OTX-008

OTX-008 is a calixarene-based small molecule inhibitor of galectin‑1 (Gal1), a carbohydrate-binding protein implicated in cancer cell proliferation, invasion, angiogenesis, and immune evasion. By binding to Gal1, OTX‑008 induces its oxidation and proteasomal degradation, leading to downregulation of Gal1 expression. This results in decreased tumor cell growth and inhibition of angiogenesis. Preclinical studies have shown that OTX‑008 inhibits proliferation and invasion of various human cancer cell lines at micromolar concentrations, with effects correlating to Gal1 expression levels. In vivo models demonstrated antitumor activity through reduced tumor growth, microvessel density, and VEGFR2 expression. The drug was originally discovered by University of Minnesota and PepTx, later licensed to OncoEthix (acquired by Merck Sharp & Dohme). It has been investigated primarily for the treatment of solid tumors[4][5][6][7].

Other names

Calixarene 0118Calixarene0118Calixarene-0118PTX-008PTX008PTX 008KM-0118KM0118KM 0118