PG-4HPR

PG-4HPR is a **polymeric prodrug** composed of **N-(4-hydroxyphenyl)retinamide (4-HPR, also known as fenretinide)** covalently linked to poly(L-glutamic acid) to improve aqueous solubility and tumor delivery. The primary rationale for developing PG-4HPR is to enhance the antitumor activity and radiosensitization properties of fenretinide by improving its pharmacokinetic profile and achieving greater tumor accumulation. Preclinical studies showed that PG-4HPR inhibits proliferation and induces apoptosis in lung cancer cells, augments the effects of radiation therapy, and demonstrates greater radiosensitization effects than unconjugated fenretinide, likely due to improved drug delivery and enhanced induction of apoptosis in tumor tissue[1]. The mechanism of action corresponds to fenretinide: acting as a synthetic retinoid, inducing apoptosis through modulation of retinoid-responsive genes and pathways, as well as additional non-retinoid cytotoxic effects.

Other names

poly(L-glutamic acid)-fenretinidepoly(L-glutamic acid)-4-HPRpolymeric fenretinide prodrug