Therapy Detail
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| Therapy Name | PC14586 |
| 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 |
|---|---|---|---|---|
| PC14586 | PC 14586|PC-14586|Rezatapopt | p53 Activator 11 | 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). |
Filtering
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- Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
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- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| TP53 Y220C | lung small cell carcinoma | predicted - sensitive | PC14586 | Case Reports/Case Series | Actionable | In a Phase I trial, 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 | stomach cancer | predicted - sensitive | PC14586 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, 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... |
| TP53 Y220C | prostate cancer | predicted - sensitive | PC14586 | Case Reports/Case Series | Actionable | In a Phase I trial, 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 | breast cancer | predicted - sensitive | PC14586 | Case Reports/Case Series | Actionable | In a Phase I trial, 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 Y220C | Advanced Solid Tumor | predicted - sensitive | PC14586 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, 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 | Advanced Solid Tumor | predicted - sensitive | PC14586 | Phase I | Actionable | In a Phase I trial, 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 | colorectal cancer | predicted - sensitive | PC14586 | Case Reports/Case Series | Actionable | In a Phase I trial, 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... |
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- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT04585750 | Phase Ib/II | PC14586 + Pembrolizumab PC14586 | 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 |
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