Tenofovir

BIKTARVY is a fixed dose combination of antiretroviral drugs bictegravir (BIC), emtricitabine (FTC), and tenofovir alafenamide (TAF) [see Microbiology (12.4) ] .

• BIKTARVY is indicated as a complete regimen for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults and pediatric patients weighing at least 14 kg: who have no antiretroviral treatment history or to replace the current antiretroviral regimen in those who are virologically-suppressed (HIV-1 RNA less than 50 copies per mL) on a stable antiretroviral regimen with no known or suspected substitutions associated with resistance to bictegravir or tenofovir.ICD-10: B20

• BIKTARVY is contraindicated to be co-administered with: dofetilide due to the potential for increased dofetilide plasma concentrations and associated serious and/or life-threatening events [see Drug Interactions (7.5) ] . rifampin due to decreased BIC plasma concentrations, which may result in the loss of therapeutic effect and development of resistance to BIKTARVY [see Drug Interactions (7.5) ] .contraindicated

Testing: Prior to or when initiating BIKTARVY test for hepatitis B virus infection. Prior to or when initiating BIKTARVY, and during treatment, assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all patients as clinically appropriate. In patients with chronic kidney disease, also assess serum phosphorus. ( 2.1 ) Recommended dosage in adults and pediatric patients weighing at least 25 kg: One tablet containing 50 mg BIC, 200 mg FTC, and 25 mg TAF taken once daily with or without food. ( 2.2 ) Recommended dosage in pediatric patients weighing at least 14 kg to less than 25 kg: One tablet containing 30 mg BIC, 120 mg FTC, and 15 mg TAF taken once daily with or without food. ( 2.3 ) Renal impairment: BIKTARVY is not recommended in patients with estimated creatinine clearance of 15 to below 30 mL/min, or below 15 mL/min who are not receiving chronic hemodialysis, or below 15 mL/min who have no antiretroviral treatment history. ( 2.4 ) Hepatic impairment: BIKTARVY is not recommended in patients with severe hepatic impairment. ( 2.5 ) 2.1 Testing When Initiating and During Treatment with BIKTARVY Prior to or when initiating BIKTARVY, test patients for hepatitis B virus infection [see Warnings and Precautions (5.1) ] . Prior to or when initiating BIKTARVY, and during treatment with BIKTARVY, assess serum creatinine, estimated creatinine clearance, urine glucose and urine protein in all patients as clinically appropriate. In patients with chronic kidney disease, also assess serum phosphorus [see Warnings and Precautions (5.4) ].

Immune reconstitution syndrome: May necessitate further evaluation and treatment. ( 5.3 ) New onset or worsening renal impairment: Assess serum creatinine, estimated creatinine clearance, urine glucose and urine protein when initiating BIKTARVY and during therapy as clinically appropriate in all patients. Also assess serum phosphorus in patients with chronic kidney disease. ( 5.4 ) Lactic acidosis/severe hepatomegaly with steatosis: Discontinue treatment in patients who develop symptoms or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity. ( 5.5 ) 5.1 Severe Acute Exacerbation of Hepatitis B in Patients Coinfected with HIV-1 and HBV Patients with HIV-1 should be tested for the presence of chronic hepatitis B virus (HBV) infection before or when initiating antiretroviral therapy [see Dosage and Administration (2.1) ] . Severe acute exacerbations of hepatitis B (e.g., liver decompensation and liver failure) have been reported in patients who are coinfected with HIV-1 and HBV and have discontinued products containing FTC and/or tenofovir disoproxil fumarate (TDF), and may occur with discontinuation of BIKTARVY. Patients coinfected with HIV-1 and HBV who discontinue BIKTARVY should be closely monitored with both clinical and laboratory follow-up for at least several months after stopping treatment. If appropriate, anti-hepatitis B therapy may be warranted, especially in patients with advanced liver disease or cirrhosis, since post-treatment exacerbation of hepatitis may lead to hepatic decompensation and liver failure.

The following adverse reactions are discussed in other sections of the labeling: Severe Acute Exacerbations of Hepatitis B [see Warnings and Precautions (5.1) ] . Immune Reconstitution Syndrome [see Warnings and Precautions (5.3) ] . New Onset or Worsening Renal Impairment [see Warnings and Precautions (5.4) ]. Lactic Acidosis/Severe Hepatomegaly with Steatosis [see Warnings and Precautions (5.5) ]. Most common adverse reactions (incidence greater than or equal to 5%, all grades) are diarrhea, nausea, and headache. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Gilead Sciences, Inc. at 1-800-GILEAD-5 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Clinical Trials in Adults with No Antiretroviral Treatment History The primary safety assessment of BIKTARVY was based on data from two randomized, double-blind, active-controlled trials, Trial 1489 and Trial 1490, that enrolled 1274 HIV-1 infected adult subjects with no antiretroviral treatment history through Week 144. After Week 144, subjects received open-label BIKTARVY in an optional extension phase for an additional 96 weeks (end of study). A total of 634 and 1025 subjects received one tablet of BIKTARVY once daily during the double-blind (Week 144) and extension phases, respectively [see Clinical Studies (14.2) ] .

