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Thyromimetic
Thyromimetic drugs are synthetic agonists of the thyroid hormone receptor's isoforms TR α1, TRα2, TRβ1, or TRβ2, mimicking some or all of the effects of endogenously produced thyroid hormones that regulate metabolism. Some thyromimetic drugs are selective for various of these receptors over others, enabling more targeted effects and reducing toxicity. Thyromimetics selective for TRβ—including eprotirome, sobetirome, resmetirom, and the prodrug VK2809—have been investigated for the treatment of non-alcoholic fatty liver disease, dyslipidemia Dyslipidemia is a metabolic disorder characterized by abnormally high or low amounts of any or all lipids (e.g. fats, triglycerides, cholesterol, phospholipids) or lipoproteins in the blood. Dyslipidemia is a risk factor for the development of ..., and other metabolic and neurodegenerative diseases. References Further reading *{{cite journal , last1=Yehuda-Shnaidman , first1=Einav , last2=Kalderon , first2=Bella , last3=Bar-Tan ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sobetirome
Sobetirome (GC-1) is a thyromimetic drug that binds to the thyroid hormone receptor TRβ1 preferentially compared to TRα1. It has been investigated for the treatment of dyslipidemia, obesity, Pitt–Hopkins syndrome, cholestatic liver disease, multiple sclerosis, bleomycin-induced lung fibrosis, and COVID-19 caused ARDS. It was designated as an orphan drug by the FDA for the treatment of X-linked adrenoleukodystrophy Adrenoleukodystrophy (ALD) is a disease linked to the X chromosome. It is a result of fatty acid buildup caused by failure of peroxisomal fatty acid beta oxidation which results in the accumulation of very long chain fatty acids in tissues throu .... References {{reflist Orphan drugs Thyroid hormone receptor beta agonists Carboxylic acids Phenols Isopropyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Omzotirome
Omzotirome (INN), formerly codenamed TRC-150094, is a thyromimetic drug which acts as a metabolic modulator which restores metabolic flexibility. It has been shown to improve insulin resistance and hyperglycemia, and is in Phase III human clinical trials for the treatment of Cardiometabolic-Based Chronic Disease (CMBCD) by improving dysglycemia Dysglycemia is a general definition for any abnormalities in blood glucose levels. They include hyperglycemia, hypoglycemia, impaired glucose tolerance test, impaired fasting glucose, among others. __TOC__ Hyperglycemia If blood sugar levels rema ..., dyslipidemia and hypertension. References {{pharm-stub Small-molecule drugs Thyroid Indenes Experimental diabetes drugs Pyrazoles Carboxylic acids ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eprotirome
Eprotirome is a thyromimetic drug that has been investigated for the treatment of dyslipidemia. A Phase III trial in humans was discontinued after the drug was found to have negative effects on cartilage Cartilage is a resilient and smooth type of connective tissue. Semi-transparent and non-porous, it is usually covered by a tough and fibrous membrane called perichondrium. In tetrapods, it covers and protects the ends of long bones at the joints ... in dogs. References {{reflist Thyroid hormone receptor beta agonists Abandoned drugs Carboxylic acids Bromobenzene derivatives Anilides Isopropyl compounds Phenols ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
VK2809
VK2809 (formerly known as MB07811) is a thyromimetic prodrug whose active form is selective for the THR-β isoform. It is being developed by Viking Therapeutics in a phase II trial for the treatment of nonalcoholic steatohepatitis and is also being investigated for glycogen storage disease type I Glycogen storage disease type I (GSD I) is an inherited disease that prevents the liver from properly breaking down stored glycogen, which is necessary to maintain adequate blood sugar levels. GSD I is divided into two main types, GSD Ia and GSD ...a. In 2023, Viking Therapeutics filed a lawsuit against the developer of ASC41, Chinese company Ascletis BioScience, accusing it of stealing Viking's trade secrets to develop ASC41 which is allegedly similar to, or identical to, VK2809. References {{reflist Thyroid hormone receptor beta agonists Prodrugs Dioxaphosphorinanes Phenols 3-Chlorophenyl compounds Isopropyl compounds Experimental drugs developed for non-alcoholic fatty ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eprotirome
Eprotirome is a thyromimetic drug that has been investigated for the treatment of dyslipidemia. A Phase III trial in humans was discontinued after the drug was found to have negative effects on cartilage Cartilage is a resilient and smooth type of connective tissue. Semi-transparent and non-porous, it is usually covered by a tough and fibrous membrane called perichondrium. In tetrapods, it covers and protects the ends of long bones at the joints ... in dogs. References {{reflist Thyroid hormone receptor beta agonists Abandoned drugs Carboxylic acids Bromobenzene derivatives Anilides Isopropyl compounds Phenols ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Triiodothyronine
Triiodothyronine, also known as T3, is a thyroid hormone. It affects almost every physiological process in the body, including growth and development, metabolism, body temperature, and heart rate. Production of T3 and its prohormone thyroxine (T4) is activated by thyroid-stimulating hormone (TSH), which is released from the anterior pituitary gland. This pathway is part of a closed-loop feedback process: Elevated concentrations of T3, and T4 in the blood plasma inhibit the production of TSH in the anterior pituitary gland. As concentrations of these hormones decrease, the anterior pituitary gland increases production of TSH, and by these processes, a feedback control system stabilizes the level of thyroid hormones in the bloodstream. At the cellular level, T3 is the body's more active and potent thyroid hormone. T3 helps deliver oxygen and energy to all of the body's cells, its effects on target tissues being roughly four times more potent than those of T4. Of the thyroid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Resmetirom
