Doravirine (MK-1439) is a non-nucleoside reverse transcriptase inhibitor, used in the treatment of HIV/AIDS.

K103N/Y181C:33 nM, Y181C:31nM, Virus (WT):12nM, K103N:21nM

Doravirine 对野生型病毒及K103N、Y181C和K103N/Y181C突变病毒展示出强大的抗病毒活性，其IC50值分别为12、21、31和33 nM。[1] MK-1439 对10种不同HIV-1亚型病毒（共93种病毒）显示出了类似的抗病毒活动。[2]

给予高脂餐后服用50 mg doravirine与轻微提升AUC时间零至无限大（AUC0-∞）和C24 h相关，但Cmax没有变化。同时给予doravirine会轻微减少Midazolam的AUC0-∞（几何平均比率0.82，90% CI 0.70, 0.97）。[3]

FS-3 substrate is solubilized in assay buffer at 500 μM and frozen at -20°C in single-use aliquots for up to 4 weeks. Recombinant autotaxin is diluted in Tris-buffered saline (140 mM NaCl, 5 mM KCl, 1 mM CaCl2, 1 mM MgCl2, 50 mM Tris, pH 8.0) and incubated with compound in DMSO or DMSO alone (final 1% DMSO) for 15 min at 37°C, and the reaction is started with the addition of FS-3 at a final concentration of 1 μM. The reaction is allowed to proceed at 37°C for 30 min and monitored at 520 nm until the uninhibited control compared with a no-enzyme control gave a Z′≥0.5. IC50s are determined in triplicate by using a four-parameter fit[1].