Vicriviroc

Summary

Vicriviroc (CHEMBL82301) is a phase-3 clinical-stage small molecule targeting CCR5; indicated across 3 conditions including hiv infectious disease and aids.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (CCR5)
• Indications: 3 conditions
• Clinical trials: 11
• Chemistry: 533.6 Da · C28H38F3N5O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL82301
Name	Vicriviroc
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	3009355
Molecular formula	C28H38F3N5O2
Molecular weight	533.6
InChIKey	CNPVJJQCETWNEU-CYFREDJKSA-N

SMILES: C[C@H]1CN(CCN1[C@@H](COC)C2=CC=C(C=C2)C(F)(F)F)C3(CCN(CC3)C(=O)C4=C(N=CN=C4C)C)C

IUPAC name: (4,6-dimethylpyrimidin-5-yl)-[4-[(3S)-4-[(1R)-2-methoxy-1-[4-(trifluoromethyl)phenyl]ethyl]-3-methylpiperazin-1-yl]-4-methylpiperidin-1-yl]methanone

Also known as: MK-7690, SCH-417690 FREE BASE, SCH-D, Vicriviroc, vicriviroc, VICRIVIROC, Vicriviroc (maleate)

Parent form; salt/anhydrous children: CHEMBL2107384

Patent coverage: 2,083 distinct patent families (8,672 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
CCR5	CCR5	Antagonist	9.1	0.7%	P51681

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: C-C chemokine receptor type 5, C-C chemokine receptor type 5.

Bioactivity

ChEMBL activities: 6 potent at pChembl ≥ 5 of 6 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CCR5	9.35	IC50	0.45	nM	CHEMBL_ACT_12149735
P51682	9.04	IC50	0.91	nM	CHEMBL_ACT_18393155
CCR5	8.92	IC50	1.2	nM	CHEMBL_ACT_5293933
CCR5	8.68	Ki	2.1	nM	CHEMBL_ACT_206150
CCR5	8.6	Ki	2.5	nM	CHEMBL_ACT_572253
CCR5	8.52	IC50	3	nM	CHEMBL_ACT_5293923

Target pathways

Aggregated over 1 target gene(s): CCR5.

Top Reactome pathways

19 total, by targets touching each:

Pathway	Targets	Genes
Cytokine Signaling in Immune system	1	CCR5
Signal Transduction	1	CCR5
HIV Life Cycle	1	CCR5
Early Phase of HIV Life Cycle	1	CCR5
HIV Infection	1	CCR5
Disease	1	CCR5
Immune System	1	CCR5
Binding and entry of HIV virion	1	CCR5
Signaling by GPCR	1	CCR5
Class A/1 (Rhodopsin-like receptors)	1	CCR5
Peptide ligand-binding receptors	1	CCR5
Chemokine receptors bind chemokines	1	CCR5
GPCR downstream signalling	1	CCR5
G alpha (i) signalling events	1	CCR5
Signaling by Interleukins	1	CCR5
GPCR ligand binding	1	CCR5
Infectious disease	1	CCR5
Interleukin-10 signaling	1	CCR5
Viral Infection Pathways	1	CCR5

Dominant GO biological processes

GO term	Targets
MAPK cascade	1
dendritic cell chemotaxis	1
calcium ion transport	1
apoptotic process	1
chemotaxis	1
inflammatory response	1
immune response	1
cellular defense response	1
cell surface receptor signaling pathway	1
G protein-coupled receptor signaling pathway	1
positive regulation of cytosolic calcium ion concentration	1
cell-cell signaling	1
release of sequestered calcium ion into cytosol by sarcoplasmic reticulum	1
calcium-mediated signaling	1
signaling	1

Indications & clinical

Indications

3 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
HIV infectious disease	3	MONDO:0005109	EFO:0000764
AIDS	3	MONDO:0012268	EFO:0000765
colorectal neoplasm	2	MONDO:0005335	EFO:0004142

Clinical trials

Total trials: 11.

Phase distribution

Phase	Trials
PHASE2	5
PHASE3	3
PHASE1	2
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00243568	PHASE3	WITHDRAWN	Vicriviroc, a CCR5 Inhibitor, Added to an Optimized Antiretroviral Therapy for Previously Treated HIV (VICTOR-E2) (Study P04285
NCT00474370	PHASE3	COMPLETED	Vicriviroc in HIV-Treatment Experienced Subjects (Study P04889AM8)(COMPLETED)
NCT00523211	PHASE3	COMPLETED	Vicriviroc in HIV-Treatment Experienced Subjects (Study P04405AM5)
NCT00082498	PHASE2	COMPLETED	Safety and Effectiveness of the Oral HIV Entry Inhibitor Vicriviroc in HIV Infected Patients
NCT00243230	PHASE2	COMPLETED	Vicriviroc (SCH 417690) in Combination Treatment With Optimized ART Regimen in Experienced Participants (VICTOR-E1) (MK-7690-020/P03672)
NCT00551018	PHASE2	COMPLETED	Efficacy and Safety of VICRIVIROC in HIV-Infected Treatment-Naïve Subjects (Study P04875)
NCT00551330	PHASE2	COMPLETED	Vicriviroc in HIV(R5/X4)-Treatment Experienced Subjects (Study P05057AM5)(COMPLETED)
NCT00766597	PHASE1/PHASE2	COMPLETED	Safety and Immune Response to Vicriviroc in Combination Regimens in HIV-Infected ART Experienced Children and Adolescents
NCT03631407	PHASE2	COMPLETED	Safety and Efficacy of Vicriviroc (MK-7690) in Combination With Pembrolizumab (MK-3475) in Participants With Advanced/Metastatic Microsatellite Stable (MSS) Colorectal Cancer (CRC) (MK-7690-046)
NCT00632073	PHASE1	COMPLETED	Effect of Vicriviroc on HIV Ribonucleic Acid (RNA) Levels in Cerebrospinal Fluid (Study P05241)
NCT02356302	PHASE1	COMPLETED	Safety and Pharmacokinetics of Intravaginal Rings Containing Vicriviroc (MK-4176) and/or MK-2048

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

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

13 molecules share ≥1 primary target. Top 13 by shared-target count:

Molecule	Source	Status	Shared targets
ABAMETAPIR	ChEMBL	Phase 4 (approved)	CCR5
DISULFIRAM	ChEMBL	Phase 4 (approved)	CCR5
MARAVIROC	ChEMBL	Phase 4 (approved)	CCR5
TERFENADINE	ChEMBL	Phase 4 (approved)	CCR5
APLAVIROC	ChEMBL	Phase 3	CCR5
CENICRIVIROC	ChEMBL	Phase 3	CCR5
ANCRIVIROC	ChEMBL	Phase 2	CCR5
AZD5672	ChEMBL	Phase 2	CCR5
BMS-741672	ChEMBL	Phase 2	CCR5
BMS-813160	ChEMBL	Phase 2	CCR5
INCB-9471	ChEMBL	Phase 2	CCR5
JNJ-17166864 CATION	ChEMBL	Phase 2	CCR5
Mavorixafor	PubChem	Approved	CCR5