NTS231

NTS231 is a novel small molecule drug candidate being developed by Nutshell Therapeutics for the treatment of solid tumors characterized by aberrant NRF2 activation. The compound functions as a covalent allosteric molecular glue that stabilizes the interaction between the KEAP1-CUL3 E3-ligase complex and the transcription factor NRF2, leading to the selective degradation of NRF2. In many cancers, constitutive NRF2 activation provides a survival advantage to tumor cells and promotes resistance to chemotherapy and radiotherapy; by inducing NRF2 degradation, NTS231 aims to inhibit tumor growth and overcome therapy resistance. The drug is currently in the IND-enabling stage of development.