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Last update 14 Apr 2025

Emtricitabine

Last update 14 Apr 2025

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(2R-cis)-4-amino-5-fluoro-1-(2-(hydroxymethyl)-1,3-oxathiolan-5-yl)-2(1H)-pyrimidinone, (−)-(2R,5S)-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine, (−)-2'-deoxy-5-fluoro-3'-thiacytidine

+ [18]

Target

Action

inhibitors

Mechanism

RT inhibitors(Reverse transcriptase inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesUrogenital Diseases+ [3]

Active Indication

HIV InfectionsAicardi-Goutieres Syndrome

Inactive Indication

CoinfectionHepatitis BHepatitis B, Chronic+ [1]

Originator Organization

Gilead Sciences, Inc.

Active Organization

Gilead Sciences Ireland UC

Gilead Sciences, Inc.

Hebei Medical University Pharmaceutical Factory

Inactive Organization

Triangle Pharmaceuticals, Inc.

Drug Highest PhaseApproved

First Approval Date

United States (02 Jul 2003),

HIV Infections

RegulationOrphan Drug (Japan)

Structure/Sequence

Molecular FormulaC8H10FN3O3S

InChIKeyXQSPYNMVSIKCOC-NTSWFWBYSA-N

CAS Registry143491-57-0

113

Clinical Trials associated with Emtricitabine

NCT03304717

/ Not yet recruitingPhase 1/2

Reverse Transcriptase Inhibitors in Aicardi Goutières Syndrome

The overall objectives are to explore the safety and efficacy of Reverse Transcriptase Inhibitors Tenofovir (TDF)/ Emtricitabine (FTC) administered in AGS affected children 2 to 18 years of age.

Start Date01 Dec 2025

Sponsor / Collaborator

The Children's Hospital of Philadelphia

[+5]

NCT06338826

/ Not yet recruitingPhase 2IIT

Interventional, Multicenter, Open-label, Randomized, Non-comparative Trial Evaluating the Safety, in Terms of HBV Virological Control At 96 Weeks, of 2 Antiviral Treatment Relief Strategies, in Patients Co-infected with the HIV-1 and HBV Viruses

The main objective of this study is to evaluate at 96 weeks the safety with respect to hepatitis B control of 2 treatment reduction strategies for patients with previously controlled HIV-HBV co-infection on continuous triple therapy

Start Date01 Feb 2025

Sponsor / Collaborator-

IRCT20240803062623N5

/ RecruitingNot ApplicableIIT

Intervention group: single dose, one oral tablets Descovy Emtricitabine 200 mg with Tenofovir Alfenamide Fumarate 25 mg as a reference product. after washout period, the volunteers received Emtricitabine 200 mgwith Tenofovir Alfenamide Fumarate 25 mg Tadbir Kalaye jam pharmaceutical Co. Iran

Start Date21 Nov 2024

Sponsor / Collaborator-

100 Clinical Results associated with Emtricitabine

100 Translational Medicine associated with Emtricitabine

100 Patents (Medical) associated with Emtricitabine

6,688

Literatures (Medical) associated with Emtricitabine

31 Dec 2025·HIV Research & Clinical Practice

Bictegravir/emtricitabine/tenofovir alafenamide in clinical practice for people with HIV: final 24-month effectiveness and safety outcomes in key populations in the observational BICSTaR cohort

Article

Author: Uriel, Alison ; Watanabe, Dai ; Robineau, Olivier ; Choy, Chiaw Yee ; Mallolas, Josep ; Marchetti, Giulia ; Thorpe, David ; Yang, Chia-Jui ; Vogelmann, Roger ; Berrevoets, Marvin ; D’Amato, Lisa ; Heinzkill, Marion ; Ramroth, Johanna ; Trottier, Benoit ; De Barra, Eoghan ; Marongiu, Andrea ; Elbirt, Daniel ; Lee, Sun Hee ; Gündüz, Alper

BACKGROUND:

BICtegravir Single Tablet Regimen (BICSTaR) is an observational cohort study evaluating the effectiveness and safety of bictegravir/emtricitabine/tenofovir alafenamide (B/F/TAF) in treatment-naïve (TN) and treatment-experienced (TE) people with HIV.

OBJECTIVE:

To present final pooled 24-month outcomes for the full cohort.

METHODS:

Prospective data were pooled from TN and TE adults with HIV initiating B/F/TAF in routine clinical practice across 14 countries (data collection: 25/06/2018-29/12/2023). Outcomes at 24 months included virologic suppression (HIV-1 RNA <50 copies/mL), immunologic effectiveness (change in CD4 cell count and CD4/CD8 ratio), persistence, and safety. Outcomes were also analysed in key populations.

