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Therapy Name | LY3214996 |
Synonyms | |
Therapy Description |
LY3214996 inhibits ERK1/2, potentially resulting in decreased growth of tumors with alterations in the RAS/MAPK pathway (AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 4973, PMID: 31744895). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
LY3214996 | Temuterkib|LY-3214996|LY 3214996 | ERK Inhibitor (pan) 21 | LY3214996 inhibits ERK1/2, potentially resulting in decreased growth of tumors with alterations in the RAS/MAPK pathway (AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 4973, PMID: 31744895). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
BRAF L597V | lung adenocarcinoma | resistant | LY3214996 | Preclinical - Patient cell culture | Actionable | In a preclinical study, cells derived from a lung adenocarcinoma patient harboring BRAF L597V were resistant to treatment with LY3214996 in culture (PMID: 32540409). | 32540409 |
BRAF T119S BRAF V600E | colorectal cancer | predicted - sensitive | LY3214996 | Preclinical - Cell culture | Actionable | In a preclinical study, a colorectal cancer cell line harboring BRAF V600E and BRAF T119S was sensitive to treatment with LY3214996 in culture, demonstrating decreased cell proliferation (PMID: 31744895). | 31744895 |
BRAF L597Q FGFR2 H167_N173del FGFR2 N550K FGFR2 L618F NRAS Q61K | intrahepatic cholangiocarcinoma | predicted - resistant | LY3214996 | Case Reports/Case Series | Actionable | In a clinical case study, acquired NRAS Q61K and FGFR2 N550K mutations were identified following progression on LY3214996 in an intrahepatic cholangiocarcinoma patient harboring BRAF L597Q, FGFR2 H167_N173del, and FGFR2 L618F (PMID: 33926920). | 33926920 |
NRAS Q61K | lung carcinoma | sensitive | LY3214996 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, patient-derived lung carcinoma cells harboring NRAS Q61K were sensitive to LY3214996 treatment in culture, and LY3214996 treatment led to reduction of tumor growth in a patient-derived xenograft (PDX) model (PMID: 33536188). | 33536188 |
BRAF G469A | lung adenocarcinoma | resistant | LY3214996 | Preclinical - Patient cell culture | Actionable | In a preclinical study, cells derived from a lung adenocarcinoma patient harboring BRAF G469A were resistant to treatment with LY3214996 in culture (PMID: 32540409). | 32540409 |
BRAF L597Q FGFR2 H167_N173del FGFR2 L618F | intrahepatic cholangiocarcinoma | no benefit | LY3214996 | Case Reports/Case Series | Actionable | In a clinical case study, LY3214996 treatment led to progressive disease after 2 months in an intrahepatic cholangiocarcinoma patient harboring BRAF L597Q, FGFR2 H167_N173del, and FGFR2 L618F (PMID: 33926920). | 33926920 |
BRAF V600E | colorectal cancer | predicted - sensitive | LY3214996 | Preclinical - Cell culture | Actionable | In a preclinical study, a lung cancer cell line harboring BRAF V600E and NF1 T2805I was sensitive to treatment with LY3214996 in culture, demonstrating decreased cell viability (PMID: 31744895). | 31744895 |
NRAS Q61L | melanoma | predicted - sensitive | LY3214996 | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring NRAS Q61L was sensitive to treatment with LY3214996 in culture, demonstrating decreased cell proliferation (PMID: 31744895). | 31744895 |
BRAF V600E | melanoma | sensitive | LY3214996 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, LY3214996 treatment in a melanoma cell line harboring BRAF V600E led to decreased cell proliferation in culture, and inhibition of tumor growth in a cell line xenograft model (PMID: 31744895). | 31744895 |
MAP2K1 Q56P | lung cancer | predicted - sensitive | LY3214996 | Preclinical - Cell culture | Actionable | In a preclinical study, a lung cancer cell line harboring MAP2K1 Q56P was sensitive to treatment with LY3214996 in culture, demonstrating decreased cell proliferation (PMID: 31744895). | 31744895 |
MAP2K1 Q56P MAP2K1 H119Y MAP2K1 D351G | colorectal cancer | predicted - sensitive | LY3214996 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, LY3214996 treatment in a colorectal cancer cell line harboring MAP2K1 Q56P, MAP2K1 H119Y, and MAP2K1 D351G led to decreased cell proliferation in culture, and inhibition of tumor growth in a cell line xenograft model (PMID: 31744895). | 31744895 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT04081259 | Phase I | LY3214996 | LY3214996 in Patients With AML Who Are Not Candidates for Standard Therapy | Recruiting | USA | 0 |
NCT04386057 | Phase II | Hydroxychloroquine + LY3214996 LY3214996 | LY3214996 +/- HCQ in Pancreatic Cancer | Completed | USA | 0 |
NCT02857270 | Phase I | LY3214996 Gemcitabine + LY3214996 + Nab-paclitaxel LY3214996 + Midazolam Abemaciclib + LY3214996 | A Study of LY3214996 Administered Alone or in Combination With Other Agents in Participants With Advanced/Metastatic Cancer | Completed | USA | FRA | AUS | 1 |