Biktarvy® (BIC/FTC/TAF)

Use for HIV-1 Post-Exposure Prophylaxis

This document is in response to your request for information regarding the use of Biktarvy® (bictegravir/emtricitabine/tenofovir alafenamide [BIC/FTC/TAF]) for HIV-1 post‑exposure prophylaxis (PEP).

Some data may be outside of the US FDA-approved prescribing information. In providing this data, Gilead Sciences, Inc. is not making any representation as to its clinical relevance or to the use of any Gilead product(s). For information about the approved conditions of use of any Gilead drug product, please consult the FDA-approved prescribing information.

The full indication, important safety information, and boxed warnings are available at:
www.gilead.com/-/media/files/pdfs/medicines/hiv/biktarvy/biktarvy_pi.

Summary

Product Labeling1

BIC/FTC/TAF is not indicated for use for HIV-1 PEP.

BIC/FTC/TAF is indicated as a complete regimen for the treatment of HIV-1 infection in adults and pediatric patients weighing ≥14 kg who have no ARV treatment history or to replace the current ARV regimen in those who are virologically suppressed (HIV-1 RNA <50 c/mL) on a stable ARV regimen with no known or suspected substitutions associated with resistance to BIC or tenofovir.

Clinical Data on BIC/FTC/TAF Use for PEP

• In a prospective, open-label cohort study that evaluated the adherence, effectiveness, and tolerability of BIC/FTC/TAF or TDF/FTC + DTG as HIV PEP (N=179), 97.8% (90/92) in the BIC/FTC/TAF group and 86.2% (75/87) in the TDF/FTC + DTG group completed 28 days of PEP (P=0.009). No HIV seroconversions occurred through follow-up Week 12. ADRs were reported in 15.2% of participants in the BIC/FTC/TAF group and in 10.3% of participants in the TDF/FTC + DTG group; all were Grade 1 to 2 in severity.2
• In a randomized controlled trial that evaluated the tolerability and adherence to 28 days of BIC/FTC/TAF as HIV PEP with text message support vs standard of care (N=119), 90/102 participants (88%) with available data completed ≥28 days of PEP. No HIV seroconversions occurred among the 66 participants tested at Week 12. AEs associated with BIC/FTC/TAF were mostly mild, and the most common AEs included fatigue (20%), nausea (12%), diarrhea (8%), and headache (8%).3
• In a single-arm, open-label trial that evaluated the safety, tolerability, and adherence to BIC/FTC/TAF for prophylaxis following potential HIV-1 exposure (N=112), 96.4% of participants completed the 28-day PEP regimen, with 98.9% adherence. There were no HIV seroconversions through 24 weeks. AEs attributed to BIC/FTC/TAF were mild and included headache (n=2), diarrhea (n=2), and nausea (n=1).4
• In a non-randomized, open-label trial that evaluated the safety, tolerability, and acceptability of BIC/FTC/TAF for prophylaxis following potential exposure to HIV-1 (N=52), 90.4% of participants completed the 28-day course of BIC/FTC/TAF with no HIV seroconversions when tested at Week 4 or at the 3-month interview. Most AEs were Grade 1 and included vomiting (15.4%), fatigue (9.6%), and diarrhea (7.7%).5

Clinical Data on BIC/FTC/TAF Use for PEP

Prospective Cohort Study of BIC/FTC/TAF vs TDF/FTC + DTG as HIV PEP2

Study design and demographics

A prospective, single-center, open-label cohort study evaluated the adherence, effectiveness, and tolerability of BIC/FTC/TAF and TDF/FTC + DTG as HIV PEP (N=179). Eligible participants were aged ≥18 years, tested negative for HIV at screening, and were exposed to HIV (including, but not limited to, via unprotected sex with someone with HIV or with someone whose status was unknown) within 72 hours of screening; participants with HBV infection were excluded. Participants chose to receive either BIC/FTC/TAF or TDF/FTC + DTG, with follow-up visits on Days 14 and 28 and Weeks 8 and 12 to assess blood and urine for HIV, HCV, HBV, and syphilis. The primary endpoint was the proportion of participants who completed 28 days of PEP. Secondary endpoints included adherence and HIV acquisition rates at Weeks 4 and 12. Baseline demographics are provided in
Table 1.

