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HPMA copolymer-alendronate-TNP-470

Development stage
Discontinued
Lead developer
Tel Aviv University
Modality
Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

HPMA copolymer-alendronate-TNP-470 is a targeted, nano-scaled polymer-drug conjugate designed for the treatment of bone-related angiogenesis-dependent malignancies, such as osteosarcoma and bone metastases. It consists of an N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer backbone conjugated to the aminobisphosphonate alendronate (ALN) and the anti-angiogenic agent TNP-470 via a cathepsin K-cleavable tetrapeptide linker (Gly-Gly-Pro-Nle). Alendronate acts as a bone-targeting moiety by binding to hydroxyapatite, while TNP-470 inhibits tumor angiogenesis by targeting methionine aminopeptidase 2 (MetAP2) in endothelial cells. Developed by academic researchers at Tel Aviv University and the University of Utah, this conjugate demonstrates enhanced anti-tumor and anti-angiogenic activity with a superior safety profile and reduced systemic toxicity compared to the free drugs.

Other names
HPMA copolymer-ALN-TNP-470
02

Targets

FDPS (Farnesyl pyrophosphate synthase)METAP2 (Methionine aminopeptidase 2)

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