Platform Success Example IV – Mechanism of Afatinib

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Business Need

Boehringer Ingelheim wanted an in-depth understanding of the interaction mechanism of Afatinib (inhibitor of EGFR, HER2, and ErbB4).

Technical Challenge

An irreversible and complex interaction mechanism.

Solution

With an experimental design for an induced-fit mechanism, Beactica untangled the interaction mechanism using its SPR-based drug discovery platform.

Results

The results from the SPR interaction analysis were used to formulate a mechanistic rationale for the distinct pharmacological features of Afatinib. The results explain the clinical activity seen in some patients resistant to antibody or kinase inhibitor therapy. The results from the collaboration were published in the Journal of Pharmacology and Experimental Therapeutics (JPET) in 2012.

Mechanism of Afatinib article

Reference

Solca F, Dahl G, Zoephel A, Bader G, Sanderson M, Klein C, Kraemer O, Himmelsbach F, Haaksma E, Adolf GR (2012) Target binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blocker. J Pharm Exp Therap, 343(2):342–50.