Chemotherapy targeted to cancers through tumoral hormone receptors

Trends Endocrinol Metab. 2004 Sep;15(7):300-10. doi: 10.1016/j.tem.2004.07.002.


Work on cytotoxic analogs of luteinizing hormone-releasing hormone (LH-RH), somatostatin and bombesin, designed for targeting chemotherapy to peptide receptors on various cancers, is reviewed here as the project is at advanced stages of development and clinical trials are pending. Cytotoxic analogs of LH-RH, AN-152 and AN-207, containing doxorubicin (DOX) or 2-pyrrolino-DOX (AN-201), respectively, target LH-RH receptors and can be used for the treatment of prostatic, breast, ovarian and endometrial cancers and melanomas. AN-201 was also incorporated into the cytotoxic analog of somatostatin, AN-238, which can be targeted to receptors for somatostatin in prostatic, renal, mammary, ovarian, gastric, colorectal and pancreatic cancers as well as glioblastomas and lung cancers, suppressing the growth of these tumors and their metastases. A cytotoxic analog of bombesin AN-215, containing 2-pyrrolino-DOX, was likewise synthesized and successfully tested in experimental models of prostate cancer, small cell lung carcinoma, gastrointestinal cancers and brain tumors expressing receptors for bombesin/gastrin-releasing peptide. This new class of targeted cytotoxic peptide analogs might provide a more effective therapy for various cancers.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents, Hormonal / therapeutic use*
  • Bombesin / analogs & derivatives
  • Bombesin / therapeutic use
  • Drug Delivery Systems*
  • Gastrin-Releasing Peptide / analogs & derivatives
  • Gastrin-Releasing Peptide / therapeutic use
  • Gonadotropin-Releasing Hormone / analogs & derivatives
  • Gonadotropin-Releasing Hormone / therapeutic use
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism*
  • Receptors, Cell Surface / drug effects*
  • Somatostatin / analogs & derivatives
  • Somatostatin / therapeutic use


  • Antineoplastic Agents, Hormonal
  • Receptors, Cell Surface
  • Gonadotropin-Releasing Hormone
  • Somatostatin
  • Gastrin-Releasing Peptide
  • Bombesin