Gene Detail

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Gene Symbol BTK
Synonyms AGMX1 | AT | ATK | BPK | IGHD3 | IMD1 | PSCTK1 | XLA
Gene Description BTK, Bruton tyrosine kinase, is a non-receptor tyrosine kinase involved in B-cell activation and development (PMID: 24658273). BTK is commonly overexpressed in various hematological malignancies (PMID: 24658273) and BTK mutations have been linked to BTK inhibitor drug resistance (PMID: 28235842).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
BTK A428D diffuse large B-cell lymphoma resistant LOXO-305 Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK A428D demonstrated resistance to LOXO-305 in culture (PMID: 35196427). 35196427
BTK A428D diffuse large B-cell lymphoma resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK A428D demonstrated resistance to Imbruvica (ibrutinib) in culture (PMID: 35196427). 35196427
BTK A428D diffuse large B-cell lymphoma resistant Fenebrutinib Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK A428D demonstrated resistance to Fenebrutinib (GDC-0853) in culture (PMID: 35196427). 35196427
BTK A428D diffuse large B-cell lymphoma resistant Vecabrutinib Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK A428D demonstrated resistance to Vecabrutinib (SNS-062) in culture (PMID: 35196427). 35196427
BTK C481A chronic lymphocytic leukemia predicted - resistant Ibrutinib Preclinical Actionable In a preclinical study, patients with BTK C481 were predicted to have resistance to Imbruvica (ibrutinib) since C481 is in the covalent binding site of the BTK inhibitor and C481A interferes with drug binding (PMID: 24869597). 24869597
BTK C481F chronic lymphocytic leukemia predicted - resistant Ibrutinib Preclinical Actionable In a preclinical study, patients with BTK C481 were predicted to have resistance to Imbruvica (ibrutinib) since C481 is in the covalent binding site of the BTK inhibitor and C481F interferes with drug binding (PMID: 24869597). 24869597
BTK C481F diffuse large B-cell lymphoma resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, the BTK C481F mutation was identified in diffuse large B-cell lymphoma cells that acquired resistance to Imbruvica (ibrutinib) in culture (PMID: 28178345). 28178345
BTK C481F diffuse large B-cell lymphoma resistant Tirabrutinib Preclinical - Cell culture Actionable In a preclinical study, diffuse large B-cell lymphoma cells that acquired resistance to Imbruvica (ibrutinib) harbored the BTK C481F mutation, and was resistant to Tirabrutinib (ONO-4059) in culture (PMID: 28178345). 28178345
BTK C481F diffuse large B-cell lymphoma resistant Idelalisib Preclinical - Cell culture Actionable In a preclinical study, diffuse large B-cell lymphoma cells that acquired resistance to Imbruvica (ibrutinib) harbored the BTK C481F mutation, and was resistant to Zydelig (idelalisib) in culture (PMID: 28178345). 28178345
BTK C481F diffuse large B-cell lymphoma resistant Idelalisib + Tirabrutinib Preclinical - Cell culture Actionable In a preclinical study, diffuse large B-cell lymphoma cells that acquired resistance to Imbruvica (ibrutinib) harbored the BTK C481F mutation, and was resistant to Zydelig (idelalisib) and Tirabrutinib (ONO-4059) combination treatment in culture (PMID: 28178345). 28178345
BTK C481S chronic lymphocytic leukemia resistant Ibrutinib Clinical Study - Cohort Actionable In a clinical study, BTK C418S was identified as an acquired mutation that confers resistance to Imbruvica by preventing irreversible binding of ibrutinib to BTK in patients with chronic lymphocytic leukemia who relapsed while on Imbruvica (ibrutinib)(PMID: 24869598). 24869598
BTK C481S chronic lymphocytic leukemia resistant Ibrutinib Preclinical - Patient cell culture Actionable In a preclinical study, primary chronic lymphocytic leukemia cells derived from patients who acquired BTK C481S following Imbruvica (ibrutinib) treatment demonstrated resistance to Imbruvica (ibrutinib) in culture (PMID: 30093506). 30093506
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 C481S hematologic cancer predicted - sensitive RXC005 Preclinical - Cell culture Actionable In a preclinical study, hematological cancer cell lines that are dependent on Btk signaling demonstrated sensitivity to RXC005 in culture (Blood 2016 128:4399). detail...