Pediatrics: Not recommended for patients weighing less than 14 kg. ( 8.4 ) 8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to BIKTARVY during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary There are insufficient human data on the use of BIKTARVY during pregnancy to inform a drug-associated risk of birth defects and miscarriage. Dolutegravir, another integrase inhibitor, has been associated with neural tube defects (NTDs) (see Data ) . Discuss the benefit-risk of using BIKTARVY with individuals of childbearing potential, particularly if pregnancy is being planned. BIKTARVY use during pregnancy has been evaluated in a limited number of women reported to the APR; consequently, there are insufficient BIC data from the APR to adequately assess the risk of major birth defects. Reports of pregnant individuals treated with other drug products containing TAF or FTC contribute to APR's overall risk assessment for these components. Available data from the APR show no statistically significant difference in the overall risk of major birth defects for FTC or TAF compared with the background rate for major birth defects of 2.7% in a U.S.

Metabolism

The pharmacokinetic (PK) properties of BIKTARVY components are provided in Table 4. The multiple dose PK parameters of BIKTARVY components (based on population pharmacokinetic analysis) are provided in Table 5.

No data are available on overdose of BIKTARVY in patients. If overdose occurs, monitor the patient for evidence of toxicity. Treatment of overdose with BIKTARVY consists of general supportive measures including monitoring of vital signs as well as observation of the clinical status of the patient. Hemodialysis treatment removes approximately 30% of the FTC dose over a 3-hour dialysis period starting within 1.5 hours of FTC dosing (blood flow rate of 400 mL/min and a dialysate flow rate of 600 mL/min). It is not known whether FTC can be removed by peritoneal dialysis. Tenofovir is efficiently removed by hemodialysis with an extraction coefficient of approximately 54%.

• Oct 26, 2001NDANDA021356Gilead Sciences Inc
• Aug 2, 2004NDANDA021752Gilead
• Aug 10, 2011NDANDA202123Gilead Sciences Inc
• Jan 18, 2012NDANDA022577Gilead Sciences Inc
• Aug 27, 2012NDANDA203100Gilead Sciences Inc
• Nov 5, 2015NDANDA207561Gilead Sciences Inc
• Mar 1, 2016NDANDA208351Gilead Sciences Inc
• Apr 4, 2016NDANDA208215Gilead Sciences Inc

1. 1Bone Density Decreased21,49523%
2. 2Chronic Kidney Disease13,64815%
3. 3Renal Failure11,92213%
4. 4Osteonecrosis11,44812%
5. 5Bone Loss11,33912%
6. 6Tooth Loss10,49511%
7. 7Multiple Fractures10,26511%
8. 8Osteoporosis9,83911%
9. 9Renal Injury9,83411%
10. 10Pain9,46510%
11. 11Emotional Distress8,7449.4%
12. 12Skeletal Injury8,6939.4%
13. 13Anxiety8,4809.1%
14. 14Anhedonia7,6668.2%
15. 15Osteopenia5,4685.9%

Recent PubMed references pinned to Tenofovir as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Comparative safety of B/F/TAF versus other antiretroviral therapy regimens for treatment-experienced people with HIV-1: a systematic literature review and network meta-analysis.
  Journal of comparative effectiveness research · 2026 · Curteis T, Eddowes LA, Karlsson A, et al.
  PMID 42206806DOI 10.57264/cer-2026-0013
• Prevotella bivia Influences Antiretroviral Pharmacokinetics and Viral Replication in an Ex Vivo Vaginal Tissue Model.
  Clinical and translational science · 2026 · Lantz AM, Collins LB, Hirsch EB, et al.
  PMID 42148717DOI 10.1111/cts.70597
• Tenofovir, Interferon Pathways, and Mucosal Immunity: Implications for People Living With HIV.
  American journal of reproductive immunology (New York, N.Y. : 1989) · 2026 · Hladik F, Hughes SM, Levy CN, et al.
  PMID 42113488DOI 10.1111/aji.70255
• A Comparative Study of Entecavir and Tenofovir Alafenamide on Quantitative HBsAg Reduction in Patients With CHB.
  Journal of medical virology · 2026 · Lee J, Jin YJ
  PMID 42101128DOI 10.1002/jmv.70958
• Tenofovir Alafenamide in the Treatment of Chronic Hepatitis B Virus Infection in the High-Replicative Low-Inflammatory Phase: A 48-Week Randomized Controlled Trial.
  Journal of medical virology · 2026 · Luo Q, Xu R, Zhang Y, et al.
  PMID 42095461DOI 10.1002/jmv.70960
• Formulation Development of Topical Inserts Containing Doxycycline and Doxycycline Combined with Tenofovir Alafenamide and Elvitegravir for the Prevention of Sexually Transmitted Infections.
  AAPS PharmSciTech · 2026 · Agrahari V, Peet MM, Monpara J, et al.
  PMID 42091755DOI 10.1208/s12249-026-03427-1
• Exposure-response modeling of QTc interval and creatine kinase-MB in healthy people and treatment-naïve adults living with HIV-1 treated with ainuovirine monotherapy or combined with lamivudine and tenofovir DF.
  European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2026 · Zhou Z, Zhang Y, Yun X, et al.
  PMID 42086178DOI 10.1016/j.ejps.2026.107544
• A minimal physiologically based pharmacokinetic model for predicting the metabolism of tenofovir prodrugs in the liver of human with fibrosis.
  Drug metabolism and disposition: the biological fate of chemicals · 2026 · He H, Zhu J, Chen J, et al.
  PMID 42085925DOI 10.1016/j.dmd.2026.100263

