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|Therapy Name||ARQ 531|
ARQ 531 is an ATP-competitive BTK inhibitor with activity against wild-type BTK and BTK C481S and has been demonstrated to inhibit migration and viability of chronic lymphocytic leukemia cells (ASH, Blood 2016 128:3232).
|Drug Name||Trade Name||Synonyms||Drug Classes||Drug Description|
|ARQ 531||ARQ531|ARQ-531||BTK inhibitor 22||ARQ 531 is an ATP-competitive BTK inhibitor with activity against wild-type BTK and BTK C481S, which may inhibit migration and viability of tumor cells (PMID: 30093506, PMID: 31992353).|
|Molecular Profile||Indication/Tumor Type||Response Type||Therapy Name||Approval Status||Evidence Type||Efficacy Evidence||References|
|Unknown unknown||chronic lymphocytic leukemia||not applicable||ARQ 531||Preclinical - Patient cell culture||Actionable||In a preclinical study, ARQ 531 treatment inhibited activation of BCR signaling and cell migration, and induced enhanced cytotoxicity in patient-derived chronic lymphocytic leukemia cells in culture, and increased survival in a transgenic mouse model (PMID: 30093506).||30093506|
|Unknown unknown||B-cell lymphoma||not applicable||ARQ 531||Preclinical||Actionable||In a preclinical study, ARQ 531 treatment increased survival in a transgenic mouse model of aggressive B-cell lymphoma similar to Richter transformation, with a median of 47 days vs. 38 days with Imbruvica (ibrutinib) (p=0.036) (PMID: 30093506).||30093506|
|Clinical Trial||Phase||Therapies||Title||Recruitment Status|
|NCT03162536||Phase I||ARQ 531||Safety, PK, PD, and Antitumor Activity of ARQ 531 in Hematologic Malignancies||Recruiting|