BTK C481S diffuse large B-cell lymphoma sensitive Ibrutinib + Venetoclax Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK C481S resulting in Imbruvica (ibrutinib) resistance demonstrated increased sensitivity to Imbruvica (ibrutinib) when also treated with Venclexta (venetoclax), demonstrating decreased cell growth in culture (PMID: 28428442). 28428442
BTK C481S mantle cell lymphoma resistant Ibrutinib Case Reports/Case Series Actionable In a clinical study, BTK C418S was identified as an acquired mutation that confers resistance to Imbruvica (ibrutinib) in two patients with mantle cell lymphoma who relapsed after a durable response (PMID: 25082755). 25082755
BTK C481S lymphoma resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, lymphoma cells expressing BTK C481S were resistant to Imbruvica (ibrutinib) in culture (PMID: 27626698) 27626698
BTK C481S chronic lymphocytic leukemia predicted - resistant Venetoclax Case Reports/Case Series Actionable In a clinical case study, a patient with chronic lymphocytic leukemia who had relapsed on treatment with Imbruvica (ibrutinib) was treated with Venclexta (venetoclax), but progressed and was found to harbor BTK C481S (PMID: 32232486). 32232486
BTK C481S chronic lymphocytic leukemia/small lymphocytic lymphoma resistant Acalabrutinib Guideline Actionable Calquence (acalabrutinib) is not indicated for use in patients with Imbruvica (ibrutinib)-refractory chronic lymphocytic leukemia/small lymphocytic lymphoma harboring BTK C481S (NCCN.org). detail...
BTK C481S chronic lymphocytic leukemia/small lymphocytic lymphoma resistant Zanubrutinib Guideline Actionable Brukinsa (zanubrutinib) is not indicated for use in patients with Imbruvica (ibrutinib)-refractory chronic lymphocytic leukemia/small lymphocytic lymphoma harboring BTK C481S (NCCN.org). detail...
BTK C481S diffuse large B-cell lymphoma sensitive NX-2127 Preclinical - Cell line xenograft Actionable In a preclinical study, NX-2127 inhibited proliferation of a diffuse large B-cell lymphoma cell line expressing BTK C481S in culture, and resulted in tumor growth inhibition in a cell line xenograft model (62nd ASH Annual Meeting and Exposition, Dec 2020, Abstract 2788). detail...
BTK C481S Advanced Solid Tumor predicted - sensitive RN486 Preclinical - Biochemical Actionable In a preclinical study, treatment with RN486 resulted in reduced Btk activity in a cell line expressing BTK C481S in culture (PMID: 33526860). 33526860
BTK C481S Advanced Solid Tumor predicted - sensitive Fenebrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Fenebrutinib resulted in reduced Btk activity in a cell line expressing BTK C481S in culture (PMID: 33526860). 33526860
BTK C481S chronic lymphocytic leukemia predicted - sensitive Fenebrutinib Case Reports/Case Series Actionable In a Phase I trial, Fenebrutinib (GDC-0853) treatment resulted in clinical activity in patients with chronic lymphocytic leukemia harboring BTK C481S including one patient with a partial response with lymphocytosis and duration of response of 2.5 months and two patients with stable disease, each with a decrease in tumor size from baseline of -44.0% and -23.0% (PMID: 29560128; NCT01991184). 29560128
BTK C481S diffuse large B-cell lymphoma resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK C481S demonstrated resistance to Imbruvica (ibrutinib) in culture (PMID: 35196427). 35196427
BTK C481S diffuse large B-cell lymphoma sensitive LOXO-305 Preclinical - Cell culture Actionable In a preclinical study, LOXO-305 treatment inhibited viability of a diffuse large B-cell lymphoma cell line harboring BTK C481S in culture (PMID: 35196427). 35196427
BTK C481S diffuse large B-cell lymphoma sensitive Fenebrutinib Preclinical - Cell culture Actionable In a preclinical study, Fenebrutinib (GDC-0853) treatment inhibited viability of a diffuse large B-cell lymphoma cell line harboring BTK C481S in culture (PMID: 35196427). 35196427
BTK C481S diffuse large B-cell lymphoma sensitive Vecabrutinib Preclinical - Cell culture Actionable In a preclinical study, Vecabrutinib (SNS-062) treatment inhibited viability of a diffuse large B-cell lymphoma cell line harboring BTK C481S in culture (PMID: 35196427). 35196427
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 C481S mantle cell lymphoma predicted - resistant Edralbrutinib Preclinical - Cell culture Actionable In a preclinical study, Edralbrutinib (TG-1701) treatment resulted in reduced sensitivity in a mantle cell lymphoma cell line expressing BTK C481S compared to the parental wild-type BTK cell line in culture (PMID: 34551904). 34551904
BTK C481S diffuse large B-cell lymphoma activated B-cell type predicted - sensitive NX-5948 Preclinical - Cell line xenograft Actionable In a preclinical study, NX-5948 treatment resulted in degradation of BTK C481S and inhibited proliferation of an activated B-cell type diffuse large B-cell lymphoma (ABC-DLBCL) cell line harboring BTK C481S in culture and inhibited tumor growth in a cell line xenograft model (Blood 2021 138 (Supp 1):2251). detail...
