2024年5月14日 · Second-generation BTKis have improved selectivity and demonstrate reduced rates of cardiovascular complications in 3 head-to-head ibrutinib studies. The emergence of BTK C481S mutation has led to the development of noncovalent, “reversible” BTKis, such as pirtobrutinib, which are agnostic to the C481S mutation.

Bruton´s tyrosine kinase (BTK) inhibitor (BTKi)s block the B-cell receptor (BCR) signaling cascade by binding to the BTK enzyme preventing the proliferation and survival of malignant and normal B cells.

In this review, we discuss the role of BTK inhibitors in treatment of CLL/SLL, review the data that led to approval of BTK inhibitors in CLL/SLL, outline the toxicity profile of each approved BTK inhibitor and management, and give practical guidance on how to select the most appropriate agent for treatment.

2025年3月20日 · Five of the nine CLL patients had partial responses, and three had stable disease with a 16-45% reduction in tumor size. Conclusions: While pirtobrutinib was the first noncovalent BTKi to receive FDA approval, more noncovalent BTKi are still in development, including docirbrutinib and nemtabrutinib, as well as dual covalent noncovalent BTKi ...

2024年12月1日 · Bruton Tyrosine Kinase inhibitors (BTKi) disrupt the BCR signaling pathway by inactivation of BTK, leading to inhibition of proliferation and survival of CLL cells. There are two classes of BTK inhibitors, covalent and non-covalent. İbrutinif is the first approved covalent BTKi (cBTKi) of its class.

2025年3月1日 · In this review, we analyzed the cardiovascular effects associated with BTKi therapy for CLL and the essential practical aspects of multidisciplinary management of patients who develop cardiovascular toxicity during treatment.

伊布替尼（Ibrutinib）为首个获批用于治疗CLL的BTKi，通过与BTK活性部位481位置的半胱氨酸残基形成共价键抑制BTK活性，阻断BCR多个下游信号通路达到治疗效果 [2]。 多个临床试验的长期随访结果表明伊布替尼可以显著延长复发/难治CLL（R/R CLL）患者和初治CLL（TN CLL）患者的无进展生存（PFS）期与总生存（OS）期，且安全性显著优于化学免疫治疗，但同时也暴露了伊布替尼的一些局限性。 首先伊布替尼对BTK的选择性欠佳，对与BTK结构相似的EGFR、ITK …

2025年3月20日 · The treatment landscape for chronic lymphocytic leukemia (CLL) has transformed significantly with the introduction of Bruton tyrosine kinase (BTK) inhibitors (BTKi) and B-cell lymphoma-2 (BCL2) inhibitors, leading to marked improvements in patient outcomes across different risk groups. 1-15 Triple combinations involving BTKi, BCL2 inhibitors ...

6 天之前 · Learn about resistance mutations in chronic lymphocytic leukemia (CLL), specifically in BTK inhibitor drugs, to understand why treatment may stop working.

2025年3月24日 · During a Case-Based Roundtable® event, John N. Allan, MD, discussed how new regimens using BTK inhibitors and venetoclax might be used in patients with chronic lymphocytic leukemia. Consider the data for the SEQUOIA (NCT03336333), ELEVATE-TN (NCT02475681), and CLL14 (NCT02242942) trials: How do ...