Drug intelligence / Profile preview

emavusertib + zanubrutinib

Development stage
Phase 2
Lead developer
Curis
Modality
Small Molecules
Administration
Oral
01

Overview

Emavusertib plus zanubrutinib is an investigational, all-oral combination therapy being developed for the treatment of B-cell malignancies, primarily chronic lymphocytic leukemia (CLL). Emavusertib (CA-4948) is a small-molecule inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) and fms-like tyrosine kinase 3 (FLT3), which targets the Toll-like receptor (TLR) and MYD88 signaling pathways. Zanubrutinib (Brukinsa) is an approved, second-generation, covalent small-molecule inhibitor of Bruton's tyrosine kinase (BTK) that blocks B-cell receptor (BCR) signaling. By combining these two agents, the therapy aims to achieve dual blockade of the complementary BCR and TLR pathways, synergistically inhibiting downstream nuclear factor-kappa B (NF-kB) signaling to overcome resistance and deepen therapeutic responses. The combination is currently being evaluated in the Phase 2 TakeAim CLL clinical trial (CA-4948-203, NCT07271667) for patients with CLL who have had a partial response or are progressing on zanubrutinib monotherapy.

Other names
Brukinsa + CA-4948Brukinsa + emavusertibCA-4948 + zanubrutinibemavusertib + BGB-3111emavusertib and zanubrutinibzanubrutinib + emavusertibzanubrutinib and emavusertib
02

Targets

BTK (Bruton tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)IRAK4 (Interleukin-1 receptor associated kinase 4)NF-κB

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