Missing content? – Request curation!
Request curation for specific Genes, variants, or PubMed publications.
Have questions, comments or suggestions? - Let us know!
Email us at : ckbsupport@jax.org
Therapy Name | LY3039478 |
Synonyms | |
Therapy Description |
LY3039478 is a pan-NOTCH inhibitor, which may limit growth and survival of cancer cells (Cancer Res April 15, 2013 73; 1131). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
LY3039478 | Crenigacestat|LY-3039478 | NOTCH Inhibitor (Pan) 5 | Crenigacestat (LY3039478) is a pan-NOTCH inhibitor, which may limit growth and survival of cancer cells (Cancer Res April 15, 2013 73; 1131, PMID: 32042099). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
NOTCH1 positive | stomach cancer | sensitive | LY3039478 | Preclinical | Actionable | In a preclinical study, LY3039478 inhibited Notch1 cleavage and downstream gene expression, demonstrated anti-tumor activity in xenograft models of gastric cancer (AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 1131). | detail... |
Unknown unknown | Advanced Solid Tumor | not applicable | LY3039478 | Phase I | Actionable | In a Phase I trial, LY3039478 treatment resulted in 80% inhibition of plasma A-beta and more than 50% inhibition of Notch1-regulated genes in patients with advanced solid tumor, leading to partial response in 0.9% (1/110) and stable disease in 32.7% (36/110) of the patients (PMID: 30060061; NCT01695005). | 30060061 detail... |
Unknown unknown | Advanced Solid Tumor | not applicable | LY3039478 | Phase I | Actionable | In a Phase I trial, treatment with LY3039478 was well-tolerated and demonstrated some preliminary efficacy in patients with advanced solid tumors (J Clin Oncol 33, 2015 (suppl; abstr 2533)). | detail... |
NOTCH1 positive | lung cancer | sensitive | LY3039478 | Preclinical | Actionable | In a preclinical study, LY3039478 inhibited Notch1 cleavage and downstream gene expression, demonstrated anti-tumor activity in xenograft models of lung cancer (AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 1131). | detail... |
Unknown unknown | leiomyosarcoma | not applicable | LY3039478 | Phase I | Actionable | In a Phase I trial, treatment with LY3039478 resulted in tumor necrosis in a patient with leiomyosarcoma (European Journal of Cancer, Volume 69, S15). | detail... |
FBXW7 mutant | Her2-receptor negative breast cancer | predicted - sensitive | LY3039478 | Phase I | Actionable | In a Phase I trial, LY3039478 treatment resulted in partial response lasted 9.5 months in a patient with hormone receptor-positive, Erbb2 (Her2)-negative breast cancer harboring FBXW7 mutation (PMID: 30060061; NCT01695005). | 30060061 |
Unknown unknown | testicular cancer | not applicable | LY3039478 | Phase I | Actionable | In a Phase I trial, a patient with testicular cancer demonstrated a metabolic response when treated with LY3039478 (European Journal of Cancer, Volume 69, S15). | detail... |
NOTCH1 positive | breast cancer | sensitive | LY3039478 | Preclinical | Actionable | In a preclinical study, LY3039478 inhibited Notch1 cleavage and downstream gene expression, demonstrated anti-tumor activity in xenograft models of breast cancer (AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 1131). | detail... |
NOTCH1 positive | glioblastoma | sensitive | LY3039478 | Preclinical | Actionable | In a preclinical study, LY3039478 inhibited Notch1 cleavage and downstream gene expression, demonstrated anti-tumor activity in xenograft models of glioblastoma (AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 1131). | detail... |
Unknown unknown | adenoid cystic carcinoma | not applicable | LY3039478 | Phase I | Actionable | In a Phase I trial, a patient with adenoid cystic carcinoma demonstrated a metabolic response when treated with LY3039478 (European Journal of Cancer, Volume 69, S15). | detail... |
NOTCH1 positive | colon cancer | sensitive | LY3039478 | Preclinical | Actionable | In a preclinical study, LY3039478 inhibited Notch1 cleavage and downstream gene expression, demonstrated anti-tumor activity in xenograft models of colon cancer (AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 1131). | detail... |
NOTCH1 positive | ovarian cancer | sensitive | LY3039478 | Preclinical | Actionable | In a preclinical study, LY3039478 inhibited Notch1 cleavage and downstream gene expression, demonstrated anti-tumor activity in xenograft models of ovarian cancer (AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 1131). | detail... |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT01695005 | Phase I | LY3039478 | A Study of LY3039478 in Participants With Advanced Cancer | Completed | USA | 5 |
NCT02784795 | Phase I | Cisplatin + Gemcitabine + LY3039478 Carboplatin + Gemcitabine + LY3039478 LY3023414 + LY3039478 Abemaciclib + LY3039478 LY3039478 + Taladegib LY3039478 LY3023414 | A Study of LY3039478 in Participants With Advanced or Metastatic Solid Tumors | Completed | USA | 3 |
NCT02518113 | Phase Ib/II | Dexamethasone LY3039478 | A Study of LY3039478 in Combination With Dexamethasone in Participants With T-ALL/T-LBL | Completed | USA | 4 |