Mechanism of Action: Dual Antagonist of Inhibitors of Apoptosis Proteins (IAPs) XIAP and cIAP
Indication: Advanced Solid Tumors and Lymphomas
How this therapy can help
Apoptosis or programmed cell death, while part of normal cell behavior, is often altered in cancer cells and can be prevented by overexpression of anti-apoptotic proteins, such as XIAP and cIAP. These IAPs are key regulators of anti-apoptotic and pro-survival signaling pathways and their dysregulation, through overexpression or loss of endogenous antagonists, occurs in various cancers. This is associated with tumor growth, poor prognosis and resistance to treatment, making IAPs attractive targets for anticancer therapy. ASTX660 has a unique IAP antagonist molecular profile, with balanced XIAP and cIAP antagonist activity. Given the importance of XIAP in regulating both extrinsic and intrinsic apoptosis pathways, improved XIAP antagonism, as demonstrated with ASTX660 compared to other IAP antagonists in the clinic, has the potential to result in enhanced pro-apoptotic activity and tumor cell death.
ASTX660 is currently being evaluated in a Phase1/2 study in patients with advanced solid tumors and lymphomas to determine safety, pharmacokinetics and preliminary activity. The Phase 2 portion of the study is currently recruiting patients into two expansion cohorts: Peripheral T-Cell Lymphoma (PTCL) and Cutaneous T-Cell Lymphoma (CTCL).
ASTX660 is also being evaluated in a Phase 1/2 combination study with ASTX727, Astex’s investigational oral hypomethylating agent.
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