molecules of the month


oral IKZF2-selective molecular glue degrader

Ph. I/Ib for adv. solid tumors

opt. of pomalidomide analog

Cell Chemical Biology, March 1, 2023

Novartis, Cambridge, MA

DKY709, oral IKZF2-selective molecular glue degrader, Ph. I/Ib for adv. solid tumors, opt. of pomalidomide analog, Cell Chemical Biology, March 1, 2023, NOVARTIS, CAMBRIDGE, MA
7 mins read

A Treg-modulating IKZF2 (Helios) glue degrader for cancer immunotherapy. Tumors can evade the immune system through the recruitment of regulatory T cells (Treg) which limit the activation and expansion of effector T cells (Teff). IKZF2 (Helios) is an Ikaros transcription factor family member that is expressed in a majority of Treg cells. NVP-DKY709 is a first-in-class selective molecular glue degrader of IKZF2 that makes Treg cells less immunosuppressive and Teff cells more active in vitro, while completely sparing the traditional pomalidomide targets IKZF1/3 from degradation. It has demonstrated significant and sustained IKZF2 degradation in a Ph. I clinical trial (NCT03891953, not recruiting) and was intended to be studied in combination with PD-1 antibody, spartalizumab in NSCLC or melanoma patients who…

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