GS-3242

Associated long-acting platforms

Not provided

Administration route

Oral, Intramuscular

Therapeutic area(s)

Use case(s)

Use of drug

Dosage

Drug information

Delivery device(s)

Not provided

Scale-up prospects

Not provided

Tentative equipment list for manufacturing

Not provided

Manufacturing

Not provided

Specific analytical instrument required for characterization of formulation

Not provided

GS-US-544-5905-05

Identifier

NCT07001319

Link

https://clinicaltrials.gov/study/NCT07001319

Phase

Phase I

Status

Completed

Sponsor

Gilead Sciences

More details

This study is part of a master study. The goal of master protocol (GS-US-544-5905, NCT05585307) is to learn how novel antiretrovirals (medicines that stop the virus from multiplying) affect the human immunodeficiency virus-1 (HIV-1) infection in people living with HIV (PWH). Substudy GS-US-544-5905-05 is to learn more about the study drug GS-3242 in PLHIV. Participants will receive single dose of GS-3242 450 mg on Days 1 and 2 in the fasted condition. On day 11, they intiate SoC or Biktarvy

Purpose

Study of GS-3242 in Participants With HIV-1; Substudy-05

Interventions

Intervention 1

Intervention 2

Intervention 3

Countries

Sites / Institutions

Not provided

Trials dates

Anticipated Start Date
Not provided

Actual Start Date
2025-05-29

Anticipated Date of Last Follow-up
2026-05-08

Estimated Primary Completion Date
2026-04-01

Estimated Completion Date
2027-02-01

Actual Primary Completion Date
2026-03-03

Actual Completion Date
2026-04-16

Studied populations

Age Cohort

• Adults
• Older Adults

Genders

• All

Accepts pregnant individuals
No

Accepts lactating individuals
No

Accepts healthy individuals
No

Comments about the studied populations

Key Inclusion Criteria: All Substudies: * Plasma human immunodeficiency virus-1 (HIV-1) ribonucleic acid (RNA) ≥ 5000 copies/mL but ≤ 400,000 copies/mL at screening. * Cluster of differentiation 4 (CD4) cell count \> 200 cells/mm\^3 at screening. * Antiretroviral (ARV) treatment-naive or treatment-experienced but naive to the investigational ARV drug class being investigated in the given substudy and have not received any ARV within 12 weeks of screening, including medications received for pre-exposure prophylaxis (PrEP) or postexposure prophylaxis (PEP) (note that current or prior receipt of long acting (LA) parenteral ARVs such as monoclonal antibodies (mAbs) targeting HIV-1, injectable cabotegravir (CAB), injectable rilpivirine (RPV) or injectable Lenacapavir (LEN) is exclusionary).

Health status

Study type

Interventional (clinical trial)

Enrollment

27

Allocation

Non-randomized

Intervention model

Sequential assignment

Intervention model description

Not provided

Masking

Open label

Masking description

Not provided

Frequency of administration

Studied LA-formulation(s)

Studied route(s) of administration

Use case

Treatment

Key resources

GS-US-544-5905

Identifier

NCT05585307

Link

https://clinicaltrials.gov/study/NCT05585307

Phase

Phase I

Status

Completed

Sponsor

Gilead Sciences

More details

Master protocol: The goal of this master clinical trial study is to learn how novel antiretrovirals (medicines that stop the virus from multiplying) affect the human immunodeficiency virus-1 (HIV-1) infection in people living with HIV (PWH). Substudy-01 (GS-US-544-5905-01) will evaluate bavtavirine in PWH. Substudy-02 (GS-US-544-5905-02) will evaluate GS-1720 in PWH. Substudy-03 (GS-US-544-5905-03) will evaluate GS-6212 in PWH. Substudy GS-US-544-5905-05 is to learn more about the study drug GS-3242 in PWH.

Purpose

Study of Novel Antiretrovirals in Participants With HIV-1

Interventions

Intervention 1

Intervention 2

Intervention 3

Intervention 4

Intervention 5

Countries

Sites / Institutions

Not provided

Trials dates

Anticipated Start Date
Not provided

Actual Start Date
2022-10-26

Anticipated Date of Last Follow-up
2025-04-18

Estimated Primary Completion Date
Not provided

Estimated Completion Date
Not provided

Actual Primary Completion Date
2024-02-17

Actual Completion Date
2024-03-18

Studied populations

Age Cohort

• Adults
• Older Adults

Genders

• All

Accepts pregnant individuals
No

Accepts lactating individuals
No

Accepts healthy individuals
No

Comments about the studied populations

Key Inclusion Criteria: All Substudies: * Plasma human immunodeficiency virus-1 (HIV-1) ribonucleic acid (RNA) ≥ 5000 copies/mL but ≤ 400,000 copies/mL at screening. * Cluster of differentiation 4 (CD4) cell count \> 200 cells/mm\^3 at screening. * Antiretroviral (ARV) treatment-naive or treatment-experienced but naive to the investigational ARV drug class being investigated in the given substudy and have not received any ARV within 12 weeks of screening, including medications received for pre-exposure prophylaxis (PrEP) or postexposure prophylaxis (PEP) (note that current or prior receipt of long acting (LA) parenteral ARVs such as monoclonal antibodies (mAbs) targeting HIV-1, injectable cabotegravir (CAB), or injectable rilpivirine (RPV) is exclusionary). * Have adequate renal function

