Resmetirom

Resmetirom is a prescription medication indicated in conjunction with diet and exercise for the treatment of adults with noncirrhotic non-alcoholic steatohepatitis (NASH) with moderate to advanced liver fibrosis (consistent with stages F2 to F3 fibrosis).

• Resmetirom is available under the following different brand names: Rezdiffra.

Common side effects of Resmetirom include:

• diarrhea 
• itching 
• vomiting 
• constipation
• nausea 
• stomach (abdominal) pain 
• dizziness

Serious side effects of Resmetirom include:

• liver injury (hepatotoxicity with signs and symptoms such as tiredness, fever, nausea, rash, pain, or tenderness in the upper middle or upper right area of the stomach (abdomen), vomiting, and skin or the white part of the eyes turning yellow)
• gallbladder problems such as gallstones, inflammation of the gallbladder, or inflammation of the pancreas from gallstones

Rare side effects of Resmetirom include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms include sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Tablet

• 60 mg
• 80 mg
• 100 mg

Non-alcoholic Steatohepatitis

Adult dosage

• Dosage is based on actual body weight
  • Less than 100 kg: 80 mg orally once a day
  • More than or equal to 100 kg: 100 mg orally once a day

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Resmetirom has severe interactions with no other drugs
• Resmetirom has serious interactions with no other drugs
• Resmetirom has moderate interactions with no other drugs
• Resmetirom has minor interactions with no other drugs

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Resmetirom?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Resmetirom?”

Cautions

• Hepatotoxicity
  • Hepatotoxicity has been observed
  • Monitor during treatment for elevated liver function tests (LFTs) and for developing liver-related adverse reactions
  • Monitor for symptoms and signs of hepatotoxicity (eg, fatigue, nausea, vomiting, right upper quadrant pain or tenderness, jaundice, fever, rash, and/or eosinophilia [more than 5%])
  • If hepatotoxicity is suspected, discontinue therapy, and continue to monitor
  • If LFTs return to baseline, weigh potential risks against the benefits of restarting
  • If LFTs do not return to baseline, consider drug-induced autoimmune-like hepatitis (DI-ALH) or autoimmune liver disease in the evaluation of elevations in liver tests
  • Instruct patients to immediately report any signs or symptoms of severe liver injury (eg, fatigue, nausea, vomiting, right upper quadrant pain or tenderness, jaundice, fever, rash) or symptoms of gallbladder adverse reactions, including cholelithiasis, cholecystitis, and obstructive pancreatitis (gallstones) to a healthcare provider
• Gallbladder-related adverse reactions
  • Cholelithiasis, acute cholecystitis, and obstructive pancreatitis (gallstone) were observed
  • If cholelithiasis is suspected, gallbladder diagnostic studies and appropriate clinical follow-up are indicated
  • If an acute gallbladder event is suspected, interrupt treatment until the event is resolved
• Drug interaction overview
  • CYP2C8 substrate
  • OATP1B1 and OATP1B3 substrate
  • Weak CYP2C8 inhibitor
    • Strong or moderate CYP2C8 inhibitors
    • Strong inhibitor (eg, gemfibrozil): Not recommended
    • Moderate inhibitor (eg, clopidogrel): Reduce dosage
    • Strong or moderate CYP2C8 inhibitors can increase Resmetirom plasma concentrations and risk of Resmetirom adverse reactions
  • OATP1B1 and OATP1B3 inhibitors
    • Not recommended
    • OATP1B1 and OATP1B3 inhibitors can increase Resmetirom plasma concentrations and risk of Resmetirom adverse reactions
  • Atorvastatin, pravastatin, rosuvastatin and simvastatin
    • Monitor for statin-related adverse reactions including but not limited to elevation of liver tests, myopathy, and rhabdomyolysis
    • Limit daily dosage of statin as recommended
  • CYP2C8 substrates
    • Monitor more frequently for substrate-related adverse reactions
    • Resmetirom increases exposure to CYP2C8 substrates, which may increase the risk of adverse reactions related to these substrates

Pregnancy and Lactation

• There are no available data on Resmetirom use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes
• There are risks to the mother and fetus related to underlying NASH with liver fibrosis
• There are risks to the mother and fetus related to underlying maternal NASH with liver fibrosis, such as increased risks of gestational diabetes, hypertensive complications, preterm birth, and postpartum hemorrhage
• Lactation
  • There is no information regarding the presence of Resmetirom in human or animal milk, its effects on breastfed infants, or its effects on milk production