BTK T474A BTK C481S Advanced Solid Tumor predicted - sensitive Ibrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Imbruvica (ibrutinib) resulted in reduced Btk activity in cell lines expressing BTK variants T474A and C481S in culture (PMID: 33526860). 33526860
BTK T474A BTK C481S Advanced Solid Tumor predicted - resistant Fenebrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Fenebrutinib (GDC-0853) failed to inhibit Btk activity in a cell line expressing BTK variants T474A and C481S in culture (PMID: 33526860). 33526860
BTK T474S BTK C481S Advanced Solid Tumor predicted - sensitive Ibrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Imbruvica (ibrutinib) resulted in reduced Btk activity in a cell line expressing BTK variants T474S and C481S in culture (PMID: 33526860). 33526860
BTK T474S BTK C481S Advanced Solid Tumor predicted - sensitive Fenebrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Fenebrutinib (GDC-0853) resulted in reduced Btk activity in a cell line expressing BTK variants T474S and C481S in culture (PMID: 33526860). 33526860
BTK T474I BTK C481S Advanced Solid Tumor predicted - resistant Ibrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Imbruvica (ibrutinib) failed to inhibit Btk activity in a cell line expressing BTK variants T474I and C481S in culture (PMID: 33526860). 33526860
BTK T474I BTK C481S Advanced Solid Tumor predicted - resistant Acalabrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Calquence (acalabrutinib) failed to inhibit Btk activity in a cell line expressing BTK variants T474I and C481S in culture (PMID: 33526860). 33526860
BTK T474I BTK C481S Advanced Solid Tumor predicted - resistant Zanubrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Brukinsa (zanubrutinib) failed to inhibit Btk activity in a cell line expressing BTK variants T474I and C481S in culture (PMID: 33526860). 33526860
BTK T474I BTK C481S Advanced Solid Tumor predicted - sensitive RN486 Preclinical - Biochemical Actionable In a preclinical study, treatment with RN486 resulted in reduced Btk activity in a cell line expressing BTK variants T474I and C481S in culture (PMID: 33526860). 33526860
BTK T474I BTK C481S Advanced Solid Tumor predicted - sensitive Fenebrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Fenebrutinib (GDC-0853) resulted in reduced Btk activity in a cell line expressing BTK variants T474I and C481S in culture (PMID: 33526860). 33526860
BTK T474I BTK C481S Advanced Solid Tumor predicted - resistant CGI1746 Preclinical - Biochemical Actionable In a preclinical study, treatment with CGI1746 failed to inhibit Btk activity in a cell line expressing BTK variants T474I and C481S in culture (PMID: 33526860). 33526860
BTK T474M BTK C481S Advanced Solid Tumor predicted - resistant Ibrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Imbruvica (ibrutinib) failied to inhibit Btk activity in a cell line expressing BTK variants T474M and C481S in culture (PMID: 33526860). 33526860
BTK T474M BTK C481S Advanced Solid Tumor predicted - resistant Acalabrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Calquence (acalabrutinib) failed to inhibit Btk activity in a cell line expressing BTK variants T474M and C481S in culture (PMID: 33526860). 33526860
BTK T474M BTK C481S Advanced Solid Tumor predicted - resistant Zanubrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Brukinsa (zanubrutinib) failed to inhibit Btk activity in a cell line expressing BTK variants T474M and C481S in culture (PMID: 33526860). 33526860
BTK T474M BTK C481S Advanced Solid Tumor predicted - sensitive RN486 Preclinical - Biochemical Actionable In a preclinical study, treatment with RN486 resulted in reduced Btk activity in a cell line expressing BTK variants T474M and C481S in culture (PMID: 33526860). 33526860
BTK T474M BTK C481S Advanced Solid Tumor predicted - sensitive Fenebrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Fenebrutinib (GDC-0853) resulted in reduced Btk activity in a cell line expressing BTK variants T474M and C481S in culture (PMID: 33526860). 33526860
BTK T474M BTK C481S Advanced Solid Tumor predicted - resistant CGI1746 Preclinical - Biochemical Actionable In a preclinical study, treatment with CGI1746 failed to inhibit Btk activity in a cell line expressing BTK variants T474M and C481S in culture (PMID: 33526860). 33526860
