ACY-7 Oral Administration of Acyline
Study Details
Study Description
Brief Summary
We propose oral dosing of gastrointestinal permeation enhancement technology [GIPET] enhanced oral acyline at 20 mg everyday for one week to determine the steady-state (multiple-dose) pharmacokinetics of oral acyline in four normal, healthy young men.
| Condition or Disease | Intervention/Treatment | Phase |
|---|---|---|
| Phase 1/Phase 2 |
Detailed Description
The purpose of this study is to test how the body responds to a new oral form of acyline given for seven days and to also look at the safety of oral acyline.
Acyline temporarily blocks the production of the hormone testosterone in healthy men. It has been tested in over 100 men in an injection form. This study will be testing acyline in a pill form for seven days.
This study may help develop an oral form of testosterone-blocker which may be useful in the treatment of diseases such as prostate cancer, premature puberty and possibly in a male contraceptive.
This study will evaluate a single dose of oral acyline given once a day for seven days and subsequent effects on Testosterone, FSH and LH blood serum concentrations.
Study Design
Outcome Measures
Primary Outcome Measures
- Testosterone Blood Serum Concentration [7 days]
Blood for measurement of serum testosterone was obtained prior to the 1st, 5th and 6th dose of GIPET™-enhanced oral acyline and 0.5,1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48 and 60 hours after the 7th dose.
Secondary Outcome Measures
- FSH Blood Serum Concentration [7 days]
Blood for measurement of serum follicle stimulating hormone concentrations was obtained prior to the 1st, 5th and 6th dose of GIPET™-enhanced oral acyline and 0.5,1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48 and 60 hours after the 7th dose.
- LH Blood Serum Concentration [7 days]
Blood for measurement of serum leutenizing hormone concentrations was obtained prior to the 1st, 5th and 6th dose of GIPET™-enhanced oral acyline and 0.5,1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48 and 60 hours after the 7th dose.
Eligibility Criteria
Criteria
Inclusion Criteria:
-
Healthy male
-
18-50 years of age
-
Non-smoker
-
Not taking any medications other than the study drug for the duration of the study.
-
Must be willing to use an accepted method of contraception during the study.
Exclusion Criteria:
-
BMI > 35
-
Abnormal evaluation on screening exam and labs
-
Known history of alcohol abuse, illicit drugs or steroids and/or use of more that 3 alcoholic beverages/day
-
History of current testosterone use or infertility
-
History of testicular disease or severe testicular trauma
-
History of major psychiatric disorder or sleep apnea
-
History of bleeding disorder or need for anticoagulation
-
Current smoker or utilizing nicotine patches or gum
-
Participation in a hormonal drug study within past month.
Contacts and Locations
Locations
| Site | City | State | Country | Postal Code | |
|---|---|---|---|---|---|
| 1 | University of Washington | Seattle | Washington | United States | 98195 |
Sponsors and Collaborators
- University of Washington
- Merrion Pharmaceuticals, LLC
Investigators
- Principal Investigator: John K Amory, MD, MPH, University of Washington
Study Documents (Full-Text)
None provided.More Information
Additional Information:
Publications
- Amory JK, Bremner WJ. Oral testosterone in oil plus dutasteride in men: a pharmacokinetic study. J Clin Endocrinol Metab. 2005 May;90(5):2610-7. Epub 2005 Feb 15.
- Amory JK, Page ST, Bremner WJ. Oral testosterone in oil: pharmacokinetic effects of 5alpha reduction by finasteride or dutasteride and food intake in men. J Androl. 2006 Jan-Feb;27(1):72-8.
- Herbst KL, Anawalt BD, Amory JK, Bremner WJ. Acyline: the first study in humans of a potent, new gonadotropin-releasing hormone antagonist. J Clin Endocrinol Metab. 2002 Jul;87(7):3215-20.
- Herbst KL, Coviello AD, Page S, Amory JK, Anawalt BD, Bremner WJ. A single dose of the potent gonadotropin-releasing hormone antagonist acyline suppresses gonadotropins and testosterone for 2 weeks in healthy young men. J Clin Endocrinol Metab. 2004 Dec;89(12):5959-65.
