Drug information

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Pronounce:
Other Names:
CAB, CAB LA, cabotegravir LA, cabotegravir sodium, cabotegravir long-acting injectable, cabotegravir extended-release injectable suspension
Drug Class:
Integrase Strand Transfer Inhibitor (INSTIs)
Molecular Formula:

C19 H17 F2 N3 O5

Registry Number:
1051375-10-0 (CAS)
Chemical Name:

(3S,11aR)-N-((2,4-difluorophenyl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydrooxazolo(3,2-a)pyrido(1,2-d)pyrazine-8-carboxamide

Chemical Class:
Carbamoyl pyridone
Organization:
ViiV Healthcare
Phase of Development:

Cabotegravir is in Phase 3 development for HIV prevention.

FDA-approved Products for HIV Treatment: Cabenuva, a two-drug regimen consisting of cabotegravir and rilpivirine extended-release injectable suspensions is FDA-approved for HIV treatment. Additionally, an oral tablet formulation of cabotegravir (brand name: Vocabria) is FDA-approved for use with oral rilpivirine for short-term HIV treatment.

 
What is cabotegravir?What is cabotegravir?

What is cabotegravir?

 

Cabotegravir is a drug that has been approved under the brand name Vocabria by the U.S. Food and Drug Administration (FDA) for use with oral rilpivirine (brand name: Edurant) for the short-term treatment of HIV infection.5 Cabotegravir is also being studied as an investigational drug to prevent HIV infection.3

Cabotegravir belongs to a group of HIV drugs called integrase inhibitors.6 Integrase inhibitors block an HIV enzyme called integrase. By blocking integrase, integrase inhibitors prevent HIV from multiplying and can reduce the amount of HIV in the body.

To learn about how investigational drugs are tested during clinical trials, read the HIVinfo What is an Investigational HIV Drug? and HIV/AIDS Clinical Trials fact sheets.

Which clinical trials are studying cabotegravir?Which clinical trials are studying cabotegravir?

Select clinical trials of cabotegravir

Cabotegravir for HIV Prevention

Study Names: ECLAIR; NCT02076178
Phase: 2a
Status: This study has been completed.
Location: United States
Purpose: The purpose of this study was to evaluate the safety, tolerability, and acceptability of cabotegravir LA for pre-exposure prophylaxis (PrEP).7,8

Study Names: HPTN 077; NCT02178800
Phase: 2a
Status: This study has been completed.
Locations: United States, Brazil, Malawi, South Africa
Purpose: The purpose of this study was to evaluate the safety, tolerability, and pharmacokinetics of cabotegravir LA in participants without HIV.9

Study Names: HPTN 083; NCT02720094
Phase: 2b/3
Status: This study is ongoing, but not recruiting participants.
Locations: United States, Argentina, Brazil, Peru, South Africa, Thailand, Vietnam
Purpose: The purpose of this study is to compare the safety and effectiveness of cabotegravir LA to oral tenofovir disoproxil fumarate/emtricitabine (Truvada) for PrEP.10

Study Names: HPTN 084; NCT03164564
Phase: 3
Status: This study is currently recruiting participants.
Locations: Botswana, Kenya, Malawi, South Africa, Swaziland, Uganda, Zimbabwe
Purpose: The purpose of this study is to compare the safety and effectiveness of cabotegravir LA to oral Truvada for PrEP.3

For more details on the studies listed above, see the Health Professional version of this drug summary.

What side effects might cabotegravir cause?What side effects might cabotegravir cause?

What side effects might cabotegravir cause?

 

One goal of HIV research is to identify new drugs that have fewer side effects. The following side effects were observed in some of the studies of cabotegravir listed above.

ECLAIR (NCT02076178):
During the oral therapy part of the ECLAIR study, treatment-related side effects were mostly mild to moderate. No serious side effects were reported with oral cabotegravir.11

The majority of participants receiving cabotegravir LA had an injection site reaction. Most of these reactions were mild to moderate in intensity and most were cases of injection-site pain. Among the participants receiving cabotegravir LA, 19% had a serious injection site reaction and four participants withdrew from the study because of injection intolerability. Other injection site reactions reported by participants receiving cabotegravir LA included mild itchiness, nodules/bumps, warmth to the touch, bruising, and hardened tissue.11

HPTN 077 (NCT02178800):

In the HPTN 077 study, ten participants discontinued cabotegravir because of drug-related side effects, including gastrointestinal problems, rash, and neurologic issues. Serious side effects reported by participants taking cabotegravir included vertigo and weakness.12 

During the injection phase of the study, the majority of participants receiving cabotegravir LA had side effects that were moderate or higher in intensity. Injection site reactions, most of which were mild to moderate, were common in participants receiving cabotegravir LA. Only one participant discontinued cabotegravir due to an injection site reaction. Two participants receiving cabotegravir LA had a severe injection site reaction, although neither participant stopped cabotegravir LA injections.12

HPTN 083 (NCT02720094)
In the HPTN 083 trial, the majority of participants receiving cabotegravir LA experienced injection site reactions, but most of these reactions were mild or moderate. Only 2.2% of participants receiving cabotegravir LA stopped treatment because of an injection-related side effect. Some other side effects that occurred in participants taking cabotegravir LA included increased blood sugar levels, fever, and common cold.10,13

Because cabotegravir is still being studied, information on possible side effects of the drug is not complete. As testing of cabotegravir continues, additional information on possible side effects will be gathered.

