Description
Introduction
Briganix (Brigatinib) is not a chemotherapy drug, but one of what are termed “targeted therapies.”
Brigatinib, originally named AP26113, is a reversible dual inhibitor of anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR). It presents selectivity against the mutant forms of EGFR compared to the wild-type. It also exhibits selectivity against 9 different Crizotinib-resistant mutants of the EML4-ALK fusion gene, which is a pivotal player in the transformation of susceptible lung parenchyma.
Brigitanib inhibits proliferation and in vitro viability of cells expressing the fusion protein EML4-ALK as well as 17 crizotinib-resistant ALK mutants. Its action is expanded to cells expressing EGFR deletions, ROS1-L2026M, FLT3-F691L and FLT3-D835Y. Brigitanib presents a dose-dependent inhibition of tumor growth, tumor burden and prolonged survival in mice EML4-ALK xenograft models. Time course of Brigatinib and exposure-response studies are still unknown.
Briganix (Brigatinib) is a broad spectrum kinase inhibitor with activity against anaplastic lymphoma kinase (ALK) and many other factors. A kinase is an enzyme that helps cells grow and divide. Non-small cell cancer cells with ALK grow and divide faster. By binding to the anaplastic lymphoma kinase and these other factors, brigatinib blocks an important pathway that promotes cell division of these malignant cells.
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