Therapy Detail
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| Therapy Name | Rezatapopt |
| Synonyms | |
| Therapy Description |
PC14586 is a small molecule that stabilizes TP53 Y220C and reactivates TP53 function, which may lead to cell cycle arrest and growth inhibition (AACR Annual Meeting Apr 2021, Session MS.LBA01, Abstract # LB006). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Rezatapopt | PC 14586|PC-14586|PC14586 | p53 Activator 12 | Rezatapopt (PC14586) is a small molecule that stabilizes TP53 Y220C and reactivates TP53 function, which may lead to cell cycle arrest and growth inhibition (AACR Annual Meeting Apr 2021, Session MS.LBA01, Abstract # LB006). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| TP53 P151R TP53 Y220C | Advanced Solid Tumor | resistant | Rezatapopt | Preclinical - Cell culture | Actionable | In a preclinical study, cancer cell lines expressing TP53 Y220C and P151R were resistant to Rezatapopt (PC14586) treatment in culture (PMID: 41504628). | 41504628 |
| TP53 Y220C TP53 R282W | Advanced Solid Tumor | resistant | Rezatapopt | Preclinical - Cell culture | Actionable | In a preclinical study, cancer cell lines expressing TP53 Y220C and R282W were resistant to Rezatapopt (PC14586) treatment in culture (PMID: 41504628). | 41504628 |
| TP53 Y220C TP53 N288fs | Advanced Solid Tumor | resistant | Rezatapopt | Preclinical - Cell culture | Actionable | In a preclinical study, cancer cell lines expressing TP53 Y220C and N288fs were resistant to Rezatapopt (PC14586) treatment in culture (PMID: 41504628). | 41504628 |
| TP53 P152R TP53 Y220C | Advanced Solid Tumor | resistant | Rezatapopt | Preclinical - Cell culture | Actionable | In a preclinical study, cancer cell lines expressing TP53 Y220C and P152R were resistant to Rezatapopt (PC14586) treatment in culture (PMID: 41504628). | 41504628 |
| TP53 Y220C TP53 R273C | Advanced Solid Tumor | resistant | Rezatapopt | Preclinical - Cell culture | Actionable | In a preclinical study, cancer cell lines expressing TP53 Y220C and R273C were resistant to Rezatapopt (PC14586) treatment in culture (PMID: 41504628). | 41504628 |
| TP53 Y220C | breast cancer | predicted - sensitive | Rezatapopt | Case Reports/Case Series | Actionable | In a Phase I trial, Rezatapopt (PC14586) treatment resulted in a partial response in a patient with breast cancer harboring TP53 Y220C (J Clin Oncol 40, no. 16_suppl (June 01, 2022) 3003); NCT04585750). | detail... |
| TP53 R175H TP53 Y220C | Advanced Solid Tumor | resistant | Rezatapopt | Preclinical - Cell culture | Actionable | In a preclinical study, cancer cell lines expressing TP53 Y220C and R175H were resistant to Rezatapopt (PC14586) treatment in culture (PMID: 41504628). | 41504628 |
| TP53 Y220C TP53 R248W | Advanced Solid Tumor | resistant | Rezatapopt | Preclinical - Cell culture | Actionable | In a preclinical study, cancer cell lines expressing TP53 Y220C and R248W were resistant to Rezatapopt (PC14586) treatment in culture (PMID: 41504628). | 41504628 |
| TP53 P152L TP53 Y220C | Advanced Solid Tumor | resistant | Rezatapopt | Preclinical - Cell culture | Actionable | In a preclinical study, cancer cell lines expressing TP53 Y220C and P152L were resistant to Rezatapopt (PC14586) treatment in culture (PMID: 41504628). | 41504628 |
| TP53 Y220C | ureter squamous cell carcinoma | predicted - sensitive | Rezatapopt | Case Reports/Case Series | Actionable | In a Phase I/II trial (PYNNACL), Rezatapopt (PC14586) treatment resulted in rapid clinical symptom improvement and radiographic stable disease lasting 6 months in a patient with metastatic squamous cell carcinoma of the ureter harboring TP53 Y220C (PMID: 41504628; NCT04585750). | 41504628 |
| TP53 F109S TP53 Y220C | Advanced Solid Tumor | resistant | Rezatapopt | Preclinical - Cell culture | Actionable | In a preclinical study, cancer cell lines expressing TP53 Y220C and F109S were resistant to Rezatapopt (PC14586) treatment in culture (PMID: 41504628). | 41504628 |
| TP53 Y220C | Advanced Solid Tumor | predicted - sensitive | Rezatapopt | Phase I | Actionable | In a Phase I trial, Rezatapopt (PC14586) treatment demonstrated safety and preliminary efficacy in patients with advanced solid tumors harboring TP53 Y220C, and resulted in 5 partial responses amongst 21 evaluable patients including confirmed partial responses in one small cell lung cancer and one breast cancer patient, and unconfirmed partial responses in one colorectal cancer and two prostate cancer patients (J Clin Oncol 40, no. 16_suppl (June 01, 2022) 3003); NCT04585750). | detail... |
