Cabotegravir

Cabotegravir, sold by itself as a tablet under the brand name Vocabria and as an injection in combination with rilpivirine injection as Cabenuva, is a medication used for the treatment of HIV/AIDS in adults.[2]

Cabotegravir
Names
IUPAC name
N-((2,4-Difluorophenyl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro(1,3)oxazolo(3,2-a)pyrido(1,2-d)pyrazine-8-carboxamide
Other names
S/GSK1265744, GSK744
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
KEGG
UNII
Properties
C19H17F2N3O5
Molar mass 405.358 g·mol−1
Pharmacology
J05AJ04 (WHO)
License data
By mouth, intramuscular
Legal status
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
N (what is YN ?)
Infobox references
Cabotegravir
Clinical data
Trade namesVocabria
License data
Identifiers
DrugBank
CompTox Dashboard (EPA)

It is an integrase inhibitor, with a carbamoyl pyridone structure similar to that of dolutegravir.[4] In investigational studies, the agent was packaged into nanoparticles (GSK744LAP) conferring an exceptionally long biological half-life of 21–50 days following a single dose. In theory, this would make possible suppression of HIV with dosing as infrequently as once every three months.[5]

Medical uses

Cabotegravir, in combination with rilpivirine, is indicated for the treatment of human immunodeficiency virus type-1 (HIV-1) in adults.

Treatment of HIV

Cabotegravir was examined in the clinical trials HPTN 083 and HPTN 084.[6][7] In 2020, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Vocabria intended for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in combination with rilpivirine injection.[8] The EMA also recommended marketing authorization be given for Rekambys (rilpivirine) and Vocabria injection (cabotegravir), to be used together for the treatment of people HIV-1 infection.[9] The two medicines are the first ARVs that come in a long-acting injectable formulation.[9] This means that instead of daily pills, people receive intramuscular injections monthly or every two months.[9] The combination of cabotegravir and rilpivirine as an injection is intended for maintenance treatment of adults who have undetectable HIV levels in the blood (viral load less than 50 copies/mL) with their current ARV treatment, and when the virus has not developed resistance to non-nucleoside reverse transcriptase inhibitors (NNRTIs) and integrase strand transfer inhibitors.[9]

Research

Pre-exposure prophylaxis

In 2020, results for some studies were released showing success in using injectable cabotegravir for long-acting pre-exposure prophylaxis (PrEP) with greater efficacy than the emtricitabine/tenofovir combination being widely used for PrEP at the time.[10][11]

Society and culture

Names

Cabotegravir is the United States Adopted Name (USAN)[12] and the International nonproprietary name (INN).[13]

References
  1. "Vocabria Product information". Health Canada. Retrieved 22 January 2021.
  2. "FDA Approves First Extended-Release, Injectable Drug Regimen for Adults Living with HIV". U.S. Food and Drug Administration (FDA) (Press release). 21 January 2021. Retrieved 21 January 2021. This article incorporates text from this source, which is in the public domain.
  3. "Vocabria EPAR". European Medicines Agency (EMA). Retrieved 22 January 2021.
  4. Borrell, Brendan (2014). "Long-acting shot prevents infection with HIV analogue". Nature. doi:10.1038/nature.2014.14819. S2CID 184399045.
  5. PrEP GSK744 Integrase Administered Monthly Perhaps Quarterly Prevents HIV-Infection in Monkeys. 20th Conference on Retroviruses and Opportunistic Infections. Atlanta, GA March 3–6, 2013.
  6. "HPTN083 — Prevention Now". HIV Prevention Trials Network. Retrieved 2 December 2017.
  7. "HPTN084 — Prevention Now". HIV Prevention Trials Network. Retrieved 2 December 2017.
  8. "Vocabria: Pending EC decision". European Medicines Agency (EMA). 16 October 2020. Retrieved 16 October 2020. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  9. "First long-acting injectable antiretroviral therapy for HIV recommended approval" (Press release). European Medicines Agency (EMA). 16 October 2020. Retrieved 16 October 2020.
  10. Ryan, Benjamin (7 July 2020). "Injectable PrEP Is Even More Effective Than Daily Truvada". Poz. Retrieved 9 November 2020.
  11. Ryan, Benjamin (9 November 2020). "For Women, Injectable Cabotegravir Is More Effective Than Truvada as PrEP". Poz. Retrieved 9 November 2020.
  12. "Adopted USANs" (PDF). American Medical Association. Retrieved 19 September 2014.
  13. World Health Organization (2015). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 73". WHO Drug Information. 29 (1): 70–1. hdl:10665/331088.
  • "Cabotegravir". Drug Information Portal. U.S. National Library of Medicine.
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