Drug intelligence / Profile preview

Falnidamol

Development stage
Phase 1
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

Falnidamol is a small molecule pyrimido-pyrimidine compound with antitumor activity. It acts primarily as an inhibitor of the intracellular tyrosine kinase domain of the Epidermal Growth Factor Receptor (EGFR), thereby blocking aberrant EGFR signaling that drives cell proliferation and survival in certain cancers. Falnidamol has also been shown to inhibit the ABCB1 transporter (P-glycoprotein), reversing multidrug resistance by increasing intracellular concentrations of chemotherapeutic agents. The drug was initially developed by Boehringer Ingelheim for oncology indications such as solid tumors and lymphoma but clinical development was suspended due to dose-limiting liver enzyme elevations, low bioavailability, and detection of inactive metabolites[1][4][5][6].

Other names
196612-93-8
02

Targets

ABCB1 (P-glycoprotein)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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