Health status

Study type

Interventional (clinical trial)

Enrollment

49

Allocation

Non-randomized

Intervention model

Sequential assignment

Intervention model description

Not provided

Masking

Open label

Masking description

Not provided

Frequency of administration

Not provided

Studied LA-formulation(s)

Studied route(s) of administration

Use case

Treatment

Key resources

GS-US-643-7710

Identifier

NCT07645287

Link

https://clinicaltrials.gov/study/NCT07645287

Phase

Phase II

Status

Recruiting

Sponsor

Gilead Sciences

More details

The study will have two parts: Part A and Part B. In Part A, the goal of the study is to compare the effectiveness of switching to the study drugs GS-3242 plus Lenacapavir (LEN) versus continuing Biktarvy (bictegravir/emtricitabine/tenofovir alafenamide (B/F/TAF)), in virologically suppressed people with HIV-1 (PWH) in treatment Group 1, 2 and 3 at Week 35. In Part B the goal of the study is to compare the effectiveness of switching to the study drugs, GS-3242 and LEN versus continuing B/F/TAF in Groups 4 and 3 at Week 26. The primary objective of part A is to evaluate the efficacy of switching to intramuscular (IM) GS-3242 plus IM LEN versus continuing on B/F/TAF PWH who are virologically suppressed in treatment Groups 1, 2, and 3 at Week 35 and Part B is to evaluate the efficacy of swit

Purpose

A Study of GS-3242 in Combination With Lenacapavir Versus Biktarvy in Virologically Suppressed People With HIV-1

Interventions

Intervention 1

Intervention 2

Intervention 3

Intervention 4

Intervention 5

Countries

Sites / Institutions

Not provided

Trials dates

Anticipated Start Date
Not provided

Actual Start Date
2026-06-15

Anticipated Date of Last Follow-up
2026-07-09

Estimated Primary Completion Date
2027-08-01

Estimated Completion Date
2033-04-01

Actual Primary Completion Date
Not provided

Actual Completion Date
Not provided

Studied populations

Age Cohort

• Adults
• Older Adults

Genders

• All

Accepts pregnant individuals
Unspecified

Accepts lactating individuals
Unspecified

Accepts healthy individuals
No

Comments about the studied populations

Key Inclusion Criteria: * Documented human immunodeficiency virus type 1 (HIV-1) ribonucleic acid (RNA) \< 50 copies/mL for ≥ 6 months before screening. * Plasma HIV-1 RNA levels \< 50 copies/mL at screening. * Receiving bictegravir/emtricitabine/tenofovir alafenamide (coformulated; Biktarvy®) (B/F/TAF) for ≥ 6 months prior to screening. * No documented resistance to GS-3242 (integrase mutation Q148H/K/R plus at least 2 of the following integrase mutations: L74I/M, T97A, E138A/K/T, or G140A/C/S). Key Exclusion Criteria: * Prior use of, or exposure to GS-3242 or LEN. * History of virologic failure while on an integrase strand transfer inhibitor (INSTI)-based regimen. * Prior use of any long-acting parenteral antiretroviral therapy (ART) medications such as monoclonal antibodies or broadl

Health status

Study type

Interventional (clinical trial)

Enrollment

175

Allocation

Randomized

Intervention model

Parallel Assignment

Intervention model description

Not provided

Masking

Open label

Masking description

Not provided

Frequency of administration

Studied LA-formulation(s)

Studied route(s) of administration

Not provided

Use case

Treatment

Key resources

GS-US-643-6557

Identifier

NCT07708727

Link

https://clinicaltrials.gov/study/NCT07708727

Phase

Phase II/III

Status

Not yet recruiting

Sponsor

Gilead Sciences

More details

The study will have two portions: Phase 2 and Phase 3. Phase 2 will further have 2 parts: Part A and Part B. The goal of Phase 2, Part A is to assess the effectiveness of study drugs GS-3242 plus Lenacapavir (LEN) versus Biktarvy (bictegravir/emtricitabine/tenofovir alafenamide (B/F/TAF)), in people with HIV-1 (PWH) who are new to treatment. This will be done in Treatment Groups 1, 2 and 3 at Week 35. The goal of Phase 2, Part B is to compare the effectiveness of study drugs, GS-3242 and LEN versus B/F/TAF in Groups 4 and 3 at Week 26. The goal of Phase 3 is to assess the long-term effectiveness of study drug GS-3242 and LEN versus B/F/TAF, at Week 52. The primary objectives of this study are: Phase 2, Part A: To evaluate the efficacy of intramuscular (IM) GS-3242 plus IM LEN versus B