RESULTS:

Of 2,074 (483 TN, 1,591 TE) participants included, most were male (85%), White (70%), and had ≥1 comorbidity (66%). Median (Q1, Q3) age was 45 (35, 54) years. At 24 months, 94% of TN and 96% of TE participants had HIV-1 RNA <50 copies/mL (missing = excluded analysis). These values were 88% and 86%, respectively, in a discontinuation = failure analysis. Effectiveness remained high across all key populations at 24 months. Median (Q1, Q3) CD4 count increased by 257 (127, 447) cells/µL in TN and 40 (-70, 153) cells/µL in TE participants (both p < 0.001). There was no reported treatment-emergent resistance to B/F/TAF. Persistence was high at 24 months (TN, 95%; TE, 91%). Drug-related adverse events occurred in 11% of TN and 12% of TE participants, leading to B/F/TAF discontinuation in 5%.

CONCLUSIONS:

B/F/TAF was generally well tolerated over 24 months, with high effectiveness and persistence observed among a broad range of people with HIV.

31 Dec 2025·HIV Research & Clinical Practice

Evaluation of the effect of 48 weeks of BIC/F/TAF and DRV/c/F/TAF on platelet function in the context of rapid ART start

Article

Author: Boffito, Marta ; Henderson, Merle ; Whitlock, Gary ; Khawaja, Akif A. ; Taylor, Graham P. ; Fidler, Sarah ; Soler-Carracedo, Alfredo ; Emerson, Michael

INTRODUCTION:

The BIC-T&T study aimed to determine the efficacy of bictegravir/emtricitabine/tenofovir alafenamide (BIC/F/TAF) and darunavir/cobicistat/emtricitabine/tenofovir alafenamide (DRV/c/F/TAF) at suppressing viral load in a two-arm, open-label, multi-centre, randomised trial under a UK test-and-treat setting. This sub-study aimed to evaluate potential off-target cardiovascular impact by examining ex vivo platelet function.

METHODS:

Platelets were isolated by centrifugation of citrated blood from participants attending Chelsea and Westminster Hospital or St Mary's Hospital at Week 48 following enrolment. Platelet activation was assessed by real-time flow cytometry to examine integrin activation and granule release and platelet aggregation was evaluated by light transmission aggregometry. Statistical significance was determined by 2-way ANOVA with a Šidák's multiple comparisons post-test.

RESULTS:

An analysis of 21 participants was performed at Week 48 (96% male and 48% white; mean (range) age was 37 (23-78) years). No difference between arms was observed in ADP-, collagen- or thrombin receptor activator for peptide (TRAP)-6-evoked platelet α_IIbβ₃ integrin activation, granule release or platelet aggregation in response to any of the agonists tested. Despite differences in the demographics between treatment arms, the presence of an unboosted integrase inhibitor or boosted protease inhibitor in a test-and-treat setting did not impact platelet function.

CONCLUSIONS:

Our study provides no evidence of differences in downstream platelet responses between participants taking BIC/F/TAF compared to DRV/c/F/TAF following 48 wk of treatment. Further data are required to explore whether there are biologically significant off-target effects, including effects on platelets and other components of the cardiovascular system between these two test-and-treat regimens.

CLINICAL TRIAL NUMBER:

NCT04653194.

01 Jun 2025·CLINICAL BIOCHEMISTRY

The case of a bloody mess – Bictegravir/emtricitabine/tenofovir alafenamide induced colitis

Article

Author: Asare-Werehene, Meshach ; Bohn, Mary Kathryn ; Selvaratnam, Rajeevan ; Ming-Freckleton, Allison

BACKGROUND:

Fecal calprotectin is a marker used to differentiate inflammatory bowel disease versus irritable bowel syndrome and is relevant in the diagnosis of ulcerative colitis and Crohn's disease. Markedly elevated calprotectin from stool samples provides evidence of colonic inflammation to support the diagnosis of pancolitis. This report is the first to demonstrate the clinical significance of fecal calprotectin in supporting the diagnosis of pancolitis induced by the anti-viral drug, Biktarvy (bictegravir/emtricitabine/tenofovir alafenamide).

CASE REPORT:

A 62-year-old male on Biktarvy for his HIV diagnosis was admitted to internal medicine with abdominal pain, bloody diarrhea and pancolitis. His white blood cell count was 15.8 (4.0-11.0x10⁹/L), neutrophil count was 9.7 (2.0-7.5 × 10⁹/L), monocyte count was 1.2 (0.2-0.8 × 10⁹/L), granulocyte count was 1.5 (≤0.1 × 10⁹/L) and hemoglobin was 163 (140-180 g/L). The patient had a C-reactive protein of 229 (≤11.0 mg/L). Serology and blood culture were negative for microbial testing and abdomino-pelvic computed tomography findings were unremarkable. A bloody stool collected had a fecal calprotectin level of 1,159 (<50 µg/g).

