Drug intelligence / Profile preview

PD168368

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intracerebroventricular, Intradermal
01

Overview

PD168368 is a potent and selective non-peptide antagonist of the Neuromedin B receptor (NMBR). Originally developed by Parke-Davis (now part of Pfizer), it is primarily utilized as a pharmacological tool in preclinical research to investigate the role of Neuromedin B (NMB) signaling in various physiological and pathological states. NMB is a bombesin-like peptide that, upon binding to NMBR, activates downstream signaling pathways such as ERK1/2 and NF-κB (p65), which are involved in cell proliferation, survival, and inflammation. In the context of oncology, PD168368 has been shown to inhibit the growth and induce apoptosis in several cancer cell lines, including cervical, lung, and breast cancer, as well as glioma, by blocking the NMB/NMBR signaling axis. Its high selectivity for NMBR over the related gastrin-releasing peptide receptor (GRPR) makes it a valuable compound for dissecting the specific contributions of NMBR to disease progression.

02

Targets

GRPR (Gastrin-releasing peptide receptor)FPR1 (Formyl peptide receptor 1)FPR2 (Formyl peptide receptor type 2)FPR3 (Formyl peptide receptor 3)NMBR (Neuromedin B receptor)

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