Drug intelligence / Profile preview

MSC2015103B

Development stage
Discontinued
Lead developer
Day One Biopharmaceuticals
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

MSC2015103B (also known as AS703988) is an oral, highly-selective small molecule allosteric inhibitor of MEK1 and MEK2, key enzymes in the MAPK signaling pathway. By selectively binding to and inhibiting the activity of MEK1/2, it prevents activation of downstream effector proteins and transcription factors, which may result in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. Dysregulation of the MAPK pathway is implicated in many cancers. The drug was initially developed by Merck KGaA (Darmstadt, Germany) and has been licensed to Day One Biopharmaceuticals for further development[1][3][5][6].

02

Targets

MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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