Multiple Ascending Oral Dose Phase I Study With Px-102

NCT ID: NCT01998672

Last Updated: 2014-11-04

Basic Information

• Recruitment Status: COMPLETED
• Clinical Phase: PHASE1
• Total Enrollment: 42 participants
• Study Classification: INTERVENTIONAL
• Study Start Date: 2012-02-29
• Study Completion Date: 2012-10-31

Brief Summary

The purpose of this study is to assess the safety and tolerability of the FXR agonist Px-102 in healthy subjects after 7 days multiple oral dosing.

Detailed Description

The study is a single-centre, double-blind, randomized, placebo-controlled, parallel group phase I study with healthy male subjects receiving ascending multiple oral oral doses of Px-102 to assess the safety and tolerability, pharmacokinetics and pharmacodynamics.

Conditions

Healthy

Study Design

• Allocation Method: RANDOMIZED
• Intervention Model: PARALLEL
• Primary Study Purpose: TREATMENT
• Blinding Strategy: TRIPLE

Study Groups

Px-102

Px-102 drinking solution, 0.5 mg/kg, 1.0 mg/kg and 1.5 mg/kg

Group Type: ACTIVE_COMPARATOR

Px-102

Intervention Type: DRUG

Px-102 drinking solution, 0.5 mg/kg, 1.0 mg/kg and 1.5 mg/kg

Placebo

Oral drinking solution

Group Type: PLACEBO_COMPARATOR

Placebo

Intervention Type: DRUG

Drinking solution

Interventions

Px-102

Px-102 drinking solution, 0.5 mg/kg, 1.0 mg/kg and 1.5 mg/kg

Intervention Type: DRUG

Placebo

Drinking solution

Intervention Type: DRUG

Eligibility Criteria

Inclusion Criteria

• Healthy male subject of Caucasian origin 18 to 45 years of age (inclusive).
• Good state of health (mentally and physically) as determined by medical history, physical examination, vital signs, ECG recording and clinical lab results.
• BMI in between 20-29 kg/m² (inclusive); with absolute weight in between 70 to 120 kg.
• Total cholesterol and liver enzyme levels [alanine aminotransferase (ALT), aspartate aminotransferase (AST), gamma-glutamyltransferase (GGT), alkaline phosphatase (AP)] strictly within the normal ranges at screening and on Day -1. Serum triglyceride not exceeding the upper limit of normal range.
• HbA1c ≤ 6.5%
• Subject has been informed both verbally and in writing and has given written consent to participation in the study prior to start and any study-related procedure.
• Negative results for HIV- and Hepatitis-B and -C serology at screening.
• Subject (including female partners of childbearing potential) has to use a highly effective method of birth control (failure rate less than 1% per year when used consistently and correctly), e.g. implants, injectables, combined oral contra-ceptives in combination with a barrier method, some intrauterine contraceptive devices or sexual abstinence.

Exclusion Criteria

• Female gender
• Use of prescription or non-prescription drugs within 7 days (30 if the drug is a possible enzyme inducer) prior to administration of study medication. Use of drugs known to induce steatosis (e.g. valproate, amiodarone or prednisone) or to affect body weight and carbohydrate metabolism
• Any acute or chronic illness or clinically relevant finding at screening and at base-line examination which may jeopardize the subject's participation in the study
• History or presence of biliary obstruction or biliary disease, hepatic encephalopathy, advanced ascites, portal hypertension, esophageal/gastric variceal bleeding, hepatocellular carcinoma, previous liver transplantation or any other chronic liver disease
• Renal dysfunction, e.g. glomerular filtration rate ≤ 80 ml/min/1.73 m2 (as determined by the formula of Cockroft-Gault)
• Type I or II Diabetes
• Any clinically relevant abnormality on screening medical assessment, laboratory examination, 12-lead ECG
• Any clinically relevant finding in the baseline telemetry within the pre-dose evaluated observation period of at least 20 hours
• Marked baseline prolongation of QT/QTc interval (QTc interval > 440 ms) in the 12-lead ECG using the Fridericia method for QTc analysis
• Heart rate < 50 bpm.
• History of pathological cardiovascular symptoms or a severe cardiovascular event
• History of severe chronic autoimmune diseases such as severe allergy, atopic eczema, chronic dermatitis, severe psoriasis, multiple sclerosis, severe asthma, lupus or related disorders
• Allergies (except for mild forms of hay fever) or history of hypersensitivity reactions
• Smoking (regular or irregular) > 5 cigarettes (or equivalent) per day
• Excessive alcohol drinking (more than approximately 20 g alcohol per day), unable to refrain from alcohol drinking from 48 hours prior to dosing until the last pharmacokinetic blood sample has been withdrawn
• Positive test for drugs or alcohol at screening or prior to the dosing session
• History of alcoholism or drug/chemical/substance abuse within past 2 years
• Investigator deems the subject unable or unwilling to comply fully with the study protocol
• Has received clinical study medication within the last 30 days prior to this study
• Donation or loss of 400 ml or more of blood within eight (8) weeks prior to dosing
• Allergic to any of the active or inactive ingredients in the study medication
• Any other reason which the Investigator considers unsuitable for the subject to participate
• Any condition or previous disease leading to pruritus or itching of the skin.

• Minimum Eligible Age: 18 Years
• Maximum Eligible Age: 45 Years
• Eligible Sex: MALE
• Accepts Healthy Volunteers: Yes

Sponsors

Phenex Pharmaceuticals AG

INDUSTRY

Sponsor Role: lead

Responsible Party

Responsibility Role: SPONSOR

Principal Investigators

Claus Kremoser, Dr.

Role: STUDY_CHAIR

Phenex Pharmaceuticals AG

Locations

FOCUS Clinical Drug Development GmbH

Neuss, , Germany

Countries

Germany

Other Identifiers

PHS-Px-102-I-02

Identifier Type: -

Identifier Source: org_study_id