varlitinib

Varlitinib is an orally active, selective, reversible small molecule inhibitor of the HER family of receptor tyrosine kinases, specifically targeting EGFR (HER1/ErbB1), HER2 (ErbB2), and HER4 (ErbB4). By binding to these receptors, varlitinib prevents their phosphorylation and activation, thereby inhibiting downstream signal transduction pathways that drive cellular proliferation and survival. This mechanism results in anti-tumor activity through inhibition of cell growth and induction of apoptosis. Varlitinib has demonstrated preclinical efficacy in models of breast, lung, epidermal carcinoma tumors, as well as clinical activity in gastric cancer, biliary tract cancer (including cholangiocarcinoma), liver cancer, solid tumors including triple negative breast cancer. It was developed by Array BioPharma and further advanced by ASLAN Pharmaceuticals. The drug has received orphan drug designation for cholangiocarcinoma and gastric cancer but development for these indications has been discontinued[1][2][3][4][6][7].

Brand names

varlitinib

Other names

varlitinibum