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CompletedNCT01401543Updated Jun 14, 2019Results posted

A Bioavailability Study of LY2452473 and Tadalafil

A Phase 1 interventional study of LY2452473 and Tadalafil in Erectile Dysfunction, sponsored by Eli Lilly and Company. Completed at 1 site in United States. Open to male participants aged 18 Years to 65 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2019-06-14.

Sponsored by Eli Lilly and Company · Phase 1, Interventional, and Treatment

Phase
Phase 1
Study type
Interventional
Enrollment
24
Allocation
Randomized
Ages
18 Years to 65 Years
Sex
Male
01

Study summary

This study compares LY2452473 taken orally as a 5 milligram (mg) capsule at the same time as a 5 mg tadalafil tablet with three different combination tablets (LY900010) of 5 mg LY2452473 and 5 mg tadalafil taken orally. The study will evaluate the amount of LY2452473 and tadalafil circulating in the blood for each treatment. Side effects will be documented. This study is approximately 34 days not including screening.

02

Conditions studied

  • Erectile Dysfunction

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Keywords

  • testosterone
  • energy
  • libido
  • erectile function
  • weak muscles
03

In context

Erectile Dysfunction

683 studies on the registry are indexed under Erectile Dysfunction; 117 are open to participants now.

This study's enrollment of 24 is below the median of 72 across 542 interventional studies indexed under Erectile Dysfunction.

Browse Erectile Dysfunction studies →

Lead sponsor

Eli Lilly and Company is the lead sponsor of 2,048 studies on the registry; 140 are open to participants now.

Of its 521 completed or terminated interventional studies of FDA-regulated products, 341 (65%) have results posted.

Counted across the registry records on this site, refreshed daily.

04

Who can participate

Ages eligible
18 Years to 65 Years
Sexes eligible
Male
Accepts healthy volunteers
Yes

Inclusion criteria

  • Overtly healthy male, as determined by medical history and physical examination
  • Are between a body mass index of 18.5 and 30 kilograms per meter squared (kg/m²), inclusive at screening
  • Have clinical laboratory test results within normal reference range for the population or investigator site, or results with acceptable deviations that are judged to be not clinically significant by the investigator
  • Normal blood pressure and heart rate (HR; sitting) as determined by the investigator
  • Have venous access sufficient to allow blood sampling
  • Are reliable and willing to make themselves available for the duration of the study, and will abide by the research unit policies and procedures and study restrictions
  • Have given written informed consent approved by Lilly and the ethical review board (ERB) governing the site
  • Men must agree to use a reliable method of birth control (for example, vasectomy, condom with contraceptive foam, abstinence, or female partner's use of oral contraceptives or Norplant®; a reliable barrier method of birth control [diaphragm with contraceptive jelly]; or intrauterine device), during the study and for 1 month following the last dose of study drug

Exclusion criteria

Exclusion Criteria:

