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crizotinib + methotrexate
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Intrathecal
01
Overview
Crizotinib is a small molecule kinase inhibitor targeting anaplastic lymphoma kinase (ALK) and ROS1, used primarily in the treatment of ALK- or ROS1-positive non-small cell lung cancer (NSCLC), as well as certain pediatric cancers. Methotrexate is an antimetabolite that inhibits dihydrofolate reductase, disrupting DNA synthesis and cell replication; it is widely used in oncology for various cancers and autoimmune diseases. The combination of crizotinib with intrathecal methotrexate has been explored for the treatment of NSCLC patients with leptomeningeal carcinomatosis, showing promising progression-free survival outcomes in case reports[1][7].
- Other names
- ALK inhibitor crizotinib combined with intrathecal methotrexatecrizotinib and methotrexate
02
Targets
ROS1 (Proto-oncogene tyrosine-protein kinase ROS)DHFR (Dihydrofolate reductase)HMGB1 (High mobility group protein B1)MET (Mesenchymal-epithelial transition factor receptor)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)
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