product name Etravirine (TMC125)
Description: Etravirine (also known as TMC125 and R 165335, ) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV. It was also approved in 2008. Etravirine, in combination with other anti-retrovirals, is indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in antiretroviral treatment-experienced adult patients, who have evidence of viral replication and HIV-1 strains resistant to a NNRTI and other antiretroviral agents.
References: J Med Chem. 2004 May 6;47(10):2550-60; Antimicrob Agents Chemother. 2004 Dec;48(12):4680-6.
435.28
Formula
C20H15BrN6O
CAS No.
269055-15-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 42 mg/mL (96.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
R-165335
other peoduct :
| In Vitro |
In vitro activity: Etravirine (TMC125), is highly active against wild-type HIV-1 with EC50 of 1.4 nM to 4.8 nM and shows some activity against HIV-2 with EC50 of 3.5 μM. TMC125 also inhibits a series of HIV-1 group M subtypes and circulating recombinant forms and a group O virus. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Etravirine has a high genetic barrier to the development of resistance. In phase IIb trials in treatment-experienced patients, including those infected with virus resistant to NNRTIs and protease inhibitors (PIs), TMC125 is active against HIV resistant to currently available NNRTIs, with a similar tolerability profile to that of the control group. |
| Animal model | |
| Formulation & Dosage | |
| References | J Med Chem. 2004 May 6;47(10):2550-60; Antimicrob Agents Chemother. 2004 Dec;48(12):4680-6; Lancet. 2007 Jul 7;370(9581):39-48. |
