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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). |
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). |
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 |
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 |