cabotegravir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
HIV integrase inhibitors 5440 1051375-10-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cabotegravir
  • cabotegravir sodium
  • vocabria
  • GSK1265744
Cabotegravir is an HIV-1 antiretroviral drug. Cabotegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration which is essential for the HIV replication cycle. It is indicated in combination with rilpivirine, an HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI), as a complete regimen for the treatment of HIV-1 infection in adults to replace the current antiretroviral regimen in those who are virologically suppressed on a stable antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine.
  • Molecular weight: 405.36
  • Formula: C19H17F2N3O5
  • CLOGP: -0.12
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 2
  • TPSA: 99.18
  • ALOGS: -3.56
  • ROTB: 3
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
30 mg O
10 mg P

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.544 High 0.86
caco2-efflux Caco-2 efflux ratio (BA/AB) 5.675 High 0.86
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 25.468 10^-6 cm/s High 0.86
dh-clint Dog hepatocyte intrinsic clearance 3.119 uL/min/10^6 cells High 0.86
dppb Dog plasma protein binding (% unbound) 45.070 % High 0.86
fcs-ppb Fetal calf serum protein binding (% unbound) 40.560 % High 0.86
herg hERG pIC50 4.521 pIC50 High 0.86
hh-clint Human hepatocyte intrinsic clearance 2.904 uL/min/10^6 cells High 0.86
hlm-clint Human liver microsomal intrinsic clearance 3.855 uL/min/mg protein High 0.86
hppb Human plasma protein binding (% unbound) 28.470 % High 0.86
kinase-safety-class EIF2AK3,GRK2,PDK1,PDK2,PDK4 5
kinase-selectivity-class PDK1 1
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 7.727 High 0.86
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 12.359 High 0.86
mh-clint Mouse hepatocyte intrinsic clearance 16.331 High 0.86
mppb Mouse plasma protein binding (% unbound) 24.030 High 0.86
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 24.717 High 0.86
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 47.990 % High 0.86
rat-kpuu-brain Rat brain Kpuu 0.022 % High 0.86
rh-clint Rat hepatocyte intrinsic clearance 5.728 uL/min/10^6 cells High 0.86
rh-fuinc Rat hepatocyte fraction unbound in incubation 81.640 % High 0.86
rppb Rat plasma protein binding (% unbound) 23.940 % High 0.86
solubility-dd Solubility at pH 7.4 in DMSO 433.511 uM High 0.86

Approvals:

DateAgencyCompanyOrphan
Jan. 21, 2021 FDA Viiv HLTHCARE
May 31, 2022 PMDA ViiV Healthcare K.K
Dec. 17, 2020 EMA ViiV Healthcare B.V.

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
Viral load increased 597.13 41.15 90 2490 1466 90624401
Product use in unapproved therapeutic environment 401.32 41.15 47 2533 73 90625794
Exposure during pregnancy 300.20 41.15 142 2438 238268 90387599
Injection site pain 260.59 41.15 117 2463 173582 90452285
Virologic failure 237.82 41.15 43 2537 2181 90623686
Blood HIV RNA increased 235.74 41.15 37 2543 787 90625080
Injection site nodule 225.46 41.15 46 2534 4427 90621440
Product dose omission issue 219.45 41.15 123 2457 291564 90334303
Product complaint 194.28 41.15 50 2530 13450 90612417
Pathogen resistance 182.33 41.15 43 2537 8072 90617795
Injection site discharge 148.21 41.15 27 2553 1424 90624443
Viral mutation identified 139.23 41.15 27 2553 1998 90623869
Product storage error 122.03 41.15 38 2542 20203 90605664
Occupational exposure to product 92.67 41.15 20 2560 2511 90623356
Wrong technique in device usage process 80.88 41.15 21 2559 5814 90620053
Injection site mass 67.81 41.15 25 2555 22065 90603802
Injection site abscess 67.61 41.15 14 2566 1440 90624427
Incorrect dose administered 63.56 41.15 35 2545 78895 90546972
Nodule 63.22 41.15 25 2555 26661 90599206
Abortion spontaneous 57.84 41.15 29 2551 54027 90571840
Hepatitis B reactivation 53.61 41.15 14 2566 3960 90621907
Atrioventricular septal defect 45.51 41.15 8 2572 343 90625524
Injection site discomfort 43.65 41.15 13 2567 5927 90619940

