HPMA copolymer-alendronate-paclitaxel

HPMA copolymer-alendronate-paclitaxel (HPMA copolymer-PTX-ALN) is a research-stage polymer-drug conjugate designed for the targeted treatment of bone metastases and bone-related malignancies, such as breast cancer bone metastases and osteosarcoma. Developed by researchers at Tel Aviv University, the conjugate consists of an N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer backbone covalently linked to two active agents: the bisphosphonate alendronate, which acts as a bone-targeting moiety with high affinity for hydroxyapatite, and the cytotoxic taxane paclitaxel. The drugs are attached via enzyme-labile peptide linkers (such as Gly-Phe-Leu-Gly and Phe-Lys-p-aminobenzyl carbonate) that are selectively cleaved by cathepsin B, a lysosomal enzyme overexpressed in tumor epithelial and endothelial cells. This targeted delivery system enhances antitumor and antiangiogenic efficacy at the bone tumor site while significantly reducing the systemic toxicities associated with free paclitaxel and alendronate.

Other names

HPMA copolymer-PTX-ALNHPMA copolymer-paclitaxel-alendronateHPMA-PTX-ALNN-(2-hydroxypropyl)methacrylamide copolymer-alendronate-paclitaxelN-(2-hydroxypropyl)methacrylamide copolymer-paclitaxel-alendronateN-(2-hydroxypropyl)methacrylamide-copolymer-paclitaxel-alendronate