| TP53 Y220C | Advanced Solid Tumor | predicted - sensitive | Rezatapopt | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Rezatapopt (PC14586) treatment reactivated Tp53 function and resulted in cell cycle arrest in cancer cell lines harboring TP53 Y220C in culture, and led to complete cure in 80% of syngeneic xenograft models (AACR Annual Meeting Apr 2021, Session MS.LBA01, Abstract # LB006). | detail... |
| TP53 Y220C | colorectal cancer | predicted - sensitive | Rezatapopt | Case Reports/Case Series | Actionable | In a Phase I trial, Rezatapopt (PC14586) treatment resulted in an unconfirmed partial response in a patient with colorectal cancer harboring TP53 Y220C (J Clin Oncol 40,no. 16_suppl (June 01, 2022) 3003); NCT04585750). | detail... |
| TP53 Y220C TP53 L265_G266del | Advanced Solid Tumor | resistant | Rezatapopt | Preclinical - Cell culture | Actionable | In a preclinical study, cancer cell lines expressing TP53 Y220C and L265_G266del were resistant to Rezatapopt (PC14586) treatment in culture (PMID: 41504628). | 41504628 |
| TP53 L145P TP53 Y220C | Advanced Solid Tumor | resistant | Rezatapopt | Preclinical - Cell culture | Actionable | In a preclinical study, cancer cell lines expressing TP53 Y220C and L145P were resistant to Rezatapopt (PC14586) treatment in culture (PMID: 41504628). | 41504628 |
| TP53 Y220C | lung small cell carcinoma | predicted - sensitive | Rezatapopt | Case Reports/Case Series | Actionable | In a Phase I trial, Rezatapopt (PC14586) treatment resulted in a partial response in a patient with small cell lung cancer harboring TP53 Y220C (J Clin Oncol 40, no. 16_suppl (June 01, 2022) 3003); NCT04585750). | detail... |
| TP53 Y220C | prostate cancer | predicted - sensitive | Rezatapopt | Case Reports/Case Series | Actionable | In a Phase I trial, Rezatapopt (PC14586) treatment resulted in unconfirmed partial responses in two patients with prostate cancer harboring TP53 Y220C (J Clin Oncol 40, no. 16_suppl (June 01, 2022) 3003); NCT04585750). | detail... |
| TP53 Y220C | head and neck carcinoma | predicted - sensitive | Rezatapopt | Case Reports/Case Series | Actionable | In a Phase I/II trial (PYNNACL), Rezatapopt (PC14586) treatment resulted in a confirmed radiographic partial response lasting 5 months in a patient with metastatic HPV-negative head and neck carcinoma harboring TP53 Y220C (PMID: 41504628; NCT04585750). | 41504628 |
| TP53 P151A TP53 Y220C | Advanced Solid Tumor | resistant | Rezatapopt | Preclinical - Cell culture | Actionable | In a preclinical study, cancer cell lines expressing TP53 Y220C and P151A were resistant to Rezatapopt (PC14586) treatment in culture (PMID: 41504628). | 41504628 |
| TP53 V147L TP53 Y220C | Advanced Solid Tumor | resistant | Rezatapopt | Preclinical - Cell culture | Actionable | In a preclinical study, cancer cell lines expressing TP53 Y220C and V147L were resistant to Rezatapopt (PC14586) treatment in culture (PMID: 41504628). | 41504628 |
| TP53 Y220C | stomach cancer | predicted - sensitive | Rezatapopt | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Rezatapopt (PC14586) treatment reactivated Tp53 function, resulted in 80% tumor regression after 3 weeks in cell line xenograft models of gastric cancer harboring TP53 Y220C (AACR Annual Meeting Apr 2021, Session MS.LBA01, Abstract # LB006). | detail... |
Filtering
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- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
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- Click on any column header arrows to sort by that column
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT04585750 | Phase Ib/II | Pembrolizumab + Rezatapopt Rezatapopt | The Evaluation of PC14586 in Patients With Advanced Solid Tumors Harboring a TP53 Y220C Mutation (PYNNACLE) | Recruiting | USA | ITA | GBR | FRA | ESP | DEU | AUS | 2 |
| NCT07372625 | Phase I | Rezatapopt | A Study to Investigate the Effects of Multiple Doses of Rezatapopt on the Pharmacokinetics of Metformin, Rosuvastatin, Repaglinide, and Midazolam in Patients With Advanced Solid Tumors Harboring a TP53 Y220C Mutation. | Recruiting | USA | 0 |
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