ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).

cIAP, XIAP^[1]

ASTX660 is an orally bioavailable dual antagonist of cIAP and XIAP, currently being investigated in a single-agent Phase 1/2 clinical trial in patients with advanced solid tumors and lymphomas. Twenty-one triple-negative breast cancer (TNBC) cell lines are treated with ASTX660 in vitro and it is found that 43% are sensitive to ASTX660^[1].

In HCC1806 xenografts in mice, ASTX660 (daily oral treatment) causes moderate tumor growth inhibition but not regression^[1].

• [1]. Tomoko Smyth, et al. Abstract 1287: The dual IAP antagonist, ASTX660, increases the anti-tumor activity of paclitaxel in preclinical models of triple-negative breast cancer in vivo. Cancer Res 2016;76(14 Suppl).