Drug intelligence / Profile preview

hpma copolymer-doxorubicin conjugate

Development stage
Unknown
Lead developer
Pfizer
Modality
Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

**hpma copolymer-doxorubicin conjugate** is a polymer-drug conjugate in which the chemotherapeutic agent doxorubicin is covalently attached to N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer. This polymeric carrier enhances drug solubility, prolongs circulation time, and enables site-specific release via pH-sensitive or enzymatically-cleavable linkers. It is designed to reduce systemic toxicity, especially doxorubicin-associated cardiotoxicity, and to improve antitumor efficacy by altering pharmacokinetics and promoting accumulation in tumor tissues. The conjugate can self-assemble into nanoparticles and show pH-sensitive drug release, releasing doxorubicin preferentially in acidic tumor microenvironments. Clinical studies (notably under code name PK1) demonstrated activity in anthracycline-naïve and chemotherapy-refractory cancer patients, with reduced toxicity and potential immunostimulatory effects. Primary indications are solid tumors including breast cancer, non-small cell lung cancer, colorectal cancer, and lymphoma, though it has not reached routine clinical use[2][3][4][5][7][8].

Other names
doxorubicin-HPMA conjugatedoxorubicin-HPMA copolymer conjugateHPMA copolymer-doxorubicin conjugateDOX–PHPMA
02

Targets

DNATOP2A (DNA topoisomerase II)

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