BTK C481T Advanced Solid Tumor resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing BTK C481T were resistant to Imbruvica (ibrutinib) in culture (PMID: 27282255). 27282255
BTK C481T lymphoma resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, lymphoma cells over expressing BTK C481T were resistant to Imbruvica (ibrutinib) in culture (PMID: 27282255). 27282255
BTK C481T Advanced Solid Tumor predicted - sensitive RN486 Preclinical - Biochemical Actionable In a preclinical study, treatment with RN486 resulted in reduced Btk activity in a cell line expressing BTK C481T in culture (PMID: 33526860). 33526860
BTK T474M BTK C481T Advanced Solid Tumor predicted - resistant Ibrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Imbruvica (ibrutinib) failed to inhibit Btk activity in a cell line expressing BTK variants T474M and C481T in culture (PMID: 33526860). 33526860
BTK T474M BTK C481T Advanced Solid Tumor predicted - resistant Acalabrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Calquence (acalabrutinib) failed to inhibit Btk activity in a cell line expressing BTK variants T474M and C481T in culture (PMID: 33526860). 33526860
BTK T474M BTK C481T Advanced Solid Tumor predicted - sensitive RN486 Preclinical - Biochemical Actionable In a preclinical study, treatment with RN486 resulted in reduced Btk activity in a cell line expressing BTK variants T474M and C481T in culture (PMID: 33526860). 33526860
BTK T474M BTK C481T Advanced Solid Tumor predicted - sensitive Fenebrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Fenebrutinib (GDC-0853) resulted in reduced Btk activity in a cell line expressing BTK variants T474M and C481T in culture (PMID: 33526860). 33526860
BTK T474M BTK C481T Advanced Solid Tumor predicted - resistant CGI1746 Preclinical - Biochemical Actionable In a preclinical study, treatment with CGI1746 failed to inhibit Btk activity in a cell line expressing BTK variants T474M and C481T in culture (PMID: 33526860). 33526860
BTK C481X chronic lymphocytic leukemia predicted - resistant Ibrutinib Phase II Actionable In a Phase II trial, BTK C481X and/or PLCG2 mutations were identified in 80% (8/10) of patients with progressive disease and in 20% (1/5) of patients with prolymphocytic transformation of chronic lymphocytic leukemia while on Imbruvica (ibrutinib) treatment (PMID: 28049639, NCT01500733). 28049639
BTK del mantle cell lymphoma predicted - resistant Edralbrutinib Preclinical - Cell culture Actionable In a preclinical study, Edralbrutinib (TG-1701) treatment resulted in reduced cell growth inhibition in a mantle cell lymphoma cell line with BTK knockout compared to the parental wild-type BTK cell line in culture (PMID: 34551904). 34551904
BTK E90K lymphoma sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, lymphoma cell lines expressing BTK E90K were sensitive to Imbruvica (ibrutinib) treatment in culture, demonstrating decreased cell viability (PMID: 33419778). 33419778
BTK K433T lymphoma sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, a lymphoma cell line expressing BTK K433T was sensitive to Imbruvica (ibrutinib) treatment in culture, demonstrating decreased cell viability (PMID: 33419778). 33419778
BTK L528W diffuse large B-cell lymphoma resistant LOXO-305 Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK L528W demonstrated resistance to LOXO-305 in culture (PMID: 35196427). 35196427
BTK L528W chronic lymphocytic leukemia predicted - resistant LOXO-305 Case Reports/Case Series Actionable In a clinical case study, two patients with chronic lymphocytic leukemia who previously responded to LOXO-305 treatment were found to have acquired BTK L528W upon disease progression (PMID: 35196427). 35196427
BTK L528W diffuse large B-cell lymphoma resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK L528W demonstrated resistance to Imbruvica (ibrutinib) in culture (PMID: 35196427). 35196427
BTK L528W diffuse large B-cell lymphoma resistant Fenebrutinib Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK L528W demonstrated resistance to Fenebrutinib (GDC-0853) in culture (PMID: 35196427). 35196427
