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Drug intelligence / Profile preview
bemarituzumab + irinotecan
- Development stage
- Phase 2
- Lead developer
- Amgen
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous
01
Overview
Bemarituzumab is a first-in-class, humanized IgG1 monoclonal antibody that selectively targets and inhibits Fibroblast growth factor receptor 2b (FGFR2b) signaling, blocking fibroblast growth factor binding to the receptor. This inhibition suppresses downstream cancer cell proliferation. Additionally, its afucosylated structure enhances antibody-dependent cellular cytotoxicity by increasing affinity for FcγRIIIa/CD16a on natural killer cells, leading to targeted destruction of Fibroblast growth factor receptor 2b (FGFR2b)-expressing tumor cells[3][5]. Irinotecan is a small molecule chemotherapeutic agent in the class of topoisomerase I inhibitors. It is converted in vivo to its active metabolite SN-38, which binds to and stabilizes the DNA topoisomerase 1 complex, preventing religation of single-strand breaks during DNA replication and transcription. This results in lethal double-stranded DNA breaks and apoptosis of rapidly dividing cancer cells[4][6][8]. The combination of bemarituzumab with irinotecan is being investigated for advanced or metastatic gastric or gastroesophageal junction adenocarcinoma after prior chemotherapy failure[1][2].
- Brand names
- Camptosar (for irinotecan)Novaplus Irinotecan Hydrochloride (for irinotecan)
- Other names
- bemarituzumab + irinotecan
02
Targets
FGFR2b (Fibroblast growth factor receptor 2 IIIb isoform)TOP1 (DNA Topoisomerase I)FGFR2 (Keratinocyte growth factor receptor)
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