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AZD4076 in Type 2 Diabetic Subjects With Non-Alcoholic Fatty Liver Disease.

Phase 1
Completed
Conditions
T2DM With NAFLD
Interventions
Drug: Placebo
Registration Number
NCT02826525
Lead Sponsor
AstraZeneca
Brief Summary

This is a phase I/IIa, randomized, single-blind, placebo-controlled, multiple-ascending dose study conducted at a single site. The study plans to include up to approximately 46 evaluable subjects with Type 2 Diabetes Mellitus (HbA1c 7-11%) and Non-Alcoholic Fatty Liver disease (liver fat content \> = 8%) on metformin monotherapy.

Three initial cohorts are planned:

* Cohort 1: 6 subjects receiving AZD4076 and 4 subjects receiving placebo

* Cohort 2: 12 subjects receiving AZD4076 and 10 subjects receiving placebo

* Cohort 3: 10 subjects receiving AZD4076 and 10 subjects receiving placebo, with the possibility to add additional subjects if drop-out rates are higher than expected

Pending review by SRC, an additional 2 cohorts, each consisting of 18 evaluable subjects may be included in the study.

The primary objectives of this clinical trial are to investigate the safety and tolerability of AZD4076 following subcutaneous administration of multiple ascending doses; to assess the effect of AZD4076 on whole body insulin sensitivity using hyperinsulinemic euglycemic clamp with tracer technique; and to assess the effect of AZD4076 on liver fat content using magnetic resonance imaging. Secondary objectives of this trial are to characterize multiple dose PK of AZD4076 and its longmer and shortmer metabolites and assess the time required to reach steady state and the degree of accumulation; to assess the efficacy of AZD4076 on 24-hour glucose; and to assess the effect of AZD4076 on homeostatic model assessment insulin resistant (HOMA-IR) and Matsuda index.

Detailed Description

This is a phase I/IIa, randomized, single-blind, placebo-controlled, multiple-ascending dose study conducted at a single site. The study plans to include up to approximately 46 evaluable subjects with Type 2 Diabetes Mellitus (HbA1c 7-11%) and Non-Alcoholic Fatty Liver disease (liver fat content \> = 8%) on metformin monotherapy

Three initial cohorts are planned:

* Cohort 1: 6 subjects receiving AZD4076 and 4 subjects receiving placebo

* Cohort 2: 12 subjects receiving AZD4076 and 10 subjects receiving placebo

* Cohort 3: 10 subjects receiving AZD4076 and 10 subjects receiving placebo, with the possibility to add additional subjects if drop-out rates are higher than expected.

Pending review by SRC, an additional 2 cohorts, each consisting of 18 evaluable subjects may be included in the study.

The planned study consists of a screening visit, followed by 12 subsequent study visits. There will be a total of three residential periods: (1) Loading phase of the treatment (visit 2, days -4 to 14), (2) maintenance phase of treatment (visit 6, days 42-43), and (3) 8 weeks post-first dose of study drug (visit 9, days 53-56). Dosing of study drug will take place on days 1, 3, 5, 7, and 9 in the loading phase; and on days 14, 21, 28, 35, and 42 during the maintenance phase. Following the maintenance phase, subjects will have four follow-up visits.

Study Objectives:

The primary objectives of this clinical trial are to investigate the safety and tolerability of AZD4076 following subcutaneous administration of multiple ascending doses; to assess the effect of AZD4076 on whole body insulin sensitivity using hyperinsulinemic euglycemic clamp with tracer technique; and to assess the effect of AZD4076 on liver fat content using magnetic resonance imaging. Secondary objectives of this trial are to characterize multiple dose PK of AZD4076 and its longmer and shortmer metabolites and assess the time required to reach steady state and the degree of accumulation; to assess the efficacy of AZD4076 on 24-hour glucose; and to assess the effect of AZD4076 on homeostatic model assessment insulin resistant (HOMA-IR) and Matsuda index.

Study Population:

Subjects participating in this study are adult males and females of non-child bearing potential, who are 18-70 years of age, body mass index 23-40 kg/m2, diagnosed with T2DM who are inadequately controlled (HbA1C 7-11%) on a stable metformin regimen, and who have hepatic steatosis (defined as liver fat content of \>=8% per MRI).

Duration of treatment:

The screening visit will occur within 42 days prior to the administration of the study drug. Total length of the treatment period is 6 weeks. The treatment period is divided in two phases: the loading phase, in which participants will receive the study drug every other day for 9 days (Days 1, 3, 5 , 7 and 9); thereafter subjects will enter the maintenance phase, where dosing will occur once weekly for four weeks (Days 14, 21, 28, 35 and 42). To ensure safety, subjects will be followed for approximately 5 months post the last dose of study drug.

Investigational product, dosage and mode of administration:

The study will utilize two study drugs: AZD4076 and placebo. Both drugs will be administered subcutaneously in the abdomen.