Resmetirom, sold under the brand name Rezdiffra, is a medication used for the treatment of noncirrhotic nonalcoholic steatohepatitis. It is a thyroid hormone receptor beta (NR1A2) agonist. The most common side effects include diarrhea and nausea. Resmetirom was approved for medical use in the United States in March 2024. The US Food and Drug Administration considers it to be a first-in-class medication. Medical uses Resmetirom is indicated, in conjunction with diet and exercise, for the treatment of adults with noncirrhotic nonalcoholic steatohepatitis with moderate to advanced liver fibrosis (consistent with stages F2 to F3 fibrosis). History In a phase III clinical trial, it was found to be effective for resolving noncirrhotic nonalcoholic steatohepatitis and improving liver fibrosis. The US Food and Drug Administration (FDA) evaluated the safety and efficacy of resmetirom based on an analysis of a surrogate endpoint at month twelve in a 54-month, randomized, double- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thyroid Hormone Receptor
The thyroid hormone receptor (TR) is a type of nuclear receptor that is activated by binding thyroid hormone. TRs act as transcription factors, ultimately affecting the regulation of gene transcription and translation. These receptors also have non-genomic effects that lead to second messenger activation, and corresponding cellular response. Structure There are four domains that are present in all TRs. Two of these, the DNA-binding (DBD) and hinge domains, are involved in the ability of the receptor to bind hormone response elements (HREs). TRs also have a ligand binding domain (LBD) that allows them to bind to thyroid hormone with high affinity. The fourth domain is a transactivation domain which allows the receptor to bind other transcription factors. Function Thyroid hormone receptors play critical roles in the regulation of metabolism, heart rate, and development of organisms. These receptors are typically associated with retinoic acid receptors (RXR), forming hetero ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thyroid Hormones
File:Thyroid_system.svg, upright=1.5, The thyroid system of the thyroid hormones T3 and T4 rect 376 268 820 433 Thyroid-stimulating hormone rect 411 200 849 266 Thyrotropin-releasing hormone rect 297 168 502 200 Hypothalamus rect 66 216 386 256 Anterior pituitary gland rect 66 332 342 374 Negative feedback rect 308 436 510 475 Thyroid gland rect 256 539 563 635 Thyroid hormones rect 357 827 569 856 Catecholamine rect 399 716 591 750 Metabolism desc bottom-left Thyroid hormones are two hormones produced and released by the thyroid gland, triiodothyronine (T3) and thyroxine (T4). They are tyrosine-based hormones that are primarily responsible for regulation of metabolism. T3 and T4 are partially composed of iodine, derived from food. A deficiency of iodine leads to decreased production of T3 and T4, enlarges the thyroid tissue and will cause the disease known as simple goitre. The major form of thyroid hormone in the blood is thyroxine (T4), whose half-life of arou ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabolism
Metabolism (, from ''metabolē'', "change") is the set of life-sustaining chemical reactions in organisms. The three main functions of metabolism are: the conversion of the energy in food to energy available to run cellular processes; the conversion of food to building blocks of proteins, lipids, nucleic acids, and some carbohydrates; and the elimination of metabolic wastes. These enzyme-catalyzed reactions allow organisms to grow and reproduce, maintain their Structures#Biological, structures, and respond to their environments. The word ''metabolism'' can also refer to the sum of all chemical reactions that occur in living organisms, including digestion and the transportation of substances into and between different cells, in which case the above described set of reactions within the cells is called intermediary (or intermediate) metabolism. Metabolic reactions may be categorized as ''catabolic''—the ''breaking down'' of compounds (for example, of glucose to pyruvate by c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Resmetirom
Resmetirom, sold under the brand name Rezdiffra, is a medication used for the treatment of noncirrhotic nonalcoholic steatohepatitis. It is a thyroid hormone receptor beta (NR1A2) agonist. The most common side effects include diarrhea and nausea. Resmetirom was approved for medical use in the United States in March 2024. The US Food and Drug Administration considers it to be a first-in-class medication. Medical uses Resmetirom is indicated, in conjunction with diet and exercise, for the treatment of adults with noncirrhotic nonalcoholic steatohepatitis with moderate to advanced liver fibrosis (consistent with stages F2 to F3 fibrosis). History In a phase III clinical trial, it was found to be effective for resolving noncirrhotic nonalcoholic steatohepatitis and improving liver fibrosis. The US Food and Drug Administration (FDA) evaluated the safety and efficacy of resmetirom based on an analysis of a surrogate endpoint at month twelve in a 54-month, randomized, double- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
