Drug intelligence / Profile preview

roneparstat

Development stage
Phase 1
Lead developer
Leadiant Biosciences
Administration
Intravenous, Subcutaneous
01

Overview

Roneparstat is a chemically modified, N-acetylated and glycol-split form of heparin with very low anticoagulant activity. It acts as a potent and competitive inhibitor of heparanase, an enzyme involved in the cleavage of heparan sulfate proteoglycans on cell surfaces and within the extracellular matrix. By inhibiting heparanase, roneparstat prevents tumor cell invasion, metastasis, and angiogenesis by blocking the release of angiogenic growth factors such as matrix metalloproteinase‑9, hepatocyte growth factor, and vascular endothelial growth factor. Roneparstat has demonstrated antitumor activity in preclinical models for multiple myeloma and various sarcomas; it also inhibits several receptor tyrosine kinases (FGF receptors, IGF receptors, ERBB family members including EGFR/ERBB4/INSR/IGF1R/PDGFR) relevant to cancer pathobiology. The drug was developed primarily for multiple myeloma but has been studied in other cancers and non-oncological conditions[1][2][4][5][6][8].

Other names
roneparstatUNII-1J0593208BUNII1J0593208BUNII 1J0593208B
02

Targets

IGF-1R (Insulin-like growth factor 1 receptor)HPSE (Heparanase)ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)FGFR (Fibroblast growth factor receptor)PDGFR (PDGFR family)

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