emtricitabine/tenofovir alafenamide
nucleoside reverse transcriptase inhibitor | |
Tenofovir alafenamide | nucleotide reverse transcriptase inhibitor |
---|---|
Clinical data | |
Trade names | Biktarvy |
AHFS/Drugs.com | Monograph |
MedlinePlus | a618012 |
License data | |
Pregnancy category |
|
Routes of administration | By mouth |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
CAS Number | |
KEGG |
Bictegravir/emtricitabine/tenofovir alafenamide, sold under the brand name Biktarvy, is a
It was approved for use in 2018 in Australia,[6] the European Union[7] and the United States[8] and in 2019 in New Zealand[9] and the United Kingdom;[10] a generic version was approved by the Drugs Controller General of India in 2019.[11] As of 2024,[update] it is recommended as a first-line choice of antiretroviral therapy in several countries, including the European Union,[12] the United Kingdom[13] and the United States.[14]
Combination therapy
Bictegravir/emtricitabine/tenofovir alafenamide is an example of a combination drug that can be taken as a complete regimen for treatment of the human immunodeficiency virus.[5]
Components
Tenofovir alafenamide (TAF) is a prodrug of tenofovir that functions as a nucleotide reverse transcriptase inhibitor (NRTI). Other prodrugs for tenofovir have been tested, but TAF is more efficient at refining HIV-1 therapy. It converts intracellularly to TFV diphosphate, which is a metabolite in HIV target cells.[19] Thus, TAF has higher active metabolite concentrations and lower plasma TFV than other Tenofovir prodrugs.[20] TAF is metabolized primarily with the kidneys, and has a lower dosage than other prodrugs, so it is less detrimental to the renal elimination system.[19]
Medical uses
This drug regimen is intended and approved for adults with HIV-1 infection who have had no previous antiretroviral treatment or for those with
Side effects
This drug should not be co-administered with dofetilide or rifampin. Dofetilide when taken with bictegravir/emtricitabine/tenofovir alafenamide can cause an increase in dofetilide plasma concentrations, which can lead to death. Rifampin and bictegravir/emtricitabine/tenofovir alafenamide when taken together can decrease bictegravir plasma concentrations and cause resistance to bictegravir/emtricitabine/tenofovir alafenamide. Other HIV-1 antiretroviral drugs should not be taken with this therapy.[citation needed]
If kidney disease or development of renal impairment is seen, the drug should be discontinued. Discontinuation of bictegravir/emtricitabine/tenofovir alafenamide in patients with hepatitis B and HIV-1 has been shown to increase the prevalence of hepatitis B, causing liver decompensation and liver failure.[citation needed]
Adverse drug reactions include, but are not limited to, diarrhea, nausea, and headache.[5]
Research
Bictegravir/emtricitabine/tenofovir alafenamide has been investigated for post-exposure prophylaxis (PEP) for preventing HIV infection after exposure and has shown positive early results. However, it has not been approved for this use as of 2024.[21][22][23][24]
References
- ^ "Bictegravir / emtricitabine / tenofovir alafenamide (Biktarvy) Use During Pregnancy". Drugs.com. 16 September 2019. Retrieved 7 March 2020.
- ^ "Regulatory Decision Summary for Biktarvy". 23 October 2014.
- ^ "Drug and medical device highlights 2018: Helping you maintain and improve your health". Health Canada. 14 October 2020. Retrieved 17 April 2024.
- ^ "Biktarvy 50 mg/200 mg/25 mg film-coated tablets - Summary of Product Characteristics (SmPC)". (emc). 25 August 2020. Retrieved 26 August 2020.
- ^ a b c d "Biktarvy- bictegravir sodium, emtricitabine, and tenofovir alafenamide fumarate tablet". DailyMed. 8 August 2019. Retrieved 7 March 2020.
- ^ "Australian Public Assessment Report for Bictegravir / Emtricitabine / Tenofovir alafenamide" (PDF). Therapeutic Goods Administration. 1 August 2019. Retrieved 22 February 2024.
- ^ "Biktarvy". European Medicines Agency. 21 June 2018. Retrieved 22 February 2024.
- ^ "U.S. Food and Drug Administration Approves Gilead's Biktarvy (Bictegravir, Emtricitabine, Tenofovir Alafenamide) for Treatment of HIV-1 Infection" (Press release). Gilead Sciences. 7 February 2018.
- ^ "BIKTARVY Data Sheet v 8.0" (PDF). Medsafe. 24 August 2023. Retrieved 22 February 2024.
- ^ "Bictegravir-emtricitabine-tenofovir alafenamide for the treatment of HIV-1 in adults". NHS England. 17 July 2019. Retrieved 22 February 2024.
- ^ "Hetero launches TAFFIC, the latest 3-in-1 single pill for HIV treatment" (Press release). Hetero Drugs. 17 December 2019. Retrieved 22 February 2024.
- ^ "Initial Regimens: ART-naïve Adults". European AIDS Clinical Society. October 2023. Retrieved 22 February 2024.
- ^ "BHIVA guidelines on antiretroviral treatment for adults living with HIV-1 2022 (2023 interim update)" (PDF). British HIV Association. 28 May 2023. p. 16. Retrieved 22 February 2024.
- ^ "Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV" (PDF). HIV.gov. 21 September 2022. p. 6. Retrieved 22 February 2024.
- ^ "FDA-Approved HIV Medicines Understanding HIV/AIDS". AIDSinfo. Retrieved 22 May 2018.
- PMID 27645238.
- ^ "Emtricitabine". PubChem. United States National Library of Medicine. Retrieved 22 May 2018.
- ^ "Emtricitabine Dosage, Side Effects". AIDSinfo. National Institutes of Health. Retrieved 22 May 2018.
- ^ PMID 26640223.
- ^ "Tenofovir Alafenamide Information for Providers". AIDSinfo. National Institutes of Health. Retrieved 22 May 2018.
- ^ "Boston study finds Biktarvy useful for HIV post-exposure prophylaxis (PEP)". CATIE. 24 February 2022. Retrieved 27 January 2024.
- S2CID 245822499.
- PMID 36719359.
- PMID 38050483.