Resmetirom

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Cat Number

API920509326

CAS Number

920509-32-6

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Product Detail Description Scientific Support Customer Q&A

CAS Number

920509-32-6

Storage

Store at -20 ºC

Synonyms

2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile; MGL-3196; VIA-3196

Molecular Formula

C17H12Cl2N6O4

Molecular Weight

435.2

Smiles

CC(C)C1=CC(=NNC1=O)OC2=C(C=C(C=C2Cl)N3C(=O)NC(=O)C(=N3)C#N)Cl

Relative Density

1.65

pKa

3.96±0.40

General Description

Resmetirom is a novel, first-in-class, selective Thyroid Hormone Receptor-beta (THR-β) partial agonist and the first FDA-approved drug for the treatment of non-cirrhotic Metabolic Dysfunction-Associated Steatohepatitis (MASH), also referred to as NASH. As a significant advancement in the treatment of this complex chronic liver disease, Resmetirom addresses a critical unmet need by targeting the underlying pathology of MASH.

Mechanism of Action

Acting via a highly specific liver-targeted transport system, Resmetirom is a partial agonist that preferentially activates the THR-β. This receptor is present in high density within liver cells and exhibits up to 28-fold selectivity for THR-β compared with the THR-α receptor, which mediates action in extra-hepatic tissues such as the heart and bone. Resmetirom can exert a functional mimicry of the physiological actions of the endogenous thyroid hormone T3 in the liver while sparing adverse effects on the cardiovascular system and bones.

Application

Resmetirom is indicated for the treatment of adult patients with non-cirrhotic MASH who have evidence of moderate to advanced liver fibrosis (F2 to F3 stage). Its use can lead to a reduction of steatosis, or the pathological accumulation of fat in the liver, as well as associated metabolic abnormalities, such as high levels of serum cholesterol and triglycerides, in order to stop disease progression.

In MASLD/MASH, decreased hepatic THR-β signaling leads to reduced mitochondrial β-oxidation of fatty acids and enhanced lipogenesis that promotes steatosis, inflammation, and fibrosis. Restoration of THR-β activity by Resmetirom is expected to increase fatty-acid catabolism and suppress VLDL secretion, and to down-regulate pro-fibrotic genes (COL1A1, ACTA2) and proinflammatory cytokines.
Preclinical models showed rapid hepatic fat lowering, improved NAFLD activity score, and decreased collagen deposition. Phase Ⅱ trials confirmed the -37 % hepatic fat reduction versus −8 % with placebo at 36 weeks with good tolerance. The phase Ⅲ MAESTRO-NASH trial met both primary endpoints at 52 weeks (MASH resolution without worsening of fibrosis and ≥1-stage improvement in fibrosis) with an associated 16 % LDL-C reduction. The MAESTRO-NAFLD-1 safety study confirmed similar rates of adverse events to placebo. Most events were mild diarrhea/nausea, and there were improvements in atherogenic lipids and hepatic stiffness. Quality-of-life analyses showed associations of ≥30 % fat reduction with clinically meaningful improvements in physical function.

Fig. 1 Resmetirom hepatic effects in MASLD/MASH. (Jamal F.; et al. 2025)

References

Jamal F, et al. Resmetirom in the Management of Metabolic Dysfunction-Associated Steatotic Liver Disease and Steatohepatitis. Life, 2025, 15(8): 1306.

Can your Resmetirom be used for commercial drug production?

Yes, we support the scale-up of Resmetirom for commercial launch and supply needs.

Why is Resmetirom a breakthrough MASH therapy?

Resmetirom is the first FDA-approved treatment for MASH, and it was developed to meet the unmet medical need by treating the fundamental pathophysiology of the liver.

What is the patient target population for Resmetirom?

Adults with non-cirrhotic MASH with moderate to advanced liver fibrosis (stages F2 to F3).

Can you supply technical information for Resmetirom purity and potency?

We provide technical datasheets that include detailed information about the purity, potency, and analytical methods used for our Resmetirom.