Omaveloxolone

Omaveloxolone is a prescription medication used for the treatment of Friedreich ataxia.

• Omaveloxolone is available under the following different brand names: Skyclarys

Common side effects of Omaveloxolone include:

• Headache 
• Nausea
• Abdominal pain
• Fatigue
• Diarrhea
• Oropharyngeal pain
• Influenza
• Vomiting
• Muscle spasms
• Back pain
• Decreased appetite
• Rash 

Serious side effects of Omaveloxolone include:

• None

Rare side effects of Omaveloxolone 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, loss of coordination, feeling 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 and pediatric dosage

Capsule

• 50 mg

Friedreich Ataxia

Adult dosage

• 150 mg (3 capsules) orally every day

Pediatric dosage

• Aged below 16 years:
• Safety and efficacy not established
• Aged above 16 years: 150 mg (3 capsules) orally every 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.

• Omaveloxolone has severe interactions with no other drugs.
• Omaveloxolone has serious interactions with at least 118 other drugs.
• Omaveloxolone has moderate interactions with at least 42 other drugs.
• Omaveloxolone 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 your products. 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, or if you have health questions or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

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

Long-Term Effects

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

Cautions

• Elevated aminotransferases
• Increased ALT and AST observed
• Monitor ALT, AST, and total bilirubin before initiating, every month for first 3 months, and periodically thereafter
• If transaminases increase to more than 5x ULN or more than 3x ULN with evidence of liver dysfunction (e.g., elevated bilirubin), immediately discontinue omaveloxolone and repeat liver function tests as soon as possible
• If transaminase levels stabilize or resolve, may reinitiate drug with increased frequency of monitoring of liver function
• Elevated B-type natriuretic peptide
• May increase B-type natriuretic peptide (BNP), a marker of cardiac function; obtain BNP before initiating
• Elevated BNP may indicate cardiac failure and should prompt an evaluation of cardiac function
• Monitor for signs and symptoms of fluid overload (e.g., sudden weight gain [more than 3 pounds in 1 day, or more than 5 pounds in a week]), peripheral edema, palpitations, and shortness of breath
• If fluid overload develops, worsens, or requires hospitalization, evaluate BNP and cardiac function, and manage appropriately
• Management of fluid overload and heart failure may require discontinuation of omaveloxolone
• Lipid abnormalities
  • May increase cholesterol levels above ULN
  • Assess lipid parameters before initiating and monitor periodically during treatment
  • Manage lipid abnormalities according to clinical guidelines
• Drug interaction overview
• Substrate of CYP3A4 (major)
• Weak inducer of CYP3A4 and CYP2C8
• Strong CYP3A4 inhibitors
  • Avoid coadministration
  • If unavoidable, reduce omaveloxolone to 50 mg/day; discontinue if adverse effects emerge
  • Strong CYP3A4 inhibitors are expected to result in clinically significant increased exposure of omaveloxolone
  • Advise patients to avoid grapefruit juice and grapefruit while receiving therapy
• Moderate inhibitors
  • Avoid coadministration
  • If unavoidable, reduce omaveloxolone to 100 mg/day; if adverse effects emerge, further reduce to 50 mg/day
  • Moderate CYP3A4 inhibitors are expected to result in clinically significant increased exposure of omaveloxolone
• CYP3 inducers
  • Strong or moderate inducers: Avoid coadministration
  • Strong or moderate CYP3A4 inducers may significantly decrease systemic exposure of omaveloxolone
• Sensitive CYP3A4 and CYP2C8 substrates
  • Caution/dosage modification
  • Omaveloxolone may reduce systemic exposure of sensitive CYP3A4 and CYP2C8 substrates which may result in decreased efficacy
• Hormonal contraceptives
  • Avoid coadministration
  • Omaveloxolone may reduce the efficacy of hormonal contraceptives (e.g., pill, patch, ring), implants, and progestin-only pills owing to weak CYP3A4 induction

Pregnancy and Lactation

• Data are inadequate on the developmental risks associated with use in pregnant females
• Contraception
  • Omaveloxolone may decrease the efficacy of hormonal contraceptives
  • Advise patients to avoid concomitant use with combined hormonal contraceptives (e.g., pill, patch, ring), implants, and progestin-only pills
  • Counsel females using hormonal contraceptives to use an alternative contraceptive method (eg, nonhormonal intrauterine system) or additional nonhormonal contraceptive (e.g., condoms) during concomitant use and for 28 days after discontinuation
• Lactation
  • Data are unavailable on presence of omaveloxolone or its metabolites in human milk, effects on milk production, and breastfed infants
  • Excreted in milk of lactating rats