BTK L528W diffuse large B-cell lymphoma resistant Vecabrutinib Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK L528W demonstrated resistance to Vecabrutinib (SNS-062) in culture (PMID: 35196427). 35196427
BTK T474I BTK L528W chronic lymphocytic leukemia predicted - resistant LOXO-305 Case Reports/Case Series Actionable In a clinical case study, a patient with chronic lymphocytic leukemia harboring BTK C481S who previously responded to LOXO-305 treatment was found to have acquired BTK T474I and BTK L528W upon disease progression (PMID: 35196427). 35196427
BTK M437R diffuse large B-cell lymphoma resistant LOXO-305 Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK M437R demonstrated resistance to LOXO-305 in culture (PMID: 35196427). 35196427
BTK M437R chronic lymphocytic leukemia predicted - resistant LOXO-305 Case Reports/Case Series Actionable In a clinical case study, a patient with chronic lymphocytic leukemia harboring BTK C481S who previously responded to LOXO-305 treatment was found to have acquired BTK M437R upon disease progression (PMID: 35196427). 35196427
BTK M437R diffuse large B-cell lymphoma sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, Imbruvica (ibrutinib) treatment inhibited phosphorylation of Btk and decreased viability of a diffuse large B-cell lymphoma cell line expressing BTK M437R in culture (PMID: 35196427). 35196427
BTK M437R diffuse large B-cell lymphoma resistant Fenebrutinib Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK M437R demonstrated resistance to Fenebrutinib (GDC-0853) in culture (PMID: 35196427). 35196427
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 P597S lymphoma resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, lymphoma cell lines expressing BTK P597S were resistant to treatment with Imbruvica (ibrutinib) in culture (PMID: 33419778). 33419778
BTK positive diffuse large B-cell lymphoma sensitive RXC005 Preclinical - Cell culture Actionable In a preclinical study, diffuse large B-cell lymphoma cells treated with RXC005 in culture, demonstrated inhibition of BTK signaling and decreased cell growth (Blood 2016 128:4399). detail...
BTK R77S lymphoma sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, lymphoma cell lines expressing BTK R77S were sensitive to Imbruvica (ibrutinib) treatment in culture, demonstrating decreased cell viability (PMID: 33419778). 33419778
BTK T316A lymphoma resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, lymphoma cells expressing BTK T316A were resistant to Imbruvica (ibrutinib) in culture (PMID: 27626698) 27626698
BTK T474A Advanced Solid Tumor predicted - sensitive Ibrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Imbruvica (ibrutinib) resulted in reduced Btk activity in cell lines expressing BTK T474A in culture (PMID: 33526860). 33526860
BTK T474A Advanced Solid Tumor predicted - sensitive Fenebrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Fenebrutinib (GDC-0853) resulted in reduced Btk activity in a cell line expressing BTK T474A in culture (PMID: 33526860). 33526860
BTK T474E Advanced Solid Tumor predicted - sensitive Ibrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Imbruvica (ibrutinib) resulted in reduced Btk activity in cell lines expressing BTK T474E in culture (PMID: 33526860). 33526860
BTK T474I Advanced Solid Tumor predicted - sensitive Ibrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Imbruvica (ibrutinib) resulted in reduced Btk activity in cell lines expressing BTK T474I in culture (PMID: 33526860). 33526860
BTK T474I chronic lymphocytic leukemia predicted - resistant LOXO-305 Case Reports/Case Series Actionable In a clinical case study, two patients with chronic lymphocytic leukemia who previously responded to LOXO-305 treatment were found to have acquired BTK T474I upon disease progression (PMID: 35196427). 35196427
BTK T474I diffuse large B-cell lymphoma sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, Imbruvica (ibrutinib) treatment inhibited phosphorylation of Btk and decreased viability of a diffuse large B-cell lymphoma cell line expressing BTK T474I in culture (PMID: 35196427). 35196427
BTK T474I diffuse large B-cell lymphoma resistant LOXO-305 Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK T474I demonstrated resistance to LOXO-305 in culture (PMID: 35196427). 35196427
