Rilpivirine
Clinical data | |
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Trade names | Edurant, Rekambys |
Other names | TMC278 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a611037 |
License data |
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Pregnancy category |
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intramuscular | |
ATC code | |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Protein binding | 99.7% |
Metabolism | CYP3A4 |
Elimination half-life | tablets: 45 hours injection: 13–28 weeks |
Excretion | 85% via faeces, 6% via urine |
Identifiers | |
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JSmol) | |
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Rilpivirine, sold under the brand names Edurant and Rekambys, is a
Medical uses
In the US, rilpivirine is approved for treatment-naive patients with a viral load of 100,000 copies/mL or less at therapy initiation. It has to be combined with other drugs against HIV.[9]
In the European Union, rilpivirine is approved in combination with
Available forms
The drug is available as tablets (brand name Edurant) and as a long-acting intramuscular injection to be given once every month or every two months (Rekambys). Before using the injection, the tablets are given for about four weeks to assess tolerability.[9][11]
Contraindications and interactions
The drug is contraindicated for use with drugs that
It is also contraindicated in combination with
Adverse effects
The most common side effects of the injectable formulation are 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 (under 10%) are
Pharmacology
Mechanism of action
Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI).[13]
Pharmacokinetics
When taken by mouth, rilpivirine reaches highest levels in the blood plasma after about four to five hours. Taking the drug without food lowers its plasma levels by 40% as compared to taking it with food, which is considered to be clinically relevant. Therefore, patients are advised to take the medication together with a meal.[13] After injection into the muscle, the substance reaches highest plasma levels after three to four days.[11]
Independently of the mode of application, rilpivirine is almost completely bound to
Elimination has only been studied for oral administration: Most of the drug is excreted via the faeces (85%), partly in unchanged form (25%), partly in form of its metabolites (60%). A minor amount is excreted via the urine (6%), almost exclusively as metabolites.[11][13]
Fixed-dose combinations
A
A fixed-dose medication combining rilpivirine with emtricitabine and
Dolutegravir/rilpivirine, sold under the brand name Juluca, is a fixed-dose combination antiretroviral medication for the treatment of HIV/AIDS. It was approved for use in the United States in November 2017 and for use in the European Union in May 2018.
In January 2021, the U.S. Food and Drug Administration (FDA) approved cabotegravir/rilpivirine (brand name Cabenuva) for the treatment of HIV-1 infections 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 and with no known or suspected resistance to either cabotegravir or rilpivirine.[20][21] This is the first FDA-approved injectable, complete regimen for HIV-infected adults that is administered once a month.[20][21] The label for rilpivirine tablets was revised to reflect the oral lead-in recommendations for use with cabotegravir.[21]
Chemistry
Like
The tablets contain rilpivirine hydrochloride,[13] while the injection contains free rilpivirine.[11]
History
Rilpivirine entered
On 15 October 2020, the
References
- ^ "Edurant 25 mg tablets - Summary of Product Characteristics (SmPC)". (emc). 21 January 2020. Retrieved 4 January 2021.
- ^ "Edurant- rilpivirine hydrochloride tablet, film coated". DailyMed. Retrieved 4 January 2021.
- ^ "Edurant EPAR". European Medicines Agency (EMA). Retrieved 4 January 2021.
- ^ a b c "Rekambys EPAR". European Medicines Agency (EMA). 13 October 2020. Retrieved 4 January 2021.
- ^ "TMC278 — A new NNRTI". Tibotec. Archived from the original on 2008-12-20. Retrieved 2010-03-07.
- PMID 17933730.
- S2CID 26078073.
- ^ Pozniak A, Morales-Ramirez J, Mohap L, et al. "48-Week Primary Analysis of Trial TMC278-C204: TMC278 Demonstrates Potent and Sustained Efficacy in ART-naïve Patients. Oral abstract 144LB". 14th Conference on Retroviruses and Opportunistic Infections. Archived from the original on October 19, 2007.
- ^ a b c d e Rilpivirine Monograph. Accessed 2021-02-23.
- ^ a b "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.
- ^ a b c d e f "Rekambys: EPAR – public assessment report" (PDF). European Medicines Agency. 2021-02-22.
- ^ "Vocabria: EPAR – Product information" (PDF). European Medicines Agency. 2021-01-05.
- ^ a b c d e f g h "Edurant: EPAR – public assessment report" (PDF). European Medicines Agency. 2021-01-04.
- PMID 23917319.
- ^ "Approval of Complera: emtricitabine/rilpivirine/tenofovir DF fixed dose combination". U.S. Food and Drug Administration (FDA). August 10, 2011.
- ^ "Eviplera". Aidsmap. Retrieved September 1, 2014.
- ^ Haberfeld H, ed. (2021). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag. Eviplera Filmtabletten.
- S2CID 7313885.
- ^ "Odefsey (emtricitabine, rilpivirine, and tenofovir alafenamide) Tablets". U.S. Food and Drug Administration (FDA). 29 November 2016. Retrieved 23 January 2021.
- ^ a b "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.
- ^ a b c "Cabenuva and Vocabria approved for HIV infection". U.S. Food and Drug Administration (FDA). 27 January 2021. Retrieved 27 January 2021. This article incorporates text from this source, which is in the public domain.
- ^ "A Clinical Trial in Treatment naïve HIV-1 Patients Comparing TMC278 to Efavirenz in Combination With Tenofovir + Emtricitabine". ClinicalTrials.gov. National Institutes of Health. October 25, 2012. Retrieved January 1, 2014.
- ^ "A Clinical Trial in Treatment naïve HIV-Subjects Patients Comparing TMC278 to Efavirenz in Combination With 2 Nucleoside/Nucleotide Reverse Transcriptase Inhibitors". ClinicalTrials.gov. National Institutes of Health. May 14, 2012. Retrieved January 1, 2014.
- ^ "Drug Approval Package: Edurant (rilpivirine) NDA #202022#". U.S. Food and Drug Administration (FDA). 20 August 2013. Retrieved 23 January 2021.
- ^ "FDA approves new HIV treatment" (Press release). U.S. Food and Drug Administration (FDA). Archived from the original on 2017-01-18. Retrieved 2011-05-20.
- ^ "Rekambys: 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.
External links
- "Rilpivirine". Drug Information Portal. U.S. National Library of Medicine.
- "Rilpivirine hydrochloride". Drug Information Portal. U.S. National Library of Medicine.