  • Have known allergies to LY2452473, tadalafil, or related compounds
  • History of severe allergies or multiple adverse drug reactions
  • Have a history or presence of cardiovascular, respiratory, hepatic (including history of cholecystectomy), renal, gastrointestinal, endocrine, hematological, or neurological disorders capable of significantly altering the absorption, metabolism, or elimination of drugs; of constituting a risk when taking the study medication; or of interfering with the interpretation of data
  • Any abnormality in the 12-lead electrocardiogram (ECG) that in the opinion of the investigator places the subject at an unacceptable risk for study participation
  • Show evidence of significant active neuropsychiatric disease
  • History of significant retinal pathology
  • Have a history of glaucoma
  • Have a history of unexplained syncope episodes
  • Show evidence of hepatitis C and/or positive hepatitis C antibody
  • Show evidence of hepatitis B and/or positive hepatitis B surface antigen
  • Show evidence of human immunodeficiency virus (HIV) and/or positive HIV antibodies
  • Intended use of over-the-counter or herbal remedies within 7 days prior to dosing or during the study
  • Intended use of prescription medication within 14 days prior to dosing or during the study
  • Are not willing to refrain from consumption of any food, or drink any beverage containing grapefruit, pomelo, or starfruit for at least 2 weeks prior to the start of the study until its conclusion
  • Heavy caffeine drinkers defined by a regular intake of more than 5 cups of coffee (or equivalent in xanthine-containing beverages) per day or subjects who have not had consistent daily caffeine consumption for 1 month prior to study entry or subjects not willing to maintain consistent caffeine consumption during the study
  • Use of drugs of abuse, as evidenced by history, and/or positive findings on urinary drug screening
  • Have an average weekly alcohol intake that exceeds 14 units per week or are unwilling to stop alcohol consumption for the duration of the study (1 unit = 12 ounces [oz] or 360 milliliters (mL) of beer; 5 oz or 150 mL of wine; 1.5 oz or 45 mL of distilled spirits)
  • Is currently a smoker or uses tobacco products on a regular basis and has not had consistent daily tobacco use for 1 month prior to study entry or subjects not willing to maintain consistent tobacco use during the study
  • Have a history of blood donation of 1 unit (approximately 450 mL) or more in the last 3 months prior to study entry
  • Have previously completed or withdrawn from this study or any other study investigating LY2452473
  • Within 30 days of the initial dose of study drug, have received treatment with a drug that has not received regulatory approval for any indication
  • Deemed unsuitable by the investigator for any other reason
  • Are currently enrolled in, or discontinued within the last 30 days from, a clinical trial involving an investigational drug or device or off-label use of a drug or device (other than the study drug/device used in this study), or are concurrently enrolled in any other type of medical research judged not to be scientifically or medically compatible with this study
05

Study design

Phase
Phase 1
Primary purpose
Treatment
Allocation
Randomized
Intervention model
Crossover assignment
Masking
None (open label)
Enrollment
24 participants (actual)

Study arms

  • Active comparator
    5 mg LY2452473 + 5 mg Tadalafil

    5-mg LY2452473 oral capsule and 5-mg tadalafil oral tablet, administered orally, once only. There will be a washout period of at least 7 days between doses of study drug.

    Drug: LY2452473 · Drug: Tadalafil

  • Experimental
    LY900010 (particle size #1)

    Single combination tablet containing 5 mg tadalafil and 5 mg LY2452473 with a smaller particle size (d90 = 10 microns), administered orally, once only. There will be a washout period of at least 7 days between doses of study drug. d90 is a measurement of the distribution of particle widths such that 90% of the particles have a diameter less than the specified value.

    Drug: LY900010

  • Experimental
    LY900010 (particle size #2)

    Single combination tablet containing 5 mg tadalafil and 5 mg LY2452473 with an intermediate particle size (d90 = 25 microns), administered orally, once only. There will be a washout period of at least 7 days between doses of study drug. d90 is a measurement of the distribution of particle widths such that 90% of the particles have a diameter less than the specified value.

    Drug: LY900010

  • Experimental
    LY900010 (particle size #3)

    Single combination tablet containing 5 mg tadalafil and 5 mg LY2452473 with a larger particle size (d90 = 40 microns), administered orally, once only. There will be a washout period of at least 7 days between doses of study drug. d90 is a measurement of the distribution of particle widths such that 90% of the particles have a diameter less than the specified value.