Purpose

Study of an Injectable Regimen of GS-3242 With Lenacapavir Compared to Biktarvy in People New to HIV-1 Treatment

Interventions

Intervention 1

Intervention 2

Intervention 3

Intervention 4

Intervention 5

Countries

Not provided

Sites / Institutions

Not provided

Trials dates

Anticipated Start Date
2026-07-01

Actual Start Date
Not provided

Anticipated Date of Last Follow-up
2026-07-13

Estimated Primary Completion Date
2030-10-01

Estimated Completion Date
2033-04-01

Actual Primary Completion Date
Not provided

Actual Completion Date
Not provided

Studied populations

Age Cohort

• Adults
• Older Adults

Genders

• All

Accepts pregnant individuals
Unspecified

Accepts lactating individuals
Unspecified

Accepts healthy individuals
No

Comments about the studied populations

Key Inclusion Criteria: * HIV-1 ribonucleic acid (RNA) ≥ 500 copies/mL at screening. * Antiretroviral (ARV) treatment-naive, except for prior use of oral daily pre-exposure prophylaxis (PrEP) or postexposure prophylaxis (PEP) up to 1 month prior to screening. Key Exclusion Criteria: * Prior usage of, or exposure to LEN or GS-3242 * Prior use of any long-acting parenteral ARV therapy (ART) medications such as monoclonal antibodies or broadly neutralizing antibodies targeting HIV-1, injectable cabotegravir (including oral cabotegravir lead-in), or injectable rilpivirine. Note: Other protocol defined Inclusion/Exclusion criteria may apply.

Health status

Not provided

Study type

Interventional (clinical trial)

Enrollment

700

Allocation

Randomized

Intervention model

Parallel Assignment

Intervention model description

Not provided

Masking

Open label

Masking description

Not provided

Frequency of administration

Studied LA-formulation(s)

Studied route(s) of administration

Use case

Treatment

Key resources

Proprietary excipients used

Not provided

Novel excipients or existing excipients at a concentration above Inactive Ingredients Database (IID) for the specified route of administration

Not provided

Residual solvents used

Not provided

There are either no relevant patents or these were not yet submitted to LAPaL

Publications

Arens, Y., & Gulick, R. M. (2025). Future options for long-acting HIV treatment and prevention. Current Opinion in HIV and AIDS, 20(1), 39-47.

Purpose of review 

The aim of this review was to describe future options for long-acting HIV treatment and preexposure prophylaxis (PrEP) regimens featuring both innovations with currently approved antiretrovirals and a profile of investigational agents in the pipeline.

Recent findings 

Newer formulations and modes of delivery for existing antiretroviral drugs and a number of investigational agents are under study for long-acting HIV treatment and PrEP. Regimens with weekly oral dosing for HIV treatment, monthly oral dosing for HIV PrEP, and injectable agents with longer dosing intervals (every 3 months or longer) for treatment and PrEP are in clinical development. Newer agents with novel mechanisms of action and newer modes of administration including vaginal rings, implants, patches, and rectal douches also are under investigation.

Summary 

Despite the success of current antiretroviral therapy and PrEP with one-pill, once-daily regimens, there is a continuing need for new formulations, investigational agents, and novel modes of delivery to overcome barriers to implementation and ensure real-world effectiveness. Newer long-acting antiretroviral regimens for HIV treatment and PrEP using novel preparations and strategies will offer choice, enhance adherence, decrease toxicity, and improve patient and provider satisfaction.

Additional documents

No documents were uploaded

Useful links

• Gilead at JP Morgan 2026 Healthcare Conference

	Collaborate for development Consider on a case by case basis, collaborating on developing long acting products with potential significant public health impact, especially for low- and middle-income countries (LMICs), utilising the referred to long-acting technology Not provided
	Share technical information for match-making assessment Provide necessary technical information to a potential partner, under confidentiality agreement, to enable preliminary assessment of whether specific medicines of public health importance in LMICs might be compatible with the referred to long-acting technology to achieve a public health benefit Not provided
	Work with MPP to expand access in LMICs In the event that a product using the referred to long-acting technology is successfully developed, the technology IP holder(s) will work with the Medicines Patent Pool towards putting in place the most appropriate strategy for timely and affordable access in low and middle-income countries, including through licensing Not provided

Not provided