Olutasidenib

What is Olutasidenib?

• Olutasidenib (Rezlidhia) is an isocitrate dehydrogenase-1 (IDH1) inhibitor.

Olutasidenib

What are the uses of this medicine?

• Olutasidenib (Rezlidhia) is a prescription medicine used to treat adults with acute myeloid leukemia (AML) with an isocitrate dehydrogenase-1 (IDH1) mutation when the disease has come back or has not improved after previous treatment(s).

How does this medicine work?

• An orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1; IDH-1; IDH1 [NADP+] soluble) with a mutation at arginine (R) 132, IDH1(R132), with potential antineoplastic activity.
• Upon administration, olutasidenib specifically inhibits IDH1(R132), thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG).
• This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing IDH(R132).
• IDH1(R132) mutations are highly expressed in certain malignancies, including gliomas; they initiate and drive cancer growth by both blocking cell differentiation and catalyzing the formation of 2HG.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.
• The following nonprescription or herbal products may interact with olutasidenib: St. John's Wort. Be sure to let your doctor and pharmacist know that you are taking this medications before you start taking olutasidenib.

Is this medicine FDA approved?

• Olutasidenib was approved for medical use in the United States in December 2022.

How should this medicine be used?

• Select patients for the treatment of relapsed or refractory AML with Rezlidhia based on the presence of IDH1 mutations in blood or bone marrow.

Recommended dosage:

• The recommended dosage of Rezlidhia is 150 mg taken orally twice daily until disease progression or unacceptable toxicity.

Administration:

• Take Rezlidhia exactly as your healthcare provider tells you to.
• Do not change your dose or stop taking Rezlidhia without talking to your healthcare provider.
• Take Rezlidhia 2 times a day (about 12 hours apart) around the same times each day.
• Take Rezlidhia on an empty stomach, at least 1 hour before or 2 hours after a meal.
• Swallow Rezlidhia capsules whole. Do not break, open or chew the capsules.
• If you vomit after taking a dose of Rezlidhia, do not take another dose. Take your next dose at your usual time.
• If you miss a dose of Rezlidhia or did not take it at the usual time, take your dose as soon as possible and at least 8 hours before your next dose. Return to your normal schedule the following day. Do not take 2 doses of Rezlidhia within 8 hours.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Capsules: 150 mg

This medicine is available in fallowing brand namesː

• Rezlidhia

What side effects can this medication cause?

The most common side effects of this medicine include:

• abnormal liver function tests
• nausea
• feeling tired or unwell
• joint pain
• constipation
• shortness of breath
• fever
• rash
• mouth sores
• diarrhea
• changes in certain blood tests

Less common, but serious side effects may include:

• Differentiation Syndrome
• Liver problems

What special precautions should I follow?

• Rezlidhia can cause differentiation syndrome. Advise patients of the risks of developing differentiation syndrome as early as 1 day after start of therapy and up to 18 months on treatment. Ask patients to immediately report any symptoms suggestive of differentiation syndrome, such as fever, cough or difficulty breathing, decreased urinary output, low blood pressure, weight gain, or swelling of their arms or legs, to their healthcare provider for further evaluation.
• Rezlidhia can cause hepatotoxicity, presenting as increased alanine aminotransferase (ALT), increased aspartate aminotransferase (AST), increased blood alkaline phosphatase, and/or elevated bilirubin. Advise patients of the potential for hepatic effects and to immediately report any associated signs and symptoms such as right upper abdominal discomfort, dark urine, jaundice, anorexia, or fatigue to their healthcare provider for further evaluation.
• Advise patients on the risks of experiencing gastrointestinal reactions such as nausea, constipation, diarrhea, vomiting, abdominal pain, and mucositis. Ask patients to report these events to their healthcare provider and advise patients how to manage them.
• Advise women not to breastfeed during treatment with Rezlidhia and for 2 weeks after the last dose.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Based on animal embryo-fetal toxicity studies, Rezlidhia may cause fetal harm when administered to a pregnant woman.
• Rezlidhia may harm your unborn baby.

Can this medicine be used in children?

• The safety and effectiveness of Rezlidhia have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• olutasidenib

Inactive ingredients:

• croscarmellose sodium, magnesium stearate, and microcrystalline cellulose. The capsule shell contains gelatin and titanium dioxide. Each capsule is printed with black ink containing ferrosoferric oxide, propylene glycol and shellac.

Who manufactures and distributes this medicine?

Manufactured by: Catalent Greenville, Inc. 1240 Sugg Pkwy, Greenville, NC

Manufactured for:

• Rigel Pharmaceuticals, Inc. South San Francisco, CA
• Rezlidhia™ is a trademark of Rigel Pharmaceuticals, Inc.

What should I know about storage and disposal of this medication?

• Store Rezlidhia at room temperature from 68°F to 77°F (20°C to 25°C).

• Dailymed label info on Olutasidenib
• FDA Olutasidenib

Olutasidenib Resources
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