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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).

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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
ARID1A dec exp	ovarian cancer	predicted - sensitive	APR-246	Preclinical - Cell line xenograft	Actionable	In a preclinical study, ovarian cancer cells with ARID1A-deficiency via knockdown were sensitive to treatment with APR-246, demonstrating decreased cell survival and reduced colony formation in culture and tumor growth suppression in cell-line xenograft models (PMID: 30686770).	30686770
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 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 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
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

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