Drug intelligence / Profile preview

mk-8353

Development stage
Discontinued
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

MK-8353 is an orally bioavailable, selective, and potent small molecule inhibitor of extracellular signal-regulated kinase 1 (ERK1) and extracellular signal-regulated kinase 2 (ERK2) (also known as mitogen-activated protein kinase 3 and mitogen-activated protein kinase 1). It was developed as an antineoplastic agent for the treatment of advanced solid tumors. MK-8353 inhibits both the phosphorylation and activation of ERK-mediated signaling pathways, thereby blocking tumor cell proliferation and survival. The compound demonstrates high selectivity for its targets with minimal off-target activity against other kinases. Preclinical studies showed significant antitumor efficacy in various models, including those with BRAF or RAS mutations. Clinical trials have evaluated its safety, tolerability, pharmacokinetics, and preliminary efficacy in patients with advanced solid tumors such as metastatic melanoma and colorectal cancer[1][2][5][6][8].

Other names
MK 8353MK8353MK-8353SCH 900353SCH900353SCH-900353
02

Targets

MAPK3 (Mitogen-activated protein kinase 1)

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