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NCT04003103

Safety and Pharmacokinetics of Oral Islatravir (MK-8591) Once Monthly in Participants at Low Risk of Human Immunodeficiency Virus 1 (HIV-1) Infection (MK-8591-016)

Completed Phase 2 Results posted Last updated 18 July 2025
What this trial tests

Phase 2 trial testing Islatravir in HIV-1 Infection in 242 participants. Completed in 24 November 2022.

Timeline
19 September 2019
Primary endpoint
18 March 2022
24 November 2022

Quick facts

Lead sponsorMerck Sharp & Dohme LLC
PhasePhase 2
StatusCompleted
Study typeINTERVENTIONAL
Allocationrandomized
Designparallel
Maskingdouble
Primary purposeprevention
Enrollment242
Start date19 September 2019
Primary completion18 March 2022
Estimated completion24 November 2022
Sites9 locations across South Africa, United States, Israel

Drugs / interventions tested

Conditions studied

Sponsor

Merck Sharp & Dohme LLC — full company profile →

Who can join

Adults 18 to 65, any sex, with HIV-1 Infection. Patients with the condition only — healthy volunteers not accepted.

Results — posted to ClinicalTrials.gov

Per-arm endpoint measurements with 95% confidence intervals where reported. Source: trial results section.

Number of Participants With ≥1 Adverse Event (AE) Through Week 36 Primary · Up to 36 weeks

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention.

GroupValue95% CI
Islatravir 60 mg66
Islatravir 120 mg63
Placebo36
Number of Participants Discontinuing From Study Therapy Due to AE Primary · Up to 20 weeks

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention.

GroupValue95% CI
Islatravir 60 mg1
Islatravir 120 mg1
Placebo0
Number of Participants Discontinuing From Study Therapy Due to ≥1 Drug-related AE Primary · Up to 20 weeks

A drug-related AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, that is considered related to the study therapy.

GroupValue95% CI
Islatravir 60 mg1
Islatravir 120 mg1
Placebo0
Number of Participants With ≥1 Drug-related AE Through Week 36 Primary · Up to 36 weeks

A drug-related AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, that is considered related to the study intervention.

GroupValue95% CI
Islatravir 60 mg9
Islatravir 120 mg14
Placebo12
Number of Participants With ≥1 Serious Adverse Event (SAE) Through Week 36 Primary · Up to 36 weeks

An SAE is defined as any untoward medical occurrence that, at any dose, results in death; is life-threatening; requires inpatient hospitalization or prolongation of existing hospitalization; results in persistent or significant disability/incapacity; is a congenital anomaly/birth defect; or is an other important medical event.

GroupValue95% CI
Islatravir 60 mg1
Islatravir 120 mg0
Placebo0
Number of Participants With a ≥1 Grade 3 to Grade 5 AE up to Week 36 Primary · Up to 36 weeks

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study therapy, whether or not considered related to the study intervention. Toxicity grading was according to the National Institutes of Health Division of AIDS (NIH DAIDS) Table for Grading the Severity of Adult and Pediatric Adverse Events version 2.1 (Grade 3 is 'severe'; Grade 4 is 'potentially life-threatening'; and Grade 5 'results in death').

GroupValue95% CI
Islatravir 60 mg5
Islatravir 120 mg4
Placebo1
Number of Participants With ≥1 Drug-related SAE Through Week 36 Primary · Up to 36 weeks

An drug-related SAE is defined as any untoward medical occurrence that, at any dose, results in death; is life-threatening; requires inpatient hospitalization or prolongation of existing hospitalization; results in persistent or significant disability/incapacity; is a congenital anomaly/birth defect; or is an other important medical event, that is considered related to study therapy.

GroupValue95% CI
Islatravir 60 mg0
Islatravir 120 mg0
Placebo0
Number of Participants With ≥1 Drug-related Grade 3 to 5 AE Through Week 36 Primary · Up to 36 weeks

A drug-related Grade 3 to Grade 5 AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention; has a toxicity Grade 3 (severe), 4 (potentially life-threatening), or 5 (results in death); and is considered related to study therapy. Toxicity grading was according to the NIH DAIDS Table for Grading the Severity of Adult and Pediatric Adverse Events (v. 2.1).

GroupValue95% CI
Islatravir 60 mg0
Islatravir 120 mg0
Placebo0
Number of Participants With an AE Resulting in Death Through Week 36 Primary · Up to 36 weeks

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention.

GroupValue95% CI
Islatravir 60 mg0
Islatravir 120 mg0
Placebo0
Area Under the Plasma Concentration-time Curve From Dosing to 672 Hours Postdose (AUC0-672) of Plasma ISL Secondary · Day 1 and Day 140: predose and 30-min postdose. On Day 2 collect ~24 hours after Day 1 dose. On Weeks 4, 8, 12 and 16, collect predose. Weeks 1, 2, 3, 21, 22, 23 and 24: collect at any time during the study visit.

The AUC0-672 of ISL after dosing on Day 1 and Day 140 is reported. Only ISL-treated participants are included in the PK analysis.

Day 1
GroupValue95% CI
Islatravir 60 mg7.88± 56.8
Islatravir 120 mg16.6± 50.5
Day 140
GroupValue95% CI
Islatravir 60 mg21.2± 140.3
Islatravir 120 mg37.6± 136.6
Maximum Plasma Concentration (Cmax) of ISL Secondary · Day 1 and Week 20, collect predose and 30-min postdose. On Day 2 collect ~24 hours after Day 1 dose. On Weeks 4, 8, 12 and 16, collect predose. Weeks 1, 2, 3, 21, 22, 23 and 24: collect at any time during the study visit.

The Cmax of ISL after dosing on Day 1 and Day 140 is reported. Only ISL-treated participants are included in the PK analysis.

Day 1
GroupValue95% CI
Islatravir 60 mg0.387± 279.9
Islatravir 120 mg0.954± 186.2
Day 140
GroupValue95% CI
Islatravir 60 mg0.376± 597.7
Islatravir 120 mg0.792± 349.6
Trough Plasma Concentration (Ctrough) of ISL Secondary · Day 1 and Week 20: predose and 30-min postdose. Day 2: 24 hours post Day 1 dose. Weeks 1, 2, 3, 21, 22, 23 and 24: any time during the study visit. Weeks 4, 8, 12 and 16: predose.

The plasma Ctrough of ISL after dosing on Day 1 and Day 140 is reported. Only ISL-treated participants are included in the PK analysis.

Day 1
GroupValue95% CI
Islatravir 60 mg0.000556± 36.6
Islatravir 120 mg0.00101± 37.0
Day 140
GroupValue95% CI
Islatravir 60 mg0.000809± 37.0
Islatravir 120 mg0.000124± 42.0

Adverse events — posted to ClinicalTrials.gov

Time frame: Up to 36 weeks. Reporting threshold: 5%. Adverse-event reports describe events observed during the trial — not all are caused by the drug.

Islatravir 60 mg
Serious: 1/97 (1%)
Deaths: 1/97
Islatravir 120 mg
Serious: 0/97 (0%)
Deaths: 0/97
Placebo
Serious: 0/48 (0%)
Deaths: 0/48

Serious adverse events (2 terms)

ReactionSystemIslatravir 60 mgIslatravir 120 mgPlacebo
Intentional self-injuryPsychiatric disorders
Loss of consciousnessNervous system disorders
Other adverse events (9 terms — click to expand)

ReactionSystemIslatravir 60 mgIslatravir 120 mgPlacebo
HeadacheNervous system disorders
NauseaGastrointestinal disorders
DiarrhoeaGastrointestinal disorders
Blood pressure increasedInvestigations
Abdominal painGastrointestinal disorders
Upper respiratory tract infectionInfections and infestations
Accidental overdoseInjury, poisoning and procedural complications
Alanine aminotransferase increasedInvestigations
DizzinessNervous system disorders

Most-reported serious reactions: Intentional self-injury, Loss of consciousness.

Data from ClinicalTrials.gov NCT04003103 adverse events section.

Sponsor's own description

This study will evaluate the safety, tolerability and pharmacokinetics (PK) of 6 once-monthly doses of oral islatravir (60 mg and 120 mg) compared with placebo in adults at low risk of HIV-1 infection

Publications & conference data

8 peer-reviewed publications reference this trial (live from Europe PMC):

  1. Avoiding Drug Resistance in HIV Reverse Transcriptase.
    Cilento ME, Kirby KA, Sarafianos SG. · · 2021 · cited 65× · PMID 33507067 · DOI 10.1021/acs.chemrev.0c00967
  2. Safety, tolerability, and pharmacokinetics of single- and multiple-dose administration of islatravir (MK-8591) in adults without HIV.
    Matthews RP, Ankrom W, Friedman E, Jackson Rudd D, et al · · 2021 · cited 37× · PMID 34463432 · DOI 10.1111/cts.13048
  3. Promise, perils and cautious optimism: the next frontier in long-acting modalities for the treatment and prevention of HIV.
    Philbin MM, Perez-Brumer A. · · 2022 · cited 23× · PMID 35225248 · DOI 10.1097/coh.0000000000000723
  4. Nose to brain delivery of antiretroviral drugs in the treatment of neuroAIDS.
    Sarma A, Das MK. · · 2020 · cited 15× · PMID 34765998 · DOI 10.1186/s43556-020-00019-8
  5. Pharmacology of HIV Cure: Site of Action.
    Devanathan AS, Cottrell ML. · · 2021 · cited 14× · PMID 33540481 · DOI 10.1002/cpt.2187
  6. Safety, Tolerability, and Pharmacokinetics of Once-Monthly Oral Islatravir: A Phase 2a Study in Participants at Low Risk for Acquiring Human Immunodeficiency Virus Type 1.
    Hillier SL, Bekker LG, Riddler SA, Hendrix CW, et al · · 2025 · cited 3× · PMID 40327547 · DOI 10.1093/infdis/jiaf222
  7. Oral abstracts of the 11th IAS Conference on HIV Science, 18-21 July 2021.
    · 2021 · cited 1× · PMID 34288453 · DOI 10.1002/jia2.25755
  8. Islatravir distribution in plasma, peripheral blood mononuclear cells, and mucosal tissues after monthly oral dosing.
    Hendrix CW, Hillier SL, Bekker LG, Badal-Faesen S, et al · · 2026 · PMID 41789892 · DOI 10.1097/qad.0000000000004477

Verify or expand the search:

Other trials of Islatravir

Trials testing the same drug.

Other recruiting trials for HIV-1 Infection

Currently open trials in the same condition.

Other Merck Sharp & Dohme LLC trials

Trials by the same sponsor.

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