This technology is a ERK kinase inhibitor, CIP-137401, for use in treating cardiomyopathy.
Inherited forms of cardiomypathy can result from mutations in different genes. One such example is mutations in the lamin A/C gene (LMNA), which causes cardiomyopathy often with associated muscular dystrophy. Inhibitors of mitogen-activated protein (MAP) protein kinases, especially MEK1 and/or MEK2 inhibitors, have been identified as having potential uses for the treatment of a variety of diseases, and increased ERK1/2 enzyme activity has been found to be involved in cardiomyopathies. However, despite current progress in MEK inhibitor research, there are currently no curative treatments for this form of cardiomyopathy.
This small-molecule, CIP-137401, is a MEK inhibitor for effectively treating cardiomyopathies, including those caused by mutations in LMNA. CIP-137401 binds and inhibits MEK1/2 kinases, which are related to disease progression and are abnormally activated. As a result, this therapy can potentially reduce the ventricle enlargement, cardiac fibrosis and skeletal muscle fatigue often related to adverse cardiac events. Additionally, CIP-137401 demonstrates anti-proliferative activity, and displays advantageous pharmacological properties, such as high oral bioavailability, longer half-life, and low brain barrier penetration, which can lead to reduced side-effects. As a result, this technology offers a versatile compound that can effectively treat various forms of cardiomyopathy, such as X-linked Emery-Dreifuss muscular dystrophy, Noonan syndrome, and other “Ras-opathies.”
This technology has been validated in a mouse model of cardiomyopathy/muscular dystrophy caused by a LMNA mutation.
Patent Pending (US 20150250762)
Patent pending (US 20110110916)
IR CU15167, 2372
Licensing Contact: Jerry Kokoshka