Effect of an Endothelin B Receptor Agonist on the Tumor Accumulation of Nanocarriers

Haitao Feng, Le Thanh Nam, Takuma Yoshikawa, Akihiro Kishimura, Takeshi Mori, Yoshiki Katayama

Research output: Contribution to journalArticlepeer-review


Enhancing blood flow to tumors is a prominent strategy for improving the tumor accumulation of macromolecular drugs through the enhanced permeability and retention (EPR) effect. IRL-1620 is an agonist of the endothelin B receptor, and is a promising molecule to enhance tumor blood flow by activating endothelial nitric oxide synthase. However, contradictory effects on tumor blood flow modulation have been reported because the effects of IRL-1620 may differ in different animal models. Here, we examined for the first time the effect of IRL-1620 on the EPR effect for PEGylated liposomes in a CT-26 murine colon cancer model. Co-injection of IRL-1620 at an optimum dose (3 nmol/kg) nearly doubled the tumor accumulation of liposomes compared with controls, indicating that IRL-1620 enhanced the EPR effect in the present colon cancer model. Co-injection of IRL-1620 is a promising strategy to improve the therapeutic effects of macromolecular drugs while reducing their side effects.

Original languageEnglish
Pages (from-to)1301-1305
Number of pages5
JournalBiological & pharmaceutical bulletin
Issue number9
Publication statusPublished - 2020

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmaceutical Science


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