Maraviroc

Summary

Maraviroc (CHEMBL256907) is an approved small molecule (ATC J05AX09) targeting CCR5; indicated across 20 conditions including hiv infectious disease and viral infectious disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: J05AX09
• Targets: 1 (CCR5)
• Indications: 20 conditions
• Clinical trials: 118
• Chemistry: 513.7 Da · C29H41F2N5O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL256907
Name	Maraviroc
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	3002977
ATC	J05AX09
Molecular formula	C29H41F2N5O
Molecular weight	513.7
InChIKey	GSNHKUDZZFZSJB-HLMSNRGBSA-N

SMILES: CC1=NN=C(N1C2C[C@H]3CC[C@@H](C2)N3CC[C@@H](C4=CC=CC=C4)NC(=O)C5CCC(CC5)(F)F)C(C)C

IUPAC name: 4,4-difluoro-N-[(1S)-3-[(1S,5R)-3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxamide

Also known as: Celsentri, Maraviroc, Rel-maraviroc, Selzentry, Uk-427,857, UK-427857, maraviroc, MARAVIROC, SID124950712, rel-Maraviroc, Maravioc, SID144206920

Patent coverage: 2 distinct patent families (5 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	8.1	0.7%	P51681

Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: Multidrug and toxin extrusion protein 1, Alpha-2A adrenergic receptor, Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK), Mu-type opioid receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, C-C chemokine receptor type 5, C-C chemokine receptor type 5, Cytochrome P450 2C9, Cytochrome P450 3A4, C-C chemokine receptor type 5.

Bioactivity

ChEMBL activities: 29 potent at pChembl ≥ 5 of 37 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CCR5	9.7	IC50	0.2	nM	CHEMBL_ACT_18482267
CCR5	9.7	IC50	0.2	nM	CHEMBL_ACT_2286295
CCR5	9.7	IC50	0.2	nM	CHEMBL_ACT_2609469
CCR5	9.7	IC50	0.2	nM	CHEMBL_ACT_5160580
P61813	9.62	Ki	0.24	nM	CHEMBL_ACT_14537047
CCR5	9.62	Ki	0.24	nM	CHEMBL_ACT_17685118
P61813	9.62	Ki	0.24	nM	CHEMBL_ACT_22839298
CCR5	9.43	IC50	0.37	nM	CHEMBL_ACT_13889916
CCR5	9.37	IC50	0.43	nM	CHEMBL_ACT_13889917
CCR5	9.09	IC50	0.82	nM	CHEMBL_ACT_24347307
CCR5	9	EC50	1	nM	CHEMBL_ACT_17962759
CCR5	8.89	IC50	1.3	nM	CHEMBL_ACT_13889918
CCR5	8.85	IC50	1.4	nM	CHEMBL_ACT_3194846
CCR5	8.8	IC50	1.6	nM	CHEMBL_ACT_13889925
CCR5	8.68	IC50	2.1	nM	CHEMBL_ACT_22839289
CCR5	8.66	IC50	2.2	nM	CHEMBL_ACT_14537052
CCR5	8.66	IC50	2.2	nM	CHEMBL_ACT_17685122
CCR5	8.52	IC50	3	nM	CHEMBL_ACT_12149743
P51682	8.28	IC50	5.2	nM	CHEMBL_ACT_18393154
CCR5	8.13	IC50	7.38	nM	CHEMBL_ACT_27107936
CCR5	8.1	IC50	8	nM	CHEMBL_ACT_18683207
CCR5	8.1	IC50	8	nM	CHEMBL_ACT_24874408
CCR5	7.88	IC50	13.1	nM	CHEMBL_ACT_15155085
CCR5	7.85	IC50	14	nM	CHEMBL_ACT_3292119
CCR5	7.6	Kd	25	nM	CHEMBL_ACT_10836315
CCR5	7.59	IC50	25.43	nM	CHEMBL_ACT_13876368
OPRM1	6.71	AC50	196.2	nM	CHEMBL_ACT_25157986
CYP3A4	5.51	IC50	3100	nM	CHEMBL_ACT_24874581
KCNH2	5.11	IC50	7750	nM	CHEMBL_ACT_27107990

