birelentinib

Birelentinib is a **first-in-class, noncovalent, dual LYN/BTK inhibitor** developed for the treatment of adult patients with relapsed or refractory chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) who have received at least two prior lines of therapy, including a BTK inhibitor and a BCL2 inhibitor. It is designed to overcome resistance associated with BTK C481X mutations and BTK-independent B-cell receptor (BCR) signaling by simultaneously inhibiting both Bruton's tyrosine kinase (BTK) and lymphocyte-specific protein tyrosine kinase (LYN). Birelentinib demonstrates full blood-brain barrier penetration, high selectivity for TEC family kinases, favorable pharmacokinetic properties, and a manageable safety profile. Clinical data show significant anti-tumor activity even in heavily pretreated and resistant cases, reflected in objective response rates exceeding 80%. Birelentinib received FDA Fast Track Designation in 2025 for relapsed/refractory CLL or SLL[1][2][3][4][5].

Other names

DZD-8586DZD8586DZD 8586