Therapy Detail
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| Therapy Name | Nutlin-3a |
| Synonyms | |
| Therapy Description |
Nutlin-3a is an MDM2 inhibitor that activates p53, potentially resulting in induction of apoptosis and senescence in tumor cells (PMID: 18451145, PMID: 32653500). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Nutlin-3a | Nutlin|Nutlin-3 | MDM2 Inhibitor 23 | Nutlin-3a is an MDM2 inhibitor that activates p53, potentially resulting in induction of apoptosis and senescence in tumor cells (PMID: 18451145, PMID: 32653500). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| TP53 mutant | neuroblastoma | resistant | Nutlin-3a | Preclinical | Actionable | In a preclinical study, neuroblastoma cell lines harboring TP53 mutant were resistant to nutlin-3 mediated growth inhibition (PMID: 21725357). | 21725357 |
| TP53 R280M | osteosarcoma | resistant | Nutlin-3a | Preclinical | Actionable | In a preclinical study, TP53 R280M resulted in secondary resistance in an osteosarcoma cell line acquired during Nutlin-3 treatment (PMID: 21643018). | 21643018 |
| MDM2 L82P | Advanced Solid Tumor | predicted - resistant | Nutlin-3a | Preclinical - Biochemical | Actionable | In a preclinical study, MDM2 L82P conferred resistance to Nutlin-3a as demonstrated by decreased restoration of Tp53 activity in reporter assays in culture, and impaired inhibition of Mdm2-Tp53 interaction in in vitro assays (PMID: 23653682). | 23653682 |
| MDM2 M62A | Advanced Solid Tumor | predicted - resistant | Nutlin-3a | Preclinical - Biochemical | Actionable | In a preclinical study, MDM2 M62A conferred resistance to Nutlin-3a as demonstrated by decreased restoration of Tp53 activity in reporter assays in culture, and impaired inhibition of Mdm2-Tp53 interaction in in vitro assays (PMID: 23653682). | 23653682 |
| MDM2 M62A | Advanced Solid Tumor | predicted - resistant | Nutlin-3a | Preclinical - Biochemical | Actionable | In a preclinical study, MDM2 M62A conferred resistance to Nutlin-3a as demonstrated by decreased restoration of Tp53 activity in a reporter assay and decreased inhibition of the Mdm2-Tp53 interaction in culture (PMID: 24278380). | 24278380 |
| TP53 E258Q | osteosarcoma | resistant | Nutlin-3a | Preclinical | Actionable | In a preclinical study, TP53 E258Q resulted in secondary resistance in an osteosarcoma cell line acquired during Nutlin-3 treatment (PMID: 21643018). | 21643018 |
| TP53 mutant | ovarian cancer | no benefit | Nutlin-3a | Preclinical | Actionable | In a preclinical study, treatment with Nutlin-3 had little effect on growth of ovarian cancer cells with TP53 mutations in culture (PMID: 25964101). | 25964101 |
| TP53 R181E | Advanced Solid Tumor | no benefit | Nutlin-3a | Preclinical - Cell culture | Actionable | In a preclinical study, Nutlin-3 treatment did not reduce cell proliferation and viability in transformed mouse cells expressing TP53 R181E in culture (PMID: 31483066). | 31483066 |
| TP53 I232S | osteosarcoma | resistant | Nutlin-3a | Preclinical | Actionable | In a preclinical study, TP53 I232S resulted in secondary resistance in an osteosarcoma cell line acquired during Nutlin-3 treatment (PMID: 21643018). | 21643018 |
| TP53 P177T | osteosarcoma | resistant | Nutlin-3a | Preclinical | Actionable | In a preclinical study, TP53 P177T resulted in secondary resistance in an osteosarcoma cell line acquired during Nutlin-3 treatment (PMID: 21643018). | 21643018 |
| MDM2 Q24R | Advanced Solid Tumor | predicted - resistant | Nutlin-3a | Preclinical - Biochemical | Actionable | In a preclinical study, MDM2 Q24R conferred resistance to Nutlin-3a as demonstrated by decreased restoration of Tp53 activity in a reporter assay and decreased inhibition of the Mdm2-Tp53 interaction in culture (PMID: 24278380). | 24278380 |
| MDM2 Q24R | Advanced Solid Tumor | predicted - resistant | Nutlin-3a | Preclinical - Biochemical | Actionable | In a preclinical study, MDM2 Q24R conferred moderate resistance to Nutlin-3a as demonstrated by decreased restoration of Tp53 activity in reporter assays in culture, and impaired inhibition of Mdm2-Tp53 interaction in in vitro assays (PMID: 23653682). | 23653682 |
| MDM2 M62V | Advanced Solid Tumor | predicted - resistant | Nutlin-3a | Preclinical - Biochemical | Actionable | In a preclinical study, MDM2 M62V conferred partial resistance to Nutlin-3a as demonstrated by decreased restoration of Tp53 activity in reporter assays in culture, and impaired inhibition of Mdm2-Tp53 interaction in in vitro assays (PMID: 23653682). | 23653682 |
| RB1 inact mut | retinoblastoma | sensitive | Nutlin-3a | Preclinical | Actionable | In a preclinical study, Nutlin-3a induced p53 pathway signaling in MDMX mouse models with retinoblastoma and 69% (70/102) of the eyes harvested from the mouse models demonstrated complete response or stable disease after 18 weeks of therapy (PMID: 21515735). | 21515735 |
| TP53 del | ovarian cancer | no benefit | Nutlin-3a | Preclinical | Actionable | In a preclinical study, treatment with Nutlin-3 had little effect on growth of ovarian cancer cells with deletion of TP53 in culture (PMID: 25964101). | 25964101 |
| MDM2 C308Y | Advanced Solid Tumor | predicted - resistant | Nutlin-3a | Preclinical - Biochemical | Actionable | In a preclinical study, MDM2 C308Y conferred moderate resistance to Nutlin-3a as demonstrated by decreased restoration of Tp53 activity in reporter assays in culture (PMID: 23653682). | 23653682 |
| MDM2 T16A | Advanced Solid Tumor | predicted - resistant | Nutlin-3a | Preclinical - Biochemical | Actionable | In a preclinical study, MDM2 T16A conferred moderate resistance to Nutlin-3a as demonstrated by decreased restoration of Tp53 activity in reporter assays in culture, and impaired inhibition of Mdm2-Tp53 interaction in in vitro assays (PMID: 23653682). | 23653682 |
| MDM2 P20L | Advanced Solid Tumor | predicted - resistant | Nutlin-3a | Preclinical - Biochemical | Actionable | In a preclinical study, MDM2 P20L conferred moderate resistance to Nutlin-3a as demonstrated by decreased restoration of Tp53 activity in reporter assays in culture, and impaired inhibition of Mdm2-Tp53 interaction in in vitro assays (PMID: 23653682). | 23653682 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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