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

20 indications (3 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	4	MONDO:0005109	EFO:0000764
viral infectious disease	4	MONDO:0005108	EFO:0000763
AIDS	3	MONDO:0012268	EFO:0000765
AIDS dementia complex	2	MONDO:0020689	EFO:0002608
rheumatoid arthritis	2	MONDO:0008383	EFO:0000685
B-cell chronic lymphocytic leukemia	2	MONDO:0004948	EFO:0000095
Hodgkins lymphoma	2	MONDO:0004952	EFO:0000183
myelodysplastic syndrome	2	MONDO:0018881	EFO:0000198
chronic myeloid leukemia	2	MONDO:0011996	EFO:0000339
diffuse large B-cell lymphoma	2	MONDO:0018905	EFO:0000403
stroke disorder	2	MONDO:0005098	EFO:0000712
graft versus host disease	2	MONDO:0013730	MONDO:0013730
hematopoietic and lymphoid system neoplasm	2	MONDO:0002334	MONDO:0044881
Kaposi’s sarcoma	2	MONDO:0005055	EFO:0000558
follicular lymphoma	2	MONDO:0018906	MONDO:0018906
severe acute respiratory syndrome	2	MONDO:0005091	MONDO:0100096
hypertriglyceridemia	1	MONDO:0005347	EFO:0004211

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

Clinical trials

Total trials: 118.

