Astellas' DGKζ Inhibitor ASP1570 Granted IND Approval in China for Locally Advanced or Metastatic Solid Tumors

On June 9, the CDE website showed that Astellas' ASP1570 tablet was approved for clinical use in patients with locally advanced or metastatic solid tumors. This is the first DGKζ inhibitor to be approved for clinical trials in China.

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 overactivation of T cells. Therefore, inhibiting DGK has the potential to enhance downstream DAG signaling, activate T cells, and exert antitumor effects.

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 enhance 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.

Currently, Astellas is conducting an expanded Phase I/II clinical trial of ASP1570 abroad for patients with locally advanced or metastatic solid tumors. This is an open-label, multi-center, multi-dose, dose-escalation Phase I/II clinical trial designed to evaluate the safety, tolerability, efficacy, pharmacokinetics, and pharmacodynamics of ASP1570.

According to the NextPharma database by PharmaCube, Bayer also has a DGKζ inhibitor, BAY 2965501, under development, currently in Phase I clinical trials.

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