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Bictegravir/emtricitabine/tenofovir alafenamide

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Bictegravir/emtricitabine/tenofovir alafenamide
Combination of
Bictegravirintegrase inhibitor
Emtricitabinenucleoside reverse transcriptase inhibitor
Tenofovir alafenamidenucleoside reverse transcriptase inhibitor
Clinical data
Trade namesBiktarvy, Taffic[1]
AHFS/Drugs.comMonograph
MedlinePlusa618012
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 fixed-dose combination antiretroviral medication for the treatment of HIV/AIDS.[6] It contains bictegravir, a human immunodeficiency virus type 1 (HIV-1) integrase strand transfer inhibitor; emtricitabine, an HIV-1 nucleoside analog reverse transcriptase inhibitor; and tenofovir alafenamide, an HIV-1 nucleoside analog reverse transcriptase inhibitor.[6]

It was approved for use in 2018 in Australia,[8] the European Union[7] and the United States[9] and in 2019 in New Zealand[10] and the United Kingdom;[11] a generic version was approved by the Drugs Controller General of India in 2019.[1] As of 2024, 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]

Medical uses

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The combination is indicated for the treatment of human immunodeficiency virus 1 (HIV 1) infection in people weighing at least 14 kilograms (31 lb) without present or past evidence of viral resistance to the integrase inhibitor class, emtricitabine or tenofovir.[6][7]

Side effects

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The US FDA prescription label contains a boxed warning about acute exacerbations of hepatitis B.[6]

Adverse drug reactions include, but are not limited to, diarrhea, nausea, and headache.[6]

Combination therapy

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Bictegravir/emtricitabine/tenofovir alafenamide is an example of a combination drug that can be taken as a complete regimen for the treatment of the human immunodeficiency virus.[6]

Combination therapy for HIV, often called highly active antiretroviral therapy (HAART), is composed of two or more types of antiretroviral drugs. Combination therapy decreases the likelihood that drug resistance will occur, because it is unlikely that the HIV-1 strains will be able to mutate enough to become resistant to all drugs being used in the combination. Combination therapy increases the length of lives of patients with HIV-1, and can greatly reduce the possibility for transmission of the virus.[15]

Components

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Bictegravir (BIC) is an integrase strand transfer inhibitor (INSTI). Bictegravir is different from other INSTIs because it contains a bridged bicyclic ring and a distinct benzyl tail with a 2,4,6-trifluorobenzyl group. This contributes to an increase in plasma protein binding and a reduction of activation of the pregnane X receptor (PXR). These changes minimize interactions between drugs, lower clearance, and increase solubility. Bictegravir was found to be less drug resistant than other drugs in the same class.[16]

Emtricitabine (FTC) is a nucleoside reverse transcriptase inhibitor (NRTI) that is a synthetic fluoro derivative of thiacytidine. Within the cell, emtricitabine becomes phosphorylated, which forms emtricitabine 5′-triphosphate within the cell. This allows for the drug to compete with the viral and host substrate and ultimately causes a termination of DNA chain elongation.[17] Underlying hepatitis B virus (HBV) can interact with emtricitabine to cause significant liver damage, but it does not have a significant detrimental effect on the liver when given to patients without HBV.[18]

Tenofovir alafenamide (TAF) is a prodrug of tenofovir that functions as a nucleotide reverse transcriptase inhibitor (NtRTI). 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]

Research

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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