The 10 most recently updated of 1,354 ClinicalTrials.gov registrations naming Tenofovir as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Early Metabolic Effects of Antiretroviral Drugs in Healthy volUnteers: a Phase 2 Randomized Study
  Recruiting · Phase 2 · Interventional · 120 enrolled · National Institute of Allergy and Infectious Diseases (NIAID)
  NCT05652478updated 2026-06-12
• A Study of GS-3242 in Combination With Lenacapavir Versus Biktarvy in Virologically Suppressed People With HIV-1
  Not yet recruiting · Phase 2 · Interventional · 175 enrolled · Gilead Sciences
  NCT07645287updated 2026-06-12
• A Study to Provide Continued Access to Study Drug to Children and Adolescents Who Have Completed Clinical Studies Involving Gilead HIV Treatments
  Recruiting · Phase 4 · Interventional · 350 enrolled · Gilead Sciences
  NCT06337032updated 2026-06-10
• Resistance Profile to Antiretroviral Medications in Individuals Living With HIV Who Failed a First-Line Regimen With Tenofovir / Lamivudina and Dolutegravir in Brasil
  Completed · Interventional · 777 enrolled · Federal University of São Paulo
  NCT07618507updated 2026-06-10
• Post-Injectable Cabotegravir Antiretroviral Salvage Strategy Options Trial
  Recruiting · Phase 4 · Interventional · 100 enrolled · University of Witwatersrand, South Africa
  NCT06485154updated 2026-06-09
• Comparative Trial Between Ainuovirine(ANV)/Lamivudine(3TC)/Tenofovir(TDF) and Efavirenz(EFV)/Lamivudine/Tenofovir Regimens
  Not yet recruiting · Phase 4 · Interventional · 60 enrolled · Shanghai Public Health Clinical Center
  NCT07631897updated 2026-06-08
• A Clinical Study of MK-8527 to Prevent Human Immunodeficiency Virus Type 1 (HIV-1) (MK-8527-011)
  Recruiting · Phase 3 · Interventional · 4,390 enrolled · Merck Sharp & Dohme LLC
  NCT07044297updated 2026-06-08
• A Clinical Study of Islatravir and Ulonivirine for People With HIV-1 Who Have Not Been Treated Before (MK-8591B-062)
  Recruiting · Phase 2 · Phase 3 · Interventional · 570 enrolled · Merck Sharp & Dohme LLC
  NCT07266831updated 2026-06-08
• Biktarvy in Treatment-Naïve Late Presenters With HIV-1 Infection
  Completed · Phase 4 · Interventional · 202 enrolled · Peking Union Medical College Hospital
  NCT04296695updated 2026-06-05
• Inhibition of HBV Replication and Biological Reversal of Cirrhosis (F3-F4) and HCC by Flavonoids
  Completed · Phase 4 · Interventional · 134 enrolled · Trieu, Nguyen Thi, M.D.
  NCT07084948updated 2026-06-05

CPIC-curated drug–gene pairs for Tenofovir. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• ABCC4CPIC D (provisional)ClinPGx 3

Frequently asked questions

How does Tenofovir work?

BIKTARVY is a fixed dose combination of antiretroviral drugs bictegravir (BIC), emtricitabine (FTC), and tenofovir alafenamide (TAF) [see Microbiology (12.4) ] .

What is Tenofovir used for?

According to FDA labeling, Tenofovir carries indications including: BIKTARVY is indicated as a complete regimen for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults and pediatric patients weighing at least 14 kg: who have no antiretroviral treatment history or to replace the current antiretroviral regimen in those who are virologically-suppressed (HIV-1 RNA less than 50 copies per mL) on a stable antiretroviral regimen with no known or suspected substitutions associated with resistance to bictegravir or tenofovir.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Tenofovir?

Tenofovir is classified as Nucleoside Reverse Transcriptase Inhibitors, Decreased Reverse Transcription to DNA, Increased Immunologically Active Molecule Activity.

What are the contraindications for Tenofovir?

Tenofovir labeling lists contraindications including: BIKTARVY is contraindicated to be co-administered with: dofetilide due to the potential for increased dofetilide plasma concentrations and associated serious and/or life-threatening events [see Drug Interactions (7.5) ] . rifampin due to decreased BIC plasma concentrations, which may result in the loss of therapeutic effect and development of resistance to BIKTARVY [see Drug Interactions (7.5) ] .. Always consult the full prescribing information and a clinician.