Drug intelligence / Profile preview

chrysin + irinotecan

Development stage
Unknown
Lead developer
Pfizer
Modality
Targeted Protein Degraders (TPDs) → Small Molecules, Prodrugs/Conditional Activator Small Molecules → Small Molecules, Multivalent & Scaffold-Based Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral (chrysin), Intravenous (irinotecan)
01

Overview

Chrysin + irinotecan is an investigational combination therapy involving the natural flavonoid chrysin and the chemotherapeutic agent irinotecan. Chrysin is a bioactive compound found in honey and propolis, known for its anti-inflammatory, antioxidant, and potential anticancer properties. Irinotecan is a topoisomerase I inhibitor widely used in the treatment of colorectal cancer. The rationale for combining these agents centers on chrysin’s ability to induce intestinal UGT1A1 enzyme activity, which enhances glucuronidation of SN-38 (the active metabolite of irinotecan), thereby reducing gastrointestinal toxicity—specifically delayed diarrhea—without compromising antitumor efficacy. Preclinical studies suggest that this combination may have synergistic anti-tumor effects in colon cancer models[1][6][8]. Early clinical data indicate that co-administration is safe and may reduce the severity of chemotherapy-induced diarrhea[6].

Other names
CPT-11CPT11CPT 11
02

Targets

TOP1 (DNA Topoisomerase I)UGT1A1 (UDP-glucuronosyltransferase 1A1)ABCG2 (Breast cancer resistance protein)

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