Antia Laboratories Inc.

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Afatinib (BIBW-2992)

CAS Number:439081-18-2

Mol. Formula: C24H25ClFN5O3

Mol. Weight: 485.94

BIBW2992 (Afatinib) is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2. In cell-free in vitro kinase assays, BIBW2992 shows potent activity against wild-type and mutant forms of EGFR and HER2, similar to gefitinib in potency for L858R EGFR, but about 100-fold more active against the gefitinib resistant L858R-T790M EGFR double mutant, with an IC50 of 10 nM. BIBW2992 was effective in inhibiting survival of lung cancer cell lines harboring wild-type (H1666) or L858R/T790M (NCI-H1975) EGFR, with IC50s below 100 nM for these isoforms resistant to first-generation inhibitors anda subnanomolar IC50 for the gefitinibsensitive L858R expressedby H3255. Assessed in a standard xenograft model of the epidermoid carcinoma cell line A431. Daily oral treatment with BIBW2992 at 20 mg/kg for 25 days resulted in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%. Like lapatinib and neratinib, afatinib is a next generation tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. Afatinib is not only active against EGFR mutations targeted by first generation TKIs like erlotinib or gefitinib, but also against those not sensitive to these standard therapies. Because of its additional activity against Her2, it is investigated for breast cancer as well as other EGFR and Her2 driven cancers.

1. Afatinib Benefits Lung Cancer Patients Who Progress on EGFR Inhibitors. Laino et al.: Oncology Times, 32, 21 34-35 2010

2.Preclinical results show that afatinib is effective in lung cancer models, including those with EGF receptor (EGFR) mutations resistant to reversible first-generation EGFR inhibitors. Vera Hirsh et al.: Future Oncology 7,7,817,2011

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