A Multiple-Dose Pharmacokinetics Study of Three Gefapixant (AF-219/MK-7264) Formulations

NCT02790840 | Completed Phase 1

• 2 other identifiers: 7264-023AF219-023
• Study Type: interventional
• Target: 32
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to compare the multiple dose pharmacokinetics (PK) of three gefapixant (AF-219) formulations; to assess the effect of Omeprazole on the multiple dose PK of three gefapixant formulations; and, to assess the safety and tolerability of gefapixant.

Conditions

Healthy

Keywords

Volunteers

Outcome Measures

Primary Outcomes (2)

• Maximum plasma concentration (Cmax) profiles of three different oral formulations of gefapixant

  Plasma gefapixant concentration versus time profiles will be plotted for each subject; similar summary plots will be constructed for each treatment period. Plasma gefapixant PK parameters will be calculated using noncompartmental methods and summarized using descriptive statistics by each treatment.

  12 hours

• Maximum plasma concentration (Cmax) profile of gefapixant following administration of Omeprazole

  Analysis of variance (ANOVA) will be performed on log normal-transformed Cmax and AUC0-t values to determine the extent of a drug interaction, if any, of Omeprazole on the plasma gefapixant PK parameters

  12 hours

Study Arms (1)

Gefapixant + Omeprazole

EXPERIMENTAL

Gefapixant oral tablets (15mg and 30 mg) administered twice daily for 15 days + Omeprazole oral capsules (20 mg or 40 mg) administered once or twice daily for 10 days

Drug: Omeprazole; Drug: Gefapixant

Interventions

Omeprazole DRUG

20 mg oral capsules administered once daily for 10 days

Also known as: Prilosec

Gefapixant + Omeprazole

Gefapixant DRUG

Gefapixant oral tablets (15 mg administered as two 7.5 mg tablets) administered twice daily for 15 days

Also known as: AF-219, MK-7264

Gefapixant + Omeprazole

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Be informed of the nature of the study and have provided written informed voluntary consent
• Be able to speak, read, and understand English;
• Be healthy males or females, of any race, between 18 and 55 years of age, inclusive;
• Have a body mass index (BMI) \>18.5 and \<32.0 kg/m2 and weigh 50 - 100 kg;
• Be in good general health with no clinically relevant abnormalities based on the medical history, physical examination, clinical laboratory evaluations (hematology, clinical chemistry, and urinalysis), and 12-lead electrocardiogram;
• Be only non-smokers or intermittent (social) smokers for at least 5 years, and able to refrain from smoking (or using nicotine) while in confinement;
• If a female of child-bearing potential or not post-menopausal, agree to use 2 forms of acceptable birth control;
• Be able to communicate effectively with the Investigator and other study center personnel and agree to comply with the study procedures and restrictions

You may not qualify if:

• Have previously received gefapixant;
• Any disease or condition that might affect drug absorption, metabolism, or excretion or clinically significant cardiovascular, hematological, renal, hepatic, pulmonary, endocrine, gastrointestinal, immunological, dermatological, neurological, or psychiatric disease;
• Clinically significant illness or clinically significant surgery within 4 weeks before the administration of study medication;
• Any past sinus surgery, upper respiratory tract infection within 2 weeks before dosing, or history of hay-fever during the time of the year that dosing will be taking place;
• History of GERD, heartburn, or nausea more than once a month, or any similar symptoms requiring the regular use of antacids, or any use of H2-histamine blockers or proton pump inhibitors within 12 months of Screening;
• QTcB \>450 msec in males or \>470 msec in females;
• Known or suspected hypersensitivity or allergic reaction to any of the components of gefapixant or omeprazole capsules;
• If female, is pregnant or breast feeding, or has a positive pregnancy test pre-dose;
• Blood loss or blood donation of \>550 mL within 90 days or plasma donation \>500 mL within 14 days before administration of the first dose of study drug;
• Chronic use of any systemic medications (other than allowable oral and implanted contraceptives and with the exception of vitamins taken at standard supplement doses); use of a drug therapy (including herbal preparations, e.g., St. John's wort) known to induce or inhibit hepatic drug metabolism within 30 days before the first dose of study medication; or use of any medications \[prescription or over-the-counter (OTC)\], including antacids, high-dose multivitamins, nutritional supplements, and herbal preparations, within 14 days before the first dose of study drug, unless deemed acceptable by the Investigator and Sponsor;
• Past or current history or evidence of drug or alcohol abuse, regular use of more than 2 units of alcohol per day (1 unit of alcohol = 150 mL of wine, 360 mL of beer, or 45 mL of alcohol 40%), use of any recreational soft drugs (e.g., marijuana) within 3 months of screening, use of any hard drugs (such as cocaine, phencyclidine (PCP), and crack) within 1 year of screening, and/or a positive screen for substances of abuse or alcohol at screening or pre-dose;
• Ingestion of grapefruit or grapefruit juice within 48 hours before dose administration;
• Positive screen for hepatitis B surface antigen (HBsAg), hepatitis C antibody, or human immunodeficiency virus (HIV) antibody;
• Receipt of an investigational product or device, or participation in a drug research study within a period of 30 days (or 5 half lives of the drug, whichever is longer) before the first dose of study medication;
• Receipt of an investigational immunomodulator or monoclonal antibody within 180 days (or 5 half lives, whichever is longer) before the first dose of study medication.

Sponsors & Collaborators

• Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA): lead

Study Sites (1)

Celerion

Tempe, Arizona, 85283, United States

Location

MeSH Terms

Interventions

Omeprazole; Gefapixant

Intervention Hierarchy (Ancestors)

2-Pyridinylmethylsulfinylbenzimidazoles; Sulfoxides; Sulfur Compounds; Organic Chemicals; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Benzimidazoles; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring

Study Officials

• Danielle Armas, MD

  Celerion

  PRINCIPAL INVESTIGATOR

Study Design

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

Study Record Dates

• First Submitted: May 27, 2016
• First Posted: June 6, 2016
• Study Start: May 16, 2016
• Primary Completion: June 15, 2016
• Study Completion: June 21, 2016
• Last Updated: April 18, 2017

Record last verified: 2017-04

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)