Drug intelligence / Profile preview

crizotinib + erlotinib

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

Overview

Crizotinib + erlotinib is an investigational combination therapy of two small molecule tyrosine kinase inhibitors used in the treatment of advanced non-small cell lung cancer (NSCLC). Crizotinib inhibits multiple receptor tyrosine kinases including anaplastic lymphoma kinase (ALK), ROS1, and MET. Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. The rationale for combining these agents is to overcome or delay resistance to EGFR inhibitors that can arise through MET amplification or activation. Clinical studies have shown that this combination can be administered at reduced doses compared to single-agent therapy due to increased exposure and overlapping toxicities. The most common adverse events include diarrhea, rash, decreased appetite, and fatigue[1][2][6]. This combination has demonstrated partial responses in some patients with activating EGFR mutations and/or MET amplification who have progressed on prior therapies[7].

Brand names
Xalkori (crizotinib)Tarceva (erlotinib)
Other names
crizotinib + erlotinib
02

Targets

MET (Mesenchymal-epithelial transition factor receptor)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)EGFR T790M (Epidermal growth factor receptor T790M mutant)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)

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