What important information does the detailed instructions for acotinib/cancostat contain?

1. Common name and trade name

Acalabrutinib is a highly selective Bruton's tyrosine kinase (BTK) inhibitor that is widely used in the treatment of hematological tumors worldwide. Its common trade name is CALQUENCE. In different materials or regions, its aliases can also be seen, such as acalabrutinib, acalabrutinib or the development code ACP-196. The emergence of these different names is usually related to the drug development stage, inclusion in the international pharmacopoeia, or marketing strategy.

2. Main indications

1. Mantle cell lymphoma (MCL; non-Hodgkin lymphoma)

Acotinib is suitable for adult patients with MCL who have received at least one previous treatment. MCL is a type of non-Hodgkin lymphoma that progresses rapidly clinically and is often accompanied by treatment relapse and drug resistance. The mechanism of action of acotinib brings new treatment options to patients.

2. Chronic lymphocytic leukemia(CLL)/small lymphocytic lymphoma (SLL)

Acotinib is approved for the treatment of adult patients with CLL and SLL. Both types of diseases are low-grade B-cell tumors, and patients often require long-term management. Because of its high targeting selectivity and good tolerability, acotinib has gradually become an important choice for first-line or later-line treatment in clinical practice.

3. Medication Management

Acotinib is usually given as an oral capsule. When taking the medicine, swallow it whole and do not crush or chew it to ensure stable release of the medicine in the body. The drug can be taken with or without food, providing flexibility. If a dose is missed and it is more than 3 hours before the next planned dose, you should directly resume the next regular dose instead of taking additional doses to avoid adverse reactions caused by fluctuations in drug concentration.

In some treatment options, acotinib can be used in combination with obinutuzumab (Obinutuzumab), and this combination has been proven to further improve the efficacy in patients with CLL. It is worth noting that if it is administered on the same day as otuzumab, acotinib needs to be taken first and then infused to optimize the therapeutic effect.

4. Adverse reactions and tolerance

In clinical trials and post-marketing experience, the adverse reactions of acotinib are mainly related to bone marrow suppression, gastrointestinal reactions and immune-related reactions. Among MCL patients, more common side effects include anemia, thrombocytopenia, neutropenia, headache, fatigue, diarrhea, and ecchymosis. In patients with CLL and SLL, joint pain, dizziness, and constipation may also be seen.

5. Supply and storage

Acotinib is supplied in the form of oral capsules, each containing 100 mg. Medications need to be stored at room temperature of 20°C-25°C (68°F-77°F), with an allowed temperature deviation of 15°C-30°C (59°F-86°F). High temperature and humid environments should be avoided to ensure the stability of the medicinal effect.

6. Mechanism of action

Acotinib, as a small molecule inhibitor ofBTK, inhibits its activity by forming an irreversible covalent bond with the cysteine residue of the BTK enzyme. BTK plays a central role in the B cell receptor (BCR) signaling pathway and can regulate the proliferation, differentiation and survival of B cells. In B-cell malignancies, BTK signaling is abnormally active, causing tumor cells to continue to grow and evade immune clearance. By blocking BTK activity, acotinib effectively cuts off abnormal signaling pathways, thereby inhibiting the growth of malignant B cells.

In preclinical studies, acotinib can significantly reduce the expression of downstream signaling proteins such asCD86 and CD69, reduce tumor cell activity, and inhibit the progression of B-cell tumors in animal models. This mechanism also provides a solid theoretical basis for its clinical efficacy.

Reference materials:https://www.calquence.com/