ProLindac™ (AP5346): A review of the development of an HPMA DACH platinum Polymer Therapeutic

被引：137

作者：

Nowotnik, David P. ^{[1
]}

Cvitkovic, Esteban ^{[2
]}

机构：

[1] Access Pharmaceut Inc, Dallas, TX 75207 USA

[2] Oncol Therapeut Dev SARL, F-93400 St Ouen, France

来源：

ADVANCED DRUG DELIVERY REVIEWS | 2009年 / 61卷 / 13期

关键词：

ProLindac; HPMA; Oxaliplatin; PARENTERAL LYOPHILIZED FORMULATION; ANTICANCER AGENT AP-5280; PHARMACEUTICAL DEVELOPMENT; PLASMA ULTRAFILTRATE; ANTITUMOR-ACTIVITY; QUALITY-CONTROL; SOLID TUMORS; IN-VITRO; PHASE-I; OXALIPLATIN;

D O I：

10.1016/j.addr.2009.06.004

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

ProLindac (TM) (AP5346) is DACH (diaminocyclohexane) platinum polymer prodrug currently in phase II clinical development. It uses a 25 kDa polymer delivery vehicle based on hydroxypropylmethacrylamide (HPMA) to target the active form of the approved drug oxaliplatin to tumors. The pH-sensitive linker that binds platinum to the polymer releases platinum more rapidly in low pH environments, as found typically in many tumors. This review summarizes the development of ProLindac to date, including preclinical efficacy studies, the phase I monotherapy clinical Study in patients with solid tumors, and the phase I/II monotherapy study in patients with recurrent ovarian cancer. Both preclinical and clinical study data indicate that ProLindac exhibits efficacy at least equal to, and likely superior to oxaliplatin, while demonstrating excellent tolerability. Additional clinical studies of ProLindac used in combination with other chemotherapeutic agents are planned. (C) 2009 Elsevier B.V. All rights reserved.

引用

页码：1214 / 1219

页数：6

共 35 条

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