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dalpiciclib + letrozole + anlotinib
- Development stage
- Preclinical
- Lead developer
- Hengrui Therapeutics
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Dalpiciclib + letrozole + anlotinib is a combination regimen under investigation for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or early breast cancer. Dalpiciclib is a selective cyclin-dependent kinase 4/6 (CDK4/6) inhibitor that blocks cell cycle progression in tumor cells. Letrozole is a non-steroidal aromatase inhibitor that suppresses estrogen synthesis and is widely used as endocrine therapy in HR+ breast cancer. Anlotinib is a multi-targeted oral tyrosine kinase inhibitor with potent anti-angiogenic and anti-tumor activity; it inhibits vascular endothelial growth factor receptors (VEGFR) 2/3, fibroblast growth factor receptors (FGFR) 1–4, platelet-derived growth factor receptors (PDGFR) α/β, c-Kit and Ret[6][8]. This triple combination aims to simultaneously block cell proliferation pathways driven by CDK4/6 and estrogen signaling while inhibiting angiogenesis and additional tumorigenic pathways via multi-kinase inhibition.
- Other names
- dalpiciclib + letrozole + anlotinib
02
Targets
CYP19A1 (Aromatase)CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)RET (Rearranged during transfection receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)
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