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
Viral load increased 1326.94 38.98 253 6869 2744 42611469
Product dose omission issue 1156.62 38.98 543 6579 153822 42460391
Injection site pain 1008.97 38.98 373 6749 57425 42556788
Product use in unapproved therapeutic environment 695.21 38.98 107 7015 251 42613962
Virologic failure 509.91 38.98 121 7001 3873 42610340
Blood HIV RNA increased 406.01 38.98 85 7037 1506 42612707
Product complaint 399.61 38.98 108 7014 5869 42608344
Pathogen resistance 392.04 38.98 123 6999 11327 42602886
Product storage error 341.39 38.98 110 7012 11030 42603183
Injection site nodule 320.62 38.98 74 7048 2087 42612126
Viral mutation identified 303.56 38.98 77 7045 3254 42610959
Product administered at inappropriate site 249.94 38.98 65 7057 3033 42611180
Wrong technique in device usage process 171.00 38.98 47 7075 2710 42611503
Inappropriate schedule of product administration 144.51 38.98 123 6999 95779 42518434
Injection site discomfort 131.74 38.98 37 7085 2309 42611904
Pain 101.50 38.98 161 6961 244687 42369526
HIV infection 95.24 38.98 26 7096 1459 42612754
Injection site mass 91.38 38.98 39 7083 8536 42605677
Syphilis 86.65 38.98 20 7102 562 42613651
Injection site swelling 85.13 38.98 46 7076 16927 42597286
Injection site reaction 82.76 38.98 44 7078 15677 42598536
Off label use 73.72 38.98 253 6869 638082 41976131
Acute hepatitis B 73.31 38.98 15 7107 235 42613978
Injection site discharge 67.40 38.98 16 7106 509 42613704
Influenza like illness 65.25 38.98 49 7073 31791 42582422
Hepatitis B 60.06 38.98 27 7095 6684 42607529
Injection site induration 58.50 38.98 22 7100 3465 42610748
Depression 57.02 38.98 81 7041 111282 42502931
Injection site abscess 56.67 38.98 16 7106 1016 42613197
Myalgia 52.32 38.98 72 7050 96008 42518205
Nodule 52.01 38.98 30 7092 12504 42601709
Pneumonia 50.05 38.98 6 7116 422143 42192070
Substance use 48.34 38.98 16 7106 1735 42612478
Product administered by wrong person 47.09 38.98 8 7114 41 42614172
CD4 lymphocytes decreased 46.88 38.98 16 7106 1905 42612308
Viral load abnormal 46.37 38.98 9 7113 106 42614107
Hepatitis B reactivation 46.06 38.98 20 7102 4558 42609655
Disseminated mycobacterium avium complex infection 44.95 38.98 10 7112 237 42613976
Acute kidney injury 44.07 38.98 5 7117 367332 42246881
Injection site warmth 41.66 38.98 16 7106 2667 42611546
Viraemia 40.31 38.98 14 7108 1756 42612457

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
Product dose omission issue 1179.99 31.42 497 5805 321285 110261712
Viral load increased 883.68 31.42 155 6147 3235 110579762
Injection site pain 736.58 31.42 301 6001 177621 110405376
Product use in unapproved therapeutic environment 532.06 31.42 73 6229 251 110582746
Product storage error 477.57 31.42 130 6172 21598 110561399
Virologic failure 412.49 31.42 87 6215 4865 110578132
Blood HIV RNA increased 411.95 31.42 76 6226 2112 110580885
Pathogen resistance 408.24 31.42 110 6192 17562 110565435
Viral mutation identified 335.87 31.42 72 6230 4347 110578650
Product complaint 290.09 31.42 80 6222 13892 110569105
Injection site nodule 255.12 31.42 58 6244 4588 110578409
Injection site discomfort 154.68 31.42 42 6260 6865 110576132
Inappropriate schedule of product administration 131.96 31.42 102 6200 203535 110379462
Wrong technique in device usage process 127.10 31.42 36 6266 6865 110576132
Injection site discharge 112.08 31.42 24 6278 1436 110581561
Hepatitis B reactivation 106.68 31.42 32 6270 7452 110575545
Product administered at inappropriate site 89.75 31.42 26 6276 5367 110577630
Injection site swelling 86.36 31.42 50 6252 61740 110521257
HIV infection 75.47 31.42 17 6285 1286 110581711
Syphilis 72.50 31.42 15 6287 759 110582238
Injection site induration 70.66 31.42 26 6276 11357 110571640
Injection site mass 66.44 31.42 31 6271 24582 110558415
Exposure during pregnancy 61.93 31.42 61 6241 167363 110415634
Hepatitis B 56.16 31.42 21 6281 9591 110573406
Substance use 54.98 31.42 15 6287 2491 110580506
Incorrect dose administered 54.46 31.42 46 6256 103595 110479402
Injection site abscess 53.44 31.42 14 6288 1992 110581005
Nodule 49.85 31.42 28 6274 32603 110550394
Myalgia 47.72 31.42 61 6241 222320 110360677
Disseminated mycobacterium avium complex infection 42.52 31.42 9 6293 509 110582488
Acute hepatitis B 41.71 31.42 9 6293 558 110582439
Product administration error 41.33 31.42 26 6276 37191 110545806
Depression 37.71 31.42 66 6236 317269 110265728
Abortion spontaneous 35.70 31.42 23 6279 34259 110548738
Oropharyngeal gonococcal infection 35.44 31.42 5 6297 22 110582975
Injection site warmth 35.19 31.42 18 6284 17387 110565610
Monkeypox 33.60 31.42 7 6295 366 110582631
Pain 32.93 31.42 124 6178 954831 109628166
Injection site erythema 32.37 31.42 33 6269 94143 110488854
Blood HIV RNA below assay limit 32.32 31.42 4 6298 4 110582993
Proctitis chlamydial 32.32 31.42 4 6298 4 110582993
Injection site necrosis 31.55 31.42 9 6293 1757 110581240

