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    Mirabegron molecular structure

    Mirabegron

    PharmaceuticalFDA Approved

    Also known as: Myrbetriq, Betmiga, Betanis, YM-178, YM178, beta3-adrenoceptor agonist

    Mirabegron is an approved prescription drug, not a research chemical. Astellas Pharma developed it as YM-178 and it was approved by the FDA in 2012 under the brand name Myrbetriq for overactive bladder, with European approval as Betmiga; the US label now also covers neurogenic detrusor overactivity in children aged three and older.

    Half-Life: Terminal half-life about 32 hours in one phase 1 multiple-dose study and about 60 hours in a second, with plasma peaks at three to five hours and steady state within seven days in healthy young and elderly adults (PMID: 23063375)Route: OralMW: 396.51 g/molCAS: 223673-61-8
    Last reviewed:
    Pharmaceutical
    Category
    FDA Approved
    Research Stage

    Overview

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    At A Glance

    Mechanism

    Mirabegron is a selective agonist of the beta-3 adrenergic receptor. In the bladder, beta-3 activation raises cyclic AMP in detrusor smooth muscle and promotes relaxation during the storage phase, which is the licensed mechanism. In adipose tissue, beta-3 stimulation drives lipol

    Half-Life
    Terminal half-life about 32 hours in one phase 1 multiple-dose study and about 60 hours in a second, with plasma peaks at three to five hours and steady state within seven days in healthy young and elderly adults (PMID: 23063375)
    Routes
    Oral
    Potential Benefits
    Increased brown adipose tissue metabolic activity and raised resting metabolic rate by 203 kcal per day in twelve healthy men after a single oral dose (PMID: 25565203)Increased brown fat activity, HDL cholesterol, apolipoprotein A-I and adiponectin and improved insulin sensitivity over four weeks in 14 healthy women (PMID: 31961826)Increased brown fat activity, resting energy expenditure, body temperature and circulating free fatty acids across six human studies in meta-analysis (PMID: 38159219)Reduced adipose tissue myofibroblasts and CXCR2 expression in people with obesity (PMID: 41087927)Reached steady state within seven days with plasma peaks at three to five hours, and about 40 percent higher exposure in women than men, in healthy young and elderly adults (PMID: 23063375)

    Overview

    Mirabegron is an approved prescription drug, not a research chemical. Astellas Pharma developed it as YM-178 and it was approved by the FDA in 2012 under the brand name Myrbetriq for overactive bladder, with European approval as Betmiga; the US label now also covers neurogenic detrusor overactivity in children aged three and older. It works by activating the beta-3 adrenergic receptor, which relaxes the bladder detrusor muscle. The reason it appears on the research chemical market has nothing to do with bladders. Beta-3 receptors are also the main adrenergic receptors on rodent brown fat, and for decades beta-3 agonists were the leading candidate for a drug that would burn calories by turning on brown adipose tissue. Mirabegron was the first beta-3 agonist available in a form that could test that idea in people. The first test worked. In twelve healthy men, a single oral dose increased brown fat metabolic activity measured by FDG PET-CT in every subject and raised resting metabolic rate by 203 kcal per day, about 13 percent (PMID: 25565203). A four-week open-label study in 14 healthy women found higher brown fat activity and resting energy expenditure with no change in body weight or composition, alongside higher HDL cholesterol, apolipoprotein A-I, adiponectin and improved insulin sensitivity on an intravenous glucose tolerance test (PMID: 31961826). The complication is dose and receptor selectivity. A Canadian group showed that human brown adipocyte thermogenesis is actually driven by the beta-2 receptor, not beta-3, and that mirabegron only raised brown fat thermogenesis when taken at the maximum allowable dose, at which point it also bound beta-1 and beta-2 receptors, producing cardiovascular effects and white fat lipolysis (PMID: 32755608). A meta-analysis of six human studies found increased brown fat activity, resting energy expenditure, body temperature and free fatty acids, but also increased heart rate, diastolic blood pressure and insulin, with no change in brown fat volume or blood glucose (PMID: 38159219). Pharmacology is well characterized because it is a licensed drug. Plasma concentrations peak at three to five hours and decline with a terminal half-life of roughly 32 to 60 hours across two phase 1 studies; exposure is about 40 percent higher in women than men, and steady state is reached within a week (PMID: 23063375). Absorption, metabolism and excretion have been mapped with radiolabeled drug (PMID: 22269146). Anyone taking mirabegron for metabolic reasons is using an approved drug off-label at or near its ceiling dose, where the cardiovascular effects are real and measured. That is a different risk profile from its licensed bladder use, and it needs a prescriber, not a supplier.

