Maucher, A. und Angerer, E. von
(1993)
Antiproliferative activity of casodex (ICI 176.334) in hormone-dependent tumours.
Journal of cancer research and clinical oncology 119 (11), S. 669-674.
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Zusammenfassung
The nonsteroidal antiandrogen casodex has been described as a peripherally selective drug for the treatment of prostatic cancer. In this study we determined its activity in various models of hormone-dependent malignancies including those of the prostate and the breast. Analysis of endocrine effects in rats after 15 days of treatment revealed a strong reduction of the weights of prostates and ...
Zusammenfassung
The nonsteroidal antiandrogen casodex has been described as a peripherally selective drug for the treatment of prostatic cancer. In this study we determined its activity in various models of hormone-dependent malignancies including those of the prostate and the breast. Analysis of endocrine effects in rats after 15 days of treatment revealed a strong reduction of the weights of prostates and seminal vesicles and a significant rise of testosterone serum levels as a result of the interference with central feedback mechanisms. The growth of androgen-sensitive human LNCaP/FGC prostate cancer cells was strongly inhibited by casodex. Unlike hydroxyflutamide, casodex was also active in hormone-depleted medium. The inhibitory effect was overcome by addition of testosterone propionate, which indicates an androgen-receptor-mediated mode of action. In rats bearing Dunning R3327-G prostate carcinomas casodex exerted a strong antitumour effect at the beginning of therapy. However, after 4 weeks of treatment tumours resumed growth whereas diethylstilboestrol-treated tumours remained static. In MXT-M3.2 mouse mammary tumours with significant quantities of androgen receptors casodex was also effective in inhibiting tumour growth. After 6 weeks of treatment, tumour weights were reduced by 69% whereas uterine weights were significantly increased, possibly because of a progestin-like activity of the drug. Csodex is very active in various models of hormone-dependent carcinomas. However, the limited duration of action in prostatic tumours and the incomplete growth inhibition in mammary tumours suggest that it should be used only combination with other endocrine therapies.
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| Dokumentenart: | Artikel |
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| Datum: | 1993 |
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| Institutionen: | Chemie und Pharmazie > Institut für Pharmazie > Lehrstuhl Pharmazeutische / Medizinische Chemie II (Prof. Buschauer) |
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| Identifikationsnummer: | | Wert | Typ |
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| 8349724 | PubMed-ID | | 10.1007/BF01215986 | DOI |
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| Klassifikation: | | Notation | Art |
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| Androgen Antagonists/pharmacology | MESH | | Anilides/pharmacology | MESH | | Animals | MESH | | Antineoplastic Agents/pharmacology | MESH | | Antineoplastic Combined Chemotherapy Protocols/therapeutic use | MESH | | Cell Division/drug effects | MESH | | Diethylstilbestrol/therapeutic use | MESH | | Female | MESH | | Flutamide/pharmacology | MESH | | Male | MESH | | Mammary Neoplasms, Experimental/drug therapy | MESH | | Mice | MESH | | Neoplasms, Hormone-Dependent/drug therapy | MESH | | Nitriles | MESH | | Prostatic Neoplasms/drug therapy | MESH | | Rats | MESH | | Rats, Inbred F344 | MESH | | Receptors, Androgen/metabolism | MESH | | Testosterone/antagonists & inhibitors | MESH | | Tosyl Compounds | MESH | | Tumor Cells, Cultured/drug effects | MESH |
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| Stichwörter / Keywords: | Nonsteroidal antiandrogen; LNCaP prostate carcinoma cells; Dunning R3327-G tumour; MXT mouse mammary tumour |
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| Dewey-Dezimal-Klassifikation: | 500 Naturwissenschaften und Mathematik > 570 Biowissenschaften, Biologie
500 Naturwissenschaften und Mathematik > 540 Chemie |
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| Status: | Veröffentlicht |
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| Begutachtet: | Ja, diese Version wurde begutachtet |
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| An der Universität Regensburg entstanden: | Ja |
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| Eingebracht am: | 01 Dez 2008 16:54 |
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| Zuletzt geändert: | 08 Mrz 2017 08:19 |
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| Dokumenten-ID: | 4758 |
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