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Therapy Name ARQ 531
Synonyms
Therapy Description

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).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
ARQ 531 ARQ531|ARQ-531|Nemtabrutinib|MK-1026|MK 1026|MK1026 BTK inhibitor 39 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).

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  • Case insensitive filtering will display rows if any text in any cell matches the filter term
  • Use simple literal full or partial string matches
  • Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
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  • Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
BTK M437R diffuse large B-cell lymphoma sensitive ARQ 531 Preclinical - Cell culture Actionable In a preclinical study, ARQ 531 treatment inhibited viability of a diffuse large B-cell lymphoma cell line harboring BTK M437R in culture (PMID: 35196427). 35196427
BTK A428D mantle cell lymphoma sensitive ARQ 531 Preclinical - Cell culture Actionable In a preclinical study, ARQ 531 inhibited viability of a mantle cell lymphoma cell line harboring BTK A428D in culture (PMID: 36661329). 36661329
BTK V416L diffuse large B-cell lymphoma sensitive ARQ 531 Preclinical - Cell culture Actionable In a preclinical study, ARQ 531 treatment inhibited viability of a diffuse large B-cell lymphoma cell line harboring BTK V416L in culture (PMID: 35196427). 35196427
BTK G480R mantle cell lymphoma sensitive ARQ 531 Preclinical - Cell culture Actionable In a preclinical study, ARQ 531 inhibited viability of a mantle cell lymphoma cell line harboring BTK G480R in culture (PMID: 36661329). 36661329
BTK C481F mantle cell lymphoma sensitive ARQ 531 Preclinical - Cell culture Actionable In a preclinical study, ARQ 531 inhibited viability of a mantle cell lymphoma cell line harboring BTK C481F in culture (PMID: 36661329). 36661329
BTK C481S diffuse large B-cell lymphoma sensitive ARQ 531 Preclinical - Cell culture Actionable In a preclinical study, ARQ 531 treatment inhibited viability of a diffuse large B-cell lymphoma cell line harboring BTK C481S in culture (PMID: 35196427). 35196427
BTK G409R mantle cell lymphoma sensitive ARQ 531 Preclinical - Cell culture Actionable In a preclinical study, ARQ 531 inhibited viability of a mantle cell lymphoma cell line harboring BTK G409R in culture (PMID: 36661329). 36661329
BTK C481S chronic lymphocytic leukemia sensitive ARQ 531 Preclinical - Patient cell culture Actionable In a preclinical study, ARQ 531 treatment inhibited activation of BCR signaling and induced cytotoxicity in Imbruvica (ibrutinib)-resistant patient-derived chronic lymphocytic leukemia cells harboring BTK C481S in culture (PMID: 30093506). 30093506
BTK V416L mantle cell lymphoma sensitive ARQ 531 Preclinical - Cell culture Actionable In a preclinical study, ARQ 531 inhibited viability of a mantle cell lymphoma cell line harboring BTK V416L in culture (PMID: 36661329). 36661329
BTK L528S mantle cell lymphoma sensitive ARQ 531 Preclinical - Cell culture Actionable In a preclinical study, ARQ 531 inhibited viability of a mantle cell lymphoma cell line harboring BTK L528S in culture (PMID: 36661329). 36661329
BTK D539H mantle cell lymphoma sensitive ARQ 531 Preclinical - Cell culture Actionable In a preclinical study, ARQ 531 inhibited viability of a mantle cell lymphoma cell line harboring BTK D539H in culture (PMID: 36661329). 36661329
FLT3 exon 14 ins acute myeloid leukemia not predictive ARQ 531 Preclinical - Patient cell culture Actionable In a preclinical study, ARQ 531 treatment induced apoptosis in acute myeloid leukemia cells harboring either FLT3 exon 14 insertion (FLT3-ITD) or wild-type FLT3, and inhibited proliferation and reduced colony formation in patient cells derived from acute myeloid leukemia independent of FLT3 status in culture (PMID: 31992353). 31992353

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT07796373 Phase II ARQ 531 Nemtabrutinib for Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Leukemia (SLL) Refractory to Covalent Bruton Tyrosine Kinase Inhibitor or Pirtobrutinib and Previously Treated With a BCL2 Inhibitor Not yet recruiting USA 0
NCT05624554 Phase III Bendamustine + Rituximab Cyclophosphamide + Fludarabine + Rituximab ARQ 531 A Study of Nemtabrutinib vs Chemoimmunotherapy for Participants With Previously Untreated Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (CLL/SLL) Without TP53 Aberrations (MK-1026-008, BELLWAVE-008) Active, not recruiting USA | TUR | ROU | POL | LTU | HUN | DNK | BRA | BGR | AUS 11
NCT06136559 Phase III Ibrutinib ARQ 531 Acalabrutinib A Study of Nemtabrutinib (MK-1026) Versus Comparator (Investigator's Choice of Ibrutinib or Acalabrutinib) in First Line (1L) Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL) (MK-1026-011/BELLWAVE-011) Recruiting USA | TUR | SWE | POL | NZL | NOR | ISR | GRC | GBR | ESP | DNK | DEU | CZE | CAN | BRA | BEL | AUS 12
NCT04728893 Phase II ARQ 531 Efficacy and Safety of Nemtabrutinib (MK-1026) in Participants With Hematologic Malignancies (MK-1026-003) Recruiting USA | TUR | ROU | POL | ITA | ISR | IRL | HUN | GBR | FRA | ESP | DNK | DEU | CZE | CHE | CAN | BRA | AUS | ARG 3
NCT03162536 Phase I ARQ 531 Safety, PK, PD, and Antitumor Activity of ARQ 531 in Hematologic Malignancies Active, not recruiting USA 0


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