    Potential Research Fields

    Brown adipose tissueBeta-3 adrenergic pharmacologyEnergy expenditureUrology

    Chemical Information

    IUPAC Name

    Not yet available

    CAS Number

    223673-61-8

    Molecular Formula

    C21H24N4O2S

    Molecular Mass

    396.51 g/mol

    Dosing & Protocols

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    Interactions

    Contraindications

    Label-based and mechanism-based: the approved product labeling should be consulted, and the documented rises in heart rate and blood pressure make uncontrolled hypertension a clear concern for off-label metabolic use (PMID: 38159219). Exposure is about 40 percent higher in women than in men, which matters for dosing decisions made by a prescriber (PMID: 23063375). Mirabegron inhibits CYP2D6, so interactions with CYP2D6 substrates such as desipramine and metoprolol are documented and require prescriber review. Off-label use for fat loss has not been studied beyond four weeks.

    Research Disclaimer

    This interaction data is compiled from published research and community reports. It may not be exhaustive. Always consult a healthcare professional before combining compounds.

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    Meldonium

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    t½ About 5.7 h after a single 5 mg oral capsule and 5.6 h after 2 mg intravenously in 18 healthy volunteers; oral bioavailability averaged 0.60 with a range of 0.27 to 0.99 and was inversely related to CYP2D6 activity (PMID: 11736884)
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    1 vendors · 1 listings

    Research Score

    30

    0 PubMed studies

    Quality Indicators

    Data Completeness

    63%
    Description
    Mechanism of Action
    Chemical Data
    Dosing Protocols
    Safety Profile
    PubMed Studies
    Interactions
    Vendor Listings

    Quick Facts

    Half-Life

    Terminal half-life about 32 hours in one phase 1 multiple-dose study and about 60 hours in a second, with plasma peaks at three to five hours and steady state within seven days in healthy young and elderly adults (PMID: 23063375)

    Molecular Weight

    396.51 g/mol

    Administration

    Oral

    CAS Number

    223673-61-8

    Trial Phase

    FDA Approved

    0

    Research Disclaimer

    This information is for educational and research purposes only. Not intended as medical advice. Consult a healthcare professional before use.

    Frequently Asked Questions

    What is Mirabegron used for in research?

    Mirabegron is an approved prescription drug, not a research chemical. Astellas Pharma developed it as YM-178 and it was approved by the FDA in 2012 under the brand name Myrbetriq for overactive bladder, with European approval as Betmiga; the US label now also covers neurogenic detrusor overactivity in children aged three and older. It works by activating the beta-3 adrenergic receptor, which relaxes the bladder detrusor muscle.

    The reason it appears on the research chemical market has nothing to do with bladders. Beta-3 receptors are also the main adrenergic receptors on rodent brown fat, and for decades beta-3 agonists were the leading candidate for a drug that would burn calories by turning on brown adipose tissue. Mirabegron was the first beta-3 agonist available in a form that could test that idea in people.

    The first test worked. In twelve healthy men, a single oral dose increased brown fat metabolic activity measured by FDG PET-CT in every subject and raised resting metabolic rate by 203 kcal per day, about 13 percent (PMID: 25565203). A four-week open-label study in 14 healthy women found higher brown fat activity and resting energy expenditure with no change in body weight or composition, alongside higher HDL cholesterol, apolipoprotein A-I, adiponectin and improved insulin sensitivity on an intravenous glucose tolerance test (PMID: 31961826).