CONCLUSIONS:

This case highlights how anti-retroviral therapies such as Biktarvy may elicit medication-induced gastrointestinal symptoms, which may underlie the cause of bloody diarrhea and pancolitis, and consequently a grossly elevated fecal calprotectin.

187

News (Medical) associated with Emtricitabine

12 Mar 2025

·pipelinereview.com

Gilead Presents New HIV Treatment and Cure Research Data at CROI 2025, Including an Investigational Long-Acting, Twice-Yearly Therapy Option

– Long-Term Outcomes Reinforce the High Efficacy of Biktarvy ® in People with HIV and HBV Coinfection – – Investigational Long-Acting, Twice-Yearly Treatment Regimen of Lenacapavir and Broadly Neutralizing Antibodies (bNAbs) Meets Primary Endpoint in Phase 2 Study and Gains Breakthrough Therapy Designation – – Late-Breaker Oral Presentation of Phase 2 Results from the First HIV Cure Clinical Trial Conducted in South Africa – FOSTER CITY, CA, USA I March 12, 2025 I Gilead Sciences, Inc. (Nasdaq: GILD) today announced the presentation of late-breaking data and multiple oral presentations from its innovative HIV treatment portfolio and pipeline at the Conference on Retroviruses and Opportunistic Infections (CROI 2025). The new findings reflect a transformative portfolio and a rapidly advancing forward-looking pipeline focused on expanding choices and enhancing outcomes for those with HIV, while continuing to reach towards a cure. “Gilead is fueling the next wave of innovation in HIV to help end the epidemic globally,” said Jared Baeten, MD, PhD, Senior Vice President, Virology Therapeutic Area Head. “Our contributions to CROI spotlight our dedication to scientific discovery, reflect our commitment to addressing the diverse treatment needs and preferences of communities affected by HIV and underscore the vital importance of catalyzing research reaching towards a cure.” Biktarvy Demonstrates High Rates of Viral Suppression in People with HIV/HBV Coinfection ALLIANCE ( NCT03547908 ) is an ongoing Phase 3 study evaluating Biktarvy versus dolutegravir 50 mg (DTG) + emtricitabine 200 mg/tenofovir disoproxil fumarate 300 mg, F/TDF, DTG+F/TDF, in adults with HIV-1/HBV co-infection initiating treatment. The ALLIANCE trial is the first randomized clinical trial of TAF- vs TDF-based regimens in treatment naïve adults with HIV/HBV coinfection. Its goal is to evaluate treatment regimens that may effectively suppress both HIV and HBV. Previously reported results demonstrated the efficacy of both antiretroviral regimens. New outcomes were presented at CROI. Week 48 outcomes from the open-label extension phase following the 96-week randomized phase reported on the longer-term efficacy and safety of the investigational use of Biktarvy in adults with HIV/HBV coinfection initiating treatment. The newly presented data shows that Biktarvy maintained high rates of HIV-1 (95.4%) and HBV (86.6%) virologic suppression, defined as HIV RNA <50 copies/ mL and HBV DNA <29 IU/ mL, respectively, in participants (n=89) following a switch to Biktarvy after 96 weeks of treatment with DTG+ F/TDF. Study drug-related treatment-emergent adverse events (TEAEs) were reported in 19% of participants and most were mild to moderate, with zero discontinuations due to TEAEs. The most commonly reported study drug–related TEAEs were weight gain (9%) and low-density lipoprotein (LDL) cholesterol increased (3%). These data demonstrate the high rates of viral suppression by Biktarvy in adults with both HIV-1 and HBV switching their treatment to Biktarvy. The use of Biktarvy in individuals with HIV/HBV co-infection is investigational and the safety and efficacy of this use have not been established. Breakthrough Therapy Designation Awarded to Long-Acting, Twice-Yearly Investigational Treatment Combination Regimen of Lenacapavir and Broadly Neutralizing Antibodies (bNAbs) In January 2025, the FDA granted lenacapavir (LEN) with bNAbs (teropavimab [GS-5423, TAB] and zinlirvimab [GS-2872, ZAB]) Breakthrough Therapy Designation, which is intended to expedite the development of new drugs that may demonstrate substantial improvement over available therapy. LEN+TAB+ZAB (LTZ) harbors the potential to be the first long-acting combination treatment regimen with twice-yearly dosing. At CROI 2025, the primary results of a Phase 2 study evaluating the investigational combination of LTZ were presented during an oral session and featured in the press program; those data announced at CROI confirm previously presented Phase 1b results. The Phase 2 ( NCT05729568 ) open-label study from Gilead’s long-acting treatment pipeline evaluated the treatment response of participants receiving the investigational combination of LTZ. Efficacy and safety results were evaluated when virologically suppressed adults switched to LTZ every 6 months versus staying on stable baseline oral antiretroviral regimen. The study met its primary endpoint, which is the proportion of participants with HIV-1 RNA ≥ 50 copies/mL at Week 26 as determined by the US FDA-defined snapshot algorithm. The Week 26 data demonstrated the high efficacy of the LTZ regimen, with 96% (n=51 of 53) of participants who received LTZ and 96% (n=26 of 27) who received SBR remained virologically suppressed. CD4 cell counts also increased from baseline to week 26 in both groups, with a mean change of +23/μL (n=143) with LTZ and +69/μL (n=203) with SBR. The most common AEs with LTZ were injection site reactions related to subcutaneous LEN administration. There were no serious adverse events (AEs) related to LTZ; there were no infusion reactions related to TAB or ZAB. One participant in the SBR arm discontinued the study due to a serious treatment-related AE. Teropavimab and zinlirvimab are investigational compounds. The use of these compounds in combination with lenacapavir are investigational. They are not approved by the U.S. Food and Drug Administration or any other regulatory authority for any use, alone or in combination with lenacapavir. Their safety and efficacy are unknown. The use