Drug intelligence / Profile preview

pentilludin

Development stage
Preclinical
Lead developer
United States Department of Veterans Affairs
Modality
Small Molecules
Administration
Oral, Subcutaneous
01

Overview

Pentilludin (NHB1109) is a novel, potent, and selective small molecule inhibitor of receptor-type protein tyrosine phosphatase D (PTPRD). It acts as a pseudoirreversible inhibitor of PTPRD's phosphatase activity with an IC50 of approximately 690 nM. Pentilludin is being developed for the treatment of stimulant use disorders (such as amphetamine and cocaine addiction), opioid use disorders, chronic neuropathic pain (allodynia), and obesity. In preclinical studies, it has demonstrated the ability to reduce amphetamine and remifentanil self-administration, alleviate mechanical and thermal allodynia in chronic constriction injury models, and reduce weight gain in mice fed normal or high-fat diets.

02

Targets

PTPRD (Receptor-type tyrosine-protein phosphatase delta)

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