Aculeus Therapeutics ENPP1 inhibitor

Aculeus Therapeutics is developing a small molecule inhibitor of ecto-nucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) for the treatment of various cancers. ENPP1 is a cell-surface enzyme that plays a critical role in immune regulation by degrading cyclic GMP-AMP (cGAMP), which is a natural ligand and activator of the Stimulator of Interferon Genes (STING) pathway. By inhibiting ENPP1, the drug prevents the breakdown of cGAMP within the tumor microenvironment, thereby promoting STING-mediated innate immune activation, the production of Type I interferons, and the subsequent recruitment of T cells to the tumor. This program was in-licensed from the CRC for Cancer Therapeutics in 2020 and is currently in the hit-to-lead stage of preclinical development, intended for use as a monotherapy or in combination with other standard-of-care treatments like chemotherapy or radiation.

Other names

ENPP1 inhibitorENPP-1 inhibitorENPP 1 inhibitor