Therapy Detail

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Therapy Name E7449
Synonyms
Therapy Description

E7449 binds to and inhibits PARP1 and PARP2, as well as TNKS1 and TNKS2, potentially resulting in increased sensitivity to DNA damaging agents and decreased growth of tumor cells with defective DNA damage repair (PMID: 26513298).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
E7449 2X-121 PARP Inhibitor (Pan) 22 Tankyrase Inhibitor 10 E7449 (2X-121) binds to and inhibits PARP1 and PARP2, as well as TNKS1 and TNKS2, potentially resulting in increased sensitivity to DNA damaging agents and decreased growth of tumor cells with defective DNA damage repair (PMID: 26513298, PMID: 32523090).

Filtering

  • Case insensitive filtering will display rows where any text in any cell matches the filter term
  • Simple literal full or partial string matches
  • Separate multiple filter terms with a spaces, order doesn't matter (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 a longer phrase which contains spaces "mtor c1483f"

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown pancreatic cancer not applicable E7449 Phase I Actionable In a Phase I trial, E7449 treatment inhibited Parp activity in peripheral blood mononuclear cells and resulted in stable disease for more than 24 weeks in 7 patients with pancreatic cancer (J Clin Oncol 36, 2018 (suppl; abstr 2505); abstr e19531; NCT01618136). detail...
ATRX inact mut Advanced Solid Tumor sensitive E7449 Preclinical Actionable In a preclinical study, E7449 inhibited proliferation of a ATRX-deficient cell line in culture, which demonstrated increased sensitivity compared to cells without DNA repair pathway mutations (PMID: 26513298). 26513298
ATM inact mut Advanced Solid Tumor sensitive E7449 Preclinical Actionable In a preclinical study, E7449 inhibited proliferation of a ATM-deficient cell line in culture, which demonstrated increased sensitivity compared to cells without DNA repair pathway mutations (PMID: 26513298). 26513298
Unknown unknown Advanced Solid Tumor not applicable E7449 Phase I Actionable In a Phase I trial, E7449 treatment demonstrated safety and resulted in an overall response rate of 4.9% (2/41, partial responses) and stable disease in 31.7% (13/41) of patients with advanced solid tumors, including stable disease lasting greater than 23 weeks in 8 patients (PMID: 32523090; NCT01618136). 32523090
Unknown unknown ovarian cancer not applicable E7449 Phase I Actionable In a Phase I trial, E7449 treatment inhibited Parp activity in peripheral blood mononuclear cells and resulted in partial response in 40% (2/5) of the patients with ovarian cancer (J Clin Oncol 36, 2018 (suppl; abstr 2505); abstr e19531; NCT01618136). detail...
RAD51C inact mut Advanced Solid Tumor sensitive E7449 Preclinical Actionable In a preclinical study, E7449 inhibited proliferation of a RAD51C-deficient cell line in culture, which demonstrated increased sensitivity compared to cells without DNA repair pathway mutations (PMID: 26513298). 26513298

Filtering

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  • Separate multiple filter terms with a spaces, order doesn't matter (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 a longer phrase which contains spaces "mtor c1483f"

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT03878849 Phase II E7449 Investigation of 2X-121 in Patients With Advanced Ovarian Cancer Selected by the 2X-121 DRP (PREDICT 2X-121) Recruiting USA 0


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