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Design, Synthesis, and Evaluation of Glucose Transporter Inhibitor-SN38 Conjugates for Targeting Colorectal Cancer

Pei-Fang Chiu1, Chun-Kai Chang1, Pin-Shuo Huang1

  • 1School of Pharmacy, College of Medicine, National Taiwan University, Taipei 100, Taiwan.

Journal of Medicinal Chemistry
|July 6, 2023
PubMed

Insights

New SN38 conjugates targeting colorectal cancer show improved efficacy and reduced side effects. These novel drug conjugates deliver SN38 specifically to tumors, enhancing treatment outcomes with lower systemic exposure.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Irinotecan, a colorectal cancer treatment, has limited specificity and significant side effects.
  • SN38 is the active metabolite of irinotecan, responsible for its therapeutic effects.
  • Targeted drug delivery aims to improve cancer treatment efficacy and reduce toxicity.

Purpose of the Study:

  • To design and synthesize novel SN38 conjugates for enhanced colorectal cancer therapy.
  • To investigate the potential of glucose transporter inhibitors as targeting moieties for SN38 delivery.
  • To evaluate the antitumor efficacy and safety profile of these novel conjugates.

Main Methods:

  • Synthesis of SN38 conjugates with phlorizin or phloretin.
  • In vivo evaluation in an orthotopic colorectal cancer mouse model.
  • Assessment of antitumor efficacy, systemic SN38 exposure, and biodistribution.

Main Results:

  • Conjugates demonstrated superior antitumor efficacy compared to irinotecan.
  • Lower systemic exposure to SN38 was observed with the conjugates.
  • Biodistribution studies confirmed higher SN38 concentration in tumors with conjugate 10.
  • No significant adverse effects were noted during conjugate treatment.

Conclusions:

  • The developed SN38 conjugates show promise for improved colorectal cancer treatment.
  • Targeted delivery of SN38 via conjugates enhances therapeutic efficacy and reduces systemic toxicity.
  • These conjugates represent a potential advancement in colorectal cancer therapy.

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