Rilpivirine HCl (TMC278; DB08864)

Description: Rilpivirine HCl (formerly known as R278474 HCl; TMC278; DB08864), an approved HIV drug, is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that has been widely used for the treatment of HIV-1 infection. Rilpivirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and reduced side-effect profile compared with older NNRTIs, such as efavirenz. Rilpivirine showed inhibitory activities to both wild-type HIV (with EC50 value of 0.51 nM) and NNRTI-resistant strains. The conformational flexibility of rilpivirine allowed it to adjust different mutations of the reverse transcriptase. For the singly mutant HIV strains such as L100I, G190S, G190A and V106A, rilpivirine showed higher retained potency than efavirenz and low EC50 values blow 1 nM.

References: J Med Chem. 2005 Mar 24; 48(6):1901-9; Antimicrob Agents Chemother. 2010 Feb; 54(2):718-27.

Related CAS: 700361-47-3 (HCl); 500287-72-9 (free base)