Resmetirom

REZDIFFRA

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Pronunciation: res-me-TIR-om (rez-DI-fra)

Resmetirom ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Resmetirom ballicule

Resmetirom REZDIFFRA mascot mnemonic cartoon — Visual mnemonic: Resmetirom mascot
**“Rez’s different metabolic ROM”**
thyroid gland → binds THR-β thyroid receptors in liver

What it isLiver-selective thyroid-receptor-beta agonist; metabolic dysfunction-associated steatohepatitis with fibrosis.

Why this oneIt was the first therapy specifically approved for MASH, targeting hepatic fat and fibrosis through liver-directed thyroid signaling.

What limits itDiarrhea and nausea occur early. Monitor for hepatotoxicity, and manage its clinically important statin interactions.

Resmetirom molecular structure (skeletal formula) — Molecular structure: Resmetirom

FDA-approved for

MASH/NASH (2024)

FDA label

Read the full label on DailyMed ↗

FDA dosing	Population	Start	Target	Max
Noncirrhotic MASH w/ moderate-advanced fibrosis (F2-F3)	<100 kg	80 mg QD	80 mg QD	80 mg QD
Noncirrhotic MASH w/ moderate-advanced fibrosis (F2-F3)	≥100 kg	100 mg QD	100 mg QD	100 mg QD

Renal No adjustment needed (mild, moderate, or severe)

Hepatic Mild (Child-Pugh A): no adjustment; avoid in moderate-severe (Child-Pugh B/C) / decompensated cirrhosis

Instructions

Swallow whole; do not split, crush, or chew
With or without food
Missed dose: skip it, resume next scheduled dose
Moderate CYP2C8 inhibitor: reduce to 60 mg QD (<100 kg) or 80 mg QD (≥100 kg); strong CYP2C8 inhibitor not recommended

Available strengths

tab 60, 80, 100 mg

Cautions

Hepatotoxicity, incl. drug-induced autoimmune-like hepatitis; monitor liver tests, discontinue if suspected
Gallbladder events (cholelithiasis, cholecystitis, gallstone pancreatitis); interrupt for acute events
Increased statin exposure (atorvastatin, pravastatin, rosuvastatin, simvastatin); monitor for myopathy/rhabdomyolysis

Adverse reactions

Diarrhea
Nausea
Pruritus
Vomiting
Constipation
Abdominal pain
Dizziness

Pregnancy No human data; animal embryo-fetal toxicity (rabbit) at maternally toxic doses

Lactation No data on presence in human milk or effects on infant

Cost

Resmetirom (REZDIFFRA)

Strength		#/mo	CostPlus
60 mg	tab	30 qd	not offered
80 mg	tab	30 qd	not offered
100 mg	tab	30 qd	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Resmetirom is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2038 est.

NO BOXED WARNINGS

Principal riskDiarrhea and nausea early

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk1 / 4

Legacy pregnancy categoryNot assigned — PLLR-era drug

Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.

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Memory aids: interaction avatars

CYP2C8 substrate

OATP inhibitor

OATP substrate

Open Resmetirom in the interactive console ↗