> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/cabotegravir-1f366d64-3197-46dd-be60-904d6e38236a
> Record changed: 2026-10-13

# Cabotegravir

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2403238)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2403238)

First approval year

2021

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2403238)

## Development status

**First approval year**

2021

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2403238)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2403238)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2403238)

**Drug name**

Cabotegravir

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2403238)

**Molecular weight**

405.36

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2403238)

**Structure (SMILES)**

C\[C@H\]1CO\[C@@H\]2Cn3cc(C(=O)NCc4ccc(F)cc4F)c(=O)c(O)c3C(=O)N12

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2403238)

### Brand names (4)

- apretude
- Apretude
- cabotegravir component of cabenuva
- Cabotegravir component of cabenuva

### Other names (44)

- 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.

## Identifiers

**CAS registry numbers**

- 1051375-10-0

**ChEMBL ID**

CHEMBL2403238

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2403238)

**InChIKey**

WCWSTNLSLKSJPK-LKFCYVNXSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2403238)

**PubChem compound IDs**

- 54713659

**RxNorm IDs (RxCUI)**

- 2475077

**FDA ingredient codes (UNII)**

- HMH0132Z1Q

### ATC classification codes (2)

- J05AJ04
- J05AX

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL2403238)

## Regulatory information

### United States

**Applicant**

VIIV HLTHCARE

**Approval date**

21 Jan 2021

**Application number**

NDA212887

### European Union

**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

Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/vocabria)

### Other regulatory facts

**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

### Drug classification

**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

### Investigated indications (3)

- **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

### Open Targets indications (8)

- **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

### Reported adverse events (39)

- **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

And 14 more, listed on the interactive page.

### Trial references (56)

- NCT00659191  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00659191)
- NCT00812318  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00812318)
- NCT00920296  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00920296)
- NCT00920426  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00920426)
- NCT01467531  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01467531)
- NCT01593046  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01593046)
- NCT01641809  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01641809)
- NCT01648257  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01648257)
- NCT01754116  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01754116)
- NCT01756131  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01756131)
- NCT02027454  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02027454)
- NCT02059031  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02059031)
- NCT02120352  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02120352)
- NCT02159131  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02159131)
- NCT02178800  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02178800)
- NCT02345707  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02345707)
- NCT02354937  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02354937)
- NCT02354950  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02354950)
- NCT02462772  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02462772)
- NCT02478463  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02478463)
- NCT02720094  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02720094)
- NCT02799264  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02799264)
- NCT02938520  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02938520)
- NCT02951052  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02951052)
- NCT03149848  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03149848)

And 31 more, listed on the interactive page.

## Dosing

**Dose**

400mg of cabotegravir and 600mg of rilpivirine

**Route**

Intramuscular

**How often**

Monthly

### Conditions of use

- Administered in the gluteal muscle at separate sites

## Chemical properties

**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

## Evidence counts

**Recorded assays**

267

**Active assays**

12

### Active assay types

- Confirmatory

## Pharmacologic actions

- HIV Integrase Inhibitors  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D019428.html)

## Biological measurements

### Observed measurements

#### 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](https://trialight.com/data/trial/a-study-to-investigate-pharmacokinetics-safety-and-3178f929-3665-4bd3-8803-5e43b4ab3408.md)
- 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

### Approved for (2)

- [HIV infectious disease](https://trialight.com/data/condition/hiv-infectious-disease-1260f28c-d667-55f9-b221-15d5017fde05.md)
- [Viral infectious disease](https://trialight.com/data/condition/viral-infectious-disease-43db42a3-adad-5b9d-b74c-f17df0674c21.md)

---

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