Olutasidenib

Olutasidenib is a prescription medication used for the treatment of relapsed or refractory acute myeloid leukemia with a confirmed IDH1 mutation (mIDH1+ R/R AML).

• Olutasidenib is available under the following different brand names: Rezlidhia

Common side effects of Olutasidenib include:

• nausea
• fatigue
• feeling unwell (malaise)
• joint pain
• constipation
• shortness of breath
• fever
• rash
• inflammation of mucus membranes
• diarrhea
• increased aspartate aminotransferase
• increased alanine aminotransferase
• decreased potassium
• decreased sodium
• increased alkaline phosphatase
• increased creatinine
• increased lymphocytes
• increased bilirubin
• high white blood cell count (leukocytosis)
• increased uric acid
• increased lipase
• elevated liver enzymes (transaminitis)

Serious side effects of Olutasidenib include:

• fever
• cough
• trouble breathing
• decreased urination
• dizziness or lightheadedness
• weight gain
• swelling of the arms or legs

Rare side effects of Olutasidenib 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 such as 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

Capsule

• 150 mg

Acute myeloid leukemia

Adult dosage

• 150 mg orally two times a day until disease progression or unacceptable toxicity
• Treat patients without disease progression or toxicity for a minimum of 6 months to allow time for clinical response

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, healthcare provider, or pharmacist first.

• Olutasidenib has severe interactions with no other drugs.
• Olutasidenib has serious interactions with at least 67 other drugs.
• Olutasidenib has moderate interactions with the following drug:
  • lenacapavir
• Olutasidenib 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 Olutasidenib?”

Long-Term Effects

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

Cautions

• Differentiation syndrome
  • Olutasidenib can cause differentiation syndrome
  • If suspected, withhold dose and initiate corticosteroids (eg, dexamethasone 10 mg IV every 12 hours for at least 3 days)
• Hepatotoxicity
  • Olutasidenib can cause hepatotoxicity, presenting as increased ALT, increased AST, increased blood alkaline phosphatase, and/or elevated bilirubin
  • Monitor frequently for clinical symptoms of hepatic dysfunction such as fatigue, anorexia, right upper abdominal discomfort, dark urine, or jaundice
  • If hepatic dysfunction occurs, withhold, reduce, or permanently discontinue Olutasidenib based on recurrence/severity
• Drug interaction overview
• CYP3A substrate and inducer
  • Strong or moderate CYP3A inducers
  • Avoid coadministration
  • Coadministration with strong or moderate CYP3A inducers decreases Olutasidenib Cmax and AUC, which may reduce the drug’s efficacy
• Sensitive CYP3A substrates
  • Avoid coadministration, unless otherwise instructed in the substrates’ prescribing information
  • If concomitant use is unavoidable, monitor for loss of therapeutic effect of these drugs

Pregnancy and Lactation

• Based on animal embryofetal toxicity studies, may cause fetal harm when administered to pregnant women
• Lactation
  • Data are not available on the presence of human milk, its effects on breastfed children, or its effects on milk production
  • Advise women not to breastfeed during treatment and for 2 weeks after the last dose