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CAS NO.877399-52-5ОбъектПодробнееХимическое названиеAbrutinibНомер по CAS936563-96-1Молекулярная форму...
CAS NO.877399-52-5
Объект | Подробнее |
Химическое название | Abrutinib |
Номер по CAS | 936563-96-1 |
Молекулярная формула | \(C_{26}H_{23}N_{7}O_{2}\) |
Молекулярная масса | 465.51 |
Молекулярная структура | Abrutinib has a structure with a central heterocyclic core. It contains a pyrrolopyrimidine ring system, which is characteristic of many kinase inhibitors. Attached to this core are various aromatic and aliphatic side chains. The specific arrangement of these groups enables it to interact with Bruton’s tyrosine kinase (BTK) in a highly specific manner. |
Внешний вид | Usually appears as a solid, often in a white to off – white powder form. |
Растворимость | Information on solubility may be limited, but like many drugs in this class, it likely has poor solubility in water and better solubility in organic solvents such as DMSO and ethanol. This solubility profile is important for formulating it into pharmaceutical products, often requiring the use of solubilizing agents or special formulation techniques. |
Фармакологический класс | Ингибитор тирозинкиназы Брутона (BTK) |
Механизм действия | Abrutinib binds irreversibly to the cysteine residue in the active site of BTK. BTK is a key enzyme in the B – cell receptor signaling pathway. By inhibiting BTK, abrutinib blocks the downstream signaling cascade that is crucial for B – cell activation, proliferation, and survival. In diseases where abnormal B – cell function is involved, such as certain lymphomas and autoimmune disorders, this disruption of the B – cell signaling pathway can lead to a reduction in the number of abnormal B – cells and a dampening of the associated immune response. |
Медицинские применения | Хронический лимфоцитарный лейкоз (ХЛЛ): Approved for the treatment of CLL in patients who have received at least one prior therapy. It has shown effectiveness in reducing the number of cancerous B – cells in the blood and bone marrow, and can improve progression – free survival. Лимфома из мантийных клеток (MCL): Also used in the treatment of relapsed or refractory MCL. It targets the abnormal B – cells characteristic of MCL, leading to tumor shrinkage and potential improvement in patient outcomes. There is also ongoing research into its use in other B – cell malignancies and autoimmune diseases such as systemic lupus erythematosus, where abnormal B – cell activity plays a role. |
Стабильность | Stable under normal storage conditions, typically at room temperature in a dry and dark place. However, exposure to high humidity, extreme temperatures, or strong oxidizing or reducing agents can cause degradation of the drug, potentially affecting its potency and safety. |
Вопросы безопасности | Common side effects include diarrhea, fatigue, upper respiratory tract infections, and headache. There is also a risk of bleeding events, as BTK inhibition can affect platelet function and the normal coagulation process. In some patients, atrial fibrillation may occur, which is an abnormal heart rhythm. Abrutinib may interact with other medications. For example, drugs that inhibit CYP3A4 (the main enzyme involved in metabolizing abrutinib) can increase its blood levels and the risk of adverse effects. On the other hand, drugs that induce CYP3A4 can decrease abrutinib levels, potentially reducing its effectiveness. |
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