Cabotegravir
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2021
- First approval year
- 2021
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Cabotegravir
- Molecular weight
- 405.36
- Structure (SMILES)
- C[C@H]1CO[C@@H]2Cn3cc(C(=O)NCc4ccc(F)cc4F)c(=O)c(O)c3C(=O)N12
- apretude
- Apretude
- cabotegravir component of cabenuva
- Cabotegravir component of cabenuva
- apretude
- APRETUDE
- cabenuva component cabotegravir
- CABENUVA COMPONENT CABOTEGRAVIR
- cabotegravir
- Cabotegravir
- cabotegravir [INN]
- CABOTEGRAVIR [JAN]
- Cabotegravir [MI]
- CABOTEGRAVIR [ORANGE BOOK]
- CABOTEGRAVIR [USAN]
- Cabotegravir [WHO-DD]
- cabotegravir inn
- cabotegravir jan
- cabotegravir mi
- cabotegravir orange book
- cabotegravir usan
- cabotegravir who dd
- gsk 1265744
- gsk 1265744a
- Gsk-1265744
- GSK-1265744A
- gsk1265744
- GSK1265744
- GSK1265744 10 mg
And 19 more, listed on the interactive page.
- CAS registry numbers
- 1051375-10-0
- ChEMBL ID
- CHEMBL2403238
- InChIKey
- WCWSTNLSLKSJPK-LKFCYVNXSA-N
- PubChem compound IDs
- 54713659
- RxNorm IDs (RxCUI)
- 2475077
- FDA ingredient codes (UNII)
- HMH0132Z1Q
- J05AJ04
- J05AX
Sources for recorded values
- Applicant
- VIIV HLTHCARE
- Approval date
- 21 Jan 2021
- Application number
- NDA212887
- Status
- Authorised
- Status date
- 17 Dec 2020
- Authorisation date
- 17 Dec 2020
- Approved indications
- Vocabria tablets are indicated in combination with rilpivirine tablets for the short-term treatment of Human Immunodeficiency Virus type 1 (HIV-1) infection in adults and adolescents (at least 12 years of age and weighing at least 35 kg) who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen without present or past evidence of viral resistance to, and no prior virological failure with agents of the non-nucleoside reverse transcriptase inhibitor (NNRTI) and integrase inhibitor (INI) class for: Oral lead in to assess tolerability of Vocabria and rilpivirine prior to administration of long acting cabotegravir injection plus long acting rilpivirine injection. Oral therapy for adults and adolescents who will miss planned dosing with cabotegravir injection plus rilpivirine injection. Vocabria injection is indicated, in combination with rilpivirine injection, for the treatment of Human Immunodeficiency Virus type 1 (HIV-1) infection in adults and adolescents (at least 12 years of age and weighing at least 35 kg) who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen without present or past evidence of viral resistance to, and no prior virological failure with agents of the non-nucleoside reverse trascriptase.
- Product number
- EMEA/H/C/004976
- Authorisation holder
- ViiV Healthcare B.V.