BTK T474I diffuse large B-cell lymphoma resistant Fenebrutinib Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK T474I demonstrated resistance to Fenebrutinib (GDC-0853) in culture (PMID: 35196427). 35196427
BTK T474I diffuse large B-cell lymphoma resistant Vecabrutinib Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK T474I demonstrated resistance to Vecabrutinib (SNS-062) in culture (PMID: 35196427). 35196427
BTK T474L Advanced Solid Tumor predicted - sensitive Ibrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Imbruvica (ibrutinib) resulted in reduced Btk activity in cell lines expressing BTK T474L in culture (PMID: 33526860). 33526860
BTK T474M Advanced Solid Tumor predicted - resistant Ibrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Imbruvica (ibrutinib) failed to inhibit Btk activity in cell lines expressing BTK T474M in culture (PMID: 33526860). 33526860
BTK T474M Advanced Solid Tumor predicted - resistant Acalabrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Calquence (acalabrutinib) failed to inhibit Btk activity in a cell line expressing BTK T474M in culture (PMID: 33526860). 33526860
BTK T474N Advanced Solid Tumor predicted - sensitive Ibrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Imbruvica (ibrutinib) resulted in reduced Btk activity in cell lines expressing BTK T474N in culture (PMID: 33526860). 33526860
BTK T474Q Advanced Solid Tumor predicted - sensitive Ibrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Imbruvica (ibrutinib) resulted in reduced Btk activity in a cell line expressing BTK T474Q in culture (PMID: 33526860). 33526860
BTK T474S Advanced Solid Tumor predicted - sensitive Ibrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Imbruvica (ibrutinib) resulted in reduced Btk activity in cell lines expressing BTK T474S in culture (PMID: 33526860). 33526860
BTK T474V Advanced Solid Tumor predicted - sensitive Ibrutinib Preclinical - Biochemical Actionable In a preclinical study, treatment with Imbruvica (ibrutinib) resulted in reduced Btk activity in cell lines expressing BTK T474V in culture (PMID: 33526860). 33526860
BTK V416L diffuse large B-cell lymphoma resistant LOXO-305 Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK V416L demonstrated resistance to LOXO-305 in culture (PMID: 35196427). 35196427
BTK V416L chronic lymphocytic leukemia predicted - resistant LOXO-305 Case Reports/Case Series Actionable In a clinical case study, a patient with chronic lymphocytic leukemia who previously responded to LOXO-305 treatment was found to have acquired a BTK V416L upon disease progression (PMID: 35196427). 35196427
BTK V416L diffuse large B-cell lymphoma sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, Imbruvica (ibrutinib) treatment inhibited phosphorylation of Btk and decreased viability of a diffuse large B-cell lymphoma cell line expressing BTK V416L in culture (PMID: 35196427). 35196427
BTK V416L diffuse large B-cell lymphoma resistant Fenebrutinib Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK V416L demonstrated resistance to Fenebrutinib (GDC-0853) in culture (PMID: 35196427). 35196427
BTK V416L diffuse large B-cell lymphoma resistant Vecabrutinib Preclinical - Cell culture Actionable In a preclinical study, a diffuse large B-cell lymphoma cell line expressing BTK V416L demonstrated resistance to Vecabrutinib (SNS-062) in culture (PMID: 35196427). 35196427
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 V568I lymphoma sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, lymphoma cell lines expressing BTK V568I were sensitive to Imbruvica (ibrutinib) treatment in culture, demonstrating decreased cell viability (PMID: 33419778). 33419778
BTK Y315N lymphoma resistant Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, lymphoma cell lines expressing BTK Y315N were resistant to treatment with Imbruvica (ibrutinib) in culture (PMID: 33419778). 33419778
BTK Y361H lymphoma sensitive Ibrutinib Preclinical - Cell culture Actionable In a preclinical study, a lymphoma cell line expressing BTK Y361H was sensitive to Imbruvica (ibrutinib) treatment in culture, demonstrating decreased cell viability (PMID: 33419778). 33419778