Biological profile of cortexolone 17α-propionate (CB-03-01), a new topical and peripherally selective androgen antagonist

Arzneimittel-Forschung/Drug Research

Volumn 54, Issue 12, 2004, Pages 881-886

  Celasco, Giuseppe ^a   Moro, Luigi ^a   Bozzella, Roberta ^a   Ferraboschi, Patrizia ^b   Bartorelli, Luisa ^a   Quattrocchi, Cinzia ^c   Nicoletti, Ferdinando ^c  

^a Cosmo SPA ^*  (Italy)

^b UNIVERSITY OF MILAN   (Italy)

^c UNIVERSITY OF CATANIA   (Italy)

Author keywords

Antiandrogens; CAS 19608 29 8; CB 03 01, antiandrogenic activity, hamster, rat; Cortexolone 17 propionate

Indexed keywords

ANDROSTANOLONE; ANTIANDROGEN; CB 03 01; CORTEXOLONE 17ALPHA PROPIONATE; CORTICOSTERONE; CORTODOXONE; CYPROTERONE ACETATE; FINASTERIDE; FLUTAMIDE; TESTOSTERONE PROPIONATE; UNCLASSIFIED DRUG;

ANDROGEN METABOLISM; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; CORTICOSTERONE BLOOD LEVEL; DRUG POTENCY; FEMALE; GONADOTROPIN RELEASE; HORMONAL REGULATION; HORMONE RECEPTOR INTERACTION; MALE; NONHUMAN; RAT; SYRIAN HAMSTER;

EID: 10644266755     PISSN: 00044172     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0031-1297043     Document Type: Article

References (17)

1. Chen, W., Thiboutot, D., Zouboulis, C. C., Cutaneous androgen metabolism: basic research and clinical perspectives. J. Invest. Dermatol. 119, 992 (2002)
2. Darley, C. R., Kirby J. D., Besser, G. M. et al., Circulating testosterone, sex hormone binding globulin and prolactin in women with the late onset or persistent acne vulgaris. Br. J. Dermatol. 106, 517 (1982)
3. Barth, J. H., Alopecia and hirsutism. Current concepts in pathogenesis and management. Drugs 35, 83 (1988)
4. Sansone, G., Reisner, R. M., Differential rates of conversion of testosterone to dihydrotestosterone in acne and in normal human skin. A possible pathogenic factor in acne. J. Invest. Dermatol. 56, 366 (1971)
5. Price, V. H., Testosterone metabolism in the skin. Arch. Dermatol. 111, 1496 (1975)
6. Chen, C., Li, X., Singh, S. M. et al., Activity of 17β-[(N-alkyl/ aryl) alkyl/arylamido]-4-methyl-4-aza-5α-androstan-3-ones as 5a-reductase inhibitors in the hamster flank organ and ear. J. Invest. Dermatol. 111, 273 (1998)
7. Brooks, J. R., Primka, R. L., Berman, C. et al., Topical anti-androgenicity of a new 4-azasteroid in the hamster. Steroids 56, 428 (1991)
8. Voigt, W., Hsia S. L., The antiandrogenic action of 4-and-rosten-3-one- 17β-carboxylic acid and its methyl ester on hamster flank organ. Endocrinology 92, 1216 (1973)
9. 4-5α-reductase (41309). Proc. Soc. Exp. Biol. Med. 169, 67 (1982)
10. Sager, D. B., Schuetz, A. W., Meyer, R. K., Effect of estrone and progestational steroids on human chorionic gonadotrophin (HCG)-induced ovarian augmentation in parabiotic rats. Endocrinology 78, 445 (1966)
11. Mattingly, D. A., simple fluorimetric method for the estimation of free 11-hydroxycorticoids in human plasma. J. Clin. Path. 15, 374 (1962)
12. Glenn, E. M., Richardson, S. L., Bowman, B. J., Biologic activity of 6-alpha-methyl compounds corresponding to progesterone, 17-alpha- hydroxyprogesterone acetate and compound S. Metabolism 8, 265 (1959)
13. Chen, C., Puy, L. A., Simard, J. et al., Local and systemic reduction by topical finasteride or flutamide of hamster flank organ size and enzyme activity. J. Invest. Dermatol. 105, 678 (1995)
14. Purr, B. J., Tucker, H., The preclinical development of bicalutamide: pharmacodynamics and mechanism of action. Urology 47 (Suppl. 1A), 13 (1996)
15. Smith, M. R., Osteoporosis during androgen deprivation therapy for prostate cancer. Urology 60 (3 Suppl. 1), 79 (2002)
16. Reid, P., Kantoff P., Oh, W., Antiandrogens in prostate cancer. Invest. New. Drugs 17, 271 (1999)
17. Poyet, P., Labrie, E, Comparison of the antiandrogenic/androgenic activities of flutamide, cyproterone acetate and megestrol acetate. Mol. Cell. Endocrinol. 42, 283 (1985)