INDICATION

BIKTARVY® is indicated as a complete regimen for the treatment of HIV-1 infection in adults who have no antiretroviral (ARV) treatment history or to replace the current ARV regimen in those who are virologically suppressed (HIV-1 RNA <50 copies per mL) on a stable ARV regimen for ≥3 months with no history of treatment failure and no known resistance to any component of BIKTARVY.

DHHS RECOMMENDED
AS AN INITIAL REGIMEN FOR
ADULTS WITH HIV-11

BIKTARVY® is a Triple Therapy STR that Combines the DESCOVY® (FTC/TAF)* Backbone With Bictegravir, a Novel and Unboosted INSTI1,2


INSTI: bictegravir 50mg plus DESCOVY (FTC/TAF) Dual-NRTI Backbone: emtricitabine 200mg/tenofovir alafenamide 25mg

Pharmacokinetics

  • Bictegravir has a long plasma half-life of 17.3 hours1,3

*emtricitabine 200 mg/tenofovir alafenamide 25 mg.

Triple Therapy Blocks Steps Essential to HIV Replication4-11

A dual-NRTI backbone and a third agent, such as an INSTI, together inhibit viral replication and reduce the risk of ARV resistance4-6



BIKTARVY Mechanism of Action (MOA)
BIKTARVY Mechanism of Action (MOA)


Dual-NRTI backbones include FTC/TAF, FTC/TDF, and ABC/3TC.

INDICATION

BIKTARVY® is indicated as a complete regimen for the treatment of HIV-1 infection in adults who have no antiretroviral (ARV) treatment history or to replace the current ARV regimen in those who are virologically suppressed (HIV-1 RNA <50 copies per mL) on a stable ARV regimen for ≥3 months with no history of treatment failure and no known resistance to any component of BIKTARVY.

DHHS RECOMMENDED
AS AN INITIAL REGIMEN FOR
ADULTS WITH HIV-11

IMPORTANT SAFETY INFORMATION

BOXED WARNING: POST TREATMENT ACUTE EXACERBATION OF HEPATITIS B

  • Severe acute exacerbations of hepatitis B have been reported in patients who are coinfected with HIV-1 and HBV and have discontinued products containing emtricitabine (FTC) and/or tenofovir disoproxil fumarate (TDF), and may occur with discontinuation of BIKTARVY. Closely monitor hepatic function with both clinical and laboratory follow-up for at least several months in patients who are coinfected with HIV-1 and HBV and discontinue BIKTARVY. If appropriate, anti-hepatitis B therapy may be warranted.

IMPORTANT SAFETY INFORMATION (cont'd)

Contraindications

  • Coadministration: Do not use BIKTARVY with dofetilide or rifampin.

Warnings and precautions

  • Drug interactions: See Contraindications and Drug Interactions sections. Consider the potential for drug interactions prior to and during BIKTARVY therapy and monitor for adverse reactions.
  • Immune reconstitution syndrome, including the occurrence of autoimmune disorders with variable time to onset, has been reported.
  • New onset or worsening renal impairment: Cases of acute renal failure and Fanconi syndrome have been reported with the use of tenofovir prodrugs. In clinical trials of BIKTARVY, there have been no cases of Fanconi syndrome or proximal renal tubulopathy (PRT). Do not initiate BIKTARVY in patients with estimated creatinine clearance (CrCl) <30 mL/min. Patients with impaired renal function and/or taking nephrotoxic agents (including NSAIDs) are at increased risk of renal-related adverse reactions. Discontinue BIKTARVY in patients who develop clinically significant decreases in renal function or evidence of Fanconi syndrome.
    Renal monitoring: Prior to or when initiating BIKTARVY and during therapy, assess serum creatinine, CrCl, urine glucose, and urine protein in all patients as clinically appropriate. In patients with chronic kidney disease, also assess serum phosphorus.
  • Lactic acidosis and severe hepatomegaly with steatosis: Fatal cases have been reported with the use of nucleoside analogs, including FTC and TDF. Discontinue BIKTARVY if clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity develop, including hepatomegaly and steatosis in the absence of marked transaminase elevations.

Adverse reactions

  • Most common adverse reactions (incidence ≥5%; all grades) in clinical studies were diarrhea (6%), nausea (5%), and headache (5%).

