Breakthrough Design of Highly Potent Antivirals Against Wild-Type HIV-1 and Lenacapavir-Resistant M66I Variant.
Lenacapavir (LEN), the first-in-class HIV-1 capsid inhibitor (CAI) with picomolar potency and long pharmacokinetics (PK), is approved for both treatment and pre-exposure prophylaxis (PrEP). However, the frequently selected M66I mutation confers complete resistance to LEN. Potent antivirals against the M66I variant rema...