NVP-AUY922 is a resorcinol-based, intravenous or intraperitoneal Phase II clinical trial HSP90 inhibitor with a Kd of 1.7 nM. It inhibits tumor cell proliferation at GI50 values of 2-40 nM, inducing G1-G2 arrest and apoptosis. [1] Daily dosing of NVP-AUY922 (50 mg/kg, iv or ip) produced statistically significant tumor inhibition or regression (treated/control) in BT474 breast, 21%; A2780 ovarian, 11%; U87MG glioblastoma, 7%; PC3 prostate, 37%; and WM266.4 melanoma, 31%. [1]

Pharmacodynamically, NVP-AUY922 induces HSP70 and depletes ERBB2, CRAF, CDK4, phospho-AKT/TotalAKT, and HIF-1a.