Activation of Brown Adipose Tissue Thermogenesis in Humans Using Formoterol Fumarate (GB10)

NCT ID: NCT05553184

Last Updated: 2023-11-28

Study Results

Results pending

The study team has not published outcome measurements, participant flow, or safety data for this trial yet. Check back later for updates.

Basic Information

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Recruitment Status

COMPLETED

Clinical Phase

NA

Total Enrollment

12 participants

Study Classification

INTERVENTIONAL

Study Start Date

2022-07-05

Study Completion Date

2023-05-29

Brief Summary

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One emerging, highly modifiable homeostatic mechanism for energy expenditure in humans is brown adipose tissue (BAT) thermogenesis. BAT is currently considered a prime target for the treatment of obesity and Type 2 diabetes (T2D).

Using acetate and fluorodeoxyglucose (FDG) positron emission tomography (PET) , It has been demonstrated that BAT thermogenesis is inducible by chronic cold exposure.

BAT activation through cold exposure is associated with improved glucose homeostasis and insulin sensitivity.

A pharmaceutical approach, which seemed to be very promising to stimulate the activation of BAT, was the use of a selective beta 3-adrenergic receptor agonist, mirabegron. Nevertheless, in a later study, It has been demonstrated that human BAT thermogenesis is under the control of beta-2, not beta-3, adrenergic receptor. The most selective beta-2 adrenergic receptor agonist approved for clinical use in Canada is formoterol fumarate, given in inhalation for the treatment of asthma (Oxeze®).

In summary, BAT contributes to cold-induced thermogenesis and is recruited by chronic cold exposure as well as by a growing number of food supplements and drugs. Intracellular triglyceride (TG) is the primary source of fuel for BAT thermogenesis under normal physiological conditions, as blocking intracellular TG lipolysis using nicotinic acid abolishes BAT thermogenesis. Beta-2 adrenergic stimulation is the pharmacological target to activate BAT thermogenesis in humans and may also lead to white adipose tissue lipolysis. Using a highly-selective beta-2 receptor agonist with and without administration of nicotinic acid would thus give the opportunity to quantify more precisely energy expenditure accounted by BAT thermogenesis and white adipose tissue metabolism in humans.

Detailed Description

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Each participant will undergo three metabolic sessions with PET imaging using \[11C\]-palmitate, \[11C\]-acetate and \[18F\]-FDG:

1. during a 3-h cold exposure (Study A, control condition)
2. after inhalation of Formoterol with oral nicotinic acid (Study B)
3. after inhalation of Formoterol only (Study C).

Conditions

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Type 2 Diabetes Obesity

Study Design

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Allocation Method

RANDOMIZED

Intervention Model

CROSSOVER

The protocol will be carried out as a within-subject, randomized, cross-over study in which each subject will serve as his/her own control
Primary Study Purpose

PREVENTION

Blinding Strategy

NONE

Study Groups

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Acute Cold Exposure

3h-acute cold exposure.

Group Type ACTIVE_COMPARATOR

Acute Cold Exposure

Intervention Type OTHER

Participants will be fitted with a liquid-conditioned tube suit. The liquid-conditioned tube suit will be perfused with 18°C water using a temperature- and flow-controlled circulation bath from time 0 to 180 min.

Positron Emission Tomography (PET)

Intervention Type DIAGNOSTIC_TEST

PET imaging using C11-palmitate (time 90), C11-acetate (time 120) and F18-Fluorodeoxyglucose (FDG) (time 150)

Indirect calorimetry

Intervention Type DIAGNOSTIC_TEST

will be repeated every hour, for 20 minutes, using Vmax29n.

dual-energy x-ray absorptiometry (DEXA scan)

Intervention Type DIAGNOSTIC_TEST

Whole body scan

Biopsy

Intervention Type PROCEDURE

After local anesthesia with 2% xylocaine without epinephrine, 100-200 mg of subcutaneous adipose tissue will be sampled by needle (14G) biopsy

iv lines

Intervention Type PROCEDURE

for stable tracer perfusion and blood sampling

Electromyogram (EMG)

Intervention Type PROCEDURE

Surface electrodes will be used to measure skeletal muscle activity and shivering intensity

Formoterol with nicotinic acid

Formoterol fumarate or Oxeze® Turbuhaler®: 48 µg (4 inhalations of 12 µg).

Nicotinic acid or Niacin: repeated doses of 150 MG every 30 minutes, for 3 hours.

Group Type EXPERIMENTAL

Formoterol Fumarate 12 micrograms Inhalation Powder

Intervention Type DRUG

At time 60 minutes, a total of 48 micrograms will be inhaled within 3 minutes: 4 inhalations of 12 micrograms of fumarate formoterol (Oxeze® Turbuhaler®).

Nicotinic Acid 50 MG Oral Tablet

Intervention Type DRUG

a total dose of 1050 MG will be ingested. From time 0 to 180 minutes, doses of 150 MG will be repeated every 30 minutes.

