BIBW-2992, a dual receptor tyrosine kinase inhibitor for the treatment of solid tumors.

摘要: The anilino-quinazoline derivative BIBW-2992, which is being developed by Boehringer Ingelheim Corp for the potential treatment of solid tumors, an oral dual receptor tyrosine kinase inhibitor human EGF (EGFR) and epidermal growth factor receptor-2 (HER-2)/neu. EGFR HER-2/neu activate numerous signaling pathways leading to cancer cell proliferation, survival migration. In vitro, BIBW-2992 effectively selectively inhibited total phosphorylation tumor proliferation in vivo. Importantly, was active against tumors overexpressing with secondary Thr790Met point mutation, confers resistance first-generation inhibitors gefitinib erlotinib. phase I/II trials, effective patients including those NSCLC activating mutations domain. generally well tolerated main adverse effects gastrointestinal or cutaneous disorders. At time publication, undergoing II trials NSCLC, breast prostate cancers, head neck carcinoma, as glioma. granted Fast-Track status FDA investigated III this indication.