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ACY-7 Oral Administration of Acyline

Oral Administration of the GnRH Antagonist Acyline in Normal Men Part II: Multiple-dose Pharmacokinetics (Acyline-7/MER 104-02)

Status
Completed
Phases
Phase 1Phase 2
Study type
Interventional
Source
ClinicalTrials.gov
Registry ID
NCT00603187
Acronym
ACY-7
Enrollment
4
Registered
2008-01-28
Start date
2008-01-31
Completion date
2008-02-29
Last updated
2011-06-09

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy

Keywords

Male Contraception, Acyline

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.

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.

Interventions

DRUGAcyline

20 mg GIPET enhanced oral dose, daily for 7-days

Sponsors

Merrion Pharmaceuticals, LLC
CollaboratorINDUSTRY
University of Washington
Lead SponsorOTHER

Study design

Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
TREATMENT
Masking
NONE

Eligibility

Sex/Gender
MALE
Age
18 Years to 50 Years
Healthy volunteers
Yes

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.

Design outcomes

Primary

MeasureTime frameDescription
Testosterone Blood Serum Concentration7 daysBlood 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

MeasureTime frameDescription
FSH Blood Serum Concentration7 daysBlood 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 Concentration7 daysBlood 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.

Countries

United States

Participant flow

Recruitment details

Subjects were recruited via fliers on the University of Washington campus.

Pre-assignment details

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.

Participants by arm

ArmCount
Oral Acyline
20 mg dose of GIPET enhanced oral acyline for 7 days
4
Total4

Baseline characteristics

CharacteristicOral Acyline
Age, Categorical
<=18 years
0 Participants
Age, Categorical
>=65 years
0 Participants
Age, Categorical
Between 18 and 65 years
4 Participants
Age Continuous40 years
STANDARD_DEVIATION 11
Region of Enrollment
United States
4 participants
Sex: Female, Male
Female
0 Participants
Sex: Female, Male
Male
4 Participants

Adverse events

Event typeEG000
affected / at risk
deaths
Total, all-cause mortality
— / —
other
Total, other adverse events
0 / 4
serious
Total, serious adverse events
0 / 4

Outcome results

Primary

Testosterone Blood Serum Concentration

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

ArmMeasureGroupValue (MEAN)Dispersion
Oral AcylineTestosterone Blood Serum Concentrationdose 7, 8 hours6.80 ng/dlStandard Deviation 3.7
Oral AcylineTestosterone Blood Serum Concentrationdose 7, 12 hours6.88 ng/dlStandard Deviation 3.81
Oral AcylineTestosterone Blood Serum Concentrationdose 7, 24 hours9.30 ng/dlStandard Deviation 4.58
Oral AcylineTestosterone Blood Serum Concentrationdose 7, 36 hours8.20 ng/dlStandard Deviation 2.71
Oral AcylineTestosterone Blood Serum Concentrationdose 7, 48 hours10.83 ng/dlStandard Deviation 4.29
Oral AcylineTestosterone Blood Serum Concentrationdose 7, 60 hours10.10 ng/dlStandard Deviation 4.61
Oral AcylineTestosterone Blood Serum ConcentrationRecovery/day 1416.5 ng/dlStandard Deviation 2.12
Oral AcylineTestosterone Blood Serum Concentrationpre-dose 114.25 ng/dlStandard Deviation 4.72
Oral AcylineTestosterone Blood Serum Concentrationpre-dose 58.53 ng/dlStandard Deviation 2.06
Oral AcylineTestosterone Blood Serum Concentrationpre-dose 69.83 ng/dlStandard Deviation 1.93
Oral AcylineTestosterone Blood Serum Concentrationpre-dose 79.83 ng/dlStandard Deviation 3.39
Oral AcylineTestosterone Blood Serum Concentrationdose 7, 0.5 hours10.10 ng/dlStandard Deviation 3.73
Oral AcylineTestosterone Blood Serum Concentrationdose 7, 1 hour9.50 ng/dlStandard Deviation 3.67
Oral AcylineTestosterone Blood Serum Concentrationdose 7, 1.5 hours10.33 ng/dlStandard Deviation 4.35
Oral AcylineTestosterone Blood Serum Concentrationdose 7, 2 hours10.65 ng/dlStandard Deviation 3.38
Oral AcylineTestosterone Blood Serum Concentrationdose 7, 3 hours9.80 ng/dlStandard Deviation 4.05
Oral AcylineTestosterone Blood Serum Concentrationdose 7, 4 hours8.78 ng/dlStandard Deviation 3.18
Oral AcylineTestosterone Blood Serum Concentrationdose 7, 6 hours7.08 ng/dlStandard Deviation 2.84
Secondary

