Drug intelligence / Profile preview

phosphocitrate

Development stage
Preclinical
Lead developer
University of Miami
Modality
Small Molecules
Administration
Intraarticular, Intraperitoneal, Oral, Subcutaneous
01

Overview

Phosphocitrate is a naturally occurring phosphorylated polycarboxylic acid originally identified in mammalian mitochondria. It acts as a highly potent inhibitor of biological crystallization (calcification) by binding stereospecifically to the faces of calcium crystals, thereby preventing their nucleation, growth, and aggregation. This includes basic calcium phosphate (BCP), calcium oxalate, and calcium pyrophosphate dihydrate (CPPD) crystals. In addition to its physical-chemical anti-calcification properties, phosphocitrate modulates crystal-induced cellular signaling pathways, reducing the expression of inflammatory mediators (such as interleukin-1 beta and cyclooxygenase-2) and matrix metalloproteinases (such as MMP-1). It is being investigated in preclinical models for the treatment of crystal-associated osteoarthritis, pseudoxanthoma elasticum (PXE), nephrolithiasis, and vascular calcification.

Other names
2-phosphonooxypropane-1,2,3-tricarboxylic acidphosphocitric acid
02

Targets

IL1B (Interleukin-1 beta)MMP1 (Matrix metalloproteinase-1)HydroxyapatitePTGS2 (Prostaglandin-Endoperoxide Synthase 2)Calcium pyrophosphate dihydrate crystal surfaces

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