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Drug Name APR-246
Trade Name
Synonyms p53 activator APR-246|PRIMA-1MET|PRIMA-1 analogue APR-246|Eprenetapopt
Drug Descriptions

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).

DrugClasses p53 Activator 11
CAS Registry Number 5291-32-7
NCIT ID C85465


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Therapy Name Drugs Efficacy Evidence Clinical Trials
Acalabrutinib + APR-246 APR-246 Acalabrutinib 0 1
APR-246 APR-246 5 0
APR-246 + Azacitidine APR-246 Azacitidine 0 3
APR-246 + Azacitidine + Venetoclax APR-246 Azacitidine Venetoclax 0 1
APR-246 + Carboplatin APR-246 Carboplatin 0 0
APR-246 + Carboplatin + Doxorubicin APR-246 Carboplatin Doxorubicin 0 1
APR-246 + Cisplatin APR-246 Cisplatin 11 0
APR-246 + Ibrutinib APR-246 Ibrutinib 0 0
APR-246 + Ibrutinib + Rituximab + Venetoclax APR-246 Ibrutinib Rituximab Venetoclax 0 0
APR-246 + Pembrolizumab APR-246 Pembrolizumab 0 1
APR-246 + Rituximab + Venetoclax APR-246 Rituximab Venetoclax 0 1
APR-246 + Venetoclax APR-246 Venetoclax 0 1

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