of lenacapavir in virologically suppressed people with HIV is investigational and the safety and efficacy of this use have not been established. Landmark HIV Cure Clinical Trial Conducted in South Africa Results from the first HIV cure trial to be conducted in South Africa, sponsored by Gilead, demonstrated that complex cure studies can be successfully conducted, alongside community, in resource-limited settings where great unmet need exists. As part of Gilead’s efforts to find a cure for HIV, the Phase 2a GS-US-382-5445 trial ( NCT05281510 ) enrolled 20 South African cisgender women from the FRESH (Females Rising through Education, Support, and Health) cohort who had received antiretroviral therapy (ART) soon after acquiring HIV and were virologically suppressed for at least 12 months. Participants received up to 10 oral doses of Gilead’s investigational TLR7 agonist, vesatolimod, every 2 weeks starting on day 0, plus IV infusions of broadly neutralizing antibodies (bNAbs) VRC07-523LS and CAP256V2LS, provided by the National Institutes of Health (NIH), on day 7. Participants began an analytical treatment interruption (ATI) on Day 35 and remained off ART until Week 48, or until they met restart criteria. Participants who reached week 48 without meeting ART restart criteria had the option of remaining off ART through the end of study follow-up at Week 60. Results presented at CROI showed the treatment combination was generally well-tolerated with no treatment-related serious adverse events (TEAEs) reported. The most common study TEAEs were infusion-related reactions (n = 18; 16 grade 1, 2 grade 2). Seventy percent of participants (n=14) met ART restart criteria. Thirty percent (n=6) remained off ART through Week 48, of which 4 remained off ART through Week 60. While the data suggest that the trial regimen alone is not sufficient as an HIV cure regimen, the mechanistic learnings will inform the development of future cure approaches. There is currently no cure for HIV or AIDS. Vesatolimod, VRC07-523LS and CAP256V2LS are investigational compounds. They are not approved by the U.S. Food and Drug Administration or any other regulatory authority for any use, alone or in combination. Their safety and efficacy are unknown. Please see below for U.S. Indications and Important Safety Information, including Boxed Warning , for Biktarvy. About Lenacapavir Lenacapavir is approved in multiple countries for the treatment of adults with multi-drug resistant HIV in combination with other antiretrovirals. The use of lenacapavir for HIV prevention is investigational and the safety and efficacy of lenacapavir for this use have not been established. The multi-stage mechanism of action of lenacapavir is distinguishable from other currently approved classes of antiviral agents. While most antivirals act on just one stage of viral replication, lenacapavir is designed to inhibit HIV at multiple stages of its lifecycle and has no known cross resistance exhibited in vitro to other existing drug classes. Lenacapavir is being evaluated as a long-acting option in multiple ongoing and planned early and late-stage clinical studies in Gilead’s HIV prevention and treatment research program. Lenacapavir is being developed as a foundation for potential future HIV therapies with the goal of offering both long-acting oral and injectable options with several dosing frequencies, in combination or as a mono agent, that help address individual needs and preferences of people and communities affected by HIV. Science Magazine named lenacapavir its 2024 “Breakthrough of the Year.” About Biktarvy Biktarvy is a complete HIV treatment that combines three powerful medicines to form the smallest 3-drug, integrase strand transfer inhibitor (INSTI)-based single-tablet regimen (STR) available, offering simple once-daily dosing with or without food, with a limited drug interaction potential and a high barrier to resistance. Biktarvy combines the novel, unboosted INSTI bictegravir with the F/TAF backbone. Biktarvy is a complete STR and should not be taken with other HIV medicines. U.S. Indication for Biktarvy Biktarvy (bictegravir 50 mg/emtricitabine 200 mg/tenofovir alafenamide 25 mg) is indicated as a complete regimen for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 14 kg 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 with no known or suspected substitutions associated with resistance to bictegravir or tenofovir. About Gilead HIV Gilead Sciences, Inc. is a biopharmaceutical company that has pursued and achieved breakthroughs in medicine for more than three decades, with the goal of creating a healthier world for all people. The company is committed to advancing innovative medicines to prevent and treat life-threatening diseases, including HIV, viral hepatitis, COVID-19, and cancer. Gilead operates in more than 35 countries worldwide, with headquarters in Foster City, California. For more than 35 years, Gilead has been a leading innovator in the field of HIV, driving advances in treatment, prevention and cure research. Gilead researchers have developed 12 HIV medications , including the first single-tablet regimen to treat HIV, the first antiretroviral for pre-exposure prophylaxis (PrEP) to help reduce new HIV infections, and the first long-acting injectable HIV treatment medication administered twice-yearly. Our advances in medical research have helped to transform HIV into a treatable, preventable, chronic condition for millions of people. Gilead is committed to continued scientific innovation to provide solutions for the evolving needs of people affected by HIV around the world. Through partnerships , collaborations and charitable giving, the company also aims to improve education, expand access and address barriers to care, with the goal of ending the HIV epidemic for everyone, everywhere. Gilead has been repeatedly recognized as one of the top two leading philanthropic funders of HIV-related programs in a report released by Funders Concerned About AIDS. SOURCE: Gilead Sciences