    Drug: LY900010

Interventions

  • DrugLY2452473

    Administered orally

  • DrugTadalafil

    Administered orally

    Also known as: LY450190, Cialis

  • DrugLY900010

    Administered orally

06

What researchers measure

Primary outcomes

  1. Pharmacokinetics: Area Under the Concentration-Time Curve From Time Zero to Infinity [AUC(0-∞)] of LY2452473

    Time frame: Predose up to 96 hours postdose for each of the 4 treatment periods

  2. Pharmacokinetics: Maximum Plasma Concentration (Cmax) of LY2452473

    Time frame: Predose up to 96 hours postdose for each of the 4 treatment periods

Secondary outcomes

  1. Pharmacokinetics: AUC(0-∞) of Tadalafil

    Time frame: Predose up to 96 hours postdose for each of the 4 treatment periods

  2. Pharmacokinetics: Cmax of Tadalafil

    Time frame: Predose up to 96 hours postdose for each of the 4 treatment periods

07

Results

Posted Jun 14, 2019

Participant flow

First Intervention
Participant flow — First Intervention
MilestoneSequence 1Sequence 2Sequence 3Sequence 4
Started6666
Completed6666
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First Washout Period of 1 Week
Participant flow — First Washout Period of 1 Week
MilestoneSequence 1Sequence 2Sequence 3Sequence 4
Started6666
Completed6666
Not completed0000
Second Intervention
Participant flow — Second Intervention
MilestoneSequence 1Sequence 2Sequence 3Sequence 4
Started6666
Completed6666
Not completed0000
Second Washout Period of 1 Week
Participant flow — Second Washout Period of 1 Week
MilestoneSequence 1Sequence 2Sequence 3Sequence 4
Started6666
Completed6666
Not completed0000
Third Intervention
Participant flow — Third Intervention
MilestoneSequence 1Sequence 2Sequence 3Sequence 4
Started6666
Completed6666
Not completed0000
Third Washout Period of 1 Week
Participant flow — Third Washout Period of 1 Week
MilestoneSequence 1Sequence 2Sequence 3Sequence 4
Started6666
Completed6666
Not completed0000
Fourth Intervention
Participant flow — Fourth Intervention
MilestoneSequence 1Sequence 2Sequence 3Sequence 4
Started6666
Completed6666
Not completed0000

