Therapy Detail
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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
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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 )
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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 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 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 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 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 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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- Click on any column header arrows to sort by that column
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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