Delving into the Latest Updates on UCM-14216 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

LPAR2

Mechanism

LPAR2 antagonists(lysophosphatidic acid receptor 2 antagonists)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

Spinal Cord Injuries

Inactive Indication-

Originator Organization

Universidad Complutense de Madrid

Active Organization

Universidad Complutense de Madrid

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Author: López-Rodríguez, María L. ; López-Vales, Rubèn ; Khiar-Fernández, Nora ; Ortega-Gutiérrez, Silvia ; Vázquez-Villa, Henar ; Puigdomenech-Poch, Maria ; Cincilla, Giovanni ; Zian, Debora ; Ray, Manisha ; Kihara, Yasuyuki ; Foronda-Sainz, Román ; Martínez, R. Fernando ; Chun, Jerold ; Escobar-Peña, Andrea ; Sánchez-Martínez, Melchor

Spinal cord injuries (SCIs) irreversibly disrupt spinal connectivity, leading to permanent neurological disabilities. Current medical treatments for reducing the secondary damage that follows the initial injury are limited to surgical decompression and anti-inflammatory drugs, so there is a pressing need for new therapeutic strategies. Inhibition of the type 2 lysophosphatidic acid receptor (LPA₂) has recently emerged as a new potential pharmacological approach to decrease SCI-associated damage. Toward validating this receptor as a target in SCI, we have developed a new series of LPA₂ antagonists, among which compound 54 (UCM-14216) stands out as a potent and selective LPA₂ receptor antagonist (E_max = 90%, IC₅₀ = 1.9 μM, K_D = 1.3 nM; inactive at LPA_1,3-6 receptors). This compound shows efficacy in an in vivo mouse model of SCI in an LPA₂-dependent manner, confirming the potential of LPA₂ inhibition for providing a new alternative for treating SCI.

100 Deals associated with UCM-14216

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