Antitumor Efficacy of Colon-Specific HPMA Copolymer/9-Aminocamptothecin Conjugates in Mice Bearing Human-Colon Carcinoma Xenografts

✍ Scribed by Song-Qi Gao; Yongen Sun; Pavla Kopečková; C. Matthew Peterson; Jindřich Kopeček

• Publisher: John Wiley and Sons
• Year: 2009
• Tongue: English
• Weight: 525 KB
• Volume: 9
• Category: Article
• ISSN: 1616-5187
• DOI: 10.1002/mabi.200900147

✦ Synopsis

Abstract

The antitumor activity of a colon‐specific N‐(2‐hydroxypropyl)methacrylamide (HPMA) copolymer – 9‐aminocamptothecin (9‐AC) conjugate (P‐9‐AC) was assessed in orthotopic and subcutaneous animal (HT29 xenograft) tumor models. P‐9‐AC treatment of mice bearing orthotopic colon tumors, with a dose of 3 mg/kg of 9‐AC equivalent every other day for 6 weeks, resulted in regression of tumors in 9 of 10 mice. A lower dose of P‐9‐AC (1.25 mg/kg of 9‐AC equivalent) every other day for 8 weeks inhibited subcutaneous tumor growth in all mice. No liver metastases were observed. Colon‐specific release of 9‐AC from polymer conjugates enhanced antitumor activity and minimized the systemic toxicity.

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