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J05AJ04 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Integrase inhibitors
FDA MoA N0000000127 HIV Integrase Inhibitors
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D019380 Anti-HIV Agents
MeSH PA D019428 HIV Integrase Inhibitors
MeSH PA D019429 Integrase Inhibitors
MeSH PA D044966 Anti-Retroviral Agents
FDA EPC N0000175887 Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor
FDA MoA N0000190110 Organic Anion Transporter 1 Inhibitors
FDA MoA N0000190111 Organic Anion Transporter 3 Inhibitors
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:67268 HIV-1 integrase inhibitor
CHEBI has role CHEBI:64946 anti-HIV agent

Related Drugs by ATC class:

J05AJ Integrase inhibitors 3 drugs
dolutegravirelvitegravirraltegravir

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

DiseaseRelationSNOMED_IDDOID
Human immunodeficiency virus I infection indication 40780007




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 11389447 June 30, 2027 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG BY MONTHLY ADMINISTRATION OF RILPIVIRINE SUSPENSION AS PART OF COMBINATION THERAPY
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 11389447 June 30, 2027 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG BY MONTHLY ADMINISTRATION OF RILPIVIRINE SUSPENSION AS PART OF COMBINATION THERAPY
EQ 30MG BASE VOCABRIA VIIV HLTHCARE N212887 Jan. 21, 2021 RX TABLET ORAL 8410103 Feb. 4, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 8410103 Feb. 4, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 8410103 Feb. 4, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 11224597 Sept. 15, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12138264 Sept. 15, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 11224597 Sept. 15, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12138264 Sept. 15, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR RE50189 Nov. 27, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR RE50189 Nov. 27, 2031 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12178815 July 18, 2038 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12178815 July 18, 2038 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12636285 Oct. 1, 2040 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12636286 Oct. 1, 2040 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12636285 Oct. 1, 2040 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR 12636286 Oct. 1, 2040 TREATMENT OF HIV-1 INFECTION IN ADULTS AND ADOLESCENTS 12 YEARS OF AGE AND OLDER AND WEIGHING AT LEAST 35 KG

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 30MG BASE VOCABRIA VIIV HLTHCARE N212887 Jan. 21, 2021 RX TABLET ORAL Jan. 21, 2026 NEW CHEMICAL ENTITY
400MG/2ML (200MG/ML);600MG/2ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR Jan. 21, 2026 NEW CHEMICAL ENTITY
600MG/3ML (200MG/ML);900MG/3ML (300MG/ML) CABENUVA KIT VIIV HLTHCARE N212888 Jan. 21, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR Jan. 21, 2026 NEW CHEMICAL ENTITY
600MG/3ML (200MG/ML) APRETUDE VIIV HLTHCARE N215499 Dec. 20, 2021 RX SUSPENSION, EXTENDED RELEASE INTRAMUSCULAR Jan. 21, 2026 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Integrase Enzyme INHIBITOR IC50 8.52 DRUG LABEL DRUG LABEL
Integrase Enzyme IC50 8.52 CHEMBL

External reference:

IDSource
D10548 KEGG_DRUG
HMH0132Z1Q UNII
1051375-13-3 SECONDARY_CAS_RN
C4310385 UMLSCUI
CHEBI:172944 CHEBI
CHEMBL2403238 ChEMBL_ID
54713659 PUBCHEM_CID
DB11751 DRUGBANK_ID
CHEMBL3137330 ChEMBL_ID
9903 INN_ID
C584914 MESH_SUPPLEMENTAL_RECORD_UI
11386 IUPHAR_LIGAND_ID
1145127006 SNOMEDCT_US
1145347005 SNOMEDCT_US
1217148000 SNOMEDCT_US
4040009 VANDF
340100 MMSL
38935 MMSL
38937 MMSL
d09653 MMSL
018236 NDDF
018309 NDDF
2475076 RXNORM
HMH0132Z1Q INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Vocabria HUMAN PRESCRIPTION DRUG LABEL 1 49702-248 TABLET, FILM COATED 30 mg ORAL NDA 27 sections