Therapy Detail
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| Therapy Name | U0126 |
| Synonyms | |
| Therapy Description |
U0126 binds and inhibits Mek1 and Mek2, which may inhibit the activation of downstream signaling targets and reduce tumor cell proliferation (PMID: 9873633). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| U0126 | MEK inhibitor (Pan) 27 MEK1 Inhibitor 27 MEK2 Inhibitor 25 | U0126 binds and inhibits Mek1 and Mek2, which may inhibit the activation of downstream signaling targets and reduce tumor cell proliferation (PMID: 9873633). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF V600E | melanoma | predicted - sensitive | U0126 | Preclinical - Cell culture | Actionable | In a preclinical study, U0126 treatment inhibited Erk phosphorylation and reduced growth of melanoma cells harboring BRAF V600E in culture (PMID: 18794803). | 18794803 |
| BRAF G469E | melanoma | resistant | U0126 | Preclinical - Cell culture | Actionable | In a preclinical study, melanoma cells harboring BRAF G469E demonstrated resistance to U0126 treatment in culture (PMID: 18794803). | 18794803 |
| BRAF T529N BRAF V600E | melanoma | sensitive | U0126 | Preclinical - Cell culture | Actionable | In a preclinical study, U0126 inhibited Erk phosphorylation and downstream signaling and viability in a melanoma cell line harboring BRAF V600E and expressing BRAF T529N in culture (PMID: 24112705). | 24112705 |
| BRAF F516G BRAF V600E | melanoma | sensitive | U0126 | Preclinical - Cell culture | Actionable | In a preclinical study, U0126 inhibited Erk phosphorylation and downstream signaling and viability in a melanoma cell line harboring BRAF V600E and expressing BRAF F516G in culture (PMID: 24112705). | 24112705 |
| BRAF L505H BRAF V600E | melanoma | resistant | U0126 | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing L505H was resistant to U0126 treatment in culture (PMID: 24112705). | 24112705 |
| FGFR3 over exp | glioblastoma | sensitive | U0126 | Preclinical | Actionable | In a preclinical study, U0126 inhibited downstream signaling and growth of glioblastoma cells over-expressing Fgfr3 in culture (PMID: 23298836). | 23298836 |
| MAP2K1 L98_K104delinsQ | Advanced Solid Tumor | resistant | U0126 | Preclinical - Cell culture | Actionable | In a preclinical study, U0126 treatment failed to inhibit activation of Mek and Erk in human cells expressing MAP2K1 L98_K104delinsQ in culture (PMID: 29768711). | 29768711 |
| BRAF K601E | melanoma | predicted - sensitive | U0126 | Preclinical - Cell culture | Actionable | In a preclinical study, U0126 treatment inhibited growth of melanoma cells harboring BRAF K601E in culture (PMID: 18794803). | 18794803 |
| BRAF D594G | melanoma | resistant | U0126 | Preclinical - Cell culture | Actionable | In a preclinical study, melanoma cells harboring BRAF D594G demonstrated resistance to U0126 treatment in culture (PMID: 18794803). | 18794803 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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