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02451 MIV-150, A POTENT HIV-1 INHIBITOR SUITABLE FOR USE IN MICROBICIDES Öberg, Bo*# MIV-150 is a non nucleoside reverse transcriptase inhibitor (NNRTI) with a tight binding to HIV reverse transcriptase. This results in an inactivation of free virus particles as well as an inhibition of HIV replication at low nanomolar concentrations. MIV-150 is a more potent inhibitor that sustiva of NNRTI resistant mutants also in the presence of human serum. The rate of in vitro resistance development to MIV-150 is 3 times slower than to sustiva. MIV-150 has shown a potent activity against SHIV in monkeys and prevented infection when dosed after SHIV inoculation and showed a good profile in preclinical safety and toxicology. A phase I clinical study showed a low oral bioavailability. Taken together these results strongly indicate the use of MIV-150 in a topical microbicide and combination studies with carraguard has shown synergy in vitro. Professor Bo Öberg |
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