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Cabotegravir/rilpivirine

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Cabotegravir/rilpivirine
Combination of
Cabotegravir Integrase strand transfer inhibitor (INSTI)
Rilpivirine Non-nucleoside reverse transcriptase inhibitor (NNRTI)
Clinical data
Trade names Cabenuva, Vocabria, Rekambys
AHFS / Drugs.com Multum Consumer Information
MedlinePlus a621009
License data
Pregnancy
category
  • AU : B1
Routes of
administration 		Intramuscular
ATC code
  • None
Legal status
Legal status
Identifiers
KEGG

Cabotegravir/rilpivirine , sold under the brand name Cabenuva , is a co-packaged antiretroviral medication for the treatment of HIV/AIDS . [3] [4] [5] [6] [7] It contains cabotegravir and rilpivirine in a package with two separate injection vials . [3] [4] [6]

The most common adverse reactions include injection site reactions, fever or feeling hot (pyrexia), fatigue , headache , musculoskeletal pain, nausea , sleep disorders, dizziness and rash . [3] [4] [8]

The co-packaged medication was approved for medical use in the United States in January 2021. [4] [8] [9] It is the first FDA-approved injectable, complete regimen for HIV-infected adults that is administered once a month. [4] [5] It is also approved for use in Canada. [1] In the European Union, the two medications are approved separately and have different brand names: Vocabria (for cabotegravir) and Rekambys (for rilpivirine). [10] [11] [12]

Medical uses [ edit ]

Cabotegravir/rilpivirine is indicated as a complete regimen for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults to replace a current antiretroviral regimen in those who are virologically suppressed on a stable antiretroviral regimen with no history of treatment failure. [3] [4] In the European Union, the combination is indicated for maintenance treatment of adults who have undetectable HIV levels in the blood ( viral load less than 50 copies/mL) with their current antiretroviral treatment, and when the virus has not developed resistance to non-nucleoside reverse transcriptase inhibitors (NNRTIs) and integrase strand transfer inhibitors . [13]

Contraindications and interactions [ edit ]

Cabotegravir/rilpivirine must not be combined with drugs that induce the liver enzyme CYP3A4 , because they accelerate the inactivation of rilpivirine, and/or the enzyme UGT1A1 , because they accelerate the inactivation of cabotegravir. These mechanisms potentially result in loss of effectiveness. Examples for such drugs are rifampicin , rifapentine , carbamazepine , oxcarbazepine , eslicarbazepine acetate , phenytoin , primidone , phenobarbital and some glucocorticoids . [3]

Adverse effects [ edit ]

The most common side effects include reactions at the injection site (in up to 84% of patients) such as pain and swelling, as well as headache (up to 12%) and fever or feeling hot (in 10%). Less common side effects (under 10%) are depressive disorders , insomnia , rashes , [12] fatigue , musculoskeletal pain, nausea , sleep disorders, and dizziness. [3]

Pharmacology [ edit ]

Further information: Cabotegravir § Pharmacology , Rilpivirine § Pharmacology , and Reverse-transcriptase inhibitor § Mechanism of action

Cabotegravir is an integrase strand transfer inhibitor . Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). [3]

History [ edit ]

The safety and efficacy of cabotegravir/rilpivirine were established through two randomized, open-label, controlled clinical trials (Trial 1/NCT02938520 and Trial 2/NCT02951052) in 1,182 HIV-infected adults who were virologically suppressed (HIV-1 RNA less than 50 copies/milliliter) before initiation of treatment with cabotegravir/rilpivirine. [4] [5] [8] Participants in both trials continued to show virologic suppression at the conclusion of each study, and no clinically relevant change from baseline in CD4+ cell counts was observed. [4] Trials were conducted at 223 sites in 24 countries including the United States. [8]

In Trial 1, participants who were never treated for the infection before, received an approved therapy for 20 weeks. [8] Those who did well after this treatment (who had HIV-1 RNA less than 50 copies/milliliter) were then randomized to receive either cabotegravir/rilpivirine (for the first four weeks they received tablets) or to remain on the same therapy for additional 44 weeks. [8] Participants and the health providers knew which treatments have been given. [8]

In Trial 2, participants who were previously successfully treated for the infection (who had HIV-1 RNA less than 50 copies/milliliter), were randomized to receive either cabotegravir/rilpivirine (for the first four weeks they received tablets) or to remain on the same therapy for additional 44 weeks. [8] Participants and the health providers knew which treatments have been given. [8]

In October 2020, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) recommended the granting of a marketing authorization for rilpivirine and cabotegravir, to be used together for the treatment of people with human immunodeficiency virus type 1 (HIV-1) infection. [13] The two medicines are the first antiretrovirals that come in a long-acting injectable formulation. [13] This means that instead of daily pills, people receive intramuscular injections monthly or every two months. [13] Rilpivirine and cabotegravir were approved for medical use in the European Union in December 2020, as two separate medications. [11] [12]