- Matthiesson KL, Amory JK, Berger R, Ugoni A, McLachlan RI, Bremner WJ. Novel male hormonal contraceptive combinations: the hormonal and spermatogenic effects of testosterone and levonorgestrel combined with a 5alpha-reductase inhibitor or gonadotropin-releasing hormone antagonist. J Clin Endocrinol Metab. 2005 Jan;90(1):91-7. Epub 2004 Oct 27.
- Page ST, Amory JK, Anawalt BD, Irwig MS, Brockenbrough AT, Matsumoto AM, Bremner WJ. Testosterone gel combined with depomedroxyprogesterone acetate is an effective male hormonal contraceptive regimen and is not enhanced by the addition of a GnRH antagonist. J Clin Endocrinol Metab. 2006 Nov;91(11):4374-80. Epub 2006 Aug 29.
- Page ST, Lin DW, Mostaghel EA, Hess DL, True LD, Amory JK, Nelson PS, Matsumoto AM, Bremner WJ. Persistent intraprostatic androgen concentrations after medical castration in healthy men. J Clin Endocrinol Metab. 2006 Oct;91(10):3850-6. Epub 2006 Aug 1.
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Study Results
Participant Flow
| Recruitment Details | Subjects were recruited via fliers on the University of Washington campus. |
|---|---|
| Pre-assignment Detail | Healthy, non-smoking male subjects between 18-50 years of age were recruited. Health was determined by physical exam, medical history intake and laboratory blood tests. |
| Arm/Group Title | Oral Acyline |
|---|---|
| Arm/Group Description | 20 mg dose of GIPET enhanced oral acyline for 7 days |
| Period Title: Overall Study | |
| STARTED | 4 |
| COMPLETED | 4 |
| NOT COMPLETED | 0 |
Baseline Characteristics
| Arm/Group Title | Oral Acyline |
|---|---|
| Arm/Group Description | 20 mg dose of GIPET enhanced oral acyline for 7 days |
| Overall Participants | 4 |
| Age (Count of Participants) | |
| <=18 years |
0
0%
|
| Between 18 and 65 years |
4
100%
|
| >=65 years |
0
0%
|
| Age (years) [Mean (Standard Deviation) ] | |
| Mean (Standard Deviation) [years] |
40
(11)
|
| Sex: Female, Male (Count of Participants) | |
| Female |
0
0%
|
| Male |
4
100%
|
| Region of Enrollment (participants) [Number] | |
| United States |
4
100%
|
Outcome Measures
| Title | Testosterone Blood Serum Concentration |
|---|---|
| Description | Blood for measurement of serum testosterone was obtained prior to the 1st, 5th and 6th dose of GIPET™-enhanced oral acyline and 0.5,1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48 and 60 hours after the 7th dose. |
| Time Frame | 7 days |
Outcome Measure Data
| Analysis Population Description |
|---|
| [Not Specified] |
| Arm/Group Title | Oral Acyline |
|---|---|
| Arm/Group Description | 20 mg dose of GIPET enhanced oral acyline for 7 days |
| Measure Participants | 4 |
| pre-dose 1 |
14.25
(4.72)
|
| pre-dose 5 |
8.53
(2.06)
|
| pre-dose 6 |
9.83
(1.93)
|
| pre-dose 7 |
9.83
(3.39)
|
| dose 7, 0.5 hours |
10.10
(3.73)
|
| dose 7, 1 hour |
9.50
(3.67)
|
| dose 7, 1.5 hours |
10.33
(4.35)
|
| dose 7, 2 hours |
10.65
(3.38)
|
| dose 7, 3 hours |
9.80
(4.05)
|
| dose 7, 4 hours |
8.78
(3.18)
|
| dose 7, 6 hours |
7.08
(2.84)
|
| dose 7, 8 hours |
6.80
(3.70)
|
| dose 7, 12 hours |
6.88
(3.81)
|
| dose 7, 24 hours |
9.30
(4.58)
|
| dose 7, 36 hours |
8.20
(2.71)
|
| dose 7, 48 hours |
10.83
(4.29)
|
| dose 7, 60 hours |
10.10
(4.61)
|
| Recovery/day 14 |
16.5
(2.12)
|
| Title | FSH Blood Serum Concentration |
|---|---|
