Drug intelligence / Profile preview

PD-0325901 + crizotinib

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

PD-0325901 + crizotinib is an investigational combination therapy consisting of two small molecule inhibitors used in oncology research. PD-0325901 is a selective inhibitor of MEK1/2 (mitogen-activated protein kinase kinases 1 and 2), which are key components of the MAPK/ERK signaling pathway involved in cell proliferation and survival. Crizotinib is a tyrosine kinase inhibitor targeting c-MET (hepatocyte growth factor receptor), ALK (anaplastic lymphoma kinase), and ROS1, but in this context its primary target is c-MET. The rationale for combining these agents stems from preclinical evidence that dual inhibition of MEK and c-MET can overcome resistance mechanisms seen with single-agent therapies, particularly in RAS-mutant colorectal cancer. This combination has been evaluated in phase I clinical trials to determine safety, tolerability, pharmacokinetics, and preliminary efficacy[4][2][3].

Brand names
Xalkori
02

Targets

MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)MST1R (Recepteur d'origine nantais)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)MET (Mesenchymal-epithelial transition factor receptor)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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