Drug intelligence / Profile preview

pd184161

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

PD184161 is a highly selective, orally active small molecule inhibitor of MEK1 and MEK2, which are kinases in the MAPK/ERK pathway involved in cell proliferation and survival[1][7]. It has demonstrated potent inhibition of MEK activity (IC50 = 10–100 nM), leading to suppression of ERK1/2 phosphorylation, inhibition of tumor cell proliferation, and induction of apoptosis in cancer cell lines[1][2]. PD184161 exhibits greater oral bioavailability and solubility than earlier MEK inhibitors. It has primarily been evaluated in preclinical models, especially for hepatocellular carcinoma, gallbladder cancer, and in animal models of MEK/ERK pathway-related disorders[1][2][6]. No clinical trial data are available[5].

02

Targets

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

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