活化標定之前趨藥物以產生高治療指數之癌症化學療法

High Therapeutic Index Chemotherapy of Cancer by Targeted Activation of Prodrugs

鄭秋敏(Chiu-min Cheng) ； 羅博倫(Steve R. Roffler) ； 鄭添祿(Tian-Lu Cheng)

《化學》 61卷4期 (2003/12) Pp. 611-620

https://doi.org/10.6623/chem.2003057

摘要

若能增加抗癌藥物對腫瘤的專一性，相信可大大改善化學療法的效率與安全性，針對此目的，目前已有幾個研究團隊朝這個目標發展，其中抗體標定酵素前驅藥物療法及基因(或病毒)表現酵素以活化前驅藥物療法最被看好。其策略是先選擇性傳送活化藥物的酵素基因或功能性蛋白質至腫瘤組織，當酵素標定表現於腫瘤組織後再系統性地打入相對非毒性的前驅藥物，使前驅藥物在腫瘤處被選擇性的活化為毒性的抗癌藥物以毒殺腫瘤細胞，此種具有選擇性的化學治療方式，預期將來在增加癌症化療指數上，將開啟新的領域。

關鍵字

前驅藥物 ； 抗體標定藥物前驅藥物療法 ； 基因（或病毒）表現前驅藥物療法

並列摘要

The efficacy of cancer chemotherapy may be greatly improved by increasing antineoplastic drug specificity for tumor cells. Several groups have developed to achieve this goal, including antibody-directed enzyme prodrug therapy (ADEPT) and Gene (or Virus)-directed enzyme prodrug therapy (G/VDEPT). The central part of enzyme/prodrug cancer therapy is to delivery drug-activating enzyme gene or functional protein to tumor tissues and a relatively non-toxic prodrug is systemically administered to allow selective enzymatic activation of the prodrug to highly toxic anti-neoplastic drug at the tumor site. The highly promising approach is expected to open a new area to increase the therapeutic index of chemotherapy.

並列關鍵字

prodrug ； Antibody-directed enzyme prodrug therapy (ADEPT) ； Gene (or Virus)-directed enzyme prodrug therapy (G/DEPT)