NVP-AUY922 is a potent inhibitor of heat shock protein 90 (Hsp90), a molecular chaperone involved in the stabilization and function of various client proteins that play critical roles in cell signaling, proliferation, and survival. By inhibiting Hsp90, NVP-AUY922 promotes the degradation of these client proteins, many of which are oncogenic and implicated in cancer progression. It has been primarily investigated for its antitumor activity in preclinical and clinical studies, particularly in cancers dependent on Hsp90 client proteins such as HER2, AKT, BRAF, and mutant p53. It shows promise in treating solid tumors including breast cancer, melanoma, and non-small cell lung cancer. Its mechanism leads to cell cycle arrest and apoptosis in cancer cells, especially under conditions of cellular stress. NVP-AUY922 has also been studied in combination with other anticancer agents, where it enhances the efficacy of chemotherapy, targeted therapy, and hormone therapy by overcoming resistance mechanisms mediated through Hsp90-dependent protein stability. Due to its ability to simultaneously disrupt multiple signaling pathways involved in tumor growth, it represents a multi-targeted approach in oncology drug development.