Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …

In contrast to the traditional mechanism of drug action that relies on the reversible,
noncovalent interaction of a ligand with its biological target, a targeted covalent inhibitor …

PURPOSE Ibrutinib has shown activity in non–germinal center B-cell diffuse large B-cell
lymphoma (DLBCL). This double-blind phase III study evaluated ibrutinib and rituximab plus …

Background: Ibrutinib is a Bruton tyrosine kinase inhibitor with remarkable efficacy against B-
cell cancers. Ibrutinib also increases the risk of atrial fibrillation (AF), which remains poorly …

Aberrant activation of Bruton's tyrosine kinase (BTK) plays an important role in pathogenesis
of B-cell lymphomas, suggesting that inhibition of BTK is useful in the treatment of …

Primary CNS lymphoma (PCNSL) harbors mutations that reinforce B cell receptor (BCR)
signaling. Ibrutinib, a Bruton's tyrosine kinase (BTK) inhibitor, targets BCR signaling and is …

The outbreak of COVID-19, the pandemic disease caused by the severe acute respiratory
syndrome coronavirus 2 (SARS-CoV-2), has spurred an intense search for treatments by the …

Background Preclinical studies have shown synergistic antitumour effects between ibrutinib
and immune-checkpoint blockade. The aim of this study was to assess the safety and activity …

Bruton tyrosine kinase signaling (BTK) is critical step for B-cell development and
immunoglobulin synthesis. Ibrutinib is an orally bioavailable bruton tyrosine kinase inhibitor …

Small molecule tyrosine kinase inhibitors (TKIs) are widely used as anticancer drugs
approved by US FDA. However, the toxicities of TKIs to multiple organs have greatly limited …