DP-053

DP-053 is a deuterated S-enantiomer of lenalidomide, a small molecule immunomodulatory drug (IMiD) developed for the treatment of hematologic malignancies. Lenalidomide naturally exists as a racemic mixture that undergoes rapid chiral inversion in vivo. DP-053 utilizes deuterium-enabled chiral switching (DECS) technology to stabilize the S-enantiomer against epimerization, potentially enhancing its pharmacokinetic profile and therapeutic index. Mechanistically, DP-053 acts as a molecular glue by binding to the E3 ubiquitin ligase cereblon (CRBN), which triggers the selective ubiquitination and proteasomal degradation of the lymphoid transcription factors IKZF1 (Ikaros) and IKZF3 (Aiolos). This degradation leads to the inhibition of malignant cell growth and modulation of the immune system. The compound was originally developed by Deuteria Pharmaceuticals and was acquired by Celgene (now Bristol Myers Squibb) in 2012.

Other names

deuterated S-lenalidomideS-lenalidomide-d