APL-102: Multi Kinase Inhibitor
APL-102 is an oral, Multi Kinase Inhibitor (mKi) 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
- RET, CSF1R, DDR1 and c-KIT
Tyrosine kinases are a group of around 90 enzymes capable of phosphorylating the amino acid tyrosine on another protein, which leads to conformational changes and typically activation of that protein. In the human genome, at least 90 tyrosine kinases have been identified. Tyrosine kinase inhibitors (TKIs) are being developed to block abnormal signaling of signal transduction pathways that are involved in cellular growth and proliferation. While some TKIs specifically inhibit one or two tyrosine kinases, most TKIs are designed to inhibit more tyrosine kinases in multiple signaling pathways.
Apollomics retains worldwide rights to APL-102 outside of China.
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.