Therapy Detail
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| Therapy Name | LY3009120 |
| Synonyms | |
| Therapy Description |
LY3009120 is a Pan-RAF inhibitor that inhibits signaling of all RAF isoforms and RAF dimers, which leads to inhibition of tumor cell growth (PMID: 26343583, PMID: 28576749). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| LY3009120 | DP-4978 | RAF Inhibitor (Pan) 27 | LY3009120 is a Pan-RAF inhibitor that inhibits signaling of all RAF isoforms and RAF dimers, which leads to inhibition of tumor cell growth (PMID: 26343583, PMID: 28576749). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF V504_R506dup | Advanced Solid Tumor | predicted - resistant | LY3009120 | Preclinical - Biochemical | Actionable | In a preclinical study, cells expressing BRAF V504_R506dup were resistant to treatment with LY3009120 in culture (PMID: 34108213). | 34108213 |
| BRAF V487_P492delinsA | pancreatic cancer | sensitive | LY3009120 | Preclinical | Actionable | In a preclinical study, a pancreatic cancer cell line harboring BRAF V487_P492delinsA were sensitive to LY3009120 in culture and in xenograft models, resulting in inhibition of tumor growth and partial tumor regression (PMID: 26732095). | 26732095 |
| TP53 D259Y | melanoma | sensitive | LY3009120 | Preclinical | Actionable | In a preclinical study, LY3009120 modestly inhibited soft agar growth of human melanoma cancer cells harboring TP53 D259Y in culture (PMID: 26343583). | 26343583 |
| BRAF V600E | high grade glioma | predicted - sensitive | LY3009120 | Preclinical - Patient cell culture | Actionable | In a preclinical study, LY3009120 treatment led to inhibition of cell viability and growth in a patient-derived glioma cell line harboring BRAF V600E in culture (PMID: 34433654). | 34433654 |
| NRAS Q61R | melanoma | predicted - sensitive | LY3009120 | Preclinical - Cell culture | Actionable | In a preclinical study, LY3009120 treatment inhibited Erk activation and reduced proliferation of melanoma cells harboring NRAS Q61R and wild-type RAF in culture (PMID: 30559419). | 30559419 |
| BRAF L505H | Advanced Solid Tumor | predicted - resistant | LY3009120 | Preclinical - Biochemical | Actionable | In a preclinical study, cells expressing BRAF L505H were resistant to treatment with LY3009120 in culture (PMID: 34108213). | 34108213 |
| NRAS Q61L | melanoma | decreased response | LY3009120 | Preclinical | Actionable | In a preclinical study, LY3009120 modestly inhibited soft agar growth of human melanoma cancer cells harboring NRAS Q61L in culture (PMID: 26343583). | 26343583 |
| MAP2K1 E41_L54del | lung cancer | no benefit | LY3009120 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed human lung cells expressing MAP2K1 E41_L54del were not sensitive to LY3009120 in culture (PMID: 32122926). | 32122926 |
| BRAF L485F | Advanced Solid Tumor | predicted - sensitive | LY3009120 | Preclinical - Biochemical | Actionable | In a preclinical study, LY3009120 treatment inhibited Erk signaling in cells expressing BRAF L485F in culture (PMID: 34108213). | 34108213 |
| BRAF L597S | melanoma | sensitive | LY3009120 | Preclinical - Cell culture | Actionable | In a preclinical study, LY3009120 inhibited growth of melanoma cells harboring BRAF L597S in culture (PMID: 29903896). | 29903896 |
| BRAF V600E | melanoma | sensitive | LY3009120 | Preclinical - Cell culture | Actionable | In a preclinical study, LY3009120 treatment inhibited Erk phosphorylation and reduced proliferation of a melanoma cells harboring either monomeric BRAF V600E or dimeric isoform (p61) of V600E in culture (PMID: 30559419). | 30559419 |
| BRAF V600E | melanoma | sensitive | LY3009120 | Preclinical | Actionable | In a preclinical study, LY3009120 inhibited growth, downstream MAPK signaling and soft agar growth in human melanoma cell lines harboring BRAF V600E in culture (PMID: 26343583). | 26343583 |
| BRAF L485_P490del | Advanced Solid Tumor | predicted - sensitive | LY3009120 | Preclinical - Cell culture | Actionable | In a preclinical study, LY3009120 inhibited phosphorylation of Mek and Erk in transformed cells expressing BRAF L485_P490del in culture (PMID: 26732095). | 26732095 |
