New approaches to treatment of various cancers based on cytotoxic analogs of LHRH, somatostatin and bombesin

Life Sci. 2003 Apr 11;72(21):2305-20. doi: 10.1016/s0024-3205(03)00113-9.


The development of targeted cytotoxic analogs of hypothalamic peptides for the therapy of various cancers is reviewed and various oncological studies on experimental tumors are summarized. Novel therapeutic modalities for breast, prostate and ovarian cancer consist of the use of targeted cytotoxic analogs of LH-RH containing doxorubicin (DOX) or 2-pyrrolino-DOX. The same radicals have been incorporated into cytotoxic analogs of somatostatin which can be also targeted to receptors for this peptide in prostatic, mammary, ovarian, renal and lung cancers, brain tumors and their metastases. A targeted cytotoxic analog of bombesin containing 2-pyrrolino-DOX has also been synthesized and successfully tried in experimental models of prostate cancer, small cell lung carcinoma and brain tumors. The development of these new classes of peptide analogs should lead to a more effective treatment for various cancers.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use*
  • Bombesin / analogs & derivatives*
  • Bombesin / chemistry
  • Cytotoxins / chemistry
  • Cytotoxins / therapeutic use*
  • Disease Models, Animal
  • Doxorubicin / analogs & derivatives
  • Doxorubicin / chemistry
  • Drug Delivery Systems
  • Gonadotropin-Releasing Hormone / analogs & derivatives*
  • Gonadotropin-Releasing Hormone / chemistry
  • Humans
  • Neoplasms, Experimental / drug therapy*
  • Somatostatin / analogs & derivatives*
  • Somatostatin / chemistry


  • Antineoplastic Agents
  • Cytotoxins
  • Gonadotropin-Releasing Hormone
  • Somatostatin
  • Doxorubicin
  • Bombesin