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  1. ^ a b "Hetero launches TAFFIC, the latest 3-in-1 single pill for HIV treatment" (Press release). Hetero Drugs. 17 December 2019. Retrieved 22 February 2024.
  2. ^ "Bictegravir / emtricitabine / tenofovir alafenamide (Biktarvy) Use During Pregnancy". Drugs.com. 16 September 2019. Retrieved 7 March 2020.
  3. ^ "Regulatory Decision Summary for Biktarvy". 23 October 2014.
  4. ^ "Drug and medical device highlights 2018: Helping you maintain and improve your health". Health Canada. 14 October 2020. Retrieved 17 April 2024.
  5. ^ "Biktarvy 50 mg/200 mg/25 mg film-coated tablets - Summary of Product Characteristics (SmPC)". (emc). 25 August 2020. Retrieved 26 August 2020.
  6. ^ a b c d e f g "Biktarvy- bictegravir sodium, emtricitabine, and tenofovir alafenamide fumarate tablet". DailyMed. 8 August 2019. Retrieved 7 March 2020.
  7. ^ a b c "Biktarvy EPAR". European Medicines Agency. 21 June 2018. Retrieved 22 February 2024. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  8. ^ "Australian Public Assessment Report for Bictegravir / Emtricitabine / Tenofovir alafenamide" (PDF). Therapeutic Goods Administration. 1 August 2019. Retrieved 22 February 2024.
  9. ^ "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.
  10. ^ "BIKTARVY Data Sheet v 8.0" (PDF). Medsafe. 24 August 2023. Retrieved 22 February 2024.
  11. ^ "Bictegravir-emtricitabine-tenofovir alafenamide for the treatment of HIV-1 in adults". NHS England. 17 July 2019. Retrieved 22 February 2024.
  12. ^ "Initial Regimens: ART-naïve Adults". European AIDS Clinical Society. October 2023. Retrieved 22 February 2024.
  13. ^ "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.
  14. ^ "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.
  15. ^ "FDA-Approved HIV Medicines Understanding HIV/AIDS". AIDSinfo. Retrieved 22 May 2018.
  16. ^ Tsiang M, Jones GS, Goldsmith J, Mulato A, Hansen D, Kan E, et al. (December 2016). "Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile". Antimicrobial Agents and Chemotherapy. 60 (12): 7086–7097. doi:10.1128/AAC.01474-16. PMC 5118987. PMID 27645238.
  17. ^ "Emtricitabine". PubChem. United States National Library of Medicine. Retrieved 22 May 2018.
  18. ^ "Emtricitabine Dosage, Side Effects". AIDSinfo. National Institutes of Health. Retrieved 22 May 2018.
  19. ^ a b Ray AS, Fordyce MW, Hitchcock MJ (January 2016). "Tenofovir alafenamide: A novel prodrug of tenofovir for the treatment of Human Immunodeficiency Virus". Antiviral Research. 125: 63–70. doi:10.1016/j.antiviral.2015.11.009. PMID 26640223.
  20. ^ "Tenofovir Alafenamide Information for Providers". AIDSinfo. National Institutes of Health. Archived from the original on 2 September 2020. Retrieved 22 May 2018.
  21. ^ "Boston study finds Biktarvy useful for HIV post-exposure prophylaxis (PEP)". CATIE. 24 February 2022. Retrieved 27 January 2024.
  22. ^ Mayer KH, Gelman M, Holmes J, Kraft J, Melbourne K, Mimiaga MJ (May 2022). "Safety and Tolerability of Once Daily Coformulated Bictegravir, Emtricitabine, and Tenofovir Alafenamide for Postexposure Prophylaxis After Sexual Exposure". Journal of Acquired Immune Deficiency Syndromes. 90 (1): 27–32. doi:10.1097/QAI.0000000000002912. PMID 34991141. S2CID 245822499.
  23. ^ Liu A, Xin R, Zhang H, Dai L, Wu RE, Wang X, et al. (November 2022). "An open-label evaluation of safety and tolerability of coformulated bictegravir/emtricitabine/tenofovir alafenamide for post-exposure prophylaxis following potential exposure to human immunodeficiency virus-1". Chinese Medical Journal. 135 (22): 2725–2729. doi:10.1097/CM9.0000000000002494. PMC 9944392. PMID 36719359.
  24. ^ Januszka JE, Drwiega EN, Badowski ME (2023). "Bictegravir/Emtricitabine/Tenofovir Alafenamide for HIV-1: What is the Hidden Potential of This Emerging Treatment?". HIV/AIDS. 15: 705–711. doi:10.2147/HIV.S385877. PMC 10693755. PMID 38050483.
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