Is Rezdiffra The Key To Unlocking Better NASH Outcomes?

In March 2024, the U.S. Food and Drug Administration (FDA) granted accelerated approval to Rezdiffra (resmetirom), marking a significant milestone as the first approved treatment for nonalcoholic steatohepatitis (NASH), in adults with moderate to advanced liver fibrosis (stages F2 to F3)

What Is Rezdiffra Medication Used For?

“Previously, patients with NASH who also have notable liver scarring did not have a medication that could directly address their liver damage,” said Nikolay Nikolov, M.D., acting director of the Office of Immunology and Inflammation in the FDA’s Center for Drug Evaluation and Research.

“Today’s approval of Rezdiffra will, for the first time, provide a treatment option for these patients, in addition to diet and exercise.” 

Rezdiffra is used to treat adults with non-alcoholic steatohepatitis (NASH) who have intermediate to advanced liver scarring (fibrosis) but not decompensated cirrhosis.

It is used along with diet and exercise and is an oral tablet taken once a day.

NASH is also known as nonalcoholic fatty liver disease or metabolic dysfunction-associated steatohepatitis [MASH].

Resmetirom received accelerated approval from the U.S. Food and Drug Administration (FDA) on March 14, 2024, which means continued approval may be based on further clinical trial results.

This is the first drug approved to treat advanced liver disease. There are currently no generics available.

How Does Rezdiffra Work?

Resmetirom’s mechanism of action involves binding to thyroid hormone receptor-beta (THR-beta), which is found primarily in liver tissue.

Activation of this receptor helps to reduce the accumulation of fat in the liver.

When excess fat is deposited in the liver, NASH develops, leading to inflammatory, fibrotic changes and, if left untreated, cirrhosis.

Resmetirom reduces triglyceride levels in liver cells by selectively targeting the THR-beta receptor, thereby potentially reducing the progression of liver injury.

Resmetirom is a THR-beta agonist.

Dosage Guidelines

The recommended dosage of Rezdiffra is weight-based:

• 80 mg once daily for individuals weighing less than 100 kg (220 lbs)
• 100 mg once daily for those weighing 100 kg or more

Patients should take Resmetirom at the same time each day, with or without food.

Rezdiffra Side Effects

Rezdiffra may cause serious side effects, including:

⭕Liver injury (hepatotoxicity): Stop taking Resmetirom and call your healthcare provider right away if you experience any of the following signs or symptoms of hepatotoxicity:

tiredness,

nausea,

vomiting,

fever, rash,

yellowing of the skin or whites of the eyes (jaundice),

or stomach pain/tenderness.

⭕Gallbladder problems. Gallbladder problems, such as gallstones, inflammation of the gallbladder, or inflammation of the pancreas caused by gallstones, can happen with MASH, and may also happen if you take Resmetirom.

‼️Call your healthcare provider right away if you have any of these signs or symptoms, including nausea, vomiting, fever, or stomach (abdominal) pain that is severe and does not go away.

The pain may travel from the abdomen to the back, and the pain may occur with or without vomiting.

The most common side effects of Rezdiffra include diarrhea, nausea, itching, stomach pain, vomiting, dizziness, and constipation.

Warnings

Before taking Rezdiffra, tell your healthcare provider about all of your medical conditions, including whether you:

👉have any liver disease other than NASH

👉have or have been told you have gallbladder problems, including gallstones

👉are taking other medications, such as gemfibrozil, which lowers cholesterol, or cyclosporine, which suppresses the immune system, as some of these may not be recommended

👉Are pregnant or plan to become pregnant

👉Are breastfeeding or plan to breastfeed

Drug Interactions

⭕CYP2C8 Inhibitors

Strong inhibitors (e.g., gemfibrozil): Concomitant use is not recommended due to a significant increase in resmetirom exposure, which may heighten the risk of adverse effects

Moderate inhibitors (e.g., clopidogrel): If co-administered, a dosage reduction of resmetirom is advised:

• For patients weighing less than 100 kg: reduce to 60 mg once daily.
• For patients weighing 100 kg or more: reduce to 80 mg once daily .

⭕OATP1B1 and OATP1B3 Inhibitors

Drugs like cyclosporine inhibit these transporters and can increase resmetirom levels. Concomitant use is not recommended

⭕Statins

Resmetirom can elevate the plasma concentrations of certain statins, increasing the risk of statin-related adverse reactions such as liver enzyme elevations, myopathy, and rhabdomyolysis.

Recommended maximum daily doses when co-administered with resmetirom are:

• Rosuvastatin and simvastatin: 20 mg
• Pravastatin and atorvastatin: 40 mg

⭕CYP2C8 Substrates

Resmetirom is a weak inhibitor of CYP2C8 and may increase the exposure of drugs metabolized by this enzyme. Monitor patients for adverse reactions when co-administering resmetirom with CYP2C8 substrates

Market Impact And Future Outlook

The approval of Rezdiffra has significant implications for the treatment of MASH, a condition affecting millions worldwide.

Analysts project that Rezdiffra could generate up to $3.5 billion in annual sales by 2030, reflecting the substantial demand for effective MASH therapies.

Furthermore, the FDA’s decision not to require liver biopsies for diagnosis may facilitate broader adoption of Rezdiffra, as non-invasive diagnostic methods become more prevalent

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Our efforts to improve the affordability of Rezdiffra medicine aim to ensure that more patients can benefit from this important medication.

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