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Therapy Detail
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| Therapy Name | MRK-003 |
| Synonyms | |
| Therapy Description |
MRK-003 is a gamma-secretase inhibitor which inhibits Notch3 signaling and induces apoptosis in cancer cells (PMID: 17804716, PMID: 23887890). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| MRK-003 | Gamma secretase inhibitor 13 | MRK-003 is a gamma-secretase inhibitor which inhibits Notch3 signaling and induces apoptosis in cancer cells (PMID: 17804716, PMID: 23887890). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| FBXW7 R465H | T-cell adult acute lymphocytic leukemia | resistant | MRK-003 | Preclinical | Actionable | In a preclinical study, FBXW7 R465H conferred resistance to gamma secretase inhibitor, MRK-003, by activation of the NOTCH pathway and stablization of MYC as demonstrated in T cell acute lymphoblastic leukemia (T-ALL) cell lines (PMID: 17646409). | 17646409 |
| FBXW7 del | T-cell adult acute lymphocytic leukemia | resistant | MRK-003 | Preclinical | Actionable | In a preclinical study, homozygous deletion of FBXW7 is conferred resistance to gamma secretase inhibitor, MRK-003, by activation of the NOTCH pathway and stablization of MYC as demonstrated in T cell acute lymphoblastic leukemia (T-ALL) cell lines (PMID: 17646409). | 17646409 |
| FBXW7 R479Q | T-cell adult acute lymphocytic leukemia | resistant | MRK-003 | Preclinical | Actionable | In a preclinical study, FBXW7 R479Q conferred resistance to gamma secretase inhibitor, MRK-003, by activation of the NOTCH pathway and stablization of MYC as demonstrated in T cell acute lymphoblastic leukemia (T-ALL) cell lines (PMID: 17646409). | 17646409 |
| FBXW7 R465C | T-cell adult acute lymphocytic leukemia | resistant | MRK-003 | Preclinical | Actionable | In a preclinical study, FBXW7 R465C conferred resistance to gamma secretase inhibitor, MRK-003, by activation of the NOTCH pathway and stablization of MYC as demonstrated in T cell acute lymphoblastic leukemia (T-ALL) cell lines (PMID: 17646409). | 17646409 |
| FBXW7 R505L | T-cell adult acute lymphocytic leukemia | resistant | MRK-003 | Preclinical | Actionable | In a preclinical study, FBXW7 R505L may conferred resistance to gamma secretase inhibitor, MRK-003, by activation of the NOTCH pathway and stablization of MYC as demonstrated in T cell acute lymphoblastic leukemia (T-ALL) cell lines (PMID: 17646409). | 17646409 |
| FBXW7 R505C | T-cell adult acute lymphocytic leukemia | resistant | MRK-003 | Preclinical | Actionable | In a preclinical study, FBXW7 R505C conferred resistance to gamma secretase inhibitor, MRK-003, by activation of the NOTCH pathway and stablization of MYC as demonstrated in T cell acute lymphoblastic leukemia (T-ALL) cell lines (PMID: 17646409). | 17646409 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
CKB BOOST