Drug interactions

  • Prescribing information: Consult the full prescribing information for BIKTARVY for more information on Contraindications, Warnings, and potentially significant drug interactions, including clinical comments.
  • Enzymes/transporters: Drugs that induce P-gp or induce both CYP3A and UGT1A1 can substantially decrease the concentration of components of BIKTARVY. Drugs that inhibit P-gp, BCRP, or inhibit both CYP3A and UGT1A1 may significantly increase the concentrations of components of BIKTARVY. BIKTARVY can increase the concentration of drugs that are substrates of OCT2 or MATE1.
  • Drugs affecting renal function: Coadministration of BIKTARVY with drugs that reduce renal function or compete for active tubular secretion may increase concentrations of FTC and tenofovir and the risk of adverse reactions.

Dosage and administration

  • Dosage: 1 tablet taken once daily with or without food.
  • Renal impairment: Not recommended in patients with CrCl <30 mL/min.
  • Hepatic impairment: Not recommended in patients with severe hepatic impairment.
  • Prior to or when initiating: Test patients for HBV infection.
  • Prior to or when initiating, and during treatment: As clinically appropriate, assess serum creatinine, CrCl, urine glucose, and urine protein in all patients. In patients with chronic kidney disease, assess serum phosphorus.

Pregnancy and lactation

  • Pregnancy: There is insufficient human data on the use of BIKTARVY during pregnancy. An Antiretroviral Pregnancy Registry (APR) has been established. Available data from the APR for FTC shows no difference in the rates of birth defects compared with a US reference population.
  • Lactation: Women infected with HIV-1 should be instructed not to breastfeed, due to the potential for HIV-1 transmission.

3TC, lamivudine; ABC, abacavir; ARV, antiretroviral; FTC, emtricitabine; INSTI, integrase strand transfer inhibitor; NRTI, nucleoside reverse transcriptase inhibitor; TAF, tenofovir alafenamide; TDF, tenofovir disoproxil fumarate.

References: 1. BIKTARVY [package insert]. Foster City, CA: Gilead Sciences, Inc.; 2018. 2. Tsiang M, Jones GS, Goldsmith J, et al. Antiviral activity of bictegravir (GS-9883), a novel potent HIV-1 integrase strand transfer inhibitor with an improved resistance profile. Antimicrob Agents Chemother. 2016;60(12):7086-7097. 3. Data on file. Gilead Sciences, Inc. 4. Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in adults and adolescents living with HIV. Department of Health and Human Services. http://aidsinfo.nih.gov/ContentFiles/AdultandAdolescentGL.pdf. Updated March 27, 2018. Accessed March 27, 2018. 5. US Department of Health and Human Services. The HIV life cycle. AIDSinfo website. https://aidsinfo.nih.gov/understanding-hiv-aids/factsheets/19/73/the-hiv-life-cycle. Updated August 18, 2017. Accessed October 26, 2017. 6. US Department of Health and Human Services. FDA-approved HIV medicines. AIDSinfo website. https://aidsinfo.nih.gov/understanding-hiv-aids/fact-sheets/21/58/fda-approved-hiv-medicines. Updated August 18, 2017. Accessed October 26, 2017. 7. Laskey SB, Siliciano RF. A mechanistic theory to explain the efficacy of antiretroviral therapy. Nat Rev Microbiol. 2014;12(11):772-780. 8. Callebaut C, Stepan G, Tian Y, Miller MD. In vitro virology profile of tenofovir alafenamide, a novel oral prodrug of tenofovir with improved antiviral activity compared to that of tenofovir disoproxil fumarate. Antimicrob Agents Chemother. 2015;59(10):5909-5916. 9. Feng JY, Ly JK, Myrick F, et al. The triple combination of tenofovir, emtricitabine and efavirenz shows synergistic anti-HIV-1 activity in vitro: a mechanism of action study. Retrovirology. 2009;6:44. 10. Ray AS, Myrick F, Vela JE, et al. Lack of a metabolic and antiviral drug interaction between tenofovir, abacavir and lamivudine. Antivir Ther. 2005;10(3):451-457. 11. US Department of Health and Human Services. Nucleoside reverse transcriptase inhibitor (NRTI). AIDSinfo website. https://aidsinfo.nih.gov/understanding-hiv-aids/glossary/902/nucleoside-reverse-transcriptase-inhibitor. Updated March 30, 2018. Accessed March 30, 2018.