Positron Emission Tomography (PET)

Intervention Type DIAGNOSTIC_TEST

PET imaging using C11-palmitate (time 90), C11-acetate (time 120) and F18-Fluorodeoxyglucose (FDG) (time 150)

Indirect calorimetry

Intervention Type DIAGNOSTIC_TEST

will be repeated every hour, for 20 minutes, using Vmax29n.

Biopsy

Intervention Type PROCEDURE

After local anesthesia with 2% xylocaine without epinephrine, 100-200 mg of subcutaneous adipose tissue will be sampled by needle (14G) biopsy

iv lines

Intervention Type PROCEDURE

for stable tracer perfusion and blood sampling

Formoterol without nicotinic acid

Formoterol fumarate or Oxeze® Turbuhaler®: 48 µg (4 inhalations of 12 µg).

Group Type EXPERIMENTAL

Formoterol Fumarate 12 micrograms Inhalation Powder

Intervention Type DRUG

At time 60 minutes, a total of 48 micrograms will be inhaled within 3 minutes: 4 inhalations of 12 micrograms of fumarate formoterol (Oxeze® Turbuhaler®).

Positron Emission Tomography (PET)

Intervention Type DIAGNOSTIC_TEST

PET imaging using C11-palmitate (time 90), C11-acetate (time 120) and F18-Fluorodeoxyglucose (FDG) (time 150)

Indirect calorimetry

Intervention Type DIAGNOSTIC_TEST

will be repeated every hour, for 20 minutes, using Vmax29n.

Biopsy

Intervention Type PROCEDURE

After local anesthesia with 2% xylocaine without epinephrine, 100-200 mg of subcutaneous adipose tissue will be sampled by needle (14G) biopsy

iv lines

Intervention Type PROCEDURE

for stable tracer perfusion and blood sampling

Interventions

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Formoterol Fumarate 12 micrograms Inhalation Powder

At time 60 minutes, a total of 48 micrograms will be inhaled within 3 minutes: 4 inhalations of 12 micrograms of fumarate formoterol (Oxeze® Turbuhaler®).

Intervention Type DRUG

Nicotinic Acid 50 MG Oral Tablet

a total dose of 1050 MG will be ingested. From time 0 to 180 minutes, doses of 150 MG will be repeated every 30 minutes.

Intervention Type DRUG

Acute Cold Exposure

Participants will be fitted with a liquid-conditioned tube suit. The liquid-conditioned tube suit will be perfused with 18°C water using a temperature- and flow-controlled circulation bath from time 0 to 180 min.

Intervention Type OTHER

Positron Emission Tomography (PET)

PET imaging using C11-palmitate (time 90), C11-acetate (time 120) and F18-Fluorodeoxyglucose (FDG) (time 150)

Intervention Type DIAGNOSTIC_TEST

Indirect calorimetry

will be repeated every hour, for 20 minutes, using Vmax29n.

Intervention Type DIAGNOSTIC_TEST

dual-energy x-ray absorptiometry (DEXA scan)

Whole body scan

Intervention Type DIAGNOSTIC_TEST

Biopsy

After local anesthesia with 2% xylocaine without epinephrine, 100-200 mg of subcutaneous adipose tissue will be sampled by needle (14G) biopsy

Intervention Type PROCEDURE

iv lines

for stable tracer perfusion and blood sampling

Intervention Type PROCEDURE

Electromyogram (EMG)

Surface electrodes will be used to measure skeletal muscle activity and shivering intensity

Intervention Type PROCEDURE

Other Intervention Names

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Oxeze Turbuhaler Niacin 50 MG

Eligibility Criteria

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Inclusion Criteria

* BMI of 18 to 30 kg/m2.

Exclusion Criteria

* Change in weight of more than 2 kg over the past 3 months or recent changes in lifestyle;
* The presence of any chronic medical condition requiring any pharmacological treatment;
* Previous intolerance or allergy to lactose, formoterol, nicotinic acid or local anesthetic agent;
* Any previous cardiac arrhythmia, long QT syndrome or hypokalemia;
* Chronic treatment with any medication other than contraceptives;
* Acute use of any drug other that acetaminophen or non-steroidal anti-inflammatory without decongestant or other stimulants;
* Smoking or consumption of more than 2 alcoholic beverages per day;
* Having participated to a research study with exposure to radiation in the last two years before the start of the study.
Minimum Eligible Age

18 Years

Maximum Eligible Age

45 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

Yes

Sponsors

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Université de Sherbrooke

OTHER

Sponsor Role lead

Responsible Party

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André Carpentier

Tenure professor

Responsibility Role PRINCIPAL_INVESTIGATOR

Principal Investigators

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André C. Carpentier, M.D.

Role: PRINCIPAL_INVESTIGATOR

Université de Sherbrooke

Locations

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Centre de recherche du CHUS

Sherbrooke, Quebec, Canada

Site Status

Countries

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Canada

Other Identifiers

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GB10-2021-3873

Identifier Type: -

Identifier Source: org_study_id