    The complication is dose and receptor selectivity. A Canadian group showed that human brown adipocyte thermogenesis is actually driven by the beta-2 receptor, not beta-3, and that mirabegron only raised brown fat thermogenesis when taken at the maximum allowable dose, at which point it also bound beta-1 and beta-2 receptors, producing cardiovascular effects and white fat lipolysis (PMID: 32755608). A meta-analysis of six human studies found increased brown fat activity, resting energy expenditure, body temperature and free fatty acids, but also increased heart rate, diastolic blood pressure and insulin, with no change in brown fat volume or blood glucose (PMID: 38159219).

    Pharmacology is well characterized because it is a licensed drug. Plasma concentrations peak at three to five hours and decline with a terminal half-life of roughly 32 to 60 hours across two phase 1 studies; exposure is about 40 percent higher in women than men, and steady state is reached within a week (PMID: 23063375). Absorption, metabolism and excretion have been mapped with radiolabeled drug (PMID: 22269146).

    Anyone taking mirabegron for metabolic reasons is using an approved drug off-label at or near its ceiling dose, where the cardiovascular effects are real and measured. That is a different risk profile from its licensed bladder use, and it needs a prescriber, not a supplier.

    What forms does Mirabegron come in?

    Mirabegron is available in capsule form.

    How much does Mirabegron cost?

    Prices start at $99.99 across 1 verified vendor.

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    Research Tools

    Related Compounds

    View All

    Albuterol (salbutamol)

    PharmaceuticalFDA Approved

    Albuterol, called salbutamol outside the United States, is a beta-2 adrenergic agonist and a standard asthma medicine worldwide.

    t½ Mean terminal half-life 3.8 hours after intravenous administration in 16 healthy adult men, with absolute oral bioavailability of 44 percent and plasma peaks one to three hours after oral administration (PMID: 3653233)
    PreclinicalView Profile

    Clascoterone

    PharmaceuticalPreclinical

    Clascoterone (brand name Winlevi; development codes CB-03-01 and, for the alopecia formulation, Breezula) is a first-in-class topical androgen receptor (AR) antagonist approved by the U.S.

    1188 studiesView Profile

    Finasteride

    PharmaceuticalPreclinical

    Finasteride is an orally-active selective type II 5α-reductase inhibitor that blocks the conversion of testosterone to dihydrotestosterone (DHT), the primary androgenic driver of both benign prostatic hyperplasia (BPH) and androgenetic alopecia (male-pattern hair loss).

    PreclinicalView Profile

    Meldonium

    PharmaceuticalApproved (Latvia)

    Meldonium, sold as Mildronate, was developed at the Latvian Institute of Organic Synthesis (PMID: 12242052) and is a licensed cardiovascular medicine in Latvia and a number of eastern European and post-Soviet countries.

    t½ Not a single simple value: in 32 healthy athlete volunteers taking oral meldonium for three weeks, plasma took several days to reach steady state and urinary elimination continued for several months after the last dose, because tissue clearance depends on slow diffusion rather than transport (PMID: 30328291)
    PreclinicalView Profile

    Tropisetron

    PharmaceuticalApproved (Japan)

    Tropisetron, coded ICS 205-930 during development and marketed as Navoban, is a serotonin 5-HT3 receptor antagonist approved as an antiemetic in Japan and in many other countries outside the United States, with ATC code A04AA03 (KEGG DRUG D02041, D02130).

    t½ About 5.7 h after a single 5 mg oral capsule and 5.6 h after 2 mg intravenously in 18 healthy volunteers; oral bioavailability averaged 0.60 with a range of 0.27 to 0.99 and was inversely related to CYP2D6 activity (PMID: 11736884)
    PreclinicalView Profile

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