| Description | Blood for measurement of serum follicle stimulating hormone concentrations was obtained prior to the 1st, 5th and 6th dose of GIPET™-enhanced oral acyline and 0.5,1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48 and 60 hours after the 7th dose. |
| Time Frame | 7 days |
Outcome Measure Data
| Analysis Population Description |
|---|
| [Not Specified] |
| Arm/Group Title | Oral Acyline |
|---|---|
| Arm/Group Description | 20 mg dose of GIPET enhanced oral acyline for 7 days |
| Measure Participants | 4 |
| pre-dose 1 |
2.80
(1.55)
|
| pre-dose 5 |
2.05
(0.60)
|
| pre-dose 6 |
2.33
(0.69)
|
| pre-dose 7 |
2.23
(0.72)
|
| dose 7, 0.5 hours |
2.48
(0.67)
|
| dose 7, 1 hour |
2.38
(0.69)
|
| dose 7, 1.5 hours |
2.45
(0.83)
|
| dose 7, 2 hours |
2.45
(0.77)
|
| dose 7, 3 hours |
2.33
(0.78)
|
| dose 7, 4 hours |
2.20
(0.92)
|
| dose 7, 6 hours |
2.05
(0.61)
|
| dose 7, 8 hours |
1.93
(0.62)
|
| dose 7, 12 hours |
2.03
(0.59)
|
| dose 7, 24 hours |
2.28
(0.62)
|
| dose 7, 36 hours |
2.48
(0.85)
|
| dose 7, 48 hours |
3.00
(1.11)
|
| dose 7, 60 hours |
2.93
(1.21)
|
| Recovery/day 14 |
3.20
(2.83)
|
| Title | LH Blood Serum Concentration |
|---|---|
| Description | Blood for measurement of serum leutenizing hormone concentrations was obtained prior to the 1st, 5th and 6th dose of GIPET™-enhanced oral acyline and 0.5,1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48 and 60 hours after the 7th dose. |
| Time Frame | 7 days |
Outcome Measure Data
| Analysis Population Description |
|---|
| [Not Specified] |
| Arm/Group Title | Oral Acyline |
|---|---|
| Arm/Group Description | 20 mg dose of GIPET enhanced oral acyline for 7 days |
| Measure Participants | 4 |
| pre-dose 1 |
4.87
(5.53)
|
| pre-dose 5 |
2.73
(1.53)
|
| pre-dose 6 |
4.78
(4.43)
|
| pre-dose 7 |
4.15
(4.60)
|
| dose 7, 0.5 hours |
5.80
(2.82)
|
| dose 7, 1 hour |
5.18
(3.90)
|
| dose 7, 1.5 hours |
5.30
(5.15)
|
| dose 7, 2 hours |
5.40
(4.56)
|
| dose 7, 3 hours |
3.83
(3.35)
|
| dose 7, 4 hours |
2.98
(2.67)
|
| dose 7, 6 hours |
2.35
(1.66)
|
| dose 7, 8 hours |
1.94
(1.46)
|
| dose 7, 12 hours |
2.40
(1.25)
|
| dose 7, 24 hours |
4.10
(2.68)
|
| dose 7, 36 hours |
6.70
(6.21)
|
| dose 7, 48 hours |
7.20
(7.88)
|
| dose 7, 60 hours |
5.80
(6.25)
|
| Recovery/day 14 |
8.10
(9.76)
|
Adverse Events
| Time Frame | ||
|---|---|---|
| Adverse Event Reporting Description | ||
| Arm/Group Title | Oral Acyline | |
| Arm/Group Description | 20 mg dose of GIPET enhanced oral acyline for 7 days | |
All Cause Mortality |
||
| Oral Acyline | ||
| Affected / at Risk (%) | # Events | |
| Total | / (NaN) | |
Serious Adverse Events |
||
| Oral Acyline | ||
| Affected / at Risk (%) | # Events | |
| Total | 0/4 (0%) | |
Other (Not Including Serious) Adverse Events |
||
| Oral Acyline | ||
| Affected / at Risk (%) | # Events | |
| Total | 0/4 (0%) | |
Limitations/Caveats
More Information
Certain Agreements
Principal Investigators are NOT employed by the organization sponsoring the study.
There is NOT an agreement between Principal Investigators and the Sponsor (or its agents) that restricts the PI's rights to discuss or publish trial results after the trial is completed.
Results Point of Contact
| Name/Title | Dr. John K. Amory |
|---|---|
| Organization | University of Washington |
| Phone | 206.616.1727 |
| jamory@u.washington.edu |
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- 07-7973-W