Therapy Detail

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Therapy Name CX-5461
Synonyms
Therapy Description

CX-5461 is an RNA polymerase I (Pol I) inhibitor that inhibits rRNA synthesis, resulting in growth arrest and apoptosis in cancer cells (PMID: 26472108).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
CX-5461 CX5461 CX-5461 is an RNA polymerase I (Pol I) inhibitor that inhibits rRNA synthesis, resulting in growth arrest and apoptosis in cancer cells (PMID: 26472108, PMID: 32719798).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
BRIP1 A349P Advanced Solid Tumor sensitive CX-5461 Preclinical - Cell culture Actionable In a preclinical study, CX-5461 inhibited survival of transformed cells expressing BRIP1 A349P in culture (PMID: 32542039). 32542039
BRIP1 K52R Advanced Solid Tumor sensitive CX-5461 Preclinical - Cell culture Actionable In a preclinical study, CX-5461 inhibited survival of transformed cells expressing BRIP1 K52R in culture (PMID: 32542039). 32542039
BRIP1 C283R Advanced Solid Tumor sensitive CX-5461 Preclinical - Cell culture Actionable In a preclinical study, CX-5461 inhibited survival of transformed cells expressing BRIP1 C283R in culture (PMID: 32542039). 32542039
BRIP1 M299I Advanced Solid Tumor no benefit CX-5461 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing BRIP1 M299I were not sensitive to CX-5461 induced growth inhibition in culture (PMID: 32542039). 32542039
BRIP1 L340F Advanced Solid Tumor no benefit CX-5461 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing BRIP1 L340F were not sensitive to CX-5461 induced growth inhibition in culture (PMID: 32542039). 32542039
BRIP1 del Advanced Solid Tumor sensitive CX-5461 Preclinical - Cell culture Actionable In a preclinical study, CX-5461 inhibited survival of transformed cells with BRIP1 knocked out by CRISPR/Cas9 in culture (PMID: 32542039). 32542039
PTEN loss prostate cancer no benefit CX-5461 Preclinical Actionable In a preclinical study, CX-5461 treatment did not result in histological change in PTEN deficient transgenic animal model of prostate cancer (PMID: 27486174). 27486174
BRIP1 C283S Advanced Solid Tumor sensitive CX-5461 Preclinical - Cell culture Actionable In a preclinical study, CX-5461 inhibited survival of transformed cells expressing BRIP1 C283S in culture (PMID: 32542039). 32542039

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT04890613 Phase I CX-5461 Study of CX-5461 in Patients With Solid Tumours and BRCA1/2, PALB2 or Homologous Recombination Deficiency (HRD) Mutation Recruiting USA | CAN 0


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