Abstract
New Drugs by Class
NRTI:
Tenofovir alafenamide fumarate (TAF) is the pro-drug of tenofovir with advantages of slight increase activity and reduced renal/bone toxicity. The phase 2 trial (Zolopa A. 2012 CROI, Abstr 99LB) compared TAF vs. another TDF prodrug (TFV, each with EFV, COBI/FTC in 170 treatment naïve patients. At 24 weeks both groups achieved VL <50 c/mL; TAF showed better renal and bone safety.
InSTI:
Dolutgravir (DTG)—New once daily DTG/2NRTIs that shows potency with good activity vs. RAL-resistant strains.
• S/GSK 1265-744 (˙744”): This is a next generation InSTI with a T1/2 of 21-50d!
NNRTI:
MK1439—This new potent NNRTI showed exceptional potency with 25 mg monotherapy once daily (Anderson M, 2013 CROI; Abstr. 100).
• RPV-LA: A novel nanosuspension of RPV with steady state release after 600 mg given SC or IM every 3 months.
Entry Inhibitors:
Cenicriviroc (CVC) antagonizes CCR5 receptor, but also CCR-2 receptors to possibly reduce immune activation. ART activity is comparable to EFV.
• BMS 663068 (or BMS 068): This is a prodrug of BMS-529 that binds gp125 to prevent HIV binding to CD4 cells. A small trial showed 42 of 48 treatment-naïve patients responded; the 6 exceptions had a genetic factor that accounted for nonresponse.
Pharmacoenhancer:
Cobicistat (COBI) is a potential substitute for RTV to boost ARVs and is already FDA-approved in combination as EVG/COBI/TDF/FTC.