HIV protease inhibitors are among the most powerful drugs in suppressing HIV
in human patients. However, HIV developed resistance to all protease inhibitor
drugs so far marketed or used in clinical trials. HIV generates resistance by mutating
its protease. The strains of HIV containing mutant proteases less vulnerable to
inhibitor drug are able to replicate better and maintain the infection. No effective
principle exists for the design of resistance-proof HIV protease inhibitors (HIVPr).
A new inhibitor has been developed based on a new concept for designing resistance
invulnerable HIVPr inhibitors. In vitro data have shown that this inhibitor is
effective against many known HIVPr mutants resistant to other HIVPr inhibitor drugs.
The new concept is, therefore, generally applicable for the design of other resistance
invulnerable HIVPr inhibitor drugs.