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- Yes
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- HIV Infections
European medicines record
- Patents
- 4
- Designations
- 2
- Earliest recorded loss of exclusivity
- 15 Sept 2031
- First in class
- No
- Fast track
- No
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- cabotegravir
- Type
- Synthetic organic
- Drug name stem
- -vir; -vir
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Parenteral
Mechanisms of action
- Mechanism
- Human immunodeficiency virus type 1 integrase inhibitor
- Action type
- Inhibitor
- Target
- Human immunodeficiency virus type 1 integrase
- Protein identifier
- Q7ZJM1
Open Targets mechanisms
- Mechanism
- Human immunodeficiency virus type 1 integrase inhibitor
- Action type
- Inhibitor
- Target
- Human immunodeficiency virus type 1 integrase
DrugCentral mechanisms
- Action type
- Inhibitor
- Gene symbol
- pol
- Protein identifier
- Q7ZJM1
- Organism
- Human immunodeficiency virus 1
- Condition
- HIV Infections
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000180
- Subject identifier
- D015658
- Condition
- Virus Diseases
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000763
- Subject identifier
- D014777
- Condition
- HIV Infections
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000764
- Subject identifier
- D015658
- Condition identifier
- EFO_0000180
- Condition identifier
- EFO_0000180
- Highest recorded phase
- 4
- Condition identifier
- EFO_0000763
- Condition identifier
- EFO_0000764
- Condition identifier
- EFO_0002950
- Condition identifier
- EFO_0010702
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005108
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005109
- Highest recorded phase
- 4
- Event
- anaemia
- Reports
- 1
- Reporting signal score
- 6.51811
- Event
- asthenia
- Reports
- 2
- Reporting signal score
- 7.11952
- Event
- blood hiv rna increased
- Reports
- 25
- Reporting signal score
- 118.753
- Event
- cd4 lymphocytes decreased
- Reports
- 7
- Reporting signal score
- 21.319
- Event
- drug hypersensitivity
- Reports
- 1
- Reporting signal score
- 7.70132
- Event
- exposure via skin contact
- Reports
- 2
- Reporting signal score
- 6.60635
- Event
- fatigue
- Reports
- 9
- Reporting signal score
- 6.70778
- Event
- hepatitis b core antibody positive
- Reports
- 2
- Reporting signal score
- 7.37555
- Event
- hepatitis b surface antibody positive
- Reports
- 2
- Reporting signal score
- 7.7068
- Event
- hodgkin's disease mixed cellularity stage unspecified
- Reports
- 2
- Reporting signal score
- 9.76586
- Event
- injection site abscess
- Reports
- 6
- Reporting signal score
- 17.5165
- Event
- injection site discharge
- Reports
- 5
- Reporting signal score
- 19.7512
- Event
- injection site indentation
- Reports
- 2
- Reporting signal score
- 6.69236
- Event
- injection site infection
- Reports
- 3
- Reporting signal score
- 6.59825
- Event
- injection site mass
- Reports
- 9
- Reporting signal score
- 11.2523
- Event
- injection site muscle atrophy
- Reports
- 2
- Reporting signal score
- 15.0858
- Event
- injection site nodule
- Reports
- 12
- Reporting signal score
- 30.8175
- Event
- injection site pain
- Reports
- 50
- Reporting signal score
- 47.5239
- Event
- labelled drug-drug interaction issue
- Reports
- 2
- Reporting signal score
- 8.94234
- Event
- labelled drug-drug interaction medication error
- Reports
- 7
- Reporting signal score
- 12.3994
- Event
- nausea
- Reports
- 3
- Reporting signal score
- 18.8376
- Event
- nodule
- Reports
- 8
- Reporting signal score
- 14.5539
- Event
- occupational exposure to product
- Reports
- 9
- Reporting signal score
- 19.1395
- Event
- papilloma
- Reports
- 2
- Reporting signal score
- 7.7068
- Event
- pathogen resistance
- Reports
- 48
- Reporting signal score
- 175.652
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And 31 more, listed on the interactive page.
