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HPG-FA-MTX

Development stage
Preclinical
Lead developer
University of British Columbia
Modality
Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

**HPG-FA-MTX** is an experimental, intravenously administered synovium-targeted macromolecular methotrexate prodrug developed in academic research at the University of British Columbia for inflammatory arthritis, particularly rheumatoid arthritis. It covalently couples methotrexate to a long-circulating hyperbranched polyglycerol carrier functionalized with folic acid and uses an ester linkage designed for gradual, inflammation-associated release of methotrexate. In preclinical rheumatoid arthritis models, the conjugate preferentially accumulated in inflamed joints and achieved anti-inflammatory activity with substantially less methotrexate and less frequent dosing than unconjugated methotrexate. ([pmc.ncbi.nlm.nih.gov](https://pmc.ncbi.nlm.nih.gov/articles/PMC11616258/))

Other names
folic acid-functionalized hyperbranched polyglycerol-methotrexateHPG-FA-MTX
02

Targets

FOLR1 (FRα)DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)

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