Drug intelligence / Profile preview

DPM-1001

Development stage
Preclinical
Lead developer
DepYmed
Modality
Small Molecules
Administration
Oral
01

Overview

DPM-1001 is a potent, specific, orally bioavailable and non-competitive small molecule inhibitor of protein tyrosine phosphatase 1B (PTP1B), with an IC50 of approximately 100 nM. It is an analog of the PTP1B inhibitor trodusquemine (MSI-1436). DPM-1001 also acts as a copper chelator, facilitating the removal of excess copper from the body. The drug has demonstrated anti-diabetic properties by enhancing insulin and leptin signaling in animal models, leading to improved metabolic outcomes such as reduced diet-induced obesity. Its dual mechanism—PTP1B inhibition and copper chelation—makes it a candidate for treating diseases involving disrupted cell signaling or metal overload. DPM-1001 is being developed primarily for Wilson disease (hepatolenticular degeneration), a rare disorder characterized by pathological copper accumulation, and has received orphan drug designation from the FDA for this indication. Development efforts have been discontinued in cancer indications such as breast cancer[2][4][8].

02

Targets

PTPN1 (Protein tyrosine phosphatase 1B)

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