Clinical trial NCT02790840: A Multiple-Dose Pharmacokinetics Study of Three Gefapixant (AF-219/MK-7264) Formulations
Official title: A Study in Healthy Subjects to Assess the Multiple- Dose Pharmacokinetics of Three AF-219 Formulations
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Keywords: Volunteers
Lead sponsor: Afferent Pharmaceuticals, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)
Sponsor class: INDUSTRY
First posted: 2016-06-06
Enrollment: 32
Sex: ALL
Minimum age (years): 18
Maximum age (years): 55
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: NA
Intervention model: SINGLE_GROUP
Primary purpose: TREATMENT

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.


Eligibility criteria: Inclusion Criteria:

* 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

Exclusion Criteria:

* 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.

Primary outcomes:
measure: Maximum plasma concentration (Cmax) profiles of three different oral formulations of gefapixant
timeFrame: 12 hours
measure: Maximum plasma concentration (Cmax) profile of gefapixant following administration of Omeprazole
timeFrame: 12 hours
Secondary outcomes:
Other outcomes:
Locations:
city: Tempe
country: United States
facility: Celerion
state: Arizona
Study officials:
affiliation: Celerion
name: Danielle Armas, MD
role: PRINCIPAL_INVESTIGATOR
References: