Drug name
Last update: Jul 2026Rilpivirine (RPV)
Developer(s)
Drug information
rilpivirine
Edurant, Rekambys, Eviplera/Complera, Odefsey
Small molecule
non-nucleoside reverse transcriptase inhibitor; NNRTI
Rilpivirine (RPV), also known as TMC278, is a HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI). RPV is a derivative of diarylpyrimidine and functions by mechanistically binding to the HIV reverse transcriptase enzyme. This interaction prevents the conversion of RNA into viral DNA, which is an essential step in HIV infection. RPV is available in multiple formulations, including short-acting oral medication (Edurant) and combination tablets (Odefsey, Juluca and Eviplera/Complera), in addition to a long-acting intramuscular injectable (Rekambys). In Jan 2021, Rekambys received U.S. FDA approval to be administered alongside Vocabria (Cabotegravir) for HIV treatment in adults and adolescents weighing 35kg or more.
An injectable long-acting formulation of rilpivirine is approved for HIV treatment, exclusively in combination with long-acting cabotegravir (marketed as Rekambys with Vocabria in the EU/UK, and as the co-packaged product Cabenuva in the USA and Canada). Oral rilpivirine is approved for HIV treatment (Edurant, and within the fixed-dose combinations such as Eviplera/Complera, Odefsey and Juluca). Rilpivirine LA is not approved for pre-exposure prophylaxis; PrEP use has been investigated only in phase I/II studies.
CAB+RPV LA injectable for treatment is recommended by WHO as an alternative switching option for adults and adolescents with undetectable HIV viral load on oral ART and without active hepatitis B infection: https://www.who.int/teams/global-hiv-hepatitis-and-stis-programmes/guidelines
Therapeutic area(s)
- HIV
- Treatment
Administration route
Oral, Intramuscular
Associated long-acting platforms
Aqueous drug particle suspension, Oral solid form
Use of drug
- Administered by a community health worker
- Administered by a nurse
- Administered by a specialty health worker
- Self-administered
- Daily
- Monthly
- Every 2 months
For treatment, the ATLAS and FLAIR trials of CAB+RPV LA showed significantly greater gains in treatment satisfaction and acceptance than daily oral ART, with the large majority of participants preferring injections to their previous oral regimen; injection-site pain and clinic dependence were the recurring concerns. For prevention, HPTN 076 assessed the acceptability of long-acting injectable rilpivirine among US and African women (https://doi.org/10.1002/jia2.25408).
Dosage
Not provided
Not provided
Not provided
Not provided
Not provided
Comment & Information
Developer(s)
Johnson & Johnson
Drug structure
Scale-up and manufacturing prospects
Compound is commercially manufactured.
Netzsch ball mill, high pressure homogenizer.
The manufacturing process for RPV is considered to be non-standard due to the inclusion of an aseptic processing step. RPV is light-sensitive, and exposure to light can induce conversion into a Z-isomer form which can affect pharmacokinetic data and activity. Therefore, all processing, manufacturing and storage stages must implement mitigation procedures and protection from light. The RPV nanosuspension is stored aseptically in single-use glass vials with a protective nitrogen atmosphere. The formulation requires refrigerated storage and is stable for up to three years at 5°C.
Laser diffractor (determine particle size), FT-IR UHPLC (chemical identification), UHPLC (chromatographic purity), paddle apparatus & UPLC/UV (determine in-vitro drug release for QC / dissolution testing).
Excipients
No proprietary excipient used
The novel excipient poloxamer 338 (P338) is used in the final G001 clinical formulation. Following both an in-vitro mammalian chromosome aberration and an Ames test, it was considered to be non-genotoxic with no evidence for mutagenicity. Further P338 fertility, genotoxicity and development studies have been conducted with no negative effects, in addition to a 6-week and 9-month minipig repeat-dose toxicity study. No adverse local or systemic toxicity was reported in the minipigs at 100mg/month (Margin of Exposure:19).
No residual solvent used
Delivery device(s)
Not provided
There are either no relevant patents or these were not yet submitted to LAPaL
Publications
There are no publication
Additional documents
No documents were uploaded
Useful links
There are no additional links
Collaborate for development
Consider on a case by case basis, collaborating on developing long acting products with potential significant public health impact, especially for low- and middle-income countries (LMICs), utilising the referred to long-acting technology
Share technical information for match-making assessment
Provide necessary technical information to a potential partner, under confidentiality agreement, to enable preliminary assessment of whether specific medicines of public health importance in LMICs might be compatible with the referred to long-acting technology to achieve a public health benefit
Work with MPP to expand access in LMICs
In the event that a product using the referred to long-acting technology is successfully developed, the technology IP holder(s) will work with the Medicines Patent Pool towards putting in place the most appropriate strategy for timely and affordable access in low and middle-income countries, including through licensing