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09:19

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Published on: February 6, 2015

Prodrugs in Oncology: Bioactivation and Impact on Therapeutic Efficacy and Toxicity

Ritika Kurian1, Hongbing Wang1

  • 1Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, MD 21201, USA.

International Journal of Molecular Sciences
|February 13, 2025
PubMed

Insights

Prodrugs are inactive molecules that become active drugs within the body. This review explores chemotherapeutic prodrugs designed to improve cancer treatment efficacy and reduce side effects by targeting tumors more effectively.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Chemotherapy is a cornerstone of cancer treatment but suffers from poor selectivity and significant toxicity.
  • Prodrugs offer a strategy to overcome limitations in drug solubility, absorption, distribution, and stability.
  • Enzymatic bioactivation of prodrugs can enhance targeted delivery of chemotherapeutic agents to tumor sites.

Purpose of the Study:

  • To review commonly used chemotherapeutic prodrugs in oncology.
  • To discuss the clinical relevance and mechanisms of bioactivation for these prodrugs.
  • To highlight the toxicity concerns associated with prodrug strategies in cancer therapy.

Main Methods:

  • Literature review of established and emerging chemotherapeutic prodrugs.
  • Analysis of prodrug design principles for enhanced efficacy and reduced toxicity.
  • Examination of enzyme-mediated bioactivation pathways specific to the tumor microenvironment.

Main Results:

  • Chemotherapeutic prodrugs, including alkylating and non-alkylating agents, demonstrate potential for improved therapeutic outcomes.
  • Targeted activation within the tumor microenvironment can enhance drug bioavailability and efficacy.
  • Prodrug strategies aim to minimize systemic toxicity, thereby improving patient quality of life.

Conclusions:

  • Prodrugs represent a valuable approach to enhance the effectiveness of chemotherapy while mitigating adverse effects.
  • Further research into tumor-specific enzyme systems can optimize prodrug design for targeted cancer therapy.
  • Understanding prodrug bioactivation and toxicity is crucial for successful clinical application in oncology.
Keywords:
CYP P450active metabolitealkylationbioactivationchemotherapycytotoxicitypharmacokineticsprodrug

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