Drug intelligence / Profile preview

selumetinib + irinotecan

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**Selumetinib + irinotecan** is an investigational combination regimen used in oncology, primarily studied in the treatment of advanced or metastatic colorectal cancer harboring K-RAS or B-RAF mutations. Selumetinib is a selective small molecule inhibitor of mitogen-activated protein kinase kinases 1 and 2 (MEK1/2), acting downstream of RAS/RAF in the MAPK/ERK signaling pathway, involved in cell proliferation and survival[1][3][5][7]. Irinotecan is a cytotoxic agent that inhibits topoisomerase I, leading to impaired DNA replication and cell death. The combination aims to enhance antitumor efficacy by dual pathway inhibition: direct interference with tumor proliferation signals (MEK) and cytotoxic DNA damage. Selumetinib is administered orally, while irinotecan is given intravenously. The combination has undergone phase I/II trials, particularly for KRAS- or BRAF-mutated metastatic colorectal cancer after progression on oxaliplatin- and bevacizumab-based regimens, with the intent to overcome resistance to standard therapies[1][3][5][7].

Brand names
Campto
Other names
selumetinib hyd-sulfate + irinotecan
02

Targets

MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)TOP1 (DNA Topoisomerase I)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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