Drug intelligence / Profile preview

FR-118487

Development stage
Discontinued
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

FR-118487 is a synthetic small molecule angiogenesis inhibitor developed by Fujisawa Pharmaceutical (now Astellas). It is a derivative of the microbial metabolite FR-111142, which is produced by the fungus *Scolecobasidium arenarium*. As a member of the fumagillin-related class of compounds, FR-118487 exerts its anti-tumor effects by targeting methionine aminopeptidase 2 (MetAP2), an enzyme critical for the post-translational modification of proteins that regulate endothelial cell function. By inhibiting MetAP2, FR-118487 prevents the formation of new blood vessels (neoangiogenesis), thereby limiting the nutrient supply to solid tumors. Preclinical research has demonstrated its efficacy in reducing tumor growth and progression in models of hepatocellular carcinoma and colon cancer. However, the compound did not advance into clinical development and is currently considered discontinued.

02

Targets

METAP2 (Methionine aminopeptidase 2)

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