MK 1439

Doravirine是一种新型的非核苷的HIV- 1逆转录酶抑制剂.

Doravirine的生物活性

Doravirine is a novel non-nucleoside inhibitor of HIV-1 reverse transcriptase with potent activity against wild-type virus (95% inhibitory concentration 19 nM, 50% human serum).
target:HIV [1]
In  vitro: Doravirine exhibits potent antiviral activity against wild-type virus and K103N, Y181C, and K103N/Y181C mutant viruses, with IC50 value of 12, 21, 31, and 33 nM, respectively. [1]  MK-1439 exhibited similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses).[2]
In vivo: Administration of 50 mg doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity (AUC0-∞) and C24 h with no change in Cmax. Midazolam AUC0-∞ is slightly reduced by coadministration of doravirine (geometric mean ratio 0.82, 90% CI 0.70, 0.97). [3]