A Phase I Study of 8-week Continuous Treatment With Polyethylene Glycol Loxenatide in Patients With Type 2 Diabetes

A Double-Blind, Multicenter, Randomized Study Evaluating the Safety, Tolerability and Pharmacokinetic/Pharmacodynamic Relationship in T2DMs Treated With 8 Weeks Injection of Polyethylene Glycol Loxenatide

Polyethylene Glycol Loxenatide (PEX168) is a new human glucagon-like peptide 1 (GLP-1) analogue that created on the basis of the Exenatide and modified by polyethylene glycol (PEG).

This study aims to evaluate the PK, PD and safety by 8-week continuous treatment of PEX168.

Study Overview

• Status: Completed
• Conditions: Type 2 Diabetes
• Intervention / Treatment: Drug: PEX168

• Study Type: Interventional
• Enrollment (Actual): 50
• Phase: Phase 1

Contacts and Locations

Study Locations

• China
  • Beijing
    • Beijing, Beijing, China
      • Beijing Tongren Hospital

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 20 years to 65 years (ADULT, OLDER_ADULT)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

1. aged 20-65 years old, male or female, diagnosis of type 2 diabetes according to the 1999 WHO criteria more than 3 months.
2. HbA1C 7.0-10.0% and fasting plasma glucose 7.0-10.0 mmol/L after treatment of diet, exercise or a single oral hypoglycemic agents (metformin , glimepiride or pioglitazone).
3. unused insulin within 3 months prior to the enrollment.
4. Body mass index within the range from 19 to 35, and body weight does not changes exceeding 10% in the past 3 months.
5. Normol liver, kidney, heart function.
6. Willing to use physical means of contraception during the trial stage.
7. voluntarily to participate in the study.

Exclusion Criteria:

1. 1 diabetes.
2. used GLP-1, GLP-1 analogs or DPP-4 inhibitors in the past 3 months.
3. have diabetic ketoacidosis , diabetic hyperosmolar nonketotic coma patients with a history
4. There is a history of severe hypoglycemia : such as low blood sugar cause drowsiness , unconsciousness , nonsense , and even coma.
5. with severe diabetes complications ( renal , retinal , nerve , vascular disease).
6. has acute and chronic pancreatitis history ;
7. heart failure , unstable angina , severe arrhythmia, patients with a history of myocardial infarction ;
8. There is a history of hypertension and blood pressure is not well controlled : SBP> 160mmHg and / or DBP> 95mmHg persons ;
9. severe chronic gastrointestinal disease ( active ulcer nearly six months ) or have been affecting drug absorption in patients treated ;
10. There are obvious blood system diseases ;
11. There are other endocrine system diseases , such as hyperthyroidism , etc. ;
12. with severe trauma or surgery , severe infection ;
13. have mental illness , drug or other substance abuse or alcoholism ( drinking at least 2 times per week , more than 100g each drink ) ;
14. used any drugs that may affect the study , within 3 months before treatment as the subjects participated in any clinical trials ;
15. within the past six months more than 400ml of blood loss (including blood , trauma or other reasons ) ;
16. were receiving steroids or are receiving cancer treatment ;
17. has been prepared during pregnancy or pregnancy test in female patients ;
18. hepatitis B HBeAg , hepatitis C antibody positive , HIV antibody positive , syphilis antibody positive .
19. skin test positive of PEX168;
20. The researchers considered any factors that the subject should not participate in this trial.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: TREATMENT
• Allocation: RANDOMIZED
• Interventional Model: PARALLEL
• Masking: QUADRUPLE

Number of Arms

5

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
EXPERIMENTAL: PEX168 50 microgram; PEX168 50 microgram qw sc. and the medication continued for 8 weeks	Drug: PEX168; A injection administered subcutaneously; Other Names: Polyethylene Glycol Loxenatide
EXPERIMENTAL: PEX168 100 microgram; PEX168 100 microgram qw sc. and the medication continued for 8 weeks	Drug: PEX168; A injection administered subcutaneously; Other Names: Polyethylene Glycol Loxenatide
EXPERIMENTAL: PEX168 200 microgram; PEX168 200 microgram qw sc. and the medication continued for 8 weeks	Drug: PEX168; A injection administered subcutaneously; Other Names: Polyethylene Glycol Loxenatide
EXPERIMENTAL: PEX168 300 microgram; PEX168 300 microgram qw sc. and the medication continued for 8 weeks	Drug: PEX168; A injection administered subcutaneously; Other Names: Polyethylene Glycol Loxenatide
PLACEBO_COMPARATOR: Placebo; Placebo qw sc. and the medication continued for 12 weeks	Drug: PEX168; A injection administered subcutaneously; Other Names: Polyethylene Glycol Loxenatide

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
To determine serum concentrations of PEX168	8 weeks

Secondary Outcome Measures

Outcome Measure	Time Frame
To determin HbA1c levels of PEX168	8 weeks

Other Outcome Measures

Outcome Measure	Time Frame
To assess number of participants with Adverse Events as a Measure of Safety and To assess number of participants with Adverse Events as a Measure of Safety and Tolerability	8 weeks

Collaborators and Investigators

• Sponsor: Jiangsu HengRui Medicine Co., Ltd.
• Collaborators: Beijing Tongren Hospital
• Investigators: Principal Investigator: Jinkui Yang, Ph.D, M.D, Beijing Tongren Hospital

Study record dates

Study Major Dates

• Study Start: June 1, 2011
• Primary Completion (ACTUAL): September 1, 2011
• Study Completion (ACTUAL): December 1, 2011

Study Registration Dates

• First Submitted: October 22, 2013
• First Submitted That Met QC Criteria: October 30, 2013
• First Posted (ESTIMATE): November 6, 2013

Study Record Updates

• Last Update Posted (ESTIMATE): November 6, 2013
• Last Update Submitted That Met QC Criteria: October 30, 2013
• Last Verified: October 1, 2013

More Information

Terms related to this study

• Keywords: PEX168, diabetes, phase I
• Additional Relevant MeSH Terms: Glucose Metabolism Disorders; Metabolic Diseases; Endocrine System Diseases; Diabetes Mellitus; Diabetes Mellitus, Type 2
• Other Study ID Numbers: PEX168-I-03