Astellas Submits IND Application in China for ASP1570, the First-in-Class DGKζ Inhibitor for Solid Tumors

On March 31, the CDE website showed that Astellas' Category 1 new drug, ASP1570 tablets, was submitted for clinical trial in China for the treatment of solid tumors.

Diacylglycerol Kinase (DGK) is a large enzyme family consisting of 10 mammalian isozymes, which can catalyze the conversion of diacylglycerol (DAG) to phosphatidic acid (PA). In T cells, DGK subtypes such as DGKζ can inhibit DAG-mediated signaling, thereby preventing T cell overactivation. Therefore, inhibiting DGK has the potential to enhance downstream DAG signaling and activate T cells.

ASP1570 is a novel DGKζ inhibitor with the potential to enhance DAG downstream signaling pathways, activate T cells independently of the PD-1 signaling pathway, and thereby strengthen tumor-killing effects. Preclinical studies have shown that ASP1570 can restore T-cell function suppressed by multiple immunosuppressive signals (PD-1, transforming growth factor β, prostaglandin E2, and adenosine) and induce tumor growth inhibition in MC38 (anti-PD-1 sensitive) and B16-F1 (tumor-infiltrating lymphocyte-depleted, anti-PD-1 insensitive) mouse models.

Astellas has initiated an open-label, multi-center, multi-dose, dose escalation/expansion Phase I/II study of ASP1570 in patients with locally advanced or metastatic solid tumors. The study will enroll approximately 168 subjects to evaluate safety, tolerability, efficacy, pharmacokinetics, and pharmacodynamics.

In addition to Astellas, Bayer also has a DGKζ inhibitor in its pipeline, which has entered Phase I clinical trials. Currently, no companies in China have布局this target.

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