Mechanisms for Activation of Beige Adipose Tissue in Humans

NCT ID: NCT04666636

Last Updated: 2025-12-17

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

RECRUITING

Clinical Phase

PHASE2

Total Enrollment

65 participants

Study Classification

INTERVENTIONAL

Study Start Date

2020-12-07

Study Completion Date

2026-12-01

Brief Summary

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Mirabegron (Myrbetriq®, Astellas) is a highly specific and well-tolerated ß3 agonist marketed for overactive bladder. This trial will assess the effects of mirabegron on glucose tolerance and adipose tissue in prediabetic patients

Detailed Description

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Among the many survival adaptations developed by mammals is a defense against the cold and hypothermia; one of these adaptations is the ability to uncouple oxidative phosphorylation and generate heat, rather than adenosine triphosphate (ATP), from lipid substrate in specialized tissues, and there has been much interest in exploiting this inefficient metabolism for the treatment of obesity and insulin resistance. Brown adipose tissue (BAT) protects against obesity in mice, and studies have documented cold-induced BAT in humans using positron emission tomography (PET-CT) scanning. Additional studies have demonstrated that white adipose tissue (WAT) can upregulate its thermogenic capacity and become "beige", and this beiging of SC WAT likely provides an additional defense against the cold.

Brown and beige fat can be activated by cold temperatures, or through catecholamines. The catecholamines epinephrine and norepinephrine have undesirable side effects. However, adipocytes are among the few cells that contain ß3 adrenergic receptors (ß3AR), whereas the heart is dominated by ß1 and ß2 receptors. Therefore, a drug that could target the ß3AR could activate brown/beige fat without cardiovascular side effects. Recently, there have been human studies performed and obese human subjects participants were treated with the ß3AR agonist mirabegron. This resulted in improved glucose homeostasis by increasing insulin sensitivity and insulin secretion. It was also found that mirabegron treatment of obese adults did not increase BAT or induce weight loss, but instead induced beige fat, along with increased insulin sensitivity, which was accompanied by an increase in type I fibers in skeletal muscle. Mirabegron treatment stimulated subcutaneous (SC) WAT beiging, lipolysis, and remodeling. However, unlike WAT, insulin-producing ß-cells and muscle do not express the ß3AR; therefore, it is thought that the beneficial effects of mirabegron treatment occurred by an indirect mechanism.

Currently, mirabegron (Myrbetriq®, Astellas) is a highly specific and well-tolerated ß3 agonist marketed for overactive bladder. It is hypothesized that mirabegron treatment of prediabetic subjects will improve glucose homeostasis through improved insulin sensitivity and ß-cell function, in addition to other changes in adipose tissue. Additionally, mirabegron treatment may change the plasma composition of proteins, lipids, metabolites, short-chain fatty acids, or exosomal miRNAs that are known to affect peripheral tissue function.

This trial will quantify the effects of the ß3 agonist mirabegron on glucose metabolism and adipose tissue in a placebo-controlled trial and determine some of the mechanistic underpinnings of these effects.

Conditions

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PreDiabetes

Study Design

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Allocation Method

RANDOMIZED

Intervention Model

PARALLEL

Primary Study Purpose

BASIC_SCIENCE

Blinding Strategy

DOUBLE

Participants Investigators

Study Groups

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Placebo

Participants in the group will receive placebo.

Group Type PLACEBO_COMPARATOR

Placebo

Intervention Type DRUG

Participants will take one pill (placebo) daily for the first week and two pills daily for the remaining 15 weeks.

Mirabegron

Participants in this group will receive Mirabegron for 16 weeks.

Group Type EXPERIMENTAL

Mirabegron

Intervention Type DRUG

Participants will take one pill (50mg Mirabegron) daily for the first week. For week two, participants will take two pills (50mg and 25mg Mirabegron). Unless there are side effects, for the remaining 14 weeks participants will take two pills (50mg each) daily.

Sub-Study: Mirabegron and the acute response to food

This sub-study will involve the recruiting of the same subjects who are eligible for this study as described above. Subjects will report to the CCTS fasting on 3 separate days. On each visit, the subject will have 5 blood draws and each blood draw will be about 8 ml, for a total of 40 ml of blood at each visit. Visit 1 will involve the participant consuming a standardized meal. At visit 2, participants will take 50mg of Mirabegron. And visit 3 will involve the participant consuming the same meal as visit 1 and also taking 50 mg of mirabegron.

