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Drug intelligence / Profile preview
rilpivirine long-acting (Tibotec)
- Development stage
- Unknown
- Lead developer
- Johnson & Johnson
- Modality
- Small Molecules
- Administration
- Intramuscular
01
Overview
Rilpivirine long-acting (TMC278 LA) is a nanosuspension formulation of rilpivirine, a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV-1 infection. This long-acting injectable formulation was developed to allow for monthly or quarterly dosing regimens, providing sustained drug release over extended periods. The nanosuspension consists of tiny drug crystals suspended in a liquid, enabling the medication to remain active longer in the body. Rilpivirine shows potent antiviral activity against wild-type HIV-1 group M isolates with EC50 values of 0.07 to 1.01 nM and against group O isolates with EC50 values of 2.88 to 8.45 nM. It maintains effectiveness against many HIV-1 strains resistant to first-generation NNRTIs.
- Brand names
- EdurantRekambys
- Other names
- RPV LA
02
Targets
POLA1 (DNA polymerase alpha)POLB (DNA polymerase beta)POLG (Mitochondrial DNA polymerase gamma)Human immunodeficiency virus type 1 reverse transcriptaseKCNH2 (Voltage-gated potassium channel subfamily H member 2)
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