Table 1. Select Baseline Demographics and Characteristics (Gan et al)2

Results

The rate of PEP completion was 97.8% (90/92) in the BIC/FTC/TAF group and 86.2% (75/87) in the TDF/FTC + DTG group (P=0.009), and the adherence rates were 99.6±2.82% and 90.2±25.29%, respectively (P=0.003). A multivariable logistic regression model that adjusted for confounding variables found that the only assessed factor associated with incomplete PEP adherence was TDF/FTC + DTG use (adjusted odds ratio, 7.02; 95% CI: 1.82–46.29; P<0.05). No HIV seroconversions occurred through follow-up Week 12. ADRs were reported in 15.2% of participants in the BIC/FTC/TAF group and in 10.3% of participants in the TDF/FTC + DTG group; all were Grade 1 to 2 in severity. The most common ADRs were dyslipidemia (5.4%), hepatic function abnormalities (2.2%), increased blood uric acid levels (2.2%), and elevated serum creatinine levels (2.2%) in the BIC/FTC/TAF group and dyslipidemia and increased blood uric acid levels (each, 3.4%) in the TDF/FTC + DTG group. One participant (1.1%) in the TDF/FTC + DTG group discontinued PEP due to a drug-related ADR of dizziness.

Tolerability and Adherence to BIC/FTC/TAF as HIV PEP3

Study design and demographics

A randomized controlled trial evaluated the tolerability and adherence to BIC/FTC/TAF as HIV PEP with text message support vs standard of care. Key inclusion criteria were HIV‑negative individuals aged ≥18 years who had initiated PEP within the past 6 days for sexual exposure and were able/willing to receive texts via mobile phone. The study was a switch study at randomization, with a median of 2 days on PEP before switching to BIC/FTC/TAF to complete 28 days of PEP. HIV status was assessed at baseline, Week 6, and Week 12. Additional outcomes included adherence, assessed via telephone call at Week 4, and AEs, assessed at Week 4 and Week 13 follow-up visits. A total of 120 participants enrolled in the trial; 1 participant was HIV seropositive at baseline and was not included in the analysis. Baseline demographics are listed in Table 2.

Table 2. Select Baseline Demographics and Characteristics (Tan et al)3

Abbreviations: MSM=men who have sex with men; Q=quartile; RAL=raltegravir.

aReport included the highest-risk type of sexual exposure.

Results

A total of 90 of the 102 participants (88%) with available data reported completing ≥28 days of PEP. No HIV seroconversions occurred among the 66 participants (55%) who were tested at Week 12. By the final visit, 28 participants (23%) had initiated PrEP. AEs associated with the study drug were mostly mild, and the most common AEs included fatigue (20%), nausea (12%), diarrhea (8%), and headache (8%). Only 10% of participants experienced AEs of Grade ≥2 severity, which included diarrhea (3%) and fatigue (2%).

Prospective Study of BIC/FTC/TAF as HIV-1 PEP4

Study design and demographics

A prospective, single-arm, open-label, single-site study evaluated the safety, tolerability, and adherence to BIC/FTC/TAF for prophylaxis following potential exposure to HIV-1. Key inclusion criteria were HIV-negative individuals aged ≥18 years who presented to the clinic within 72 hours after potential sexual exposure to HIV-1. Each participant received a fixed-dose formulation of BIC/FTC/TAF and was instructed to take 1 tablet once daily for 28 days. Participants were assessed with laboratory tests at baseline and 2, 4, 12, and 24 weeks; tests included serologies, biochemistry, liver function tests, glucose, and lipids. HIV RNA was tested to exclude participants with acute-stage HIV. Analyzed endpoints included HIV diagnosis, completion of PEP, and PEP adherence via self-reports and pill counts. A total of 112 participants enrolled in the trial. Baseline demographics are listed in Table 3.

Table 3. Select Baseline Demographics and Characteristics (Liu et al)4

Results

Through 24 weeks, there were no HIV seroconversions. Most participants (96.4%) completed the 28-day PEP regimen, with an adherence rate to all expected doses of 98.9% by self-report and 98.5% by pill count. Two participants did not complete the PEP regimen because the source partner was found to be HIV negative; 1 participant was excluded due to HBV; and 1 participant discontinued due to their own decision. AEs attributed to study drug were mild and included headache (n=2), diarrhea (n=2), and nausea (n=1), all of which resolved on their own without discontinuation of BIC/FTC/TAF. Laboratory abnormalities included Grade 1 elevation of SCr level in 4 participants.

Single-Arm Trial of BIC/FTC/TAF as nPEP5

Study design and demographics

A non-randomized, single-site, open-label, single-arm trial evaluated the safety, tolerability, and acceptability of a fixed-dose formulation of BIC/FTC/TAF for prophylaxis following potential non-occupational exposure to HIV-1. The study enrolled 52 HIV-negative participants with possible high-risk sexual exposure to HIV-1 recent enough to permit them to receive the first dose of study medication within 72 hours from the end of the exposure. Participants received a fixed-dose formulation of BIC/FTC/TAF and were instructed to take 1 tablet once a day for 28 days. Participants were assessed at 2 and 4 weeks and at 3 months. The primary endpoints were nPEP failure, as measured with HIV seroconversion during study participation, and safety and tolerability of BIC/FTC/TAF.

