Drug intelligence / Profile preview

FOLFIRI + trebananib

Development stage
Unknown
Lead developer
Amgen
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Peptide-Protein Conjugates → Peptide Conjugates → Peptides, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

FOLFIRI + trebananib is a combination therapy used in clinical trials for metastatic colorectal cancer. FOLFIRI is a chemotherapy regimen consisting of folinic acid (leucovorin), fluorouracil (5-FU), and irinotecan. Folinic acid enhances the effectiveness of 5-FU, which disrupts DNA synthesis in rapidly dividing cells, while irinotecan inhibits topoisomerase I to block DNA replication[2][3][5]. Trebananib (AMG 386) is an investigational peptide-Fc fusion protein that neutralizes angiopoietins-1 and -2 from binding to the Tie2 receptor, thereby inhibiting angiogenesis—the formation of new blood vessels that tumors need for growth[1]. The combination was studied as a second-line treatment for patients with metastatic colorectal cancer who had progressed after prior chemotherapy. In phase 2 studies, adding trebananib to FOLFIRI did not significantly prolong progression-free survival compared with FOLFIRI alone; toxicities were manageable and consistent with known profiles for both agents[1].

02

Targets

TOP1 (DNA Topoisomerase I)ANGPT1 (Angiopoietin-1)TS (Thymidylate synthase)

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