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palbociclib + binimetinib
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Fragment-Derived Small Molecules → Multivalent & Scaffold-Based Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Palbociclib + binimetinib is a combination of two oral small molecule kinase inhibitors used in clinical trials for the treatment of RAS-mutant cancers, including metastatic colorectal cancer and low-grade serous ovarian cancer. Palbociclib is a cyclin-dependent kinase 4/6 (CDK4/6) inhibitor that blocks cell cycle progression from G1 to S phase by inhibiting phosphorylation of the retinoblastoma protein, thereby suppressing tumor cell proliferation. Binimetinib is a mitogen-activated protein kinase kinase (MEK) inhibitor that targets MEK1 and MEK2 within the MAPK pathway, which is frequently activated in RAS-mutant tumors. The combination aims to provide dual blockade of key signaling pathways involved in tumor growth and survival, with evidence suggesting synergistic antitumor activity in preclinical models and early-phase clinical trials[1][6][8]. Palbociclib was developed by Pfizer; binimetinib was developed by Array BioPharma.
- Other names
- none
02
Targets
MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)
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