伊鲁替尼（Ibrutinib）120mg
1. Composition:
The active ingredient of ibrutinib is ibrutinib itself, and its chemical name is: 1-[(3R)-3-[4-amino-3-(4-phenoxy)phenyl]-1-piperidinyl]-2-propen-1-one. It is an orally absorbed BTK inhibitor that specifically targets key proteins in cancer cell signaling pathways, thereby inhibiting the proliferation and growth of cancer cells.
2. Pharmacodynamics:
Ibrutinib works by inhibiting the activity of BTK, blocking the B-cell receptor signaling pathway, and interfering with the survival and proliferation of B-cells. B-cells are abnormally active in certain types of blood cancers, and BTK plays a critical role in this signaling pathway. By inhibiting BTK, ibrutinib effectively reduces the growth of cancer cells and leads them to apoptosis.
3. Usage Instructions:
- Dosage Form: Ibrutinib is typically available in capsule or tablet form for oral administration.
- Administration: Taken once daily, usually with water, and can be taken regardless of meal times.
- Dosage: The common dosage is 140 mg capsules, taken in several capsules at once, with the total dosage depending on the type of disease and the patient’s response. The usual dose for treating chronic lymphocytic leukemia (CLL) is 420 mg/day, while the dose for treating Waldenström's macroglobulinemia is 560 mg/day.
- Course: Patients should take ibrutinib long-term as prescribed by a doctor, until the condition stabilizes or intolerable side effects occur.
4. Research & Development History:
- Ibrutinib was jointly developed by Pharmacyclics and Janssen Biotech, a subsidiary of Johnson & Johnson, and was first approved by the U.S. FDA in 2013 for the treatment of chronic lymphocytic leukemia (CLL).
- Since then, its indications have expanded to include several blood cancers, such as mantle cell lymphoma (MCL) and small lymphocytic lymphoma (SLL).
- The development of this drug is based on in-depth research of the B-cell signaling pathway, particularly the role of the BTK protein in blood cancers. By blocking BTK, ibrutinib has significantly changed the treatment outlook for these diseases.
5. Pharmacological Mechanism
Ibrutinib mainly exerts its effect by irreversibly inhibiting BTK. BTK is a crucial component of the B-cell receptor signaling pathway, involved in the survival, proliferation, and migration of cancer cells. In B-cell malignancies, BTK is often overly active, promoting the rapid growth and drug resistance of cancer cells. By inhibiting BTK’s enzymatic activity, ibrutinib disrupts the signaling in these cancer cells, leading to their death or inability to continue proliferating.
6. Summary:
As an innovative targeted drug, ibrutinib provides a new option for the treatment of blood malignancies such as chronic lymphocytic leukemia and mantle cell lymphoma. Compared to traditional chemotherapy, it has lower toxicity, greater specificity, and can be used in a broader range of patient groups. Clinical studies have shown that ibrutinib can effectively extend patients' progression-free survival (PFS) and overall survival (OS).
