BIBX1382

BIBX1382 is an EGFR inhibitor (IC₅₀ = 3 nM).¹ It is selective for EGFR over HER2 (IC₅₀ = 3,400 nM), as well as insulin-like growth factor 1 receptor (IGF-1R), β-insulin receptor kinase (β-InsRK), c-Met, c-Src, and VEGFR2 (IC₅₀s = >10 µM for all). BIBX1382 inhibits proliferation and colony formation in A549 cancer cells expressing mutant K-Ras, as well as FaDu cancer cells expressing wild-type K-Ras when used at a concentration of 5 µM.² It enhances radiation-induced cytotoxicity in mutant K-Ras-expressing A549 and MDA-MB-231 cancer cells, but not FaDu, HTB-35, or HH4dd cancer cells that express wild-type K-Ras. BIBX1382 reduces tumor growth in A431 and FaDu mouse xenograft models when administered at doses of 70 and 60 mg/kg per day, respectively.¹

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1. Solca, F.F., Baum, A., Langkopf, E., et al. Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives. J. Pharmacol. Exp. Ther. 311(2), 502-509 (2004).

2. Toulany, M., Dittmann, K., Baumann, M., et al. Radiosensitization of ras-mutated human tumor cells in vitro by the specific EGF receptor antagonist BIBX1382BS. Radiother. Oncol. 74(2), 117-129 (2005).