The median age of participants was 37.2 years. Reasons for initiating nPEP included having oral intercourse (57.7%), condomless receptive anal intercourse (51.9%), insertive anal intercourse (42.3%), and insertive or receptive vaginal intercourse (5.8% for each). Over half of participants (55.8%) reported ≥1 potential exposure, and 15.4% reported having unprotected intercourse with a partner known to be HIV positive.

Results

Most participants (90.4%) completed the 28-day BIC/FTC/TAF course with no HIV seroconversions detected when tested at Week 4 or at the 3-month interview. Five participants were lost to follow-up.

The most commonly reported AEs included nausea with or without vomiting (15.4%), fatigue (9.6%), and diarrhea (7.7%). All AEs were Grade 1, except for a single report of Grade 2 fatigue, which was associated with discontinuation of BIC/FTC/TAF. Laboratory abnormalities were observed in 9 participants: 7 had decreased CrCl, including 4 with Grade 2 decreased CrCl, and 2 had Grade 1 increased transaminases. All laboratory abnormalities returned to normal upon completion of the BIC/FTC/TAF course.

References

1. Enclosed, Gilead Sciences Inc. BIKTARVY® (bictegravir, emtricitabine, and tenofovir alafenamide) tablets, for oral use. US Prescribing Information. Foster City, CA.

2. Gan L, Xie X, Fu Y, et al. Safety and adherence of bictegravir/emtricitabine/tenofovir alafenamide for HIV post-exposure prophylaxis among adults in Guiyang China: a prospective cohort study. BMC Infect Dis. 2024;24(1):565.

3. Tan DHS, Persaud R, Qamar A, et al. BIC/FTC/TAF as HIV PEP Was Well-Tolerated With High Adherence and No Seroconversions. [Poster 1134]. Paper presented at: Conference on Retroviruses and Opportunistic Infections (CROI); March 3-6, 2024; Denver, Colorado.

4. Liu A, Xin R, Zhang H, et al. 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. 2022;135(22):2725-2729. https://www.ncbi.nlm.nih.gov/pubmed/36719359

5. Mayer K. H, Gelman M, Holmes J, Kraft J, Melbourne K, Mimiaga M. J. Safety and Tolerability of Once Daily Coformulated Bictegravir, Emtricitabine, and Tenofovir Alafenamide for Postexposure Prophylaxis After Sexual Exposure. J Acquir Immune Defic Syndr. 2022;90(1):27-32.

Abbreviations

ADR=adverse drug reaction
AE=adverse event
BIC=bictegravir
DTG=dolutegravir
FTC=emtricitabine
nPEP=non-occupational post-exposure prophylaxis
PEP=post-exposure prophylaxis
PrEP=pre-exposure prophylaxis
TAF=tenofovir alafenamide
TDF=tenofovir disoproxil fumarate

Product Label

For the full indication, important safety information, and boxed warning(s), please refer to the Biktarvy US Prescribing Information available at:
www.gilead.com/-/media/files/pdfs/medicines/hiv/biktarvy/biktarvy_pi.

Follow-Up

For any additional questions, please contact Gilead Medical Information at:

☎1‐866‐MEDI‐GSI (1‐866‐633‐4474) or   www.askgileadmedical.com

Adverse Event Reporting

Please report all adverse events to:

Gilead Global Patient Safety ☎ 1-800-445-3235, option 3 or
 www.gilead.com/utility/contact/report-an-adverse-event

FDA MedWatch Program by ☎ 1-800-FDA-1088 or MedWatch, FDA, 5600 Fishers Ln, Rockville, MD 20852 or   www.accessdata.fda.gov/scripts/medwatch

Data Privacy

The Medical Information service at Gilead Sciences may collect, store, and use your personal information to provide a response to your medical request. We may share your information with other Gilead Sciences colleagues to ensure that your request is addressed appropriately. If you report an adverse event or concern about the quality of a Gilead or Kite product, we will need to use the information you have given us in order to meet our regulatory requirements in relation to the safety of our medicines.

It may be necessary for us to share your information with Gilead’s affiliates, business partners, service providers, and regulatory authorities located in countries besides your own. Gilead Sciences has implemented measures to protect the personal information you provide. Please see the Gilead Privacy Statement (www.gilead.com/privacy-statements) for more information about how Gilead handles your personal information and your rights. If you have any further questions about the use of your personal information, please contact privacy@gilead.com.

BIKTARVY, GILEAD, and the GILEAD logo are registered trademarks of Gilead Sciences, Inc., or its related companies.
© 2025 Gilead Sciences, Inc.