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Therapy Name APR-246
Synonyms
Therapy Description

APR-246 is an analogue of PRIMA-1, which modifies the core domain of mutant p53, resulting in restoration of wild-type p53 conformation and reactivation of normal p53 function, leading to increased cell cycle arrest and tumor cell death (PMID: 20498645, PMID: 29670092).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
APR-246 p53 activator APR-246|PRIMA-1MET|PRIMA-1 analogue APR-246|Eprenetapopt p53 Activator 11 APR-246 is an analogue of PRIMA-1, which modifies the core domain of mutant p53, resulting in restoration of wild-type p53 conformation and reactivation of normal p53 function, leading to increased cell cycle arrest and tumor cell death (PMID: 20498645, PMID: 29670092).

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 )
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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
TP53 V173M acute myeloid leukemia predicted - sensitive APR-246 Case Reports/Case Series Actionable In a Phase I trial, APR-246 demonstrated safety and preliminary clinical activity in patients with hematological cancers, including an acute myeloid leukemia patient harboring TP53 V173M that achieved a decrease in bone marrow blast percentage from 46% to 26% (PMID: 22965953). 22965953
TP53 wild-type melanoma sensitive APR-246 Preclinical - Cell line xenograft Actionable In a preclinical study, APR-246 inhibited growth of TP53 wild-type melanoma cells in 3D culture and in cell line xenograft models (PMID: 21239882). 21239882
TP53 R273L lung small cell carcinoma sensitive APR-246 Preclinical - Cell line xenograft Actionable In a preclinical study, APR-246 demonstrated efficacy in cell line xenograft models of small cell lung cancer harboring TP53 R273L (PMID: 21415220). 21415220
TP53 inact mut lung small cell carcinoma sensitive APR-246 Preclinical - Cell line xenograft Actionable In a preclinical study, APR-246 induced apoptosis in small-cell lung cancer (SCLC) cell lines and decreased tumor growth in SCLC cell line xenograft models harboring Tp53 inactivating mutations (PMID: 21415220). 21415220
TP53 S241F lung small cell carcinoma sensitive APR-246 Preclinical - Cell line xenograft Actionable In a preclinical study, APR-246 demonstrated efficacy in xenograft models of small cell lung cancer harboring TP53 S241F (PMID: 21415220). 21415220

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  • Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries


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