Outcome measures

PrimaryPharmacokinetics: Area Under the Concentration-Time Curve From Time Zero to Infinity [AUC(0-∞)] of LY2452473
Time frame:
Predose up to 96 hours postdose for each of the 4 treatment periods
Reported as:
Mean · nanograms*hours per milliliter (ng*h/mL)
Pharmacokinetics: Area Under the Concentration-Time Curve From Time Zero to Infinity [AUC(0-∞)] of LY2452473
nanograms*hours per milliliter (ng*h/mL)5 mg LY2452473 and 5 mg TadalafilLY900010 (Particle Size #1)LY900010 (Particle Size #2)LY900010 (Particle Size #3)
Pharmacokinetics: Area Under the Concentration-Time Curve From Time Zero to Infinity [AUC(0-∞)] of LY2452473514 ± 152495 ± 159453 ± 123463 ± 140
Statistical analysis
  • 5 mg LY2452473 and 5 mg Tadalafil vs LY900010 (Particle Size #1) · Geometric least squares (ls) mean ratio: 0.96 · 90% CI 0.91 to 1.01Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • 5 mg LY2452473 and 5 mg Tadalafil vs LY900010 (Particle Size #2) · Geometric ls mean ratio: 0.89 · 90% CI 0.85 to 0.93Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • LY900010 (Particle Size #1) vs LY900010 (Particle Size #2) · Geometric ls mean ratio: 0.93 · 90% CI 0.88 to 0.97Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • 5 mg LY2452473 and 5 mg Tadalafil vs LY900010 (Particle Size #3) · Geometric ls mean ratio: 0.90 · 90% CI 0.86 to 0.95Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • LY900010 (Particle Size #1) vs LY900010 (Particle Size #3) · Geometric ls mean ratio: 0.94 · 90% CI 0.90 to 0.99Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • LY900010 (Particle Size #2) vs LY900010 (Particle Size #3) · Geometric ls mean ratio: 1.02 · 90% CI 0.97 to 1.07Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
PrimaryPharmacokinetics: Maximum Plasma Concentration (Cmax) of LY2452473
Time frame:
Predose up to 96 hours postdose for each of the 4 treatment periods
Reported as:
Mean · nanograms per milliliter (ng/mL)
Pharmacokinetics: Maximum Plasma Concentration (Cmax) of LY2452473
nanograms per milliliter (ng/mL)5 mg LY2452473 and 5 mg TadalafilLY900010 (Particle Size #1)LY900010 (Particle Size #2)LY900010 (Particle Size #3)
Pharmacokinetics: Maximum Plasma Concentration (Cmax) of LY245247332.5 ± 8.1627.1 ± 6.6225.6 ± 7.4124.7 ± 5.66
Statistical analysis
  • 5 mg LY2452473 and 5 mg Tadalafil vs LY900010 (Particle Size #1) · Geometric ls mean ratio: 0.84 · 90% CI 0.77 to 0.91Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • 5 mg LY2452473 and 5 mg Tadalafil vs LY900010 (Particle Size #2) · Geometric ls mean ratio: 0.78 · 90% CI 0.71 to 0.85Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • LY900010 (Particle Size #1) vs LY900010 (Particle Size #2) · Geometric ls mean ratio: 0.93 · 90% CI 0.85 to 1.01Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • 5 mg LY2452473 and 5 mg Tadalafil vs LY900010 (Particle Size #3) · Geometric ls mean ratio: 0.77 · 90% CI 0.70 to 0.84Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • LY900010 (Particle Size #1) vs LY900010 (Particle Size #3) · Geometric ls mean ratio: 0.91 · 90% CI 0.84 to 1.00Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • LY900010 (Particle Size #2) vs LY900010 (Particle Size #3) · Geometric ls mean ratio: 0.99 · 90% CI 0.91 to 1.08Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
SecondaryPharmacokinetics: AUC(0-∞) of Tadalafil
Time frame:
Predose up to 96 hours postdose for each of the 4 treatment periods
Reported as:
Mean · nanograms*hours per milliliter (ng*h/mL)
Pharmacokinetics: AUC(0-∞) of Tadalafil
nanograms*hours per milliliter (ng*h/mL)5 mg LY2452473 and 5 mg TadalafilLY900010 (Particle Size #1)LY900010 (Particle Size #2)LY900010 (Particle Size #3)
Pharmacokinetics: AUC(0-∞) of Tadalafil2410 ± 8932400 ± 10702240 ± 6762290 ± 825
Statistical analysis
  • 5 mg LY2452473 and 5 mg Tadalafil vs LY900010 (Particle Size #1) · Geometric ls mean ratio: 0.99 · 90% CI 0.93 to 1.05
  • 5 mg LY2452473 and 5 mg Tadalafil vs LY900010 (Particle Size #2) · Geometric ls mean ratio: 0.94 · 90% CI 0.89 to 1.00
  • LY900010 (Particle Size #1) vs LY900010 (Particle Size #2) · Geometric ls mean ratio: 0.96 · 90% CI 0.90 to 1.02
  • 5 mg LY2452473 and 5 mg Tadalafil vs LY900010 (Particle Size #3) · Geometric ls mean ratio: 0.96 · 90% CI 0.90 to 1.02
  • LY900010 (Particle Size #1) vs LY900010 (Particle Size #3) · Geometric ls mean ratio: 0.97 · 90% CI 0.91 to 1.03
  • LY900010 (Particle Size #2) vs LY900010 (Particle Size #3) · Geometric ls mean ratio: 1.01 · 90% CI 0.95 to 1.08
SecondaryPharmacokinetics: Cmax of Tadalafil
Time frame:
Predose up to 96 hours postdose for each of the 4 treatment periods
Reported as:
Mean · nanograms per milliliter (ng/mL)
Pharmacokinetics: Cmax of Tadalafil
nanograms per milliliter (ng/mL)5 mg LY2452473 and 5 mg TadalafilLY900010 (Particle Size #1)LY900010 (Particle Size #2)LY900010 (Particle Size #3)
Pharmacokinetics: Cmax of Tadalafil102 ± 31.274.4 ± 28.072.4 ± 19.070.0 ± 17.5
Statistical analysis
  • 5 mg LY2452473 and 5 mg Tadalafil vs LY900010 (Particle Size #1) · Geometric ls mean ratio: 0.72 · 90% CI 0.68 to 0.77Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • 5 mg LY2452473 and 5 mg Tadalafil vs LY900010 (Particle Size #2) · Geometric ls mean ratio: 0.71 · 90% CI 0.66 to 0.76Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • LY900010 (Particle Size #1) vs LY900010 (Particle Size #2) · Geometric ls mean ratio: 0.98 · 90% CI 0.92 to 1.05Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • 5 mg LY2452473 and 5 mg Tadalafil vs LY900010 (Particle Size #3) · Geometric ls mean ratio: 0.69 · 90% CI 0.65 to 0.74Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • LY900010 (Particle Size #1) vs LY900010 (Particle Size #3) · Geometric ls mean ratio: 0.96 · 90% CI 0.90 to 1.02Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.
  • LY900010 (Particle Size #2) vs LY900010 (Particle Size #3) · Geometric ls mean ratio: 0.98 · 90% CI 0.91 to 1.04Formulation, sequence, and period were included in the model as fixed effects, and participant as a random factor.

