Aifenib is an oral inhibitor of isocitrate dehydrogenase-1 (IDH1) that targets the activity of mutant IDH1 enzyme, reducing the production of carcinogenic metabolite 2-hydroxyglutarate (2-HG), thereby inducing malignant cell differentiation and inhibiting tumor growth.

1、 Drug name

1. Common name: Ivosidenib

2. Product Name: TIBSOVO ®

2、 Indications

Suitable for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (AML) confirmed by FDA approved testing to carry susceptible IDH1 mutations.

3、 Specifications and characteristics

1. Specification: 250mg/tablet;

2. Appearance: Tablets.

4、 Main components

Active ingredient: Albemarle; Auxiliary materials include colloidal silica, cross-linked carboxymethyl cellulose sodium, hydroxypropyl methylcellulose acetate succinate, etc.

5、 Usage and dosage

1. Conventional dose: 500mg orally, once daily, taken with meals or on an empty stomach, avoiding high-fat diet.

2. Omission treatment: If missed, make up for it within 12 hours; If vomiting occurs, there is no need to take additional medication. Follow the original plan for the next dose.

3. Course of treatment: Continue medication until disease progression or intolerable toxicity occurs, for at least 6 months to evaluate efficacy.

6、 Dose adjustment

1. QTc prolongation: Discontinue medication when QTc>480ms, and reduce to 250mg/day after recovery; >If 500ms or accompanied by arrhythmia, the medication will be permanently discontinued.

2. Differentiation syndrome: Medication should be temporarily suspended and corticosteroid treatment should be given. Medication should be resumed after symptoms are relieved.

3. Combination use of strong CYP3A4 inhibitors: dose reduced to 250mg/day.

7、 Medication precautions

1. Dietary impact: Avoid taking high-fat meals together (such as fried eggs, bacon, whole milk).

2. Drug interactions: Avoid using strong CYP3A4 inducers (such as rifampicin) or QTc prolonging drugs (such as fluoroquinolones) in combination.

3. Monitoring requirements: During the initial stage of treatment, weekly monitoring of electrocardiogram, blood routine, and electrolytes is required.

8、 Medication for special populations

1. Pregnant women: May cause fetal damage, contraception is necessary during medication.

2. Breastfeeding period: Breastfeeding is prohibited for at least one month after discontinuation of medication.

3. Elderly patients: No need to adjust dosage, but need to strengthen monitoring.

9、 Adverse reactions

1. Common (≥ 20%): including fatigue, leukocytosis, joint pain, diarrhea, dyspnea, edema, nausea, mucosal inflammation, etc;

2. Serious adverse reactions: including differentiation syndrome (19%), QTc prolongation (9%), and Guillain Barr é syndrome (<1%).

10、 Contraindications

There are no clear contraindications, but it is contraindicated for those who are allergic to the ingredients.

11、 Drug interactions

1. CYP3A4 inhibitor: Increasing the blood concentration of ezetimibe requires adjusting the dosage.

2. Hormonal contraceptive pills: may reduce efficacy, it is recommended to switch to non hormonal contraceptive measures.

12、 Storage method

Store at room temperature (20 ° C-25 ° C) and avoid moisture.

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