MK-6186

Description

MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants K103N and Y181C . MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants Y188L and V106I/Y188L show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most 70 % viruses show more than 10-fold resistance to efavirenz EFV , while only 29 % of mutant viruses show more than 10-fold resistance to MK-6186.