Ivosidenib

What is Ivosidenib?

• Ivosidenib (Tibsovo) is an isocitrate dehydrogenase-1 (IDH1) inhibitor used to treat acute myeloid leukemia (AML) with an isocitrate dehydrogenase-1 (IDH1) mutation and bile duct cancer (cholangiocarcinoma).

Ivosidenib

What are the uses of this medicine?

• Ivosidenib (Tibsovo) used to treat:

acute myeloid leukemia (AML) with an isocitrate dehydrogenase-1 (IDH1) mutation in:

• adults with newly diagnosed AML treated in combination with Tibsovo and azacitidine who are 75 years or older or who have health problems that prevent the use of certain chemotherapy treatments.
• adults with newly diagnosed AML who are 75 years or older or who have health problems that prevent the use of certain chemotherapy treatments.
• adults with AML when the disease has come back or has not improved after previous treatment(s).

adults with bile duct cancer (cholangiocarcinoma) that has spread:

• who have already received previous treatment(s) and
• whose tumor has a certain type of abnormal IDH1 mutation

How does this medicine work?

• Ivosidenib (eye" voe sid' i nib) is a small molecule inhibitor of isocitrate dehydrogenase-1 (IDH1), an enzyme rearranged and mutated in some forms of leukemia and lymphoma.
• The mutated IDH promotes unregulated cell growth and proliferation and is overexpressed in some leukemias.
• Ivosidenib has been found to inhibit mutated IDH1 and in several clinical trials was found to induce objective responses in a proportion of patients with refractory AML with detectable IDH1 mutations.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.
• Especially tell your healthcare provider if you take hormonal contraceptives. Tibsovo may affect how hormonal contraceptives work and may cause them to not work as well.

Be sure to mention any of the following:

• amiodarone (Nexterone, Pacerone), ciprofloxacin (Cipro), disopyramide (Norpace), dofetilide (Tikosyn), fluconazole (Diflucan), gemifloxacin (Factive), granisetron (Sancuso, Sustol),itraconazole (Sporanox, Tolsura), ketoconazole, levofloxacin, moxifloxacin, ofloxacin, ondansetron (Zofran), palonosetron (in Akynzeo), posaconazole (Noxafil), procainamide, quinidine (in Nuedexta), rifampin (Rifadin, Rimactane), sotalol (Betapace, Sorine, Sotylize), and voriconazole (Vfend).

Is this medicine FDA approved?

• Ivosidenib received accelerated approval for use refractory or relapsed AML with mutated IDH1 in the United States in 2018. A specific small molecule inhibitor of IDH2, enasidenib, was approved as therapy of AML with mutations in IDH2 in 2017.
• In May 2019, ivosidenib was approved in the United States for newly diagnosed acute myeloid leukemia (AML) with a susceptible IDH1 mutation, as detected by an FDA-approved test, in patients who are at least 75 years old or who have comorbidities that preclude the use of intensive induction chemotherapy.
• In August 2021, the FDA approved ivosidenib for adults with previously treated, locally advanced or metastatic cholangiocarcinoma with an isocitrate dehydrogenase-1 (IDH1) mutation as detected by an FDA-approved test.

How should this medicine be used?

• Select patients for the treatment of AML with Tibsovo based on the presence of IDH1 mutations in the blood or bone marrow.
• Select patients for the treatment of locally advanced or metastatic cholangiocarcinoma with Tibsovo based on the presence of IDH1 mutations.

Recommended dosage: Newly Diagnosed AML (Combination Regimen):

• The recommended dosage of Tibsovo is 500 mg taken orally once daily until disease progression or unacceptable toxicity.

Newly Diagnosed AML and Relapsed or Refractory AML (Monotherapy Regimen):

• The recommended dosage of Tibsovo is 500 mg taken orally once daily until disease progression or unacceptable toxicity.

Cholangiocarcinoma:

• The recommended dosage of Tibsovo is 500 mg taken orally once daily until disease progression or unacceptable toxicity.

Dosage Modification for Use with Strong CYP3A4 Inhibitors:

• If a strong CYP3A4 inhibitor must be coadministered, reduce the Tibsovo dose to 250 mg once daily.
• If the strong inhibitor is discontinued, increase the Tibsovo dose (after at least 5 half-lives of the strong CYP3A4 inhibitor) to the recommended dose of 500 mg once daily.

Administration:

• Ivosidenib comes as a tablet to take by mouth.
• It is usually taken with or without food once daily.
• Do not take it with a high fat meal (such as fried foods or fast food).
• Take ivosidenib at around the same time every day.
• If you vomit after taking ivosidenib, do not take another dose.
• Continue your regular dosing schedule.

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

This medicine is available in fallowing doasage form:

• As Tablets: 250 mg

This medicine is available in fallowing brand namesː

• Tibsovo

What side effects can this medication cause?

The most common side effects of Tibsovo when used in combination with azacitidine or alone in adults with AML include:

• changes in certain blood cell counts
• diarrhea
• increased blood sugar
• fatigue
• changes in certain liver function tests
• swelling of arms or legs
• decreased levels of electrolytes in the blood
• nausea
• vomiting
• decreased appetite
• joint pain
• shortness of breath
• uric acid increased
• stomach (abdominal) pain
• changes in certain kidney function tests
• pain or sores in your mouth or throat
• rash
• irregular heart rhythm or heartbeat (QTc prolongation)
• differentiation syndrome
• muscle pain

The most common side effects of Tibsovo in adults with Cholangiocarcinoma include:

• fatigue
• nausea
• abdominal pain
• diarrhea
• cough
• decreased appetite
• fluid and swelling in your stomach area
• vomiting
• hemoglobin decreased (anemia)
• rash
• changes in liver function tests

Tibsovo may cause serious side effects, including:

• Differentiation Syndrome
• QTc prolongation
• Guillain-Barré syndrome

What special precautions should I follow?

• Patients treated with Tibsovo can develop QT (QTc) prolongation. Monitor electrocardiograms and electrolytes. If QTc interval prolongation occurs, dose reduce or withhold, then resume dose or permanently discontinue Tibsovo.
• Guillain-Barré syndrome can develop in patients treated with Tibsovo. Monitor patients for signs and symptoms of new motor and/or sensory findings. Permanently discontinue Tibsovo in patients who are diagnosed with Guillain-Barré syndrome.
• Patients with newly diagnosed AML treated with Tibsovo plus azacitidine experienced differentiation syndrome. If differentiation syndrome is suspected, initiate dexamethasone 10 mg IV every 12 hours (or an equivalent dose of an alternative oral or IV corticosteroid).
• Ivosidenib is associated with a moderate rate of serum aminotransferase elevations during therapy and is suspected to be the cause of rare instances of clinically apparent acute liver injury.

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, Tibsovo may cause fetal harm when administered to a pregnant woman.
• There are no available data on Tibsovo use in pregnant women to inform a drug-associated risk of major birth defects and miscarriage.

Can this medicine be used in children?

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

What are the active and inactive ingredients in this medicine?

• Active ingredient: ivosidenib
• Inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, hypromellose acetate succinate, magnesium stearate, microcrystalline cellulose, and sodium lauryl sulfate. The tablet coating includes FD&C blue #2, hypromellose, lactose monohydrate, titanium dioxide, and triacetin.

Who manufactures and distributes this medicine?

• Manufactured for Servier Pharmaceuticals LLC, Boston, MA

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

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

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• Dailymed label info on Ivosidenib
• FDA Ivosidenib

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