FSH Blood Serum Concentration

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

ArmMeasureGroupValue (MEAN)Dispersion
Oral AcylineFSH Blood Serum Concentrationpre-dose 62.33 iu/LStandard Deviation 0.69
Oral AcylineFSH Blood Serum Concentrationpre-dose 72.23 iu/LStandard Deviation 0.72
Oral AcylineFSH Blood Serum Concentrationdose 7, 0.5 hours2.48 iu/LStandard Deviation 0.67
Oral AcylineFSH Blood Serum Concentrationdose 7, 1 hour2.38 iu/LStandard Deviation 0.69
Oral AcylineFSH Blood Serum Concentrationdose 7, 1.5 hours2.45 iu/LStandard Deviation 0.83
Oral AcylineFSH Blood Serum Concentrationdose 7, 2 hours2.45 iu/LStandard Deviation 0.77
Oral AcylineFSH Blood Serum Concentrationdose 7, 3 hours2.33 iu/LStandard Deviation 0.78
Oral AcylineFSH Blood Serum Concentrationdose 7, 24 hours2.28 iu/LStandard Deviation 0.62
Oral AcylineFSH Blood Serum Concentrationdose 7, 36 hours2.48 iu/LStandard Deviation 0.85
Oral AcylineFSH Blood Serum Concentrationpre-dose 12.80 iu/LStandard Deviation 1.55
Oral AcylineFSH Blood Serum Concentrationpre-dose 52.05 iu/LStandard Deviation 0.6
Oral AcylineFSH Blood Serum Concentrationdose 7, 4 hours2.20 iu/LStandard Deviation 0.92
Oral AcylineFSH Blood Serum Concentrationdose 7, 6 hours2.05 iu/LStandard Deviation 0.61
Oral AcylineFSH Blood Serum Concentrationdose 7, 8 hours1.93 iu/LStandard Deviation 0.62
Oral AcylineFSH Blood Serum Concentrationdose 7, 12 hours2.03 iu/LStandard Deviation 0.59
Oral AcylineFSH Blood Serum Concentrationdose 7, 48 hours3.00 iu/LStandard Deviation 1.11
Oral AcylineFSH Blood Serum Concentrationdose 7, 60 hours2.93 iu/LStandard Deviation 1.21
Oral AcylineFSH Blood Serum ConcentrationRecovery/day 143.20 iu/LStandard Deviation 2.83
Secondary

LH Blood Serum Concentration

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

ArmMeasureGroupValue (MEAN)Dispersion
Oral AcylineLH Blood Serum Concentrationdose 7, 1.5 hours5.30 iu/LStandard Deviation 5.15
Oral AcylineLH Blood Serum Concentrationdose 7, 2 hours5.40 iu/LStandard Deviation 4.56
Oral AcylineLH Blood Serum Concentrationdose 7, 1 hour5.18 iu/LStandard Deviation 3.9
Oral AcylineLH Blood Serum Concentrationdose 7, 3 hours3.83 iu/LStandard Deviation 3.35
Oral AcylineLH Blood Serum Concentrationdose 7, 4 hours2.98 iu/LStandard Deviation 2.67
Oral AcylineLH Blood Serum Concentrationdose 7, 24 hours4.10 iu/LStandard Deviation 2.68
Oral AcylineLH Blood Serum Concentrationdose 7, 36 hours6.70 iu/LStandard Deviation 6.21
Oral AcylineLH Blood Serum Concentrationdose 7, 48 hours7.20 iu/LStandard Deviation 7.88
Oral AcylineLH Blood Serum Concentrationpre-dose 14.87 iu/LStandard Deviation 5.53
Oral AcylineLH Blood Serum Concentrationpre-dose 52.73 iu/LStandard Deviation 1.53
Oral AcylineLH Blood Serum Concentrationpre-dose 64.78 iu/LStandard Deviation 4.43
Oral AcylineLH Blood Serum Concentrationpre-dose 74.15 iu/LStandard Deviation 4.6
Oral AcylineLH Blood Serum Concentrationdose 7, 0.5 hours5.80 iu/LStandard Deviation 2.82
Oral AcylineLH Blood Serum Concentrationdose 7, 6 hours2.35 iu/LStandard Deviation 1.66
Oral AcylineLH Blood Serum Concentrationdose 7, 8 hours1.94 iu/LStandard Deviation 1.46
Oral AcylineLH Blood Serum Concentrationdose 7, 12 hours2.40 iu/LStandard Deviation 1.25
Oral AcylineLH Blood Serum Concentrationdose 7, 60 hours5.80 iu/LStandard Deviation 6.25
Oral AcylineLH Blood Serum ConcentrationRecovery/day 148.10 iu/LStandard Deviation 9.76

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026