tasquinimod

Tasquinimod is an orally active small molecule and a second-generation quinoline-3-carboxamide linomide analogue with antiangiogenic, immunomodulatory, and potential antineoplastic activities. It targets the tumor microenvironment by modulating immunosuppressive myeloid cells (notably myeloid-derived suppressor cells and tumor-associated macrophages), inhibiting their pro-tumorigenic, pro-metastatic, and pro-angiogenic functions. Tasquinimod binds to the S100A9 protein, blocking its interaction with receptors such as TLR4 (Toll-like receptor 4) and RAGE (receptor for advanced glycation end products), thereby reducing immunosuppression in the tumor milieu. It also inhibits histone deacetylase 4 (HDAC4), leading to reduced expression of hypoxia-inducible factor 1-controlled genes involved in angiogenesis. Tasquinimod has been investigated primarily for prostate cancer (including castration-resistant prostate cancer) but development was discontinued after phase III due to lack of overall survival benefit despite improved progression-free survival. Ongoing clinical development focuses on blood cancers such as multiple myeloma and myelofibrosis[1][3][4][5][6][7].

Other names

tasquinimod