Steady-state pharmacokinetics of oral testosterone undecanoate with concomitant inhibition of 5α-reductase by finasteride

International Journal of Andrology

Volumn 34, Issue 6 PART 1, 2011, Pages 541-547

  Roth, M Y ^a   Dudley, R E ^b   Hull, L ^c   Leung, A ^c   Christenson, P ^c   Wang, C ^c   Swerdloff, R ^c   Amory, J K ^a  

^a UNIVERSITY OF WASHINGTON   (United States)

^b Clarus Therapeutics Inc   (United States)

^c LOS ANGELES BIOMEDICAL RESEARCH INSTITUTE   (United States)

Author keywords

5 reductase; Androgen; Dihydrotestosterone (DHT); Drug delivery; Oestradiol

Indexed keywords

ANDROSTANOLONE; ESTRADIOL; FINASTERIDE; STEROID 5ALPHA REDUCTASE; TESTOSTERONE; TESTOSTERONE UNDECANOATE;

ADULT; ARTICLE; CONTROLLED STUDY; CROSSOVER PROCEDURE; DEPRESSION; DRUG INDUCED HEADACHE; DYSPEPSIA; ESTRADIOL BLOOD LEVEL; EVENING DOSAGE; GASTROESOPHAGEAL REFLUX; HOT FLUSH; HUMAN; HUMAN EXPERIMENT; HYPOGONADISM; MALE; MAXIMUM PLASMA CONCENTRATION; MONOTHERAPY; MORNING DOSAGE; NORMAL HUMAN; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SCROTAL PAIN; STEADY STATE; TESTOSTERONE BLOOD LEVEL;

ADMINISTRATION, ORAL; ADOLESCENT; ADULT; CHOLESTENONE 5 ALPHA-REDUCTASE; CROSS-OVER STUDIES; DIHYDROTESTOSTERONE; ENZYME INHIBITORS; FINASTERIDE; HUMANS; MALE; MIDDLE AGED; TESTOSTERONE; YOUNG ADULT;

EID: 81455131693     PISSN: 01056263     EISSN: 13652605     Source Type: Journal    
DOI: 10.1111/j.1365-2605.2010.01120.x     Document Type: Article

References (33)