| NRAS mutant | Advanced Solid Tumor | no benefit | LY3009120 | Case Reports/Case Series | Actionable | In a Phase I trial, LY3009120 did not achieve expected pharmacodynamic effects, resulted in stable disease as best overall response in 1 of 5 patients with advanced or metastatic cancer harboring NRAS mutations (PMID: 31645440; NCT02014116). | 31645440 |
| NRAS G13D | melanoma | sensitive | LY3009120 | Preclinical | Actionable | In a preclinical study, LY3009120 inhibited soft agar growth of human melanoma cancer cells harboring NRAS G13D in culture (PMID: 26343583). | 26343583 |
| NRAS mutant | melanoma | sensitive | LY3009120 | Preclinical | Actionable | In a preclinical study, LY3009120 inhibited growth of NRAS mutant human melanoma cell lines in culture (PMID: 26343583). | 26343583 |
| BRAF mutant | Advanced Solid Tumor | no benefit | LY3009120 | Case Reports/Case Series | Actionable | In a Phase I trial, LY3009120 did not achieve expected pharmacodynamic effects, resulted in stable disease as best overall response in 5 of 12 patients with advanced or metastatic cancer harboring BRAF mutations (PMID: 31645440; NCT02014116). | 31645440 |
| BRAF K601N | hematologic cancer | sensitive | LY3009120 | Preclinical - Cell culture | Actionable | In a preclinical study, a hematological tumor cell line harboring BRAF K601N demonstrated sensitivity to LY3009120 in culture (PMID: 26732095). | 26732095 |
| BRAF G469R NRAS Q61K | melanoma | sensitive | LY3009120 | Preclinical | Actionable | In a preclinical study, LY3009120 inhibited soft agar growth of human melanoma cancer cells harboring BRAF G469R and NRAS Q61K in culture (PMID: 26343583). | 26343583 |
| BRAF G469V NRAS Q61K | melanoma | sensitive | LY3009120 | Preclinical - Cell culture | Actionable | In a preclinical study, LY3009120 inhibited growth of a melanoma cell line harboring BRAF G469V and NRAS Q61K in culture (PMID: 29903896). | 29903896 |
| BRAF R506_K507insLLR | Advanced Solid Tumor | predicted - resistant | LY3009120 | Preclinical - Biochemical | Actionable | In a preclinical study, cells expressing BRAF R506_K507insLLR were resistant to treatment with LY3009120 in culture (PMID: 34108213). | 34108213 |
| BRAF N486_P490del | ovarian cancer | sensitive | LY3009120 | Preclinical | Actionable | In a preclinical study, an ovarian cancer cell line harboring BRAF N486_P490del was sensitive to LY3009120, resulting in inhibition of cell growth and decreased phosphorylation of MEK and ERK in culture (PMID: 26732095). | 26732095 |
| NRAS mutant | acute myeloid leukemia | sensitive | LY3009120 | Preclinical | Actionable | In a preclinical study, LY3009120 inhibited proliferation of human NRAS mutant acute myeloid leukemia cell lines in culture (PMID: 26343583). | 26343583 |
| MAP2K1 E41_L54del | Advanced Solid Tumor | no benefit | LY3009120 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing MAP2K1 E41_L54del were not sensitive to LY3009120 in culture (PMID: 32122926). | 32122926 |
| BRAF N486_P490del | pancreatic ductal adenocarcinoma | predicted - sensitive | LY3009120 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, a patient-derived xenograft (PDX) model with pancreatic ductal adenocarcinoma harboring BRAF N486_P490del demonstrated partial inhibition of Erk phosphorylation and moderate inhibition of tumor growth when treated with LY3009120 (PMID: 34011980). | 34011980 |
| NRAS Q61K | melanoma | sensitive | LY3009120 | Preclinical | Actionable | In a preclinical study, LY3009120 inhibited soft agar growth of human melanoma cancer cells harboring NRAS Q61K in culture (PMID: 26343583). | 26343583 |
| BRAF L485_P490delinsY | lung non-small cell carcinoma | sensitive | LY3009120 | Preclinical | Actionable | In a preclinical study, a non-small cell lung carcinoma cell line harboring BRAF L485_P490delinsY was sensitive to LY3009120 in both culture and xenograft models, resulting in significant tumor regression and inhibition of MEK and ERK phosphorylation (PMID: 26732095). | 26732095 |
Filtering
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- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
Sorting
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- Click on any column header arrows to sort by that column
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT02014116 | Phase I | LY3009120 | A Study of LY3009120 in Participants With Advanced Cancer or Cancer That Has Spread to Other Parts of Their Body | Terminated | USA | FRA | ESP | AUS | 0 |
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