AVS100

AVS100 is a highly selective, orally bioavailable small molecule inhibitor of histone deacetylase 6 (HDAC6), developed by Avstera Therapeutics for the treatment of locally advanced or metastatic solid tumors. It is designed to be used as monotherapy or in combination with PD-1 inhibitors such as pembrolizumab. Mechanistically, AVS100 inhibits HDAC6 activity and suppresses the polarization of tumor-associated macrophages toward pro-tumoral (M2) phenotypes while promoting anti-tumoral (M1) macrophage responses within the tumor microenvironment. This immunomodulatory effect enhances T cell infiltration and effector function in tumors. Preclinical studies have demonstrated that AVS100 reduces tumor growth and increases the M1/M2 macrophage ratio without significant mutagenicity or cardiotoxicity. The drug has received FDA Orphan Drug Designation for advanced stage melanoma and has IND clearance to begin Phase Ia/b clinical trials targeting solid tumors[1][5][6][7][8].

Other names

5-[2-[(3,4-dichlorobenzoyl)amino]ethyl]-N-hydroxy-3-isoxazolecarboxamide