Clinical ResultPhase 2Phase 3Drug ApprovalBreakthrough Therapy

12 Mar 2025

·pipelinereview.com

First Clinical Data for Gilead’s Investigational Once-Yearly Lenacapavir for HIV Prevention Presented at CROI 2025 and Published in The Lancet

– Phase 1 Data Indicate Potential for Use of Once-Yearly Lenacapavir for HIV Prevention, with Plans to Launch a Phase 3 Trial in 2H 2025 – – Also at CROI: New PURPOSE 1 Data Showcasing Preference for Twice-Yearly Lenacapavir vs. Once-Daily Orals and In-Depth Look at Adolescent Pharmacokinetic, Safety and Efficacy Data – FOSTER CITY, CA, USA I Marcch 11, 2025 I Gilead Sciences, Inc. (Nasdaq: GILD) today presented the first data from its ongoing Phase 1 study investigating two novel, once-yearly formulations of lenacapavir, the company’s injectable HIV-1 capsid inhibitor, for the investigational use of HIV prevention as pre-exposure prophylaxis (PrEP). The data were presented during an oral abstract session at the Conference on Retroviruses and Opportunistic Infections (CROI 2025) and were also published today in The Lancet . Data will support the future development of once-yearly lenacapavir for PrEP, for which Gilead plans to launch a Phase 3 study in the second half of 2025. The Phase 1 study data showed that the two different formulations of once-yearly lenacapavir administered via intramuscular injection achieved and maintained plasma concentrations exceeding those associated with HIV prevention efficacy observed in the Phase 3 PURPOSE 1 trial ( NCT04994509 ) and PURPOSE 2 trial ( NCT04925752 ). The previously reported PURPOSE 1 and PURPOSE 2 data showed that twice-yearly subcutaneous lenacapavir demonstrated superiority at reducing HIV infections when compared to background HIV incidence (bHIV) and once-daily oral Truvada® (emtricitabine 200mg and tenofovir disoproxil fumarate 300mg; F/TDF) in a broad and geographically diverse range of people. “Gilead is continuing to innovate in our work to develop additional person-centered long-acting injectable and oral options to help people find an HIV prevention choice that is right for them,” said Jared Baeten, MD, PhD, Senior Vice President, Virology Therapeutic Area Head, Gilead Sciences. “Once-yearly lenacapavir, if approved, could become an important new HIV prevention option that could help address PrEP adherence and persistence challenges for individuals who need or want PrEP around the world.” Promising once-yearly lenacapavir for PrEP pharmacokinetic profiles over 52 weeks The Phase 1 study evaluated the pharmacokinetics, safety and tolerability of two intramuscular single-dose 5000mg lenacapavir formulations. The trial included 40 healthy adults at low risk of HIV acquisition, between the ages of 18 and 55 years, with a body mass index of less than or equal to 35.0 kg/m 2 . Lenacapavir plasma concentrations for participants remained above the 95% effective concentration for at least 56 weeks with both formulations. Furthermore, median trough concentrations of both formulations of once-yearly lenacapavir at Week 52 (57.0 ng/mL and 65.6 ng/mL) were higher than those observed with twice-yearly lenacapavir in the PURPOSE 1 and PURPOSE 2 trials at Week 26 (23.4 ng/mL). Data from the study confirmed that both once-yearly formulations of lenacapavir warrant further investigation. Safety data demonstrated both formulations of once-yearly lenacapavir for PrEP were well tolerated, with no new safety signals Once-yearly lenacapavir is being investigated as an intramuscular injection. This is different from the subcutaneous formulation of lenacapavir, which is being investigated for twice-yearly dosing. The most commonly reported adverse event for both intramuscular formulations studied was injection site pain, which was mostly mild in severity and resolved within 1 week (occurred in 80% of participants receiving formulation 1, and 75% receiving formulation 2), and was reduced by pretreatment with an ice pack. Medication-emergent adverse events were similar between the two cohorts and mostly mild to moderate in severity. New PrEP modality preference data demonstrate preference for twice-yearly lenacapavir vs. once-daily orals in PURPOSE 1 survey participants New quantitative survey data and late-breaking qualitative survey data from the PURPOSE 1 trial, evaluating twice-yearly subcutaneous lenacapavir for PrEP among cisgender women in sub-Saharan Africa, were also presented at CROI in two poster sessions. An interim analysis of surveys included 2,561 trial participants’ self-reported preferences for twice-yearly lenacapavir for PrEP injections and once-daily pills, with approximately two-thirds of survey respondents preferring twice-yearly lenacapavir at Week 52 of their trial participation, compared to fewer than one-third of respondents preferring once-daily pills. Additionally, at Week 52, most respondents (61%) reported they would feel more protected from HIV with twice-yearly PrEP injections compared with once-daily pills, and 61% of respondents also reported they would feel more confident about not missing a PrEP dose with twice-yearly injections compared with once-daily pills. Qualitative data among 108 participants also showed that respondents, particularly adolescents aged 16 and 17 years, noted that twice-yearly injections better suited their lifestyles compared with once-daily pills. New study population data from PURPOSE 1 show comparable pharmacokinetic and safety profiles for both adolescent and adult trial participants Additional adolescent-related data from the PURPOSE 1 trial were also presented at CROI yesterday during an oral abstract session and press conference. PURPOSE 1 is the first adult Phase 3 HIV prevention trial to intentionally include adolescents aged 16 and 17 years, and trial enrollment was much higher than in typical adolescent-dedicated studies (124 adolescents, 56 of whom were assigned to the lenacapavir group). The data showed that observed lenacapavir plasma concentrations were comparable between adolescent and adult trial groups, with participants in both groups experiencing the same most common adverse events. There were zero incident HIV infections across the adolescent and adult groups receiving lenacapavir. Given these results, data submitted to regulatory authorities support the potential use of twice-yearly lenacapavir for adolescents who need or want PrEP The use of lenacapavir for the prevention of HIV is investigational and has not been determined to be safe or efficacious and is not approved anywhere globally. There is currently no cure for HIV or AIDS. About Lenacapavir Lenacapavir is approved in multiple countries for the treatment of adults with multi-drug resistant HIV in combination with other antiretrovirals. The use of lenacapavir for HIV prevention is investigational and the safety and efficacy of lenacapavir for this use have not been established. The multi-stage mechanism of action of lenacapavir is distinguishable from other currently approved classes of antiviral agents. While most antivirals act on just one stage of viral replication, lenacapavir is designed to inhibit HIV at multiple stages of its lifecycle and has no known cross resistance exhibited in vitro to other existing drug classes. Lenacapavir is being evaluated as a long-acting option in multiple ongoing and planned early and late-stage clinical studies in Gilead’s HIV prevention and treatment research program. Lenacapavir is being developed as a foundation for potential future HIV therapies with the goal of offering both long-acting oral and injectable options with several dosing frequencies, in combination or as a mono agent, that help address individual needs and preferences of people and communities affected by HIV. Science Magazine named lenacapavir its 2024 “Breakthrough of the Year.” About the PURPOSE Program Gilead’s landmark PURPOSE program is the most comprehensive and diverse HIV prevention trial program ever conducted. The program comprises five HIV prevention trials around the world that are focused on innovation in science, trial design, community engagement and health equity. The PURPOSE trials are evaluating the safety and efficacy of an investigational, twice-yearly injectable medicine, lenacapavir, to reduce the chance of getting HIV. The Phase 2 and 3 program, consisting of PURPOSE 1-5, is assessing the potential of lenacapavir to help a diverse range of people around the world who could benefit from PrEP. More information about the PURPOSE program, including individual trial descriptions, populations and locations, can be found at www.purposestudies.com . About Gilead HIV For more than 35 years, Gilead has been a leading innovator in the field of HIV, driving advances in treatment, prevention and cure research. Gilead researchers have developed 12 HIV medications , including the first single-tablet regimen to treat HIV, the first antiretroviral for pre-exposure prophylaxis (PrEP) to help reduce new HIV infections, and the first long-acting injectable HIV treatment medication administered twice-yearly. Our advances in medical research have helped to transform HIV into a treatable, preventable, chronic condition for millions of people. Gilead is committed to continued scientific innovation to provide solutions for the evolving needs of people affected by HIV around the world. Through partnerships , collaborations and charitable giving, the company also aims to improve education, expand access and address barriers to care, with the goal of ending the HIV epidemic for everyone, everywhere. Gilead was recognized as one of the leading philanthropic funders of HIV-related programs in a report released by Funders Concerned About AIDS. SOURCE: Gilead Sciences

