Islatravir

Summary

Islatravir (CHEMBL517231) is a phase-3 clinical-stage small molecule; indicated across 2 conditions including hiv infectious disease.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 2 conditions
• Clinical trials: 13
• Chemistry: 293.25 Da · C12H12FN5O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL517231
Name	Islatravir
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	6483431
Molecular formula	C12H12FN5O3
Molecular weight	293.25
InChIKey	IKKXOSBHLYMWAE-QRPMWFLTSA-N

SMILES: C#C[C@]1([C@H](C[C@@H](O1)N2C=NC3=C(N=C(N=C32)F)N)O)CO

IUPAC name: (2R,3S,5R)-5-(6-amino-2-fluoropurin-9-yl)-2-ethynyl-2-(hydroxymethyl)oxolan-3-ol

Also known as: Islatravir, Islatravir anhydrous, Mk-8591, MK-8591, ISLATRAVIR

Parent form; salt/anhydrous children: CHEMBL5095163

Patent coverage: 487 distinct patent families (1,427 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 928 (65%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

1 disease in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
HIV infectious disease	2	MONDO:0005109	EFO:0000180

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 13.

Phase distribution

Phase	Trials
PHASE1	7
PHASE2	5
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04644029	PHASE3	TERMINATED	Oral ISL QM as PrEP in Cisgender Women at High Risk for HIV-1 Infection (MK-8591-022)
NCT03272347	PHASE2	COMPLETED	Islatravir (MK-8591) With Doravirine and Lamivudine in Participants Infected With Human Immunodeficiency Virus Type 1 (MK-8591-011)
NCT04003103	PHASE2	COMPLETED	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)
NCT04564547	PHASE2	COMPLETED	Dose Ranging, Switch Study of Islatravir (MK-8591) and Ulonivirine (MK-8507) Once-Weekly in Virologically-Suppressed Adults With Human Immunodeficiency Virus Type 1 (HIV-1) [MK-8591-013]
NCT05115838	PHASE2	WITHDRAWN	Radiopaque Matrix MK-8591 Implant in Participants at Low-Risk for Human Immunodeficiency Virus Type 1 (HIV-1) Infection (MK-8591-043)
NCT05130086	PHASE2	WITHDRAWN	A Study of Islatravir (MK-8591) in Trans and Gender Diverse Participants (MK-8591-035)
NCT02217904	PHASE1	COMPLETED	A Study of Islatravir (MK-8591) in Anti-Retroviral Therapy-Naive, Human Immunodeficiency Virus-1 Infected Participants (MK-8591-003)
NCT04303156	PHASE1	COMPLETED	Pharmacokinetics of Islatravir in Participants With Severe Renal Impairment (MK-8591-026)
NCT04515641	PHASE1	COMPLETED	Single-Dose Islatravir in Moderate Hepatic Impairment (MK-8591-030)
NCT04568603	PHASE1	COMPLETED	Islatravir and Methadone Pharmacokinetics (MK-8591-029)
NCT06619678	PHASE1	COMPLETED	A Study of MK-8507 and Islatravir (MK-8591) in Healthy Adult Participants (MK-8507-016)
NCT06719570	PHASE1	COMPLETED	A Study of Doravirine and Islatravir as a Single Entity or Combination Therapy and the Effect of Food in Healthy Adult Participants (MK-8591A-055)
NCT06811246	PHASE1	COMPLETED	A Clinical Study of Islatravir and Its Interaction With Lamivudine (MK-8591-058)

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).