Overview

NCI Definition [1]:
An orally available small molecule inhibitor of methionine adenosyltransferase II alpha (MAT2A) with potential antineoplastic activity. Upon administration, AG-270 inhibits the activity of MAT2A, a metabolic enzyme responsible for the production of S-Adenosyl-L-methionine (SAM), a primary donor of methyl groups in cellular transmethylation reactions that regulate gene expression, cell growth, and differentiation. MAT2A activity is selectively essential in cancer cells deficient in methylthioadenosine phosphorylase (MTAP), a critical enzyme in the methionine salvage pathway, that is deleted in some human cancers. Inhibition of MAT2A may potentially inhibit tumor cell growth in MTAP-deleted cancers that rely heavily on SAM synthesis.

Ag-270 has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating ag-270, 1 is phase 1 (1 open).

CDKN2A Loss and MTAP Loss are the most frequent biomarker inclusion criteria for ag-270 clinical trials.

Adenocarcinoma of the gastroesophageal junction, gastric adenocarcinoma, and head and neck squamous cell carcinoma are the most common diseases being investigated in ag-270 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Ag-270
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating ag-270 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]:
ag 270, ag270, mat2a inhibitor ag-270
Drug Target(s) [2]:
MAT2A
NCIT ID [1]:
C153180

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.