Enasidenib Idhifa LuciEna 50mg

Product Name: LuciEna

Chinese Name: Enasidenib

English Name: Enasidenib

Specification: 50 mg/tablet; 30 tablets/box.

[Summary]

Enasidenib is an isocitrate dehydrogenase-2 (IDH2) inhibitor. The tricarboxylic acid cycle (TCA cycle) is critical for numerous biochemical signaling pathways; IDH2 is a key enzyme within this cycle. Certain mutated forms of this protein (R140Q, R172S, R172K) lead to elevated levels of a specific metabolite, 2-hydroxyglutarate (2-HG). Enasidenib acts by reducing 2-HG levels, thereby inducing the differentiation of leukemia cells.

[Indications]

Indicated for the treatment of adult patients with acute myeloid leukemia (AML) harboring an IDH2 mutation.

[Storage]

Store at 20°C to 25°C (68°F to 77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F).

[Dosage and Administration]

The recommended dosage is 100 mg taken orally once daily. It may be taken with or without food. Treatment should be continued until disease progression or unacceptable toxicity occurs. If neither disease progression nor unacceptable toxicity is observed, treatment should be continued for at least 6 months. [Adverse Reactions]

>10%:

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

2. Gastrointestinal: Nausea (50%), diarrhea (43%), decreased appetite (34%), vomiting (34%), anorexia (12%)

3. Hematologic and Oncologic: Abnormal phosphorus levels (27%; Grade ≥3: 8%; decreased), differentiation syndrome (14%), leukocytosis (12%; Grade ≥3: 6%; non-infectious)

4. Hepatic: Increased serum bilirubin (81%)

1% - 10%:

1. Hematologic and Oncologic: Tumor lysis syndrome (6%)

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

[Contraindications]

Women who are pregnant or breastfeeding should not take Enasidenib, as it may cause harm to the developing fetus or newborn infant.

[Precautions]

1. Embryo-Fetal Toxicity: Based on animal embryo-fetal toxicity studies, administration of Enasidenib to pregnant women may 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 Enasidenib and for at least 2 months after the last dose.

Pregnant women, patients who become pregnant while taking Enasidenib, or male patients with pregnant female partners should be informed of the potential risk to the fetus.

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

3. Non-infectious Leukocytosis: Enasidenib may induce myeloid proliferation, leading to a rapid increase in white blood cell counts.

4. Tumor Lysis Syndrome (TLS): Enasidenib may induce myeloid proliferation, leading to a rapid reduction in tumor cells, which may result in a risk of TLS.

[Efficacy and Safety]

The efficacy of Enasidenib was established in a single-arm study involving 199 patients with relapsed or refractory AML harboring an IDH2 mutation. The results showed that, after receiving treatment for a minimum of 6 months, approximately 19% of patients achieved complete remission, with a median duration of remission of 8.2 months. 4% of patients achieved partial hematologic remission, with a median duration of remission of 9.6 months. Among the 157 patients requiring blood or platelet transfusions due to AML, 34% no longer required transfusions after receiving treatment with Enasidenib.