Drug intelligence / Profile preview

FT671

Development stage
Preclinical
Lead developer
Novo Nordisk
Modality
Small Molecules
Administration
Oral (in Animal Studies)
01

Overview

FT671 is a potent, selective, non-covalent small molecule inhibitor of **ubiquitin-specific protease 7** (USP7), with an IC50 of 52 nM and a Kd of 65 nM for the USP7 catalytic domain[1][3][5][6]. FT671 was developed as a research tool to explore the biological function of USP7, which deubiquitinates key regulatory proteins including MDM2, thereby regulating the tumor suppressor p53. Inhibition of USP7 by FT671 leads to destabilization and degradation of MDM2, stabilization and increased levels of p53, induction of p55 target genes (such as p21), and inhibition of tumor growth in multiple cancer cell lines and xenograft models[1][3]. FT671 shows high selectivity for USP7 versus other deubiquitinases. It has been shown to promote anti-tumor activity by enhancing the degradation of substrates like SP1 and β-catenin and inhibiting the growth of tumor xenografts in mice without significant toxicity[1][3]. FT671 is intended for research use only and not for human clinical use; as of the latest update, no clinical trials in humans have been reported for this molecule[4]. FT671 was discovered and optimized by Forma Therapeutics[3].

02

Targets

USP7

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