CFT7455 is an orally bioavailable MonoDAC™ degrader (or monofunctional degradation activating compound) of IKZF1 (Ikaros) and IKZF3 (Aiolos) currently in a Phase 1/2 clinical trial for the treatment of multiple myeloma and non-Hodgkin’s lymphomas. We designed CFT7455 to bind with high affinity to the E3 ligase adapter protein, Cereblon, to target and degrade IKZF1/3, key proteins for multiple myeloma and non-Hodgkin’s lymphomas. In early clinical data, CFT7455 demonstrated deep and durable degradation of IKZF1/3.

Opportunity for Targeted Protein Degradation

IKZF1/3 are transcription factors required for cancer cell growth and survival in multiple myeloma and non-Hodgkin’s lymphomas. However, transcription factors do not have an active site binding pocket; this means inhibitors cannot target these important proteins. Rather, degraders are the only therapeutic approach. Today, approved IKZF1/3 degraders (lenalidomide and pomalidomide) are widely used in multiple myeloma treatment, but there remains a high unmet medical need for therapies to treat relapsed/refractory multiple myeloma.

Scientific Presentations and Publications