Oral DGKα Inhibitor

Enhances Anti-PD-1

Unlike existing DGKα inhibitors, this compound combines high kinase selectivity, favorable ADME properties, and oral bioavailability, enabling robust in vivo antitumor activity in combination with anti-PD-1.

Ding, Xiao · Aliper, Alexander M. · Ren, Feng · Zhavoronkov, Alex A.

Journal of Medicinal Chemistry 2025

Advantages

Novel DGKα inhibitor with excellent kinase selectivity

Orally bioavailable

Robust in vivo antitumor activity in combination with anti-PD-1