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The purpose of this study is to assess the safety, tolerability and pharmacokinetics of CTP-499 following single dose administration.
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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part A | Placebo Comparator | 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 |
|
| Part B | Active Comparator | 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. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| CTP-499 | Drug | 600 mg, 1200 mg, 1800 mg and 2400 mg |
| |
| CTP-499 |
| 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 |
| 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. |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Gregory Tracey, MD | Frontage Clinical Services | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Frontage | Hackensack | New Jersey | 07601 | United States |
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| ID | Term |
|---|---|
| D003928 | Diabetic Nephropathies |
| ID | Term |
|---|---|
| D007674 | Kidney Diseases |
| D014570 | Urologic Diseases |
| D052776 | Female Urogenital Diseases |
| D005261 | Female Urogenital Diseases and Pregnancy Complications |
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| ID | Term |
|---|---|
| C000626018 | 1-(5-hydroxyhexyl)-3,7-dimethylxanthine |
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| Drug |
400 mg immediate release capsule |
|
| 2 days |
| D000091642 | Urogenital Diseases |
| D052801 | Male Urogenital Diseases |
| D048909 | Diabetes Complications |
| D003920 | Diabetes Mellitus |
| D004700 | Endocrine System Diseases |