maraviroc 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antivirals CCR5 (Chemokine CC motif receptor 5) receptor antagonists 1635 376348-65-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • MD6P741W8A
  • UK-427857
  • maravirok
  • marawirok
  • maraviroc
  • celsentri
  • selzentry
Maraviroc is a member of a therapeutic class called CCR5 co-receptor antagonists. Maraviroc selectively binds to the human chemokine receptor CCR5 present on the cell membrane, preventing the interaction of HIV-1 gp120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells. CXCR4-tropic and dual-tropic HIV-1 entry is not inhibited by maraviroc.
  • Molecular weight: 513.68
  • Formula: C29H41F2N5O
  • CLOGP: 3.26
  • LIPINSKI: 1
  • HAC: 6
  • HDO: 1
  • TPSA: 63.05
  • ALOGS: -4.68
  • ROTB: 8
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.60 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 8 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 33.37 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 23 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 2.30 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 9.40 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.25 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 12.80 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Aug. 6, 2007 FDA VIIV HLTHCARE

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Pathogen resistance 89.69 58.08 20 817 6378 63481807
Virologic failure 87.85 58.08 16 821 1846 63486339
Exposure during pregnancy 75.77 58.08 38 799 155509 63332676
Viral mutation identified 75.39 58.08 14 823 1796 63486389
Abortion spontaneous 68.32 58.08 25 812 47170 63441015
Lipodystrophy acquired 65.39 58.08 12 825 1440 63486745

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Virologic failure 283.55 26.57 61 2136 3419 34951315
Viral mutation identified 219.35 26.57 48 2149 2906 34951828
Pathogen resistance 104.35 26.57 34 2163 9448 34945286
Drug resistance 99.76 26.57 43 2154 25884 34928850
Immune reconstitution inflammatory syndrome 63.51 26.57 23 2174 8736 34945998
Blood HIV RNA increased 53.74 26.57 13 2184 1217 34953517
CSF HIV escape syndrome 43.63 26.57 8 2189 193 34954541
Progressive multifocal leukoencephalopathy 43.50 26.57 18 2179 9746 34944988
Viral load increased 40.09 26.57 12 2185 2515 34952219
Hodgkin's disease 31.86 26.57 8 2189 873 34953861
Anal cancer 31.42 26.57 7 2190 456 34954278
Treatment failure 29.47 26.57 24 2173 46673 34908061
Kidney enlargement 27.68 26.57 7 2190 785 34953949
Congenital renal disorder 27.67 26.57 5 2192 111 34954623
Congenital vesicoureteric reflux 27.22 26.57 4 2193 22 34954712
Hepatic failure 26.66 26.57 20 2177 34511 34920223

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Virologic failure 298.69 30.48 58 2331 4133 79737866
Viral mutation identified 248.05 30.48 49 2340 3809 79738190
Pathogen resistance 146.67 30.48 41 2348 14301 79727698
Drug resistance 106.74 30.48 42 2347 42171 79699828
Immune reconstitution inflammatory syndrome 73.93 30.48 24 2365 13817 79728182
CSF HIV escape syndrome 72.66 30.48 12 2377 335 79741664
Viral load increased 67.33 30.48 16 2373 2932 79739067
Drug interaction 47.33 30.48 60 2329 415123 79326876
Lipodystrophy acquired 47.08 30.48 13 2376 4312 79737687
Progressive multifocal leukoencephalopathy 46.80 30.48 19 2370 20581 79721418
Treatment noncompliance 45.94 30.48 25 2364 52243 79689756
Antiviral drug level below therapeutic 43.78 30.48 6 2383 44 79741955
CD4 lymphocytes decreased 43.42 30.48 11 2378 2623 79739376
CSF test abnormal 41.61 30.48 8 2381 535 79741464
Hyperbilirubinaemia 40.38 30.48 18 2371 24500 79717499
Generalised anxiety disorder 40.32 30.48 10 2379 2187 79739812
Abortion spontaneous 40.24 30.48 19 2370 29488 79712511
Hodgkin's disease 37.95 30.48 8 2381 852 79741147
Acquired immunodeficiency syndrome 32.90 30.48 6 2383 301 79741698
Social avoidant behaviour 32.56 30.48 10 2379 4804 79737195
HIV-associated neurocognitive disorder 32.08 30.48 6 2383 346 79741653
Blood HIV RNA increased 32.03 30.48 8 2381 1800 79740199
White matter lesion 31.14 30.48 8 2381 2014 79739985
Exposure during pregnancy 30.89 30.48 25 2364 101107 79640892