Safety analysis:

The key outcomes for the safety analyses are: adverse events, vital signs, safety laboratory parameters, ECGs, telemetry; and structured neurological and physical examination, as well as injection site assessment. Pharmacodynamic parameters will be derived from data generated from the clamp procedure, MRI, HOMA, OGTT and 24-hour glucose AUC. For pharmacokinetic parameters, plasma and urine concentrations of AZD4076 and its metabolites will be measured

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
14
Inclusion Criteria

Not provided

Exclusion Criteria

Not provided

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
ControlPlaceboSubjects in this arm will receive placebo
TreatmentAZD4076Subjects in this arm will receive AZD4076
Primary Outcome Measures
NameTimeMethod
The safety and tolerability of AZD4076 by assessment of blood pressureFrom screening until 26 weeks post first dose

To assess the safety and tolerability of multiple ascending doses of AZD4076

The safety and tolerability of AZD4076 by assessment of pulseFrom screening until 26 weeks post first dose

To assess the safety and tolerability of multiple ascending doses of AZD4076

Reduction in liver fat content (%) per MRIScreening and 54 days post first dose

To assess the effect of AZD4076 on liver fat content using magnetic resonance imaging

The safety and tolerability of AZD4076 by assessing the number of participants with adverse eventsFrom screening until 26 weeks post first dose

To assess the safety and tolerability of multiple ascending doses of AZD4076

The safety and tolerability of AZD4076 by assessment of oral temperatureFrom day -2 until day 42

To assess the safety and tolerability of multiple ascending doses of AZD4076

The safety and tolerability of AZD4076 by assessing clinical chemistryFrom screening until 26 weeks post first dose

Percentage of patients with clinically significant changes in laboratory tests.

The safety and tolerability of AZD4076 by assessment of digital electrocardiogram readingsFrom predose until 24 hours post-dose on days 1 and 42

To assess the safety and tolerability of multiple ascending doses of AZD4076

The safety and tolerability AZD4076 by assessment of physical examinationFrom screening until 26 weeks post first dose

Percentage of patients with abnormal physical examination

The safety and tolerability of AZD4076 by assessing the injection siteFrom day 1 until day 42

Percentage of patients with dermatological adverse events

The safety and tolerability of AZD4076 by assessing the number of adverse eventsFrom screening until 26 weeks post first dose

To assess the safety and tolerability of multiple ascending doses of AZD4076

The safety and tolerability of AZD4076 by assessing urinalysisFrom screening until 26 weeks post-first dose

To assess the safety and tolerability of multiple ascending doses of AZD4076

The safety and tolerability of AZD4076 by assessing hematologyFrom screening until 26 weeks post first dose

To assess the safety and tolerability of multiple ascending doses of AZD4076

The safety and tolerability of AZD4076 by assessment of electrocardiogram readingsFrom screening until 26 weeks post first dose

To assess the safety and tolerability of multiple ascending doses of AZD4076

Glucose infusion rate at hyperinsulinemic clampDay -1 and 56 days post first dose

To assess the effect of AZD4076 on whole body insulin sensitivity using hyperinsulinemic euglycemic clamp with tracer technique

Secondary Outcome Measures
NameTimeMethod
Fasting Endogenous Glucose ProductionDay -1 and day 56

To assess the effect of AZD4076 on endogenous glucose production (EGP).

AUC0-24 of AZD4076 and longmer and shortmer metabolitesDosing day 1 and day 42

To characterize pharmacokinetics of AZD4076 by area under the curve to 24 hours

Cmax of AZD4076 and longmer and shortmer metabolitesDosing day 1 and day 42

To characterize pharmacokinetics of AZD4076 by peak concentration

24 hour glucose area under the curveDay -2 and day 55

To assess the effect of AZD4076 on 24-hour glucose.

Matsuda IndexDay -2 and day 55

To assess the effect of AZD4076 on Matusda Index

Tmax of AZD4076 and longmer and shortmer metabolitesDosing day 1 and day 42

To characterize pharmacokinetics of AZD4076 by time to peak concentration

Ae of AZD4076 and longmer and shortmer metabolitesDosing day 1 and day 42

To characterize pharmacokinetics of AZD4076 by amount excreted in urine

AUCt of AZD4076 and longmer and shortmer metabolitesDosing day 1 and day 42

To characterize pharmacokinetics of AZD4076 by area under the curve to time

HOMA-IRDay -2 and day 55

To assess the effect of AZD4076 on homeostatic model assessment insulin resistant (HOMA-IR)

CLR of AZD4076 and longmer and shortmer metabolitesDay 1 and 42

To characterize pharmacokinetics of AZD4076 by clearance

fe% of AZD4076 and longmer and shortmer metabolitesDosing day 1 and day 42

To characterize pharmacokinetics of AZD4076 by fraction excreted in urine

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