Overview

Generic Name(s):
selumetinib
NCI Definition [1]:
An orally active, small molecule with potential antineoplastic activity. Selumetinib is an ATP-independent inhibitor of mitogen-activated protein kinase kinase (MEK or MAPK/ERK kinase) 1 and 2. MEK 1 and 2 are dual specificity kinases that are essential mediators in the activation of the RAS/RAF/MEK/ERK pathway, are often upregulated in various cancer cells, and are drivers of diverse cellular responses, including proliferation. Inhibition of both MEK1 and 2 by selumetinib prevents the activation of MEK1/2 dependent effector proteins and transcription factors, thereby leading to an inhibition of cellular proliferation in various cancers.

Selumetinib has been investigated in 32 clinical trials, of which 28 are open and 4 are closed. Of the trials investigating selumetinib, 8 are phase 1 (6 open), 6 are phase 1/phase 2 (6 open), 14 are phase 2 (13 open), and 4 are phase 3 (3 open).

KRAS Mutation, NF1 Loss, and NF1 Mutation are the most frequent biomarker inclusion criteria for selumetinib clinical trials.

Non-small cell lung carcinoma, malignant solid tumor, and neurofibromatosis type 1 are the most common diseases being investigated in selumetinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Selumetinib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Selumetinib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating selumetinib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
azd6244, arry-142886, arry 142886, mek inhibitor azd6244, selumetinib, mek inhibitor azd6244, azd-6244, azd 6244, arry142886
Drug Categories [2]:
MEK inhibitors, Serine/threonine kinase inhibitors
Drug Target(s) [2]:
MAP2K1, MAP2K2
NCIT ID [1]:
C66939

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.