Phase distribution

Phase	Trials
PHASE4	29
PHASE2	26
PHASE1	25
Not specified	14
PHASE3	10
PHASE2/PHASE3	9
PHASE1/PHASE2	4
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00666705	PHASE4	COMPLETED	A Study To Evaluate An Interaction Between Maraviroc And Raltegravir In Healthy Subjects
NCT00717067	PHASE4	COMPLETED	Pharmacokinetics, Safety And Toleration Of Maraviroc Administered To Subjects With Various Degrees Of Renal Impaired And Normal Renal Function
NCT00735072	PHASE4	COMPLETED	Maraviroc as an Immunomodulatory Drug for Antiretroviral-treated HIV Infected Patients Exhibiting Immunologic Failure
NCT00782301	PHASE4	WITHDRAWN	Maraviroc Versus Etravirine In Combination With Antiretroviral Therapy In Drug Experienced HIV And Hepatitis Co-Infected Patients
NCT00853840	PHASE4	COMPLETED	Study To Investigate The Hemodynamic Effects Of Single Dose Vardenafil In Subjects Receiving Maraviroc
NCT00875368	PHASE4	COMPLETED	Maraviroc Immune Recovery Study
NCT00884858	PHASE4	COMPLETED	Maraviroc in Immunological Non-Responder (INR) HIV-1-infected Subjects
NCT00925756	PHASE4	COMPLETED	CCR5 Inhibitor Treatment Intensification on CD4+ T-cell Recovery
NCT00966329	PHASE4	COMPLETED	Switching the Non-nucleoside Reverse Transcriptase Inhibitor (NNRTI) or Protease Inhibitor (PI) to Maraviroc in HIV Subjects
NCT00981773	PHASE4	TERMINATED	The St. Marys and The Mater Switch Study
NCT01013987	PHASE4	UNKNOWN	Maraviroc (Celsentri) With Raltegravir and Darunavir/Ritonavir for the Treatment of Triple Class Failure in Adult HIV-1 Infected Patients
NCT01049204	PHASE4	TERMINATED	Impact of Maraviroc on the Immune Function in HIV-1 Infected Subjects Receiving Immunisation With Novel Antigens
NCT01190293	PHASE4	COMPLETED	PK Switch Efavirenz to Maraviroc in Patients Initially Suppressed on an Efavirenz-containing Regimen
NCT01235013	PHASE4	UNKNOWN	Effect of Maraviroc (MCV) on the Immunological Recovery of HIV-1 Discordant Patients With CD4 Lymphocyte Counts Below 200 Cells/mm3
NCT01327547	PHASE4	COMPLETED	A Study Of Maraviroc In HIV Co-Infected Subjects With Hepatitis C And/Or Hepatitis B
NCT01367210	PHASE4	TERMINATED	Switch to Darunavir/r + Maraviroc Quaque Die in Patients With R5 Tropism by Viral DNA Genotyping (GUSTA)
NCT01384682	PHASE4	COMPLETED	Maraviroc Switch Collaborative Study
NCT01389063	PHASE4	UNKNOWN	Maraviroc Abacavir STudy - Effect on Endothelial Recovery
NCT01449006	PHASE4	COMPLETED	A Study of the Neurological Effects of Adding Maraviroc to HAART Regimen in Patients With HIV (HANDmac)
NCT01533272	PHASE4	COMPLETED	Study Comparing Two Alternatives of Antiretroviral Therapy as Post-exposure Prophylaxis to HIV-1:FOVIR+EMTRICITABINA + LOPINAVIR/RITONAVIR VS TENOFOVIR+EMTRICITABINA + MARAVIROC (MARAVI-PEP)
NCT01637259	PHASE4	COMPLETED	MARCH Renal Substudy
NCT01680536	PHASE4	COMPLETED	A Study to Assess Cerebrospinal Fluid INflammatory Markers After Addition of Maraviroc to MONotherapy Darunavir/Ritonavir - The CINAMMON Study
NCT01866267	PHASE4	COMPLETED	Switching Undetectables to Selzentry
NCT02519777	PHASE4	COMPLETED	Integrase and Maraviroc Intensification in Neurocognitive Dysfunction (InMIND)
NCT02881762	PHASE4	COMPLETED	Maraviroc Efficacy for Hepatitis C
NCT02990312	PHASE4	WITHDRAWN	Impact of Sirolimus and Maraviroc on CCR5 Expression and the HIV-1 Reservoir in HIV-infected Kidney Transplant Recipients
NCT03218592	PHASE4	COMPLETED	ENLIGHTEN: Establishing Novel Antiretroviral (ARV) Imaging for Hair to Elucidate Non-Adherence
NCT03402815	PHASE4	COMPLETED	Efficacy of Maraviroc in Modulating Atherosclerosis in HIV Patients.
NCT04965662	PHASE4	COMPLETED	The Role of Home Packs of HIV PEPSE in High Risk Individuals
NCT06974084	PHASE2/PHASE3	NOT_YET_RECRUITING	Investigating Measurable PRO Acuity Trial (IMPACT) is a Multi-Center Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy of Maraviroc and Atorvastatin to Improve Neurocognitive and Physical Function of Subjects With Long COVID-19/Post-Acute Sequelae of COVID-19 (PASC).
NCT00098293	PHASE3	COMPLETED	Trial of Maraviroc (UK-427,857) in Combination With Zidovudine/Lamivudine Versus Efavirenz in Combination With Zidovudine/Lamivudine
NCT00098306	PHASE2/PHASE3	COMPLETED	Trial of Maraviroc (UK-427,857) in Combination With Optimized Background Therapy Versus Optimized Background Therapy Alone for the Treatment of HIV-1 Infected Subjects
NCT00098722	PHASE2/PHASE3	COMPLETED	Trial of Maraviroc (UK-427,857) in Combination With Optimized Background Therapy Versus Optimized Background Therapy Alone for the Treatment of HIV-1 Infected Subjects
NCT00098748	PHASE2/PHASE3	COMPLETED	Trial of Maraviroc (UK-427,857) in Combination With Optimized Background Therapy Versus Optimized Background Therapy Alone for the Treatment of Antiretroviral-Experienced NonCCR5-Tropic HIV-1 Infected Subjects
NCT00426660	PHASE3	COMPLETED	Expanded Access Program for Maraviroc At Multiple Centers
NCT00478231	PHASE3	COMPLETED	Multicenter, Safety Study Of Maraviroc
NCT00537394	PHASE3	COMPLETED	Optimizing Treatment for Treatment-Experienced, HIV-Infected People
NCT00719823	PHASE3	WITHDRAWN	Maraviroc Compassionate Use
NCT00808002	PHASE3	COMPLETED	Efficacy of Treatment Intensification With Maraviroc on HIV-1 Viral Latency in Recently Infected Hiv-1 naïve Patients Starting Raltegravir Plus Tenofovir/Emtricitabine
NCT00844519	PHASE3	COMPLETED	Effect of Maraviroc on Endothelial Function in HIV-Infected Patients

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 6 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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
TERFENADINE	ChEMBL	Phase 4 (approved)	CCR5
APLAVIROC	ChEMBL	Phase 3	CCR5
CENICRIVIROC	ChEMBL	Phase 3	CCR5
VICRIVIROC	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