- Dose
- 400mg of cabotegravir and 600mg of rilpivirine
- Route
- Intramuscular
- How often
- Monthly
Conditions of use
- Administered in the gluteal muscle at separate sites
- Hydrogen bond acceptors
- 6
- Hydrogen bond donors
- 2
- Polar surface area
- 100.87
- Calculated partition coefficient (ALogP)
- 0.96
- Calculated partition coefficient (XLogP)
- 2.1
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 3
- Heavy atoms
- 29
- Molecular formula
- C19H17F2N3O5
- Monoisotopic mass
- 405.11362698
- Natural product
- No
- Recorded assays
- 267
- Active assays
- 12
Active assay types
- Confirmatory
- HIV Integrase Inhibitors
Distribution coefficient (LogD)
- Median
- 3.49
- Mean
- 3.49
- Minimum
- 3.49
- Maximum
- 3.49
- Unit
- unitless
- Assays
- 1
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- LogD
Solubility
- Median
- 42
- Mean
- 42
- Minimum
- 42
- Maximum
- 42
- Unit
- ug/mL
- Assays
- 1
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- Solubility
Oral bioavailability
- Median
- 7.1
- Mean
- 7.1
- Minimum
- 6.2
- Maximum
- 8
- Unit
- %
- Assays
- 2
- Standard deviation
- 1.27279
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- F
Related records
Trials (77)
- A Healthy Volunteer And Patient Study To Assess The Safety, Tolerability And Pharmacokinetics Of GSK1265744
- A Randomized Study to Assess the Relative Bioavailability of New Formulations of GSK1265744 Long Acting Parental (LAP) in Healthy Adult Subjects
- A Real-life Study of the Use of Cabotegravir Plus Rilpivirine Long-acting in ART-experienced Pre-treated People With HIV
- A Single Dose Escalation Study to Investigate the Safety, Tolerability and Pharmacokinetics of Intramuscular and Subcutaneous Long Acting GSK1265744 in Healthy Subjects
- A Study Evaluating Implementation Strategies for the Delivery of APRETUDE for Black cis-and Transgender Women in United States EHE Territories
- A Study Evaluating Implementation Strategies for the Delivery of Cabotegravir in Low and High-Volume PrEP Site in the United States
- A Study to Assess the Food Effect and the Relative Bioavailability of the Cabotegravir (CAB) Pediatric Dispersible Tablet (DT) Formulation
- A Study to Assess The Relative Bioavailability of New Tablet Formulations of GSK1265744 in Healthy Adult Subjects
- A Study to Evaluate Efficacy and Safety of Cabotegravir (CAB) Long Acting (LA) Plus (+) Rilpivirine (RPV) LA Versus BIKTARVY® (BIK) in Participants With Human Immunodeficiency Virus (HIV)-1 Who Are Virologically Suppressed
- A Study to Evaluate Pharmacokinetic (PK) and Safety of GSK1265744 in Subjects With Hepatic Impairment and Control Healthy Volunteers
- A Study to Evaluate the Effect of High Fat Meal on Cabotegravir
- A Study to Evaluate the Efficacy, Safety, Participant Choice and Preference of an Oral Once-daily Regimen or a Long-acting Injectable Regimen Every Two Months for Treatment of Human Immunodeficiency Virus (HIV-1) in Adults Who Have Not Previously Taken Antiretroviral Therapy
- A Study to Evaluate the Pharmacokinetics and Safety of GSK1265744 and Rilpivirine and Dolutegravir and Rilpivirine in Healthy Adult Subjects
- A Study to Investigate if Long Acting Cabotegravir (CAB) and Lenacapavir (LEN) Injections Are Tolerable and Acceptable When Administered to Healthy Adults Without HIV
- A Study to Investigate Pharmacokinetics, Safety and Tolerability of Long-Acting Cabotegravir Plus Recombinant Human Hyaluronidase PH20 in Healthy Adult Participants
- A Study to Investigate the Pharmacokinetics, Safety, and Tolerability of Two Different Formulations of Long-acting Cabotegravir in Healthy Adult Participants
- A Study to Investigate the Safety, Tolerability and Pharmacokinetics of Repeat Dose Administration of Long-Acting GSK1265744 and Long-Acting TMC278 Intramuscular and Subcutaneous Injections in Healthy Adult Subjects
- A Study to Investigate the Virologic Efficacy and Safety of VH3810109 + Cabotegravir Compared to Standard of Care (SOC) in Male and Female Adults Living With Human Immunodeficiency Virus (HIV)
- A Sub-study of Cabotegravir (CAB) and Rilpivirine (RPV) in Human Immunodeficiency Viruses (HIV)-Infected Participants
- Acceptability and Feasibility of Injectable Cabotegravir Pre-exposure Prophylaxis (PrEP) Versus Oral PrEP in Routine Care up to 15 Months in Private Pharmacies in South Africa