Drug intelligence / Profile preview

ZPL-868087

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules
Administration
Intraperitoneal, Oral
01

Overview

**ZPL-868087** is a selective, peripherally acting histamine H3 receptor (H3R) antagonist designed to spare central nervous system effects, developed initially by Ziarco Pharma and later associated with Pfizer. It demonstrates analgesic efficacy in preclinical models of neuropathic pain, including chronic constriction injury (CCI)-induced mechanical hypersensitivity in mice (effective at 3-10 mg/kg i.p.) and streptozotocin (STZ)-induced diabetic hypersensitivity (effective at 100 mg/kg p.o.), without impacting heat or cold hypersensitivity. Originally advanced for allergic rhinitis, it highlights peripheral H3R as a potential target for chronic pain modulation, with localized administration confirming its peripheral mechanism.

02

Targets

HRH3 (Histamine Receptor H3)

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