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Updated: Aug 8, 2026
Electrochemotherapy of Tumours
Published on: December 15, 2008
Chemotherapy targeted to cancers through tumoral hormone receptors
Andrew V Schally1, Attila Nagy
1Endocrine, Polypeptide and Cancer Institute, Veterans Affairs Medical Center and Department of Medicine, Tulane University School of Medicine, New Orleans, LA 70112, USA. dcallai@tulane.edu
Abstract:
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.
Insights
Targeted chemotherapy using peptide analogs shows promise for treating various cancers. These novel cytotoxic agents are nearing clinical trials, offering a potential new therapeutic avenue for difficult-to-treat tumors.
Area of Science:
- Oncology
- Medicinal Chemistry
- Pharmacology
Background:
- Peptide receptors are overexpressed on various cancer cells, presenting a target for drug delivery.
- Luteinizing hormone-releasing hormone (LH-RH), somatostatin, and bombesin receptors are found on numerous cancer types.
Purpose of the Study:
- To review the development of cytotoxic peptide analogs for targeted cancer therapy.
- To evaluate the potential of these analogs in preclinical and clinical settings.
Main Methods:
- Synthesis of cytotoxic analogs of LH-RH, somatostatin, and bombesin.
- Incorporation of cytotoxic agents like doxorubicin (DOX) and 2-pyrrolino-DOX into peptide carriers.
- Testing of analogs in experimental models of various cancers.
Main Results:
- LH-RH analogs (AN-152, AN-207) target LH-RH receptors for prostatic, breast, ovarian, endometrial cancers, and melanomas.
- Somatostatin analog (AN-238) targets somatostatin receptors for prostatic, renal, mammary, ovarian, gastric, colorectal, pancreatic cancers, glioblastomas, and lung cancers.
- Bombesin analog (AN-215) targets bombesin/gastrin-releasing peptide receptors for prostate cancer, small cell lung carcinoma, gastrointestinal cancers, and brain tumors.
Conclusions:
- Cytotoxic peptide analogs represent a promising new class of targeted cancer therapeutics.
- These agents are advanced in development, with clinical trials pending.
- Targeted delivery may improve efficacy and reduce side effects in cancer treatment.
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