A Bioavailability Study of LY2452473 and Tadalafil

NCT01401543 | Completed Phase 1 Results

• 2 other identifiers: 13326I4K-MC-GPEA
• Study Type: interventional
• Target: 24
• Locations: 1 country
• Sites: 1

Brief 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.

Conditions

Erectile Dysfunction

Keywords

testosterone; energy; libido; erectile function; weak muscles

Outcome Measures

Primary Outcomes (2)

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

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

• Pharmacokinetics: Maximum Plasma Concentration (Cmax) of LY2452473

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

Secondary Outcomes (2)

• Pharmacokinetics: AUC(0-∞) of Tadalafil

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

• Pharmacokinetics: Cmax of Tadalafil

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

Study Arms (4)

5 mg LY2452473 + 5 mg Tadalafil

ACTIVE COMPARATOR

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

LY900010 (particle size #1)

EXPERIMENTAL

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

LY900010 (particle size #2)

EXPERIMENTAL

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

LY900010 (particle size #3)

EXPERIMENTAL

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

LY2452473 DRUG

Administered orally

5 mg LY2452473 + 5 mg Tadalafil

Tadalafil DRUG

Administered orally

Also known as: LY450190, Cialis

5 mg LY2452473 + 5 mg Tadalafil

LY900010 DRUG

Administered orally

LY900010 (particle size #1); LY900010 (particle size #2); LY900010 (particle size #3)

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• 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

You may not qualify if:

• 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

Sponsors & Collaborators

• Eli Lilly and Company: lead

Study Sites (1)

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

Location

MeSH Terms

Conditions

Erectile Dysfunction

Interventions

LY2452473; Tadalafil

Condition Hierarchy (Ancestors)

Genital Diseases, Male; Genital Diseases; Urogenital Diseases; Sexual Dysfunction, Physiological; Male Urogenital Diseases; Sexual Dysfunctions, Psychological; Mental Disorders

Intervention Hierarchy (Ancestors)

Carbolines; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Indole Alkaloids; Indoles; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds, 3-Ring

Results Point of Contact

• Title: Chief Medical Officer
• Organization: Eli Lilly and Company

800-545-5979

Study Officials

• 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)

  Eli Lilly and Company

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: GT60
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 21, 2011
• First Posted: July 25, 2011
• Study Start: July 1, 2011
• Primary Completion: September 1, 2011
• Study Completion: September 1, 2011
• Last Updated: June 14, 2019
• Results First Posted: June 14, 2019

Record last verified: 2019-03

Locations

US (1)