Conference Reports for NATAP

XVII International HIV Drug Resistance Workshop June 10-14, 2008 Sitges, Spain Back

Hexadecyloxypropyl Tenofovir (CMX157) Has Enhanced Potency in Vitro against NRTI Resistant HIV Relative to Tenofovir and a Favorable Preclinical Profile       Reported by Jules Levin 17th Intl HIV Drug Resistance Workshop June 10-12, 2008 Sitges, Spain   Randall Lanier, PhD Chimerix Inc, Research Triangle Park, NC, USA   AUTHOR SUMMARY/CONCLUSIONS   CMX157 is >300 fold more potent than TFV (tenofovir) in vitro against wt (wild-type) and clinically relevant HIV mutants   The amount of active drug produced in human PBMCs is much higher following exposure to CMX157 vs TFV   Toxicology and TK data reveal high exposure to CMX157 in plasma with minimal toxicity   Activity of CMX157 against HIV   CMX157 IC50s against HIV-1 subtypes (A-G,O) ranged from <1 to 7 nM -- TFV IC50s against HIV-1 subtypes (A-G,O) ranged from 1600 to 4900 nM1   IC50s against NRTI resistant HIV ranged from <1-57 nM -- median of 359-fold more potent than TFV (range 295-472)