Ensidipine is used to treat acute myeloid leukemia (AML) in adults with an IDH2 mutation.

Ensidipine Instructions

Product Name: LuciEna

Manufacturer: Lucius Pharmaceuticals

Chinese name: Ensidipine

English Name: Enasidenib
Drug approval number: 09 L 1019/23

 

 

【Summary】

Enasidenib is an isocitrate dehydrogenase 2 (IDH2) inhibitor. The tricarboxylic acid cycle (TCA cycle) is crucial for many biochemical signaling pathways. IDH2 is a key enzyme in the tricarboxylic acid cycle. Certain mutant forms of this protein (R140Q, R172S, R172K) lead to an increase in the specific metabolite 2-hydroxyglutarate (2-HG). Enasidenib can reduce the content of 2-HG and induce leukemia cell differentiation.

 

【Indications】

For the treatment of acute myeloid leukemia (AML) in adults with an IDH2 mutation.

 

【Specification】  

50 mg/ tablet, 30 tablets / box.

 

【Storage】

Store at 20°C to 25°C (68°C to 77°F) ; short-distance transport is permitted within the temperature range of 15 to 30°C (59–86°F) .

 

【Usage and Dosage】

The dosage is 100 mg once daily, with or without food, until disease progression or unacceptable toxicity occurs. If there is no disease progression or unacceptable toxicity, treatment is required for at least 6 months.

 

【Adverse Reactions】

>10%:

1. Endocrine and metabolism: serum calcium decreased (74%), serum potassium decreased (41%)

2. Gastrointestinal: nausea (50%), diarrhea (43%), decreased appetite (34%), vomiting (34%), loss of appetite (12%)

3. Blood and tumors: abnormal phosphorus levels (27%; ≥ grade 3: 8%; decreased), differentiation syndrome (14%), leukocytosis (12%; ≥ grade 3: 6%; non-infectious)

4. Liver: elevated serum bilirubin (81%)

1% -10%:

1. Hematology and tumors: tumor lysis syndrome (6%)

2. Respiratory system: acute respiratory distress (≤10%), pulmonary edema (≤10%)

 

【Taboo】

Women who are pregnant or breastfeeding should not take ensidipine because it may cause harm to a developing fetus or newborn baby. 

 

【Notes】

 1. Embryo-fetal toxicity: Based on animal embryo-fetal toxicity studies, administration of emdesipine to pregnant women can cause embryo-fetal harm. Women of reproductive potential and men with female partners of reproductive potential are advised to use effective contraception during treatment with emdesipine and for at least 2 months after the last dose.

Pregnant women, patients who become pregnant, or male patients with pregnant female partners who are taking ensidipine should be apprised of the potential risk to the fetus.

2. Increased bilirubin: Ensidipine may interfere with bilirubin metabolism by inhibiting UGT1A1.

3. Non-infectious leukocytosis: Ensidipine can induce bone marrow hyperplasia, leading to a rapid increase in white blood cell count

4. Tumor lysis syndrome: Ensidipine can induce myeloid proliferation, leading to a rapid reduction in tumor cells, which may lead to TLS risk.

 

【Efficacy and safety】

The efficacy of enasidenib was demonstrated in a single-arm study involving 199 patients with relapsed or refractory AML harboring an IDH2 mutation.

The results showed that after a minimum of 6 months of treatment, approximately 19% of patients achieved complete remission, with a median duration of remission of 8.2 months. 4% of patients achieved partial hematological remission, with a median duration of remission of 9.6 months. Among 157 patients who required blood transfusions or platelets for AML, 34% no longer required blood transfusions after receiving Enasidenib treatment.