Phase 3Clinical ResultPhase 1Phase 2Drug Approval

12 Mar 2025

·firstwordpharma.com

Merck & Co. moves closer to FDA filing for HIV therapy that maintains viral suppression

Merck & Co. is pushing forward with a simplified oral HIV treatment – a once-daily, two drug regimen that combines Pifeltro (doravirine) with its experimental nucleoside reverse transcriptase translocation inhibitor islatravir – aiming to file for regulatory approval by mid-2025.The announcement Wednesday follows positive data from two Phase III trials demonstrating that the regimen is just as effective as standard HIV therapies in maintaining viral suppression in adults with HIV-1. Merck first shared topline results in December and unveiled more detail at the Conference on Retroviruses and Opportunistic Infections (CROI) on Wednesday.In one of studies, called MK-8591A-052, the Pifeltro/islatravir combo was tested against Gilead Sciences' HIV treatment Biktarvy (bictegravir/emtricitabine/tenofovir alafenamide) in 513 HIV patients who had virologic suppression for at least three months while on Biktarvy. At 48 weeks, 91.5% of patients who switched to Merck's regimen kept their viral load under control, compared to 94.2% of those on Biktarvy, meeting the bar for non-inferiority. Although the regimen did not achieve superiority over the Gilead's drug.The second trial, dubbed MK-8591A-051, compared Pifeltro/islatravir to patients' existing antiretroviral therapy (bART). Here, 95.6% of patients on Pifeltro/islatravir maintained viral suppression at 48 weeks, versus 91.9% seen in the bART group.If approved, Merck's treatment would be the first two-drug HIV regimen that doesn't include an integrase inhibitor to demonstrate comparable efficacy and safety to the three-drug InSTI-based Biktarvy regimen in a Phase III trial, according to Eliav Barr, chief medical officer at Merck Research Laboratories."These data and our work on the longer-acting islatravir-based therapies in our pipeline show our continued commitment to help find new options that address the evolving needs of people living with HIV," Barr added.The regimen's safety profile was generally comparable to the comparator antiretroviral regimens across both trials. At week 48, the mean percent change in total lymphocyte and CD4 counts were similar between Pifeltro/islatravir and comparator treatments, an issue that had stalled the programme a few years ago. There was also no treatment-emergent resistance to Pifeltro or islatravir in either trial.Beyond this daily oral combination, Merck is also advancing a once-weekly combination of islatravir with Gilead's capsid inhibitor lenacapavir, which showed positive Phase II results in October.

Clinical ResultPhase 3Phase 2

100 Deals associated with Emtricitabine

External Link

KEGG	Wiki	ATC	Drug Bank
D01199	Emtricitabine	J05AF09	DB00879

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
HIV Infections	United States	Gilead Sciences, Inc.	02 Jul 2003

