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, PMID: 32719798). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| CX-5461 | CX5461|Pidnarulex|CX 5461 | 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 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 |
| 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 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 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 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 |
| 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 |
| 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 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT07069699 | Phase Ib/II | CX-5461 | Testing the Safety of Anti-Cancer Drug, CX-5461 (Pidnarulex), in Treating Lymphoma With Specific Changes in the MYC Gene | Recruiting | USA | 0 |
| 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 |
| NCT07147231 | Phase Ib/II | CX-5461 Cemiplimab + CX-5461 | Testing the Effectiveness of the Anti-cancer Drug Pidnarulex (CX-5461), in Combination With Another Anti-cancer Drug Cemiplimab (REGN2810), in Treating Refractory Microsatellite Stable Colorectal Cancer | Recruiting | USA | 0 |
| NCT06606990 | Phase I | CX-5461 | Testing How the Body Responds to the Drug CX-5461 (Pidnarulex) in Patients With Metastatic Solid Cancers | Recruiting | USA | 0 |
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