In January 2021, the U.S. Food and Drug Administration (FDA) granted the approval of Cabenuva to ViiV Healthcare . [4] [8]

The combination was approved for medical use in Australia in February 2021. [14] [15]

Cabotegravir/rilpivirine is not yet available in lower and middle income countries and it is unclear if this will be feasible in the next few years. [16] The first study testing its use in African countries reported positive results in 2024. [17]

References [ edit ]

  1. ^ a b "Cabenuva Product information" . Health Canada . 25 April 2012 . Retrieved 22 January 2021 .
  2. ^ "Summary Basis of Decision (SBD) for Vocabria/Cabenuva" . Health Canada . 23 October 2014 . Retrieved 29 May 2022 .
  3. ^ a b c d e f g h "Cabenuva- cabotegravir and rilpivirine kit" . DailyMed . Retrieved 13 February 2021 .
  4. ^ a b c d e f g h i j "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 . Public Domain This article incorporates text from this source, which is in the public domain .
  5. ^ a b c d "Cabenuva and Vocabria approved for HIV infection" . U.S. Food and Drug Administration (FDA) . 27 January 2021 . Retrieved 27 January 2021 . Public Domain This article incorporates text from this source, which is in the public domain .
  6. ^ a b "ViiV Healthcare announces FDA approval of Cabenuva (cabotegravir, rilpivirine), the first and only complete long-acting regimen for HIV treatment" . ViiV Healthcare. 21 January 2021 . Retrieved 21 January 2021 – via Business Wire.
  7. ^ Howe ZW, Norman S, Lueken AF, Huesgen E, Farmer EK, Jarrell K, et al. (August 2021). "Therapeutic review of cabotegravir/rilpivirine long-acting antiretroviral injectable and implementation considerations at an HIV specialty clinic". Pharmacotherapy . 41 (8): 686?699. doi : 10.1002/phar.2605 . PMID   34130357 . S2CID   235451020 .
  8. ^ a b c d e f g h i j "Drug Trials Snapshot: Cabenuva" . U.S. Food and Drug Administration (FDA) . 20 January 2021 . Retrieved 17 February 2021 . Public Domain This article incorporates text from this source, which is in the public domain .
  9. ^ "Drug Approval Package: Cabotegravir" . U.S. Food and Drug Administration (FDA) . 3 March 2021 . Retrieved 14 September 2021 .
  10. ^ "Janssen Announces European Commission Authorisation of the First Complete Long-Acting Injectable HIV Treatment in Europe" (Press release). Janssen . Retrieved 22 January 2021 – via Business Wire.
  11. ^ a b "Rekambys EPAR" . European Medicines Agency (EMA) . 13 October 2020 . Retrieved 4 January 2021 .
  12. ^ a b c "Vocabria EPAR" . European Medicines Agency (EMA) . 5 January 2021 . Retrieved 5 January 2021 .
  13. ^ a b c d "First long-acting injectable antiretroviral therapy for HIV recommended approval" . European Medicines Agency (EMA) (Press release). 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.
  14. ^ "Australian Public Assessment Report for Cabotegravir sodium and cabotegravir/rilpivirine" (PDF) . Therapeutic Goods Administration (TGA) . Australian Government Department of Health. May 2021.
  15. ^ "TGA eBS - Product and Consumer Medicine Information Licence" .
  16. ^ Pebody R (2 August 2023). "Injectable HIV treatment unlikely to be arriving soon in the global south" . aidsmap . Retrieved 10 March 2024 .
  17. ^ Alcorn K (4 March 2024). "Injectable treatment just as effective as standard HIV combination in Africa" . aidsmap . Retrieved 10 March 2024 .

External links [ edit ]

  • "Cabotegravir" . Drug Information Portal . U.S. National Library of Medicine.
  • "Rilpivirine" . Drug Information Portal . U.S. National Library of Medicine.
  • Clinical trial number NCT02938520 for "Study to Evaluate the Efficacy, Safety, and Tolerability of Long-acting Intramuscular Cabotegravir and Rilpivirine for Maintenance of Virologic Suppression Following Switch From an Integrase Inhibitor in HIV-1 Infected Therapy Naive Participants" at ClinicalTrials.gov
  • Clinical trial number NCT02951052 for "Study Evaluating the Efficacy, Safety, and Tolerability of Switching to Long-acting Cabotegravir Plus Long-acting Rilpivirine From Current Antiretroviral Regimen in Virologically Suppressed HIV-1-infected Adults" at ClinicalTrials.gov
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