Additional information on side effects known to be associated with cabotegravir can be found in the FDA-approved Full Prescribing Information for Cabenuva and Vocabria.4,5

Where can I get more information about clinical trials studying cabotegravir?Where can I get more information about clinical trials studying cabotegravir?

Where can I get more information about clinical trials studying cabotegravir?

 

More information about cabotegravir-related research studies is available from ClinicalTrials.gov.

Some clinical trials may be looking for volunteer participants. Your health care provider can help you decide whether participating in a clinical trial is right for you. For more information, visit NIH Clinical Research Trials and You.

ReferencesReferences

References

 

  1. United States National Library of Medicine. ChemIDplus Advanced: cabotegravir. https://chem.nlm.nih.gov/chemidplus/rn/1051375-10-0. Accessed January 29, 2021
  2. Whitfield T, Torkington A, van Halsema C. Profile of cabotegravir and its potential in the treatment and prevention of HIV-1 infection: evidence to date. HIVAIDS Auckl NZ. 2016;8:157-164.
  3. National Institute of Allergy and Infectious Diseases (NIAID). A Phase 3 double blind safety and efficacy study of long-acting injectable cabotegravir compared to daily oral TDF/FTC for pre-exposure prophylaxis in HIV-uninfected women. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on May 22, 2017. NLM Identifier: NCT03164564. https://clinicaltrials.gov/ct2/show/NCT03164564. Accessed January 29, 2021
  4. ViiV Healthcare Company: Cabenuva: full prescribing information, January 2021. DailyMed. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1698baf3-f895-4c42-a1b1-e9ee3f20da36. Accessed January 29, 2021
  5. ViiV Healthcare Company. Vocabria: full prescribing information, January 2021. DailyMed. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=66d450fb-cca4-476c-b0c7-c0730e3e4cf3. Accessed January 29, 2021
  6. National Institute of Allergy and Infectious Diseases (NIAID). NIAID ChemDB, HIV Drugs in Development. https://chemdb.niaid.nih.gov/DrugDevelopmentHIV.aspx. Accessed January 29, 2021
  7. ViiV Healthcare. A Phase IIa study to evaluate the safety, tolerability and acceptability of long acting injections of the HIV integrase inhibitor, GSK1265744, in HIV uninfected men (ECLAIR). In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on February 27, 2014. NLM Identifier: NCT02076178. https://clinicaltrials.gov/ct2/show/NCT02076178. Accessed January 29, 2021
  8. Markowitz M, Frank I, Grant RM, et al. Safety and tolerability of long-acting cabotegravir injections in HIV-uninfected men (ECLAIR): a multicentre, double-blind, randomised, placebo-controlled, phase 2a trial. Lancet HIV. 2017;4(8):e331-e340.
  9. National Institute of Allergy and Infectious Diseases (NIAID). A Phase IIa study to evaluate the safety, tolerability and pharmacokinetics of the investigational injectable HIV integrase inhibitor, GSK1265744, in HIV-uninfected men and women. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on June 27, 2014. NLM Identifier: NCT02178800. https://clinicaltrials.gov/ct2/show/NCT02178800. Accessed January 29, 2021
  10. National Institute of Allergy and Infectious Diseases (NIAID). A Phase 2b/3 double blind safety and efficacy study of injectable cabotegravir compared to daily oral tenofovir disoproxil fumarate/emtricitabine (TDF/FTC), for pre-exposure prophylaxis in HIV-uninfected cisgender men and transgender women who have sex with men. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on March 21, 2016. NLM Identifier: NCT02720094. https://clinicaltrials.gov/ct2/show/NCT02720094. Accessed January 29, 2021
  11. Murray M, Markowitz M, Frank I, et al. Satisfaction and acceptability of cabotegravir long-acting injectable suspension for prevention of HIV: Patient perspectives from the ECLAIR trial. HIV Clin Trials. 2018;19:1-10. doi:10.1080/15284336.2018.1511346
  12. Landovitz R, Li S, Grinsztejn B, et al. Safety, tolerability, and pharmacokinetics of long-acting injectable cabotegravir in low-risk HIV-uninfected women and men HPTN 077. Slides presented at: International AIDS Society (IAS) Conference on HIV Science; July 23-26, 2017; Paris, France. http://programme.ias2017.org/PAGMaterial/PPT/2899_91/IAS2017_Landovitz_Final_072417.pptx. Accessed January 29, 2021
  13. Landovitz R. HPTN 083 final results: pre-exposure prophylaxis containing long-acting injectable cabotegravir is safe and highly effective for cisgender men and transgender women who have sex with men. International AIDS Conference (IAC); July 6-10, 2020. Levin: Conference reports for National AIDS Treatment Advocacy Project (NATAP); 2020. http://www.natap.org/2020/IAC/IAC_28.htm. Accessed January 29, 2021
 

Last Reviewed: January 29, 2021