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First-in-human study of LY3039478, an Oral Notch signaling inhibitor in advanced or metastatic cancer.

08:00 EDT 28th July 2018 | BioPortfolio

Summary of "First-in-human study of LY3039478, an Oral Notch signaling inhibitor in advanced or metastatic cancer."

Deregulated Notch signaling due to mutation or overexpression of ligands and/or receptors is implicated in various human malignancies. Gamma-secretase inhibitors inhibit Notch signaling by preventing cleavage of transmembrane domain of Notch protein. LY3039478 is a novel, potent Notch inhibitor decreases Notch signaling and its downstream biologic effects. In this first-in-human study, we report the safety, pharmacokinetic (PK) profile, pharmacodynamic effects, and antitumor activity of LY3039478 in patients with advanced or metastatic cancer.

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Journal Details

This article was published in the following journal.

Name: Annals of oncology : official journal of the European Society for Medical Oncology
ISSN: 1569-8041
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Medical and Biotech [MESH] Definitions

A disintegrin and metalloproteinase domain-containing protein that cleaves the membrane-bound precursor of TUMOR NECROSIS FACTOR-ALPHA to its mature form. It cleaves several other CELL SURFACE PROTEINS, including INTERLEUKIN-1 RECEPTOR TYPE II; TRANSFORMING GROWTH FACTOR ALPHA; L-SELECTIN; MUCIN-1; and AMYLOID BETA-PROTEIN PRECURSOR. It can also function as an activator of the Notch signaling pathway by mediating the cleavage of NOTCH RECEPTORS.

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