Rezdiffra

Rezdiffra is used to treat metabolic dysfunction-associated steatohepatitis (MASH), formerly known as noncirrhotic nonalcoholic steatohepatitis (NASH) in adults with moderate to advanced liver fibrosis, but not with cirrhosis of the liver, alongside diet and exercise changes. It is taken once daily and was the first FDA-approved treatment for NASH.

NASH has been renamed to MASH (metabolic dysfunction-associated steatohepatitis) to replace potentially stigmatizing language (nonalcoholic). NASH/MASH is a condition in which excess liver fat leads to inflammation and scarring. Rezdiffra works by targeting a liver receptor called THR-beta, helping to reduce fat buildup in liver cells, which can slow the progression of MASH.

In the pivotal Phase 3 MAESTRO-NASH trial (NCT03900429), patients taking Rezdiffra were significantly more likely to see improvement in liver scarring (fibrosis) and resolution of NASH/MASH compared with placebo, with improvements in liver enzymes seen in as little as 3 months.

Rezdiffra (resmetirom) gained FDA approval on March 14, 2024, under the accelerated approval pathway. Continued approval may depend on confirmatory trials demonstrating ongoing clinical benefit. There is no generic version of Rezdiffra currently available.

• Take Rezdiffra exactly as your healthcare provider tells you to take it.
• Your dose is based on your body weight.
• Take Rezdiffra by mouth, 1 time a day, with or without food.
• Swallow Rezdiffra tablets whole. Do not split, crush, or chew the tablets,
• If you miss a dose of Rezdiffra, skip the missed dose and take your next dose at the regular time.

Before you take Rezdiffra, tell your healthcare provider about all of your medical conditions, including if you:

• Have any liver problems other than NASH/MASH
• Have gallbladder problems or have been told you have gallbladder problems, including gallstones
• Are pregnant or plan to become pregnant. It is not known if Rezdiffra will harm your unborn baby. Pregnancy Safety Study. There is a pregnancy safety study for women who are or become pregnant during treatment with Rezdiffra. The purpose of this pregnancy safety study is to collect information about your health and your baby’s health. You or your healthcare provider can report your pregnancy by visiting https://pregnancyregistry.madrigalpharma.com/ or calling 1-800-905-0324.
• Are breastfeeding or plan to breastfeed. It is not known if Rezdiffra passes into your breast milk. Talk to your healthcare provider about the best way to feed your baby while you are taking it.

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Rezdiffra and other medicines may affect each other, causing side effects. Rezdiffra may affect the way other medicines work, and other medicines may affect how Rezdiffra works.

• Especially tell your healthcare provider if you take medicines that contain gemfibrozil to help lower your triglycerides because Rezdiffra is not recommended in patients taking these medicines.
• Tell your healthcare provider if you are taking medicines such as clopidogrel to thin your blood or statin medicines to help lower your cholesterol.

Know the medicines you take. Keep a list of them to show your healthcare provider and pharmacist when you get a new medicine.

Common side effects

The most common side effects of Rezdiffra are:

• Diarrhea
• Nausea
• Itching
• Stomach (abdominal) pain
• Vomiting
• Dizziness.
• Constipation.

Serious side effects

Rezdiffra may cause serious side effects, including liver injury and gallbladder problems.

• Liver injury (hepatotoxicity). Stop taking Rezdiffra and call your healthcare provider right away if you develop tiredness, nausea, vomiting, fever, rash, yellowing of the skin or whites of the eyes (jaundice), or pain or tenderness in the upper middle or upper right area of your abdomen.
• Gallbladder problems. Gallstones, gallbladder inflammation, or inflammation of the pancreas from gallstones can occur with MASH and may occur while taking Rezdiffra. Call your healthcare provider right away if you develop nausea, vomiting, fever, or severe abdominal pain that will not go away. The pain may radiate from your abdomen to your back and may occur with or without vomiting.

It is not known if Rezdiffra is safe and effective in children under the age of 18.

These are not all the possible side effects of Rezdiffra. For more information, ask your healthcare provider or pharmacist. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects to www.fda.gov/medwatch.

The cost for prescription drugs varies depending on your insurance plan and which pharmacy you use.

Eligible commercially insured patients may pay as little as $0 a month with the Rezdiffra Copay Savings Card. Ask your doctor or pharmacist if you qualify or refer to our Rezdiffra price guide page for more information about the cost of this medicine.

Dose of Rezdiffra for NASH/MASH

• Weight <100 kg: 80 mg orally once a day
• Weight ≥100 kg: 100 mg orally once a day.

Rezdiffra (resmetirom) works by partially activating a liver-specific receptor called thyroid hormone receptor-beta (THR-beta), which helps reduce fat buildup in the liver. It selectively targets THR-beta while having much less effect on THR-alpha, the receptor responsible for thyroid hormone activity in the heart and bones. This selective action allows resmetirom to reduce liver fat with a lower risk of affecting other organs.

Rezdiffra belongs to the drug class known as thyroid hormone receptor-beta (THR-beta) agonists.

The cost of Rezdiffra varies depending on your insurance plan and pharmacy. You may be eligible for a Rezdiffra savings card or coupon, ask your doctor or pharmacist if you qualify. Refer to our Drugs.com price guide page for more information about Rezdiffra Prices, Coupons, Copay Cards & Patient Assistance.

You may also be eligible for a Rezdiffra savings card or coupon. Ask your doctor or pharmacist if you qualify.

Rezdiffra is not typically associated with weight loss because it works primarily to reduce fat buildup in the liver rather than throughout the body. However, some patients may experience minor weight loss as a result of gastrointestinal side effects such as diarrhea, nausea, or vomiting, which can temporarily reduce appetite. Rezdiffra is not a weight loss medication and should not be used for that purpose.

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Rezdiffra can interact with several other medicines:

• Strong CYP2C8 inhibitors, such as gemfibrozil, should not be taken with Rezdiffra. Moderate CYP2C8 inhibitors, such as clopidogrel, can be used, but the Rezdiffra dose should be reduced.
• Certain statins used to lower cholesterol, including atorvastatin, pravastatin, rosuvastatin, and simvastatin, can be taken with Rezdiffra, but the daily statin dose should be limited as recommended.
• For medicines that are CYP2C8 substrates (those broken down by the same liver enzyme), patients should be monitored more closely for side effects related to those medicines.

This is not a complete list of interactions. Know the medicines you take. Keep a list of them to show your healthcare provider and pharmacist when you get a new medicine.

Store Rezdiffra at room temperature between 68ºF and 77ºF (20ºC and 25ºC).

Active ingredient: resmetirom.

Inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, magnesium stearate, mannitol, and microcrystalline cellulose.

Film coating: polyethylene glycol, polyvinyl alcohol, talc, titanium dioxide, red iron oxide (100 mg tablets), and yellow iron oxide (80 mg and 100 mg tablets).

Rezdiffra is manufactured and distributed by Madrigal Pharmaceuticals, West Conshohocken, PA.