The Role of 5-alpha Reductase in Mediating Testosterone Actions (5aR)

clinicaltrials.gov/ct2/show/NCT00493987

Responsible Party: Boston University Medical Center ( Dr. Shalender Bhasin )
ClinicalTrials.gov Identifier: NCT00493987 History of Changes
Other Study ID Numbers: R01HD043348, R01HD043348
Study First Received: June 28, 2007
Last Updated: May 12, 2010 (STUDY COMPLETED)
Health Authority: United States: Food and Drug Administration

[b]Testosterone, the predominant circulating androgen in men, also serves as a prohormone that is converted in the body to two active metabolites, estradiol 17 β and 5-α DHT (DHT). Testosterone serves as the active hormone in some target tissues; however, androgen effects in other target organs require its conversion to estradiol or DHT. The role of 5-α reduction of testosterone in mediating its effects on the muscle and sexual function remains unclear. Therefore, the primary objective of this project is to determine whether 5-α reduction of testosterone to DHT is obligatory for mediating its effects on fat-free mass, muscle size, muscle strength, and leg power in men. The secondary objective is to determine whether 5-α reduction of testosterone is necessary for maintenance of androgen effects on sexual function (sexual desire, overall sexual activity, nocturnal penile tumescence (NPT), response to visual erotic stimulus, and penile rigidity) in men. In order to test these hypotheses about the role of 5-α reduction, we will compare testosterone dose response curves for each outcome measure in the absence and presence of a novel, potent 5-α reductase inhibitor (dutasteride) that inhibits both type 1 and type 2 steroid 5-α -reductase isoenzymes. Healthy young men, 21-40 years of age, will be treated with a long acting GnRH agonist to suppress endogenous testosterone production, and concomitantly, randomly assigned to one of 8 groups: group 1, testosterone enanthate (TE) 50-mg weekly, plus placebo tablets daily; group 2, TE 125-mg weekly plus placebo daily; group 3, TE 300-mg weekly plus placebo daily; group 4, TE 600 mg TE weekly plus placebo; group 5, 50-mg weekly, plus dutasteride 2.5-mg daily; group 6, TE 125-mg weekly, plus dutasteride daily; group 7, TE 300 mg weekly, plus dutasteride daily; group 8, 600-mg TE plus dutasteride daily. Energy and protein intake, and exercise stimulus will be standardized. The following outcomes will be measured at baseline and after 20 weeks: body composition by DEXA scan, deuterium oxide and sodium bromide dilution; thigh muscle volume by MRI scan; muscle performance by measurements of 1-repetition maximum strength and leg power; sexual function by International Index of Erectile Function, Sexual Desire Inventory, and daily logs of sexual activity; and penile erections and rigidity during EEG-coupled, NPT recoding and in response to a visual erotic stimulus; total and free testosterone, DHT, estradiol, SHBG, and LH levels. For safety, we will follow hemoglobin/hematocrit, sleep apnea scores, AST and ALT, PSA, plasma lipids, apolipoproteins, and lipoprotein particles, and prostate examinations. A multi-disciplinary team of investigators, the use of a previously validated “Leydig Cell Clamp” model, the use of a potent inhibitor of both subtypes of 5-alpha reductase enzyme, attention to potential confounding variables such as energy intake and exercise stimulus, and power and effect size should help elucidate the role of 5-alpha reduction in mediating androgen action. This study will enhance our understanding of the biologic role of the steroid 5-alpha-reductase system, and has immediate clinical relevance in establishing whether selective androgen receptor modulators(SARM) that do not undergo 5-alpha reduction would be useful as anabolic agents.

Eligibility

Ages Eligible for Study: 18 Years to 50 Years
Genders Eligible for Study: Male
Accepts Healthy Volunteers: Yes

Criteria
Inclusion Criteria:

•Healthy males between 18 and 50 years of age.
•Ambulatory, physically active, but not in competitive sports.
•Eugonadal: Normal Serum Testosterone (300-1100 nmol/L).
•Normal LH
•Normal FSH
•Able and willing to comply with the trial protocol.
Exclusion Criteria:

•Known to have a primary or secondary hypogonadism? (e.g. pituitary disease, HIV infection, Klinefelter’s Syndrome)
•BMI > 35
•Disability that precludes participation in exercise testing
•Alcohol or illicit drug use in the preceding 6 months that would interfere with participation and compliance with the protocol
•Known disorder that would be exacerbated by androgen treatment e.g. benign prostate hyperplasia, prostate Ca, erythrocytosis, sleep apnea)
•Any abnormalities in the following laboratory tests PSA > 4 ng/ml AST, ALT or Alkaline Phosphatase > 3x ULN? Creatinine level > 2 mg/dL Hematocrit > 51%
•Osteoporosis by DEXA BMD T-Score < -2.5
•Use of medications that affect muscle or bone metabolism within the previous 3 months ?(e.g. glucocorticoids, growth hormone, androgenic steroids, oral androgen precursors -i.e. androstenedione or DHEA)
•Use of medications that affect androgen metabolism, action or clearance within the previous 3 months? (e.g. dilantin, phenobarbital, aldactone, flutamide, finasteride and Ketoconazole)
•Use of ketoconazole or other potent CYP3A4 inhibitors that may affect clearance of dutasteride
•Use investigational medication as part of a research study in the last 3 months?

did you find the results for this?

No but supposely the study is complete…It would be interesting to see the SARM results though.

I am gonna call this guy Dr. Shalender Bhasin and see if he will give me the results of the study!

i called him but he is on vacation. the nurse gave me the email for him but i think she gave me the wrong address. I really cant wait to get a hold of this! gene expression change takes and wont accept the testosterone might accept something else… if i am understanding this right he is looking to find out if there is a way to modulate the androgen receptors another way - i think like nolvadex is for estrogen… EDIT I just noticed that it says “useful as an anabolic agent” not as an androgenic agent

Keep on this…That’s my thinking bro…

We are getting close…

someone from their office at Boston Medical just left gave me the number to his assistant and I called and left a message for her…