ChemoCentryx Identifies Novel Orally Administered Immune Checkpoint Inhibitor CCX559 for Next Generation Cancer Treatment

-- Study to be presented at American Association for Cancer Research (AACR) meeting showed the Company’s orally administered small molecule checkpoint inhibitors led to marked inhibition of PD-1/PD-L1 interaction and signaling in vitro and potent anti-tumor effects in animal models --

MOUNTAIN VIEW, Calif., June 24, 2020 (GLOBE NEWSWIRE) -- ChemoCentryx, Inc., (NASDAQ: CCXI) today announced that it has identified an orally administered checkpoint inhibitor, CCX559, and plans to initiate clinical development in the first half of 2021. Data to be presented on Wednesday, June 24 at 10:35 a.m. ET, during the virtual meeting of the American Association for Cancer Research (AACR), showed that the Company’s optimized checkpoint inhibitors led to marked inhibition of the PD-1/PD-L1 interaction and signaling in vitro and potent anti-tumor effects in animal models.

“Our new highly-potent, highly-specific orally administered checkpoint inhibitor furthers the Company’s aim to advance novel medications that offer precise modes of action with convenient dosing and favorable safety for patients in need,” said Thomas J. Schall, Ph.D., President and Chief Executive Officer of ChemoCentryx. “Beyond ease of use, our orally administered small molecule approach provides flexibility in dosing schedules to more specifically fine tune checkpoint inhibition to combat tumors and avoid side effects. We believe this approach may more effectively penetrate the tumor microenvironment as well, allowing us to target certain cancers that antibodies can't reach. Finally, we see potential for CCX559 as both a monotherapy or as a complement to antibody therapy regimens. We plan to advance CCX559 into clinical development in the first half of 2021, furthering our long-term goal of becoming a fully-integrated pharmaceutical company, driving revenue and re-investing in our pipeline.”

The PD-1/PD-L1 pathway protects tumor cells from the immune system’s cancer-fighting activity. Inhibition of PD-L1 has the potential to prevent PD-1 binding to PD-L1, thereby exposing tumor cells to the full force of the immune system’s anti-tumor response.

ChemoCentryx optimized several small molecule PD-L1 inhibitors it designed to disrupt the interaction of PD-1 with PD-L1. Active compounds were found to be highly potent in several functional cell-based assays, a mixed lymphocyte reaction (MLR) assays, and by human peripheral blood mononuclear cell (PBMC)-mediated tumor cell killing assessments. Potential clinical candidate compounds were selected for potency and oral bioavailability and were evaluated in vivo using murine tumor models. Assessment of the tumor microenvironment demonstrated that the lead compounds almost completely blocked the interaction of PD-L1 on tumor cells with PD-1 on immune effector cells, thus enhancing the immune responses against tumor. Importantly, the in vivo anti-tumor effects of ChemoCentryx’s small molecules were consistently as good or better than the antibody therapeutics to the PD-1/PD-L1 pathway in these models.