Crossfire Oncology BV has disclosed CFON-026, a potent, highly selective and macrocyclic noncovalent inhibitor of wild-type (WT) Bruton tyrosine kinase (BTK) and all clinically relevant BTK resistance mutations, with best-in-class potential for the treatment of cancer.
Bruton tyrosine kinase (BTK) enzyme inhibitors used to treat B-cell cancers, including chronic lymphocytic leukemia and non-Hodgkin lymphoma, also produce resistance by causing mutations in the protein. Now, a study on the BTK degrader NX-2127 showed the compound could be effective in eliminating BTK regardless of its mutations.
Bruton tyrosine kinase (BTK) enzyme inhibitors used to treat B-cell cancers, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma, also produce resistance by causing mutations in the protein. Now, a study on the BTK degrader NX-2127 showed the compound could be effective in eliminating BTK regardless of its mutations.
Researchers at Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College have disclosed pyrrolopyrimidine compounds acting as Bruton tyrosine kinase (BTK) inhibitors reported to be useful for the treatment of chronic lymphocytic leukemia, lymphoma, primary central nervous system, non-Hodgkin lymphoma, and rheumatoid arthritis.
Rheumatoid arthritis (RA) is a systemic autoimmune disorder where Bruton tyrosine kinase (BTK) and Janus kinase 3 (JAK3) are among the most relevant signaling pathways involved.
Eli Lilly and Co., through its Loxo@Lilly oncology unit, secured its second accelerated approval for non-covalent Bruton’s tyrosine kinase (BTK) inhibitor Jaypirca (pirtobrutinib), this time to treat adults with chronic lymphocytic leukemia or small lymphocytic lymphoma. The U.S. FDA approval of 100-mg and 50-mg tablets is for patients who have received two prior lines of therapy, including another BTK inhibitor and a BCL-2 inhibitor. It is based on phase I/II data from a subset of 108 patients participating in the open-label, single-arm, multi-cohort Bruin trial.
Shenzhen Targetrx Biotechnology Co. Ltd. has disclosed cycloalkyl or heterocyclyl substituted heteroaryl compounds acting as Bruton tyrosine kinase (BTK) and BTK (C481S mutant) inhibitors reported to be useful for the treatment of cancer, inflammation, allergy and autoimmune disease.
It has been previously demonstrated that the Bruton tyrosine kinase (BTK) pathway plays a key role promoting cell adhesion and chemotaxis, and that increased adhesion and aberrant chemotaxis contribute to pathogenesis of myelofibrosis (MF). At the recent EHA meeting, researchers from Telios Pharma Inc. presented preclinical data for TL-895, a novel BTK inhibitor currently in clinical development for the treatment of patients with chronic lymphocytic leukemia and MF.
Watchers of the Bruton’s kinase (BTK) inhibitor space may be casting renewed skepticism in that direction after Merck KGaA disclosed April 12 that the U.S. FDA placed a partial clinical hold on the sign-up of more patients in work testing evobrutinib in relapsing multiple sclerosis (MS) – but BTK efforts in MS continue in various quarters.
A few weeks after Gossamer Bio Inc. said it was pausing enrollment in a phase Ib/II study of CNS-penetrant BTK inhibitor GB-5121 in relapsed/refractory CNS lymphoma, citing the drug’s risk/benefit profile observed to date and a prioritization of resources, the company is dropping the drug’s development entirely.
