恩西地平 (Enasidenib) 50mg
1. Composition:
The active ingredient in Enasidenib is Enasidenib, with the chemical name N-[(2S)-1-(2-chlorophenyl)-2-hydroxyethyl]-3-[(2-fluorophenyl)amino]pyridine-2-carboxamide. Its molecular formula is C19H17ClFN3O3, and its molecular weight is 389.8 g/mol.
2. Pharmacological Effects:
Enasidenib is primarily used to treat patients with IDH2 mutations in relapsed or refractory acute myeloid leukemia (AML). It works by inhibiting the activity of the mutated IDH2 enzyme, restoring the normal differentiation process of hematopoietic precursor cells, stopping the proliferation of leukemia cells, and promoting the apoptosis of leukemia cells.
Key pharmacological effects include:
- Improving hematopoiesis and reducing leukemia cells.
- Alleviating symptoms associated with acute myeloid leukemia.
- Increasing patient survival rates and quality of life, especially in cases where standard treatments are ineffective.
3. Usage Method:
Enasidenib is usually administered in oral tablet form, with a recommended initial dose of 50 mg once daily, which can be taken on an empty stomach or with food. The duration of the treatment cycle is generally determined by the physician based on the patient's response to therapy. Patients need to be regularly monitored for the drug's effectiveness and possible side effects.
4. Research and Development History:
Enasidenib was developed by Agios Pharmaceuticals and collaborated with Celgene for late-stage clinical studies. Due to the high correlation of IDH2 mutations in acute myeloid leukemia, researchers developed specific inhibitors targeting IDH2. Enasidenib received FDA approval in 2017 for the treatment of patients with relapsed or refractory acute myeloid leukemia with IDH2 mutations.
5. Mechanism of Action:
The mechanism of action of Enasidenib is to inhibit the mutated IDH2 enzyme. In patients with acute myeloid leukemia, mutations in the IDH2 enzyme cause metabolic disorders in cells and prevent hematopoietic precursor cells in the bone marrow from differentiating into mature blood cells. This abnormal differentiation leads to the proliferation of cancer cells and eventually triggers leukemia. Enasidenib specifically binds to and inhibits the mutated IDH2 enzyme, restoring normal differentiation functions in cells and suppressing the proliferation and survival of leukemia cells.
6. Summary:
Enasidenib is a targeted drug for acute myeloid leukemia that addresses IDH2 mutations. By inhibiting the abnormal activity of the IDH2 enzyme, it restores cell differentiation and suppresses the proliferation of leukemia cells. This medication is particularly suitable for patients with AML who have had ineffective standard treatments or relapses.
