Drug intelligence / Profile preview

KLS-13019

Development stage
Preclinical
Lead developer
Neuropathix
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

KLS-13019 is a cannabidiol-derived small molecule neuroprotective agent developed to improve upon the potency, safety, and bioavailability of cannabidiol. It is structurally modified on the side chain to enhance solubility and tissue penetration. KLS-13019 acts primarily as an antagonist at G protein-coupled receptor 55 (GPR55) and modulates the mitochondrial sodium-calcium exchanger 1 (NCX1), conferring both neuroprotective and anti-inflammatory properties. Preclinical studies have demonstrated that it is significantly more potent and safer than cannabidiol, with improved oral bioavailability. Unlike cannabidiol, KLS-13019 has been shown to both prevent and reverse neuropathic pain in models of chemotherapy-induced peripheral neuropathy (CIPN), without binding to opioid receptors or presenting a risk for chemical dependency. The drug also shows potential for treating other neuroinflammatory conditions such as hepatic encephalopathy, traumatic brain injury, peripheral nerve injuries, inflammation-related disorders, and possibly Parkinson’s disease[1][2][3][4][5][6][7].

02

Targets

GPR55 (G protein-coupled receptor 55)NCX1 (Sodium/calcium exchanger 1)

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