APL-102: Multi Kinase Inhibitor
APL-102 is an oral, small molecule multi-tyrosine kinase inhibitor (MTKI) targeting several key oncogenic drivers. APL-102 inhibits several receptor tyrosine kinases (RTKs), including the following:
- Angiogenesis via Vascular Endothelial Growth Factor Receptors (VEGFR)
- Mitogen-Activated Protein Kinases (MAPK) pathway via B-RAF and C-RAF
- Colony stimulating factor 1 receptor (CSF1R).
Receptor tyrosine kinases are enzymes responsible for the activation of many proteins by signal transduction cascade. RTKs are involved in cell proliferation and differentiation, cell survival, cell motility, invasion, and angiogenesis, all of which contribute to tumor progression. The VEGF family of growth factors receptors constitute one of the most important signaling pathways in angiogenesis. APL-102 may inhibit tumor angiogenesis and tumor cell growth by inhibiting VEGFR pathway and B-RAF/C-RAF/MAPK pathway. In addition, it may also inhibit CSF1R, thereby regulating tumor-related macrophages and promoting the immune response to tumor cells.
TKIs are a type of targeted therapy that inhibits tyrosine kinases. MTKIs are inhibitors designed to target a wide range of tyrosine kinases, and may be effective in reducing the side effect and overcoming the drug resistance in combination therapy. In addition to monotherapy, MTKIs are increasingly used in combination with chemotherapeutic drugs and immune checkpoint inhibitors to prevent drug resistance.
Apollomics retains worldwide rights to APL-102.
Shown to inhibit several kinases which are aberrantly activated in cancer cells, including VEGFR, MAP4K5, c-RAF and DDR1
Favorable preclinical pharmacokinetic (PK) and safety profiles with no serious off-target activity observed
The potential to be used as single agent or in combination with other oncology drugs
- Shown anti-tumor activity as a single agent and in combination with an anti-PD-1 antibody