Therapy Detail

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Therapy Name Fenebrutinib
Synonyms
Therapy Description

Fenebrutinib (GDC-0853) is a small molecule inhibitor of BTK, including BTK C481S, which may result in reduced BTK activity, increased cytotoxicity, and antitumor activity (PMID: 30018078, PMID: 29560128).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Fenebrutinib GDC-0853 BTK inhibitor 39 Fenebrutinib (GDC-0853) is a small molecule inhibitor of BTK, including BTK C481S, which may result in reduced BTK activity, increased cytotoxicity, and antitumor activity (PMID: 30018078, PMID: 29560128).

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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 )
  • Filtering will only apply to rows that are already loaded on the page. Filtering has no impact on query parameters.
  • 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 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 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 - 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 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 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 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 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 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 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 L528S mantle cell lymphoma resistant Fenebrutinib Preclinical - Cell culture Actionable In a preclinical study, a mantle cell lymphoma cell line developed resistance to Fenebrutinib (GDC-0853) after prolonged exposure in culture, and was subsequently found to have acquired BTK L528S (PMID: 36661329). 36661329
BTK D539H mantle cell lymphoma resistant Fenebrutinib Preclinical - Cell culture Actionable In a preclinical study, a mantle cell lymphoma cell line developed resistance to Fenebrutinib (GDC-0853) after prolonged exposure in culture, and was subsequently found to have acquired BTK D539H (PMID: 36661329). 36661329
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 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 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 G480R mantle cell lymphoma resistant Fenebrutinib Preclinical - Cell culture Actionable In a preclinical study, a mantle cell lymphoma cell line developed resistance to Fenebrutinib (GDC-0853) after prolonged exposure in culture, and was subsequently found to have acquired BTK G480R (PMID: 36661329). 36661329
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

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  • Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
  • Filtering will only apply to rows that are already loaded on the page. Filtering has no impact on query parameters.
  • Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

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  • Generally, the default sort order for tables is set to be first column ascending; however, specific tables may set a different default sort order.
  • Click on any column header arrows to sort by that column
  • Hold down the Shift key and click multiple columns to sort by more than one column. Be sure to set ascending or descending order for a given column before moving on to the next column.

Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries


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