Therapy Detail
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| Therapy Name | E7449 |
| Synonyms | |
| Therapy Description |
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). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| E7449 | 2X-121 | PARP Inhibitor (Pan) 29 Tankyrase Inhibitor 11 | 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 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")
Sorting
- 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
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| 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 |
| 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
- 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")
Sorting
- 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 |
|---|---|---|---|---|---|---|
| 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 | GBR | 0 |
| NCT05571969 | Phase I | Dovitinib + E7449 E7449 | Study to Determine the Maximum Tolerated Dose (MTD) of PARPi 2X-121 Monotherapy and the MTD of Dovitinib in Combination With 2X-121 in Patients With Advanced Solid Tumors | Recruiting | USA | 0 |
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