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

Concert Pharmaceuticals

Status and phase: Completed; Phase 1

Conditions: Diabetic Nephropathy

Treatments: Drug: CTP-499

Study type: Interventional

Funder types: Industry

Identifiers

NCT01328821

CP505.1001 CTP-499

Details and patient eligibility

About

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

Full 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.

Enrollment: 38 patients

Sex: All

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

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

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Single Group Assignment

Masking: Quadruple Blind

---

38 participants in 2 patient groups, including a placebo group

Part A

Placebo Comparator group

Description:

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

Treatment:

Drug: CTP-499

Drug: CTP-499

Part B

Active Comparator group

Description:

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.

Treatment:

Drug: CTP-499

Drug: CTP-499