Drug intelligence / Profile preview

irinotecan + carboplatin + cetuximab

Development stage
Unknown
Lead developer
Pfizer
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

This is a combination regimen consisting of three agents: irinotecan, carboplatin, and cetuximab. Irinotecan is a topoisomerase I inhibitor that acts as a prodrug, converted in vivo to SN-38, which stabilizes the DNA-topoisomerase I complex and prevents religation of single-strand breaks during DNA replication, leading to double-stranded DNA breaks and apoptosis[5][6]. Carboplatin is a platinum-based chemotherapeutic agent that forms DNA crosslinks and inhibits DNA synthesis and transcription. Cetuximab is an epidermal growth factor receptor (EGFR) monoclonal antibody that blocks EGFR signaling pathways involved in cell proliferation and survival[6]. This combination has been studied primarily for metastatic colorectal cancer (especially RAS wild-type), metastatic breast cancer (including triple-negative subtypes), and other solid tumors where synergistic effects are hypothesized or observed[2][3][4]. The addition of cetuximab to irinotecan-based regimens can restore sensitivity to irinotecan in some resistant cancers by inhibiting EGFR-mediated resistance mechanisms[2].

Other names
irinotecancarboplatincetuximabCPT-11CPT11CPT 11NSC-616348NSC616348NSC 616348cis-diammine(1,1-cyclobutanedicarboxylato)platinum(II)IMC-C225IMC-C-225IMC-C 225
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)TOP1 (DNA Topoisomerase I)

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