American Association for Cancer Research (AACR) Annual Meeting 2021 had been held in a virtual format on April 10-15, 2021. At the meeting, Zenshine Pharma disclosed three anti-cancer programs in its pipeline as shown below:
ZX-101A, a next generation PI3Kδ/γ inhibitor, was Zenshine’s 1st program to enter the clinical stage. Its IND was approved in June 2020 and phase I clinical trial is ongoing in the United States. Preclinical animal models demonstrated ZX-101A’s superior efficacy in both blood cancers and solid tumors with improved safety margin and preliminary phase 1 result showed that ZX-101A is well tolerated. The IND application in China will be submitted in the second quarter of 2021.
ZX-4081 is a highly selective PI3Kγ inhibitor with an IC50 of 1.5 nM and greater than 1000-fold selectivity over the other isoforms (α, β, and δ) in biochemical assay. ZX-4081 has a significant inhibitory effect on PI3Kγ-AKT activation by down-regulating the T308 and S473 phosphorylation in a time-dependent and dose-dependent manner. Additionally, ZX-4081 could effectively facilitate macrophage polarization toward M1-like phenotype and reduce both IL-10 protein and mRNA levels in M2-like macrophages. In animal models, ZX-4081 showed significant single agent effect, and tumor growth inhibition (TGI) could reach 95% when combined with immune checkpoint inhibitors (ICIs). IND application will be filed to FDA in the second quarter of 2021.
A series of novel ENPP1 inhibitors was discovered through rational design and lead optimization. ENPP1 inhibitors block the hydrolysis of 2’3’-cGAMP by ENPP1, subsequently activating STING pathway. Indirect activation of STING pathway by ENPP1 inhibition has the potential to reduce side effects of direct STING activators and improve the antitumor effect through multiple mechanisms. In a CT26 syngeneic mouse model, treatment of ZXP-8202 achieved 70% tumor growth inhibition (TGI). No body weight loss was observed during treatment.
About Zenshine Pharma
Zenshine is a clinical stage biopharmaceutical company, focused on small molecule therapeutics in the areas of cancer, viral infection and inflammation. Our mission is to apply the best science to serve patients. Zenshine leverages the team’s extensive expertise and experience in developing proprietary chemical entities with well-defined differentiation to benefit the patients. By targeting key biological pathways to disrupt virus replication, directly block tumor growth and enhance anti-tumor immune responses, Zenshine commits to providing bench-side to bed-side solutions and delivering the best-in-class or first-in-class therapeutics.
The American Association for Cancer Research (AACR) is the first and largest cancer research organization dedicated to accelerating the conquest of cancer. Covering the most cutting-edge advances and regarded globally as the very pinnacle of cancer research, the AACR Annual Meeting is one of the largest and most anticipated scientific events in the cancer research field globally.