1. Amory JK & Bremner WJ. (2005) Oral testosterone in oil plus dutasteride: a pharmacokinetic study in men. J Clin Endocrinol Metab 90, 2610-2617.
2. Amory JK, Page ST & Bremner WJ. (2006) Oral testosterone in oil: pharmacokinetic effects of 5α-reduction with finasteride or dutasteride and food intake in men. J Androl 27, 72-78.
3. Amory JK, Wang C, Swerdloff RS, Anawalt BD, Matsumoto AM, Bremner WJ, Walker SE, Haberer LJ & Clark RV. (2007) The effect of 5α-reductase inhibition with dutasteride and finasteride on semen parameters and serum hormones in healthy men. J Clin Endocrinol Metab 92, 1659-1665.
4. Amory JK, Kalhorn TF & Page ST. (2008) Pharmacokinetics and pharmacodynamics of oral testosterone enanthate in oil plus dutasteride for four weeks in normal men: implications for male hormonal contraception. J Androl 29, 260-271.
5. Andriole GL, Bostwick DG, Brawley OW, Gomella LG, Marberger M, Montorsi F et al. (2010) Effect of dutasteride on the risk of prostate cancer. N Engl J Med 362, 1192-1202.
6. Araujo AB, Esche GR, Kupelian V, O'Donnell AB, Travison TG, Williams RE, Clark RV & McKinlay JB. (2007) Prevalence of symptomatic androgen deficiency in men. J Clin Endocrinol Metab 92, 4241-4247.
7. Bramson HN, Hermann D, Batchelor KW, Lee FW, James MK & Frye SV. (1997) Unique preclinical characteristics of GG745, a potent dual inhibitor of 5AR. J Pharmacol Exp Ther 282, 1496-1502.
8. Carlin JR, Höglund P, Eriksson LO, Christofalo P, Gregoire SL, Taylor AM & Andersson KE. (1992) Disposition and pharmacokinetics of [14C] finasteride after oral administration in humans. Drug Metab Dispos 20, 148-155.
9. Coert A, Geelen J, de Visser J & van der Vies J. (1975) The pharmacology and metabolism of testosterone undecanoate (TU), a new orally active androgen. Acta Endocrinol (Copenh) 79, 789-800.
10. Daggett PR, Wheeler MJ & Nabarro JDN. (1978) Oral testosterone, a reappraisal. Hormone Res 9, 121-129.
11. Franchimont P, Kicovic PM, Mattei A & Roulier R. (1978) Effects of oral testosterone undecanoate in hypogonadal male patients. Clin Endocrinol (Oxf) 9, 313-320.
12. Friedl KE, Hannan CJ, Jr, Jones RE & Plymate SR. (1990) High-density lipoprotein cholesterol is not decreased if an aromatizable androgen is administered. Metabolism 39, 69-74.
13. Gann PH, Hennekens CH, Ma J, Longcope C & Stampfer MJ. (1996) Prospective study of sex hormone levels and risk of prostate cancer. J Natl Cancer Inst 88, 1118-1126.
14. Gill JK, Wilkens LR, Pollak MN, Stanczyk FZ & Kolonel LN. (2010) Androgens, growth factors, and risk of prostate cancer: the multiethnic cohort. Prostate 70, 906-915.
15. Gooren LJ. (1994) A ten-year safety study of the oral androgen testosterone undecanoate. J Androl 15, 212-215.
16. Herbst KL, Coviello AD, Page ST, Amory JK, Anawalt BD & Bremner WJ. (2004) A single dose of the potent gonadotropin-releasing hormone antagonist acyline suppresses gonadotropins and testosterone for 2weeks in healthy young men. J Clin Endocrinol Metab 89, 5959-5965.
17. Hong BS & Ahn TY. (2007) Recent trends in the treatment of testosterone deficiency syndrome. Int J Urol 14, 981-985.
18. Horst HJ, Holtje WJ, Dennis M, Coert A, Geelen J & Voigt KD. (1976) Lymphatic absorption and metabolism of orally administered testosterone undecanoate in man. Klin Wochenschr 54, 875-879.
19. Houwing NS, Maris F, Schnabel PG & Bagchus WM. (2003) Pharmacokinetic study in women of three different doses of a new formulation of oral testosterone undecanoate, Andriol Testocaps. Pharmacotherapy 23, 1257-1265.
20. Katznelson L, Finkelstein JS, Schoenfeld DA, Rosenthal DI, Anderson EJ & Klibanski A. (1996) Increase in bone density and lean body mass during testosterone administration in men with acquired hypogonadism. J Clin Endocrinol Metab 81, 4358-4365.
21. Maisey NM, Bingham J, Marks V, English J & Chakraborty J. (1981) Clinical efficacy of testosterone undecanoate in male hypogonadism. Clin Endocrinol (Oxf) 14, 625-629.
22. Nieschlag E, Mauss J, Coert A & Kicovic P. (1975) Plasma androgen levels in men after oral administration of testosterone and testosterone undecanoate. Acta Endocrinol (Copenh) 79, 366-374.
23. Page ST, Lin DW, Mostaghel E, Marck B, Wright J, Wu J, Amory JK, Nelson PS & Matsumoto AM. (2010) Exogenous dihydrotestosterone does not increase intraprostatic dihydrotestosterone concentrations or androgen action in healthy men: a randomized-controlled trial. Poster P1-388 presented at the 90th Annual Meeting of the Endocrine Society, San Diego, CA.
24. Schnabel PG, Bagchus W, Lass H, Thomsen T & Geurts TB. (2007) The effect of food composition on serum testosterone levels after oral administration of Andriol Testocaps. Clin Endocrinol (Oxf) 66, 579-585.
25. Shiraishi S, Lee PW, Leung A, Goh VH, Swerdloff RS & Wang C. (2008) Simultaneous measurement of serum testosterone and dihydrotestosterone by liquid chromatography-tandem mass spectrometry. Clin Chem 54, 1855-1863.
26. Skakkebaek NE, Bancroft J, Davidson DW & Warner P. (1981) Androgen replacement with oral testosterone undecanoate in hypogonadal men: a double blind controlled study. Clin Endocrinol (Oxf) 14, 49-61.
27. Snyder PJ, Peachey H, Berlin JA, Hannoush P, Haddad G, Dlewati A et al. (2000) Effects of testosterone replacement in hypogonadal men. J Clin Endocrinol Metab 85, 2670-2677.
28. Steiner JF. (1996) Clinical pharmacokinetics and pharmacodynamics of finasteride. Clin Pharmacokinet 30, 16-27.
29. Swerdloff RS, Wang C, Cunningham G, Dobs A, Iranmanesh A, Matsumoto AM, Snyder PJ, Weber T, Longstreth J & Berman N. (2000) Long-term pharmacokinetics of transdermal testosterone gel in hypogonadal men. J Clin Endocrinol Metab 85, 4500-4510.
30. Thompson IM, Goodman PJ, Tangen CM, Lucia MS, Miller GJ, Ford LG et al. (2003) The influence of finasteride on the development of prostate cancer. New Engl J Med 349, 215-224.
31. Turani H, Levi J, Zevin D & Kessler E. (1983) Hepatic lesions in patients on anabolic androgenic therapy. Isr J Med Sci 19, 332-337.
32. Wang C, Alexander G, Berman N, Salehian B, Davidson T, McDonald V, Steiner B, Hull L, Callegari C & Swerdloff RS. (1996) Testosterone replacement therapy improves mood in hypogonadal men - a clinical research center study. J Clin Endocrinol Metab 81, 3578-3583.
33. Westaby D, Ogle SJ, Paradinas FJ, Randell JB & Murray-Lyon IM. (1977) Liver damage from long-term methyltestosterone. Lancet 2, 262-263.