Adverse events

Non-serious events are listed at a 4% frequency threshold.

Adverse event summary by group
GroupDeathsSeriousOther
5 mg LY2452473 and 5 mg Tadalafil—0/24 (0%)3/24 (12.5%)
LY900010 (Particle Size #1)—0/24 (0%)7/24 (29.2%)
LY900010 (Particle Size #2)—0/24 (0%)5/24 (20.8%)
LY900010 (Particle Size #3)—0/24 (0%)3/24 (12.5%)
Most frequent other events
Showing 10 of 21
Most frequent other events
Event5 mg LY2452473 and 5 mg TadalafilLY900010 (Particle Size #1)LY900010 (Particle Size #2)LY900010 (Particle Size #3)
HeadacheNervous system disorders1/245/242/241/24
Scleral hyperaemiaEye disorders0/241/240/240/24
Abdominal discomfortGastrointestinal disorders0/240/240/241/24
Abdominal painGastrointestinal disorders1/240/240/240/24
DiarrhoeaGastrointestinal disorders0/240/240/241/24
NauseaGastrointestinal disorders0/241/241/240/24
VomitingGastrointestinal disorders0/240/241/240/24
FatigueGeneral disorders0/241/240/240/24
Feeling hotGeneral disorders0/241/240/240/24
Sensation of pressureGeneral disorders0/240/241/240/24

Baseline characteristics

Age, Continuous
Age, Continuous(years)Entire Study Population
Mean39.6 ± 13.8
Sex: Female, Male
Sex: Female, Male(Participants)Entire Study Population
Female0
Male24
Ethnicity (NIH/OMB)
Ethnicity (NIH/OMB)(Participants)Entire Study Population
Hispanic or Latino1
Not Hispanic or Latino23
Unknown or Not Reported0
Region of Enrollment
Region of Enrollment(Participants)Entire Study Population
United States24
Race, Customized
Race, Customized(Participants)Entire Study Population
Black or African American4
White20
08

Study locations

1 site
  • For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician.
    Madison, Wisconsin 53704, United States
09

Updates

Tracking since Sep 25, 2026
No changes since tracking began. The registry record was last updated on Jun 14, 2019, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
10

Registry details

Key details

Study ID
NCT01401543
Lead sponsor
Eli Lilly and Company
Responsible party
Sponsor
First posted
Jul 25, 2011
Start date
Jul 2011
Primary completion
Sep 2011
Completion
Sep 2011
Results posted
Jun 14, 2019
Last update
Jun 14, 2019

Study contacts

Call 1-877-CTLILLY (1-877-285-4559) or 1-317-615-4559 Mon - Fri 9 AM - 5 PM Eastern time (UTC/GMT - 5 hours, EST)
study director · Eli Lilly and Company

Oversight

Data monitoring committee
No
View the source record on ClinicalTrials.gov ↗

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