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[Irinotecan hydrochloride (CPT-11)]

H Furue1

  • 1Fourth Dept. of Internal Medicine, Teikyo University School of Medicine, Kawasaki, Japan.

Gan to Kagaku Ryoho. Cancer & Chemotherapy
|April 1, 1994
PubMed
Summary

Irinotecan hydrochloride (CPT-11) is a potent chemotherapy drug that shows effectiveness against various cancers. Its active metabolite, SN-38, is significantly more potent, supporting its use in combination therapy trials.

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Area of Science:

  • Oncology
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Irinotecan hydrochloride (CPT-11) is a semi-synthetic derivative of camptothecin.
  • CPT-11 functions as a prodrug, converting to the highly potent metabolite SN-38 in vivo.
  • SN-38 exhibits 1,000-fold greater in vitro potency compared to its parent compound.

Purpose of the Study:

  • To highlight the efficacy of Irinotecan hydrochloride (CPT-11) as a topoisomerase I inhibitor.
  • To summarize the broad spectrum of experimental antitumor activity observed with CPT-11.
  • To present clinical findings supporting CPT-11's effectiveness in treating various cancers.

Main Methods:

  • Review of experimental data on CPT-11's mechanism of action.
  • Analysis of in vitro potency of CPT-11 and its metabolite SN-38.
  • Evaluation of clinical trial results for CPT-11 in cancer treatment.

Main Results:

  • CPT-11 demonstrates potent topoisomerase I inhibition.
  • Significant experimental antitumor activity has been documented for CPT-11.
  • Clinical trials indicate CPT-11 is effective against lung, cervix, and ovary cancers.

Conclusions:

  • Irinotecan hydrochloride (CPT-11) is a clinically effective chemotherapeutic agent.
  • The potent metabolite SN-38 contributes to CPT-11's anticancer activity.
  • Comparative trials of combination chemotherapy are warranted based on CPT-11's success.

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