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NEO212 + regorafenib
- Development stage
- Phase 2
- Lead developer
- NEONC Technologies
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
NEO212 + regorafenib is a combination therapy being investigated for the treatment of metastatic colorectal cancer (mCRC) with uncontrolled brain metastases. **NEO212** is an orally administered investigational small molecule compound derived from conjugating temozolomide (a DNA-alkylating agent) and perillyl alcohol (a monoterpene with anti-cancer activity). It is designed to provide targeted cytotoxicity to tumor cells and potentially improve CNS penetration and efficacy over temozolomide alone. **Regorafenib** is an approved oral small molecule multikinase inhibitor (targeting VEGFR, PDGFR, KIT, RET, RAF, BRAF, among others) that blocks multiple protein kinases involved in tumor angiogenesis, oncogenesis, and the tumor microenvironment. This combination aims to exploit both direct cytotoxic and anti-angiogenic/kinase-inhibitory mechanisms to treat resistant or advanced cancers, especially brain metastases[1][3][5][6].
- Other names
- regorafenibRégorafénibRegorafenibum
02
Targets
BRAF (B-Raf proto-oncogene, serine/threonine kinase)DNAFGFR1 (Fibroblast growth factor receptor 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)AGT (O6-methylguanine-DNA methyltransferase)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)TEK (Tie2)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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