Drug intelligence / Profile preview

2-carba-cyclic phosphatidic acid

Development stage
Phase 2
Lead developer
Orient Europharma
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intraarticular, Intravenous
01

Overview

2-carba-cyclic phosphatidic acid (2ccPA) is a chemically stabilized derivative of cyclic phosphatidic acid (cPA), a naturally occurring lipid mediator. In 2ccPA, one of the phosphate oxygen atoms in cPA is replaced with a methylene group at the sn-2 position, enhancing its metabolic stability[6][8]. 2ccPA exhibits anti-inflammatory and neuroprotective properties. It inhibits chronic and acute inflammation, attenuates neuropathic pain, and has shown efficacy in reducing symptoms of osteoarthritis by stimulating hyaluronic acid synthesis and suppressing matrix metalloproteinases (MMP-1, -3, -13) production in synoviocytes and chondrocytes[1]. In preclinical models of brain injury and multiple sclerosis, it protects oligodendrocytes via suppression of mitochondrial apoptosis pathways and reduces demyelination as well as neuroinflammation[3][6]. Mechanistically, it modulates inflammatory responses partly by downregulating cyclooxygenase-2 (Cox-2) mRNA expression and prostaglandin E₂ production[7], regulates blood coagulation after brain injury by promoting platelet aggregation around lesions while supporting fibrinolysis[2], and promotes phenotypic switching from M1 to M2 microglia. Clinical development includes phase I/II studies for osteoarthritis pain relief[4].

Other names
2-carba-cyclic phosphatidic acid2ccPA sodium
02

Targets

MMP3 (Matrix metalloproteinase-3)MMP13 (Matrix metalloproteinase-13)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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