Group Type EXPERIMENTAL

Mirabegron 50 MG

Intervention Type DRUG

Participants will take one pill (50mg Mirabegron) daily between visit 2 and visit 3

Sub-Study: Mirabegron dosing and Oral Glucose Tolerance Tests (Optional)

Studies have found that larger doses of mirabegron do not elicit the same improvements in insulin sensitivity. Therefore, we aim to perform a dose-response study to gain an improved understanding of mirabegron dosing and changes in insulin sensitivity.

This sub-study will have 4 total visits. visit 1 is a baseline oral glucose tolerance test. At the end of visit 1, participants will be given 6 weeks of mirabegron (25 mg) and will take 1 pill once per day for 4-6 weeks leading up to visit 2. Visit 2 will also be a standard oral glucose tolerance test. At the end of visit 2, participants will be given 6 weeks of mirabegron (50 mg) and take 1 pill once per day for 4-6 weeks leading up to visit 3. Visit 3 will also be a standard oral glucose tolerance test. At the end of visit 3, participants will be given 6 weeks of mirabegron (10 mg) and take 1 pill once per day for 4-6 weeks. Visit 4 will be the final visit and will also be a standard oral glucose tolerance test.

Group Type EXPERIMENTAL

Mirabegron 100 mg

Intervention Type DRUG

participants will be given 6 weeks of mirabegron (25 mg) and will take 1 pill once per day for 4-6 weeks. Next participants will be given 6 weeks of mirabegron (50 mg) and take 1 pill once per day for 4-6 weeks. Last participants will be given 6 weeks of mirabegron (100 mg) and take 1 pill once per day for 4-6 weeks.

Interventions

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Placebo

Participants will take one pill (placebo) daily for the first week and two pills daily for the remaining 15 weeks.

Intervention Type DRUG

Mirabegron

Participants will take one pill (50mg Mirabegron) daily for the first week. For week two, participants will take two pills (50mg and 25mg Mirabegron). Unless there are side effects, for the remaining 14 weeks participants will take two pills (50mg each) daily.

Intervention Type DRUG

Mirabegron 50 MG

Participants will take one pill (50mg Mirabegron) daily between visit 2 and visit 3

Intervention Type DRUG

Mirabegron 100 mg

participants will be given 6 weeks of mirabegron (25 mg) and will take 1 pill once per day for 4-6 weeks. Next participants will be given 6 weeks of mirabegron (50 mg) and take 1 pill once per day for 4-6 weeks. Last participants will be given 6 weeks of mirabegron (100 mg) and take 1 pill once per day for 4-6 weeks.

Intervention Type DRUG

Other Intervention Names

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Myrbetriq Myrbetriq Myrbetriq

Eligibility Criteria

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Inclusion Criteria

* BMI 27-45
* prediabetes (A1c 5.7-6.4)
* impaired fasting glucose or impaired glucose tolerance

Exclusion Criteria

* diabetes
* chronic use of anti-diabetic medication
* acute or chronic inflammatory condition
* unstable medical condition
* cancer
* renal insufficiency
* any contraindication for Mirabegron
* BMI \>45
Minimum Eligible Age

35 Years

Maximum Eligible Age

65 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

Yes

Sponsors

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National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)

NIH

Sponsor Role collaborator

Philip Kern

OTHER

Sponsor Role lead

Responsible Party

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Philip Kern

Professor

Responsibility Role SPONSOR_INVESTIGATOR

Principal Investigators

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Philip Kern, MD

Role: PRINCIPAL_INVESTIGATOR

University of Kentucky

Locations

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University of Kentucky

Lexington, Kentucky, United States

Site Status RECRUITING

Countries

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United States

Central Contacts

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Philip Kern, MD

Role: CONTACT

859-323-5821

Facility Contacts

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Philip Kern, MD

Role: primary

859-323-2615

Other Identifiers

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R01DK124626

Identifier Type: NIH

Identifier Source: secondary_id

View Link

60821

Identifier Type: -

Identifier Source: org_study_id