AV-412

AV-412 is a second-generation, orally bioavailable small molecule dual kinase inhibitor that targets both the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2/ErbB2). By binding to and inhibiting these receptor tyrosine kinases—including mutant forms such as EGFR L858R and T790M—AV-412 blocks downstream signaling pathways involved in tumor cell proliferation and angiogenesis. This mechanism may result in inhibition of tumor growth, angiogenesis suppression, and regression of tumors expressing EGFR/HER2. Preclinical studies demonstrated activity against various solid tumors including non-small cell lung cancer (NSCLC), metastatic breast cancer, pancreatic cancer, head & neck cancer, and hormone-refractory prostate cancer. AV-412 was developed to address resistance to first-generation EGFR inhibitors such as erlotinib or gefitinib. The drug was originally developed by Mitsubishi Tanabe Pharma Corporation with further development by AVEO Pharmaceuticals; however, clinical development has been discontinued[1][3][4][5].

Other names

AV-412 TosylateAV412 TosylateAV 412 Tosylate451493-31-5UNII-Z541VW0W40UNII-Z-541VW0W40UNII-Z 541VW0W40