Delavirdine (mesylate)

Delavirdine (U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC₅₀=0.26 μM) over DNA polymerase α (IC₅₀=440 μM) and polymerase δ (IC₅₀>550 μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs^[1]. IC50 & Target: IC50: 0.26 μM (HIV-1 RT); 440 μM (DNA polymerase α); >550 μM (DNA polymerase δ)^[1] In Vitro: Delavirdine has an 50% cytotoxicity at concentrations >100 μM in H9 and PBMC cultures.Delavirdine has low cellular cytotoxicity, causing less than 8% reduction in peripheral blood lymphocyte viability at 100 μM^[1].
Delavirdine inhibits HIV-1 reverse transcriptase (RT) wild type with an IC₅₀ value of 0.26 μM, and it inhibits Y181C-substituted RT and K103N-substituted RT with IC₅₀ values of 8.32 uM and 7.7 uM, respectively^[1].
In Vivo: Delavirdine (U 90152) mesylate (oral gavage; 10 mg/kg, 200 mg/kg, 250 mg/kg; single dose) is absorbed and metabolized rapidly, that it constitutes a minor component in circulation, that its pharmacokinetics are nonlinear, and that its metabolism to desalkyl delavirdine is capacity limited or inhibitable in CD-1 mice (PK study)^[1].