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Aicardi-Goutieres Syndrome	Phase 2	United States	Gilead Sciences, Inc.	01 Dec 2025
Hepatitis B, Chronic	Phase 2	United States	Gilead Sciences, Inc.	01 Sep 2007
Hepatitis B, Chronic	Phase 2	Australia	Gilead Sciences, Inc.	01 Sep 2007
Hepatitis B, Chronic	Phase 2	Canada	Gilead Sciences, Inc.	01 Sep 2007
Hepatitis B, Chronic	Phase 2	France	Gilead Sciences, Inc.	01 Sep 2007
Hepatitis B, Chronic	Phase 2	Germany	Gilead Sciences, Inc.	01 Sep 2007
Hepatitis B, Chronic	Phase 2	Hong Kong	Gilead Sciences, Inc.	01 Sep 2007
Hepatitis B, Chronic	Phase 2	New Zealand	Gilead Sciences, Inc.	01 Sep 2007
Hepatitis B, Chronic	Phase 2	Poland	Gilead Sciences, Inc.	01 Sep 2007
Hepatitis B, Chronic	Phase 2	Singapore	Gilead Sciences, Inc.	01 Sep 2007

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02150993 (FIT-2, Pubmed) Manual	Phase 2	HIV Infections First line	210	Tenofovir-boEmtricitabineirLamivudineZidovudine	ycchdzsfde(rnddmgoclq) = bzpiudnahv jqmnnsjxpt (oprjhdtott ) View more	Positive	01 Jun 2024
				tenofovirirEmtricitabineLamivudine	tflkamwler(jmiiajsuug) = ofxnhmnfds ohydjhhldt (mogbkgpffg, 47 - 66) View more
Rainbow study (Pubmed \| Int J Antimicrob Agents)	Phase 4	HIV Infections HIV-RNA	30	BIC/FTC/TAF	yleztzdjzh(azvnajazar) = Two participants developed IRIS garwdehana (jmgocfrwdi ) View more	Positive	01 Jan 2024
NCT03917420 (CTgov)	Phase 1	Acquired Immunodeficiency Syndrome	10	Tenofovir 300Mg Oral Tablet+Emtricitabine 200 MG	ibkbewjghc(dqaphlldct) = ksatnsuzas qxhgiykfcj (spxhnqxfsr, 819.0428) View more	-	12 Apr 2023
SIMPLâ??HIV (IAS2022)	Not Applicable	Maintenance	187	Dolutegravir plus Emtricitabine	npdwxjrziy(ucyofsbpzh) = wcqnhchqew zxnxquhiny (szipncerdx ) View more	Positive	01 Jan 2022
				Combined Antiretroviral Therapy	npdwxjrziy(ucyofsbpzh) = zzgafvzdqt zxnxquhiny (szipncerdx ) View more
IAS2021	Not Applicable	-	43	Bictegravir/emtricitabine/tenofovir alafenamide	ezjfmwubqf(eandnabrre) = gkitcojxuy icchngadqn (fewgpijsgn )	-	01 Jan 2021
IAS2021	Not Applicable	-	86	Bictegravir/emtricitabine/tenofovir alafenamide (B/F/TAF)	xdrkbnkrzk(zeflykagte) = Median CD4 counts were stable rxxjwnxowe (wxgozxxkqb )	-	01 Jan 2021
NCT01335620 (CTgov)	Phase 4	HIV Infections	19	Truvada+Raltegravir	teqycpmmfm(hffsuhevii) = tlqjwjnqva aoseplngib (xxdaoxhnvn, ynrbjpcbqt - qjhlynavsj) View more	-	20 Nov 2019
NCT02616783 (Pubmed) Manual	Phase 3	HIV Infections	167	Emtricitabine+Tenofovir+Elvitegravir+Cobicistat	jwraayeeti(niyywdhnsz) = ofpveygzbv mtkfzixatj (zxqoyhqgtq, 2.20) View more	Superior	01 Oct 2019
				therapy containing tenofovir disoproxil fumarate	jwraayeeti(niyywdhnsz) = iwisbzcknv mtkfzixatj (zxqoyhqgtq, 2.20) View more
NCT01529749 (CTgov)	Phase 4	Fibrosis \| HIV Infections \| Neurocognitive Disorders	48	EFV/FTC/TDF (EFV/FTC/TDF)	bbtizhtqab = xxjfpbkjhx zvovsbhppu (hgppjtsslz, dfadlsnrpi - pilerzkfjo) View more	-	02 Aug 2019
				FTC+EFV+TDF+Losartan (EFV/FTC/TDF + Losartan)	bbtizhtqab = tkitgrblon zvovsbhppu (hgppjtsslz, lpzhsyoedc - tizrpnchxw) View more
Studies 1844 and 1878 (IAS2019)	Not Applicable	HIV Infections	510	Bictegravir/Emtricitabine/Tenofovir Alafenamide (B/F/TAF)	dlbshljsvh(fvsrfeuqbf) = dugllalqis uzcleprpcl (knprxebfuw ) View more	Positive	01 Jan 2019
				Dolutegravir (DTG)	fgyfmdsvxk(klricoxmtu) = igaumsgmqm zhdzruulds (zigmvtaqbg ) View more

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