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AX09 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Other antivirals
FDA MoA N0000175445 Chemokine Co-receptor 5 Antagonists
FDA EPC N0000175572 CCR5 Co-receptor Antagonist
MeSH PA D019380 Anti-HIV Agents
MeSH PA D000890 Anti-Infective Agents
MeSH PA D044966 Anti-Retroviral Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D065100 CCR5 Receptor Antagonists
MeSH PA D023581 HIV Fusion Inhibitors
CHEBI has role CHEBI:36044 antiviral drugs
CHEBI has role CHEBI:59886 HIV fusion inhibitors
CHEBI has role CHEBI:63673 CCR5 antagonist

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
CCR5 Tropic Drug Resistant HIV Infection indication
Myocardial infarction contraindication 22298006 DOID:5844
Orthostatic hypotension contraindication 28651003
Infectious disease contraindication 40733004
Viral hepatitis C contraindication 50711007 DOID:1883
Acute nephropathy contraindication 58574008
Chronic type B viral hepatitis contraindication 61977001
Chronic renal failure syndrome contraindication 90688005
Kidney disease contraindication 90708001 DOID:557
Disease of liver contraindication 235856003 DOID:409
Drug-induced hepatitis contraindication 235876009
Cardiovascular event risk contraindication 395112001
Breastfeeding (mother) contraindication 413712001
Disorder of coronary artery contraindication 414024009
Myocardial ischemia contraindication 414795007 DOID:3393




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.8 Basic
pKa2 5.07 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
20MG/ML SELZENTRY VIIV HLTHCARE N208984 Nov. 4, 2016 RX SOLUTION ORAL Oct. 30, 2023 NEW PATIENT POPULATION
20MG/ML SELZENTRY VIIV HLTHCARE N208984 Nov. 4, 2016 RX SOLUTION ORAL April 30, 2024 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
C-C chemokine receptor type 5 GPCR ANTAGONIST Kd 7.60 CHEMBL CHEMBL
Multidrug and toxin extrusion protein 1 Transporter IC50 4.76 CHEMBL
C-C chemokine receptor type 5 GPCR IC50 8.28 CHEMBL
C-C chemokine receptor type 5 GPCR Ki 9.62 CHEMBL

External reference:

IDSource
4026629 VUID
N0000179791 NUI
D06670 KEGG_DRUG
4026629 VANDF
C1667052 UMLSCUI
CHEBI:63608 CHEBI
CHEMBL1201187 ChEMBL_ID
D000077592 MESH_DESCRIPTOR_UI
DB04835 DRUGBANK_ID
806 IUPHAR_LIGAND_ID
8450 INN_ID
MD6P741W8A UNII
3002977 PUBCHEM_CID
620216 RXNORM
118030 MMSL
24072 MMSL
356432 MMSL
d06852 MMSL
012282 NDDF
427805000 SNOMEDCT_US
429603001 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Maraviroc HUMAN PRESCRIPTION DRUG LABEL 1 31722-579 TABLET, FILM COATED 150 mg ORAL ANDA 27 sections
Maraviroc HUMAN PRESCRIPTION DRUG LABEL 1 31722-580 TABLET, FILM COATED 300 mg ORAL ANDA 27 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-223 TABLET, FILM COATED 150 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-223 TABLET, FILM COATED 150 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-223 TABLET, FILM COATED 150 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-224 TABLET, FILM COATED 300 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-224 TABLET, FILM COATED 300 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-224 TABLET, FILM COATED 300 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-233 TABLET, FILM COATED 25 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-233 TABLET, FILM COATED 25 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-233 TABLET, FILM COATED 25 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-235 TABLET, FILM COATED 75 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-235 TABLET, FILM COATED 75 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-235 TABLET, FILM COATED 75 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-237 SOLUTION 20 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-237 SOLUTION 20 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 49702-237 SOLUTION 20 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 50090-6238 TABLET, FILM COATED 150 mg ORAL NDA 30 sections
SELZENTRY HUMAN PRESCRIPTION DRUG LABEL 1 54868-5809 TABLET, FILM COATED 300 mg ORAL NDA 32 sections
Maraviroc HUMAN PRESCRIPTION DRUG LABEL 1 72865-231 TABLET, FILM COATED 150 mg ORAL ANDA 31 sections
Maraviroc HUMAN PRESCRIPTION DRUG LABEL 1 72865-232 TABLET, FILM COATED 300 mg ORAL ANDA 31 sections