Bioavailability of KBP-5074 Tablet vs Capsule Formulations

NCT03340753 | Completed Phase 1 FDA Drug

• 1 other identifier: KBP5074-1-004
• Study Type: interventional
• Target: 20
• Locations: 1 country
• Sites: 1

Brief Summary

This is an open-label, partial crossover, single-dose study to evaluate the pharmacokinetics (PK), dose proportionality, and safety/tolerability of tablet versus capsule formulations of KBP-5074 in healthy subjects. The study is designed to evaluate the PK of a new tablet formulation versus that of the current capsule formulation. Data derived from this study, in addition to preclinical data and chemistry, manufacturing, and controls, will provide a basis for dose selection in future studies.

Conditions

Bioequivalence

Outcome Measures

Primary Outcomes (1)

• AUClast

  Area under the plasma concentration-time curve (AUC) from time 0 to the time of the last quantifiable plasma concentration

  Through 312 hours

Study Arms (2)

KBP-5074 Capsule

ACTIVE COMPARATOR

KBP-5074 capsule, 0.5 mg or 1.0 mg, QD, single dose

Drug: KBP-5074 Capsule

KBP-5074 Tablet

EXPERIMENTAL

KBP-5074 tablet, 0.5 mg or 1.0 mg, QD, single dose

Drug: KBP-5074 Tablet

Interventions

KBP-5074 Capsule DRUG

KBP-5074 (0.5 mg or 1.0 mg) capsule formulation single dose, in a 2-period crossover design with a 2-week washout/follow-up period

Also known as: MRA

KBP-5074 Capsule

KBP-5074 Tablet DRUG

KBP-5074 (0.5 mg or 1.0 mg) tablet formulation single dose, in a 2-period crossover design with a 2-week washout/follow-up period

Also known as: MRA

KBP-5074 Tablet

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Physically and mentally healthy male and females, aged 18 to 45, inclusive;
• Body mass index (BMI) between 18 to 30 kg/m2, inclusive;
• Nicotine-free (cigarettes, pipe, cigar, chewing tobacco, nicotine patches, etc.) for at least 6 months prior to Screening until the end of the study;
• Normal renal function as defined by estimated glomerular filtration rate \>90 mL/min/1.73m2;
• Willing to remain in the study facility for the duration of the domicile period and able to return for all out-patient visits;
• Ability to understand and sign written informed consent, which must be obtained prior to any study-related procedures being completed;
• Willing to avoid adding salt substitutes that contain potassium chloride or potassium lactate to food from 7 days prior to dosing through the duration of the study;
• Women of childbearing potential (WOCBP), must agree to 2 medically accepted, effective methods of birth control during the study and for 90 days after the end of the study. Adequate methods of contraception are defined as those that result in a low failure rate (\<1% per year) when used consistently and correctly. Such methods include the use of oral contraceptives, other hormonal contraceptives (vaginal products, skin patches, or implanted or injectable products), or mechanical products (such as an intrauterine diaphragm, condoms, or spermicides);
• Women of childbearing potential are defined as women who are not surgically or chemically sterilized, including hysterectomy or bilateral oophorectomy (tubal ligation is not acceptable), and who are between menarche and 1 year post-menopause; and
• Post-menopausal is defined as amenorrhoeic for at least 1 year prior to screening AND, if aged under 45 years have a serum follicle stimulating hormone (FSH) level of at least 30 IU/L. Women who are taking hormone replacement therapy (HRT) do not have to have FSH assessments, but the amenorrhea (before starting HRT) must have been naturally (spontaneously) occurring and have been accompanied by an appropriate clinical profile (e.g., age appropriate, history of vasomotor symptoms);
• Males with partners who are WOCBP must agree to use condoms plus spermicide and their female partner must also be using contraception (e.g., hormonal or intra-uterine device). This double contraception must be used from the first dose of study drug until at least 90 days after the last dose of study drug;
• Males must also refrain from donating sperm during the study and for 90 days after the last dose;
• Negative urine test for drugs of abuse (opiates, benzodiazepines, amphetamines, cannabinoids including tetrahydrocannabinol, cocaine, barbiturates, and phencyclidine), nicotine/cotinine, and breath alcohol test at Screening and Check-in; and
• Is in good general health as determined by the Investigator's review of medical history, concomitant medications, physical examination, and clinical laboratory and electrocardiogram (ECG) evaluations at the Screening Visit.

You may not qualify if:

• History of any illness, that, in the opinion of the Investigator, could confound the results of the study or pose an additional risk to the subject by their participation in the study ;
• History or presence of significant cardiovascular, pulmonary, hepatic, renal, hematological, gastrointestinal, endocrine, immunologic, dermatologic, neurological, or psychiatric disease;
• Any surgical or medical condition that could interfere with the absorption, distribution, metabolism, or excretion of the IMP;
• History of any clinically significant drug allergy as per the Investigator's judgment;
• History of alcohol abuse or illicit drug use within 2 years of Screening;
• Use of marijuana (including prescribed marijuana) within 3 months prior to Screening;
• Use of nicotine within 6 months prior to screening;
• Use of any prescription or over-the-counter medication, vitamins/herbal supplements (with the exception of hormonal contraceptives or HRT and sporadic use of acetaminophen or ibuprofen) within 7 days (14 days if the drug is a potential enzyme inducer) prior to study allocation;
• Has taken any investigational medicinal product (IMP) within 30 days or 5 half-lives of that IMP (whichever is longer) prior to dosing;
• Donation of blood or blood products within 30 days of dosing;
• Acute illness within 14 days of dosing; acute illness occurring prior to the 14 days before dosing must show signs of complete recovery;
• Regular caffeine consumption of \>300 mg/day (i.e., approximately 3 cups \[8 fluid ounces\] of coffee or 10 cans \[12 fluid ounces\] of cola) 7 days prior to dosing. Inability to restrict consumption of caffeine during the domicile period;
• Positive serologic findings for human immunodeficiency virus (HIV), hepatitis B virus (HBV) or hepatitis C virus (HCV);
• Diets that could alter metabolism (i.e., vegetarian, high protein, Slim Fast®, Nutrisystem®, etc.) 7 days prior to dosing;
• Weight loss or gain of ≥10% in the 30 days prior to dosing;

Sponsors & Collaborators

• KBP Biosciences: lead
• Medpace, Inc.: collaborator

Study Sites (1)

Medpace CLinical Pharmacology

Cincinnati, Ohio, 45227, United States

Location

MeSH Terms

Interventions

KBP-5074

Study Design

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

Study Record Dates

• First Submitted: November 7, 2017
• First Posted: November 13, 2017
• Study Start: October 26, 2017
• Primary Completion: November 22, 2017
• Study Completion: December 19, 2017
• Last Updated: December 16, 2025

Record last verified: 2025-12

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)