PEN-866

PEN-866 is a small molecule drug conjugate (SMDC), also referred to as a miniature drug conjugate, developed by Tarveda Therapeutics. It is designed to selectively target and bind to the activated form of Heat Shock Protein 90 (HSP90), a molecular chaperone that is highly expressed and in an activated state within the tumor microenvironment. The conjugate consists of an HSP90-binding ligand linked to a cytotoxic payload, SN-38, which is the active metabolite of the topoisomerase 1 inhibitor irinotecan. Upon binding to HSP90 within tumor cells, PEN-866 releases SN-38, leading to DNA damage and apoptosis. This targeting strategy is intended to enhance the therapeutic index of SN-38 by increasing its concentration and retention within tumors while reducing systemic exposure. PEN-866 is currently being investigated in Phase 1/2 clinical trials, including a study sponsored by the National Cancer Institute (NCI) evaluating its safety and efficacy in combination with vincristine and temozolomide for adolescents and young adults with relapsed or refractory solid tumors, specifically Ewing sarcoma and rhabdomyosarcoma.

Other names

HSP90-SN38 conjugateHSP-90-SN38 conjugateHSP 90-SN38 conjugate