On April 1, 2019 Apollomics, Inc. (the "Company"), an innovative biopharmaceutical company committed to the discovery and development of oncology combination therapies, reported positive data for the Company’s multi-kinase inhibitor, APL-102, as both a single agent and in combination with an anti-PD-1 antibody in multiple preclinical studies (Press release, Apollomics, APR 1, 2019, View Source [SID1234534819]).

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"Our preclinical data presented today demonstrates a mechanism of action for APL-102 anti-tumor activity and a synergistic effect of the agent when combined with a check-point inhibitor (CPI)," said Sanjeev Redkar, PhD, President. "APL-102 treatment increased the total T-cells and the CD8 T-cells, and significantly decreased macrophages in the tumor, both as a single agent and in combination with an anti-PD1 antibody. We see a potential path forward for the agent as a single agent or in combination with CPIs which may improve the efficacy of APL-102 and broaden the efficacy of CPIs."

The studies, in multiple murine models, evaluated the effect of anticancer therapies that target components within the tumor microenvironment (TME) as opposed to the tumor itself. Colony stimulating factor 1 receptor (CSF-1R) was a key target as a means of controlling tumor associated macrophages in the TME. As a monotherapy, the results demonstrated that APL-102 inhibits CSF-1R in a radiometric enzyme activity assay with an IC50 of 43nM, and that APL-102 inhibited growth in cells dependent on CSF1-CSF1R signaling. APL-102 also demonstrated targeting of Vascular Endothelial Growth Factor Receptors (VEGFR) dependent angiogenesis and the Mitogen-Activated Protein Kinases (MAPK) pathway.

When APL-102 was given in combination with an anti-PD1 antibody, the results produced a more robust response than either single agent alone in syngeneic mouse models, which was associated with macrophage inhibition in the TME.

About APL-102

APL-102 is an oral, small molecule multi-kinase Inhibitor targeting several key oncogenic drivers. APL-102 inhibits both receptor tyrosine kinase (RTKs) and serine/threonine-kinases, including: angiogenesis via Vascular Endothelial Growth Factor Receptors (VEGFR) and Platelet-Derived Growth Factor Receptors (PDGFR); Mitogen-Activated Protein Kinases (MAPK) pathway via B-RAF and C-RAF; and, RET, CSF1R, DDR1 (discoidin domain receptor tyrosine kinase 1) and c-KIT. APL-102 is currently in preclinical, IND-enabling studies. The agent has demonstrated broad and potent antitumor activity in patient derived xenografts of liver cancer, breast cancer, colorectal cancer, gastric, esophageal and non-small cell lung cancer models with excellent oral bioavailability, biopharmaceutical properties, and a well-tolerated safety profile in a chronic safety study. Apollomics retains worldwide rights to APL-102.