Use of Cyproterone Acetate in Prostate Cancer

Goldenberg, S. Larry; Bruchovsky, Nicholas

doi:10.1016/s0094-0143(21)01398-7

Cited by 70 publications

(4 citation statements)

References 41 publications

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“…The steroidal antiandrogens possess partial agonistic activity and overlapping effects with other hormonal systems, leading to many complications including severe cardiovascular problems, gynecomastia, loss of libido, and erectile dysfunction. [4][5][6] The nonsteroidal antiandrogens show fewer side effects and have improved oral bioavailability; therefore, they are favored over the steroidal antiandrogens. However, antiandrogen withdrawal syndrome has been discovered in patients receiving nonsteroidal antiandrogens for several months.…”

Section: Introductionmentioning

confidence: 99%

“…The therapeutic agents used clinically include steroidal antiandrogens, such as cyproterone acetate, and nonsteroidal antiandrogens, such as flutamide and bicalutamide. The steroidal antiandrogens possess partial agonistic activity and overlapping effects with other hormonal systems, leading to many complications including severe cardiovascular problems, gynecomastia, loss of libido, and erectile dysfunction. − The nonsteroidal antiandrogens show fewer side effects and have improved oral bioavailability; therefore, they are favored over the steroidal antiandrogens. However, antiandrogen withdrawal syndrome has been discovered in patients receiving nonsteroidal antiandrogens for several months. , Long-term drug usage probably leads to mutation of the AR, and the nonsteroidal antiandrogens now exhibit agonistic activity to the mutant AR …”

Section: Introductionmentioning

confidence: 99%

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Antitumor Agents. 250. Design and Synthesis of New Curcumin Analogues as Potential Anti-Prostate Cancer Agents

et al. 2006

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In a continuing study of curcumin analogues as potential drug candidates to treat prostate cancer at both androgen-dependent and androgen-refractory stages, we designed and synthesized over 40 new analogues classified into four series: monophenyl analogues (series A), heterocycle-containing analogues (series B), analogues bearing various substituents on the phenyl rings (series C), and analogues with various linkers (series D). These new compounds were tested for cytotoxicity against two human prostate cancer cell lines, androgen-dependent LNCaP and androgen-independent PC-3. Antiandrogenic activity was also evaluated in LNCaP cells and PC-3 cells transfected with wild-type androgen receptor. Ten compounds possessed potent cytotoxicity against both LNCaP and PC-3 cells, seven only against LNCaP, and one solely against PC-3. This study established an advanced structure-activity relationship (SAR), and these correlations will guide the further design of new curcumin analogues with better anti-prostate cancer activity.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Antitumor Agents. 250. Design and Synthesis of New Curcumin Analogues as Potential Anti-Prostate Cancer Agents

et al. 2006

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“…After taking a history and performing a clinical evaluation of the lesions, tumor sections were taken from the diagnosed animals for histopathological examination and immunohistochemical assessment of AR and ER receptors using a 0.6 cm diameter skin trepan. Histopathological examination carried out according to the histological classification of skin tumors according to AFIP/WHO revealed 24 adenomas, 12 epitheliomas, and five carcinomas [16]. The immunohistochemical staining showed mainly nuclear expression of AR and ER in the neoplastic cells.…”

Section: Methodsmentioning

confidence: 99%

Pharmacological Treatment of Perianal Gland Tumors in Male Dogs

Brodzki

Łopuszyński

Brodzki

et al. 2023

Animals

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The presence of androgen (AR) and estrogen (ER) receptors has been demonstrated both in normal perianal (hepatoid) glands and in perianal tumors. The aim of this study was to demonstrate the relationship between the expression of AR and ER in perianal gland tumors and the effectiveness of antihormonal treatment. The study was performed on 41 male dogs with neoplastic lesions of the anal region. Histopathological evaluation of the lesions revealed 24 adenomas, 12 epitheliomas, and five carcinomas. Treatment was administered orally with tamoxifen at a dose of 1 mg/kg BW and cyproterone acetate at a dose of 5 mg/kg. Tumor diameters were measured regularly with calipers and recorded in millimeters starting with the measurement before treatment, and then after 1, 2, 3, 6, 12, 18, and 24 months of therapy. The results show that hepatoid adenomas that are characterized by high expression of AR and ER receptors respond positively to antihormonal therapy, resulting in complete tumor regression. For locally malignant hepatoid epitheliomas and carcinomas with low expression of AR and ER receptors, antihormonal therapy makes it possible to reduce the size of the tumor, but does not make it possible to cure it completely.

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“…Cyproterone is an antiandrogen that suppresses the actions of testosterone. It blocks androgen receptors, and its acetate form is used in the treatment of hypersexuality in males, treatment of prostate cancer (Goldenberg and Bruchovsky, 1991;Neumann and Kalmus, 1991), and, in combination with estrogen, for the therapy of hyperandrogenism (e.g. severe acne and hirsutism) in females (van der Spuy et al, 2003).…”

Section: Introductionmentioning

confidence: 99%