Drug intelligence / Profile preview

APL-102

Development stage
Phase 1
Lead developer
Apollomics
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

APL-102 is an oral, small molecule multi-kinase inhibitor (MTKi) developed by Apollomics for the treatment of cancer. It targets several key oncogenic drivers by inhibiting both receptor tyrosine kinases (RTKs) and serine/threonine kinases. Its primary mechanisms include inhibition of angiogenesis via vascular endothelial growth factor receptors (VEGFRs), platelet-derived growth factor receptors (PDGFRs), and the mitogen-activated protein kinase (MAPK) pathway through B-RAF and C-RAF. Additional targets include RET, CSF1R, DDR1, and c-KIT. Preclinical studies have shown that APL-102 can increase T-cell infiltration while reducing tumor-associated macrophages in the tumor microenvironment. The drug has demonstrated antitumor activity as a single agent and in combination with anti-PD1 antibodies in preclinical models[1][3][5][6][8].

02

Targets

KIT (c-KIT proto-oncogene receptor tyrosine kinase)RAF1 (c-Raf-1 (Y340D/Y341D))PDGFR (PDGFR family)RET (Rearranged during transfection receptor tyrosine kinase)CSF1R (Macrophage colony-stimulating factor receptor)BRAF (B-Raf proto-oncogene, serine/threonine kinase)DDR1 (Discoidin domain receptor 1)VEGFR (VEGFR family)

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