Safety, Tolerability, and Pharmacokinetics (PK) of CTP-499

A Randomized, Double-blind, Placebo-controlled, Single-ascending-dose, Safety, Tolerability, Pharmacokinetics, and Relative Bioavailability Study of CTP-499 in Healthy Adults

The purpose of this study is to assess the safety, tolerability and pharmacokinetics of CTP-499 following single dose administration.

Study Overview

• Status: Completed
• Conditions: Diabetic Nephropathy
• Intervention / Treatment: Drug: CTP-499; Drug: CTP-499

Detailed Description

This is a double-blind, single ascending dose administration study of four doses of CTP-499. Following dosing safety and tolerability will be assessed. Blood and urine samples will be taken for pharmacokinetics (PK) and bioavailability. Safety assessments will include monitoring of adverse events, vital signs (blood pressure, pulse rate, respiratory rate and oral temperature), clinical laboratory findings, 12-lead ECGs, and physical examination findings.

The plasma concentration time data for CTP-499 and its metabolites will be analyzed using noncompartmental methods. Actual dosing and sampling times will be used for analysis. The primary pharmacokinetics parameters are: Cmax, Tmax, T1/2, AUClast and AUCinf for plasma; relative bioavailability; and Ae and CLr for urine.

• Study Type: Interventional
• Enrollment (Actual): 38
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • New Jersey
    • Hackensack, New Jersey, United States, 07601
      • Frontage

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• healthy volunteers
• ages 18 to 55 years old
• nonsmokers
• BMI of 18 to 30 kg/m2

Exclusion Criteria:

• Significant history of gastrointestinal, cardiovascular, musculoskeletal, endocrine, hematologic, psychiatric, renal, hepatic, bronchopulmonary, neurologic, immunologic, lipid metabolism disorders of drug hypersensitivity
• Systolic Blood pressure < 90 or > 140, diastolic bp > 90

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Single Group Assignment
• Masking: Quadruple

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Placebo Comparator: Part A; Single ascending dose administration of four doses of CTP-499 as tablets under fasting condition. 8 subjects per dose group will be enrolled with a 3:1 randomization of active drug to placebo. Dose levels: 600mg -> 1200mg -> 1800mg -> 2400mg	Drug: CTP-499; 600 mg, 1200 mg, 1800 mg and 2400 mg; Drug: CTP-499; 400 mg immediate release capsule
Active Comparator: Part B; Part B will consist of a single 400 mg dose of an immediate release capsule of CTP-499 administered under fasting conditions. In Part B 6 subjects will be enrolled.	Drug: CTP-499; 600 mg, 1200 mg, 1800 mg and 2400 mg; Drug: CTP-499; 400 mg immediate release capsule

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
To assess safety and tolerability of CTP-499	Assessments will include monitoring of adverse events, vital signs (blood pressure, pulse rate, respiratory rate and oral temperature), clinical laboratory findings, 12 lead ECGs, and physical examination findings. Safety data will be summarized using descriptive statistics for all subjects who receive at least 1 dose. Adverse events will be summarized by frequency. Abnormal laboratory and physical exam findings will be summarized by dose and treatment.	5 days

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
To assess Pharmacokinetics, Pharmacodynamics and relative bioavailability	Pharmacokinetics: individual and mean concentration time profiles will be presented graphically. Alll PK parameters will be summarized by dose group using descriptive statistics (eg n, arithmetic mean, SD, geometric mean, median, CV). Relative bioavailability will be estimated using the geometric mean values of dose normalized AUC for each dose. Pharmacodynamics: From the 12 lead ECG data, VR, PR, QRS, QT, QTcF andd QTcB will be reported for each time point and summarized using descriptive statistics. Mean temporal profiles for 12 lead ECG and vital signs will be presented graphically.	2 days

Collaborators and Investigators

• Sponsor: Concert Pharmaceuticals
• Investigators: Principal Investigator: Gregory Tracey, MD, Frontage Clinical Services

Publications and helpful links

Helpful Links

• Related Info

Study record dates

Study Major Dates

• Study Start: March 1, 2011
• Primary Completion (Actual): April 1, 2011
• Study Completion (Actual): June 1, 2011

Study Registration Dates

• First Submitted: March 30, 2011
• First Submitted That Met QC Criteria: April 4, 2011
• First Posted (Estimate): April 5, 2011

Study Record Updates

• Last Update Posted (Estimate): October 26, 2011
• Last Update Submitted That Met QC Criteria: October 25, 2011
• Last Verified: June 1, 2011

More Information

Terms related to this study

• Keywords: Healthy volunteers; Safety; Pharmacokinetics; Tolerability
• Additional Relevant MeSH Terms: Kidney Diseases; Urologic Diseases; Endocrine System Diseases; Diabetes Complications; Diabetes Mellitus; Diabetic Nephropathies; Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Vasodilator Agents; Enzyme Inhibitors; Platelet Aggregation Inhibitors; Protective Agents; Antioxidants; Phosphodiesterase Inhibitors; Free Radical Scavengers; Radiation-Protective Agents; Pentoxifylline
• Other Study ID Numbers: CP505.1001 CTP-499