Dapivirine

Summary

Dapivirine (CHEMBL70663) is a phase-3 clinical-stage small molecule (ATC G01AX17); indicated across 4 conditions including hiv infectious disease and aids.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: G01AX17
• Indications: 4 conditions
• Clinical trials: 21
• Chemistry: 329.4 Da · C20H19N5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL70663
Name	Dapivirine
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	214347
ATC	G01AX17
Molecular formula	C20H19N5
Molecular weight	329.4
InChIKey	ILAYIAGXTHKHNT-UHFFFAOYSA-N

SMILES: CC1=CC(=C(C(=C1)C)NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C

IUPAC name: 4-[[4-(2,4,6-trimethylanilino)pyrimidin-2-yl]amino]benzonitrile

Also known as: AIDS-105293, Dapivirina, Dapivirine, Gel-02, R-147681, TMC-120, Tmc120, dapivirine, DAPIVIRINE, DAPIVIRINE (TMC120), DapivirineÊ, Dapivirine (TMC120)

Parent form; salt/anhydrous children: CHEMBL1257032

Patent coverage: 362 distinct patent families (994 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 850 (86%) 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

2 diseases 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	3	MONDO:0005109	EFO:0000764
AIDS	1	MONDO:0012268	EFO:0000765

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

Clinical trials

Total trials: 21.

Phase distribution

Phase	Trials
PHASE1	10
PHASE1/PHASE2	7
PHASE3	2
PHASE2	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01337570	PHASE3	WITHDRAWN	A Safety and Efficacy Trial of Dapivirine Vaginal Ring in Africa
NCT01337583	PHASE3	WITHDRAWN	A Safety and Efficacy Trial of Dapivirine Vaginal Ring in Africa
NCT00303576	PHASE1/PHASE2	COMPLETED	A Safety and Tolerability Study of Dapivirine (TMC120) Vaginal Microbicide Gel
NCT00304668	PHASE1/PHASE2	WITHDRAWN	A Safety Study of Dapivirine (TMC120) Vaginal Microbicide Gel in South Africa
NCT00309205	PHASE1/PHASE2	COMPLETED	A Safety Study of Dapivirine (TMC120) Vaginal Microbicide Gel in Belgium
NCT00799058	PHASE1/PHASE2	COMPLETED	A Safety Study of Two Dapivirine (TMC120) Vaginal Gels in the United States
NCT00917891	PHASE1/PHASE2	COMPLETED	An Expanded Safety Study of Dapivirine Gel 4759 in Africa
NCT00917904	PHASE1/PHASE2	COMPLETED	An Expanded Safety Study of Dapivirine Gel 4789 in Africa
NCT01071174	PHASE1/PHASE2	COMPLETED	A Safety Study of Dapivirine Vaginal Ring in Africa
NCT02028338	PHASE2	COMPLETED	Study of Dapivirine Vaginal Ring (VR) in Adolescents
NCT03074786	PHASE2	WITHDRAWN	Reversing the Epidemic in Africa With Choices in HIV Prevention (REACH)
NCT00304642	PHASE1	COMPLETED	A Study to Assess the Pharmacokinetics of Dapivirine (TMC120) Vaginal Microbicide Gel
NCT00332995	PHASE1	COMPLETED	Safety and Feasibility Study of Dapivirine (TMC120) Vaginal Ring in Belgium
NCT01144676	PHASE1	COMPLETED	A Safety Study to Assess the Delivery of Dapivirine From a Matrix Vaginal Ring
NCT01277640	PHASE1	COMPLETED	Male Tolerance Study of Dapivirine Gel Following Multiple Topical Penile Exposures
NCT01731574	PHASE1	COMPLETED	DDI Potential: Dapivirine Vaginal Ring and Miconazole Nitrate
NCT01924091	PHASE1	COMPLETED	PK/PD of Single Dose Dapivirine Vaginal Film
NCT01952561	PHASE1	COMPLETED	Expanded Use PK of Dapivirine Vaginal Ring
NCT02808949	PHASE1	COMPLETED	Pharmacokinetic Study of the Dapivirine Vaginal Ring in Lactating Women
NCT02847286	PHASE1	COMPLETED	To Assess the Drug-drug Interaction Potential Between Dapivirine Vaginal Ring-004, Containing 25 mg of Dapivirine, and Clotrimazole 10 mg/g (1%)
NCT05416021	PHASE1	COMPLETED	Relative Bioavailability Trial of Dapivirine Ring-004 and Ring-008

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

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