danusertib

03/01/2015 - "Danusertib did not meet pre-specified protocol criteria for clinically relevant activity in any of the treated cancers. "
06/21/2012 - "PHA-739358 inhibited proliferation and induced apoptosis independently of Bcr/Abl, the T315I mutation, or presence of the tumor suppressor p53, but the degree of effectiveness varied between different ALL samples. "
02/25/2012 - "To characterize the effects of Danusertib at the transcriptional level we carried out gene expression profiling of wt and TP53 mutant tumor cells showing differential cell cycle response upon drug treatment. "
09/01/2009 - "In vivo, administration of PHA-739358 resulted in significant tumor growth inhibition at a well-tolerated dose. "
12/01/2007 - "We conclude that PHA-739358, which is currently tested in clinical trials, has great therapeutic potential in anticancer therapy in a wide range of cancers."

01/01/2020 - "These findings suggest a novel strategy to enhance the anticancer efficacy of danusertib in melanoma by blocking autophagy."
01/01/2020 - "In this study, we investigated the role of danusertib on the induction of autophagy in melanoma and determined the impact of autophagy induction on its anticancer activity against melanoma. "
04/01/2013 - "In this study, the antiproliferative and anti-invasive effects of PHA-739358 were investigated in melanoma cell lines. "
04/01/2013 - "PHA-739358 is currently one of the most advanced clinical compounds being tested in phase II clinical trials; however, its antitumor effect has not been tested in melanoma. "
01/01/2020 - "Thus, the induction of autophagy by danusertib appears to be a survival mechanism in melanoma cells that may counteract its anticancer effects. "

01/01/2010 - "Therefore, combined Aurora and Bcr-Abl inhibition (the latter including high-grade resistance conferring mutations) with compounds such as Danusertib represents a promising new strategy for treatment of Bcr-Abl positive leukemias, especially those in second and third line of treatment."
04/15/2008 - "Thus, PHA-739358 represents a promising new strategy for treatment of IM-resistant BCR-ABL-positive leukemias, including those harboring the T315I mutation. "
04/15/2008 - "Pharmacologic synergism of IM and PHA-739358 was observed in leukemia cell lines with subtotal resistance to IM. "
03/01/2012 - "As a single agent, danusertib may show more promise in the treatment of leukemias than in solid tumors."
11/28/2016 - "Danusertib (Danu) is a pan-inhibitor of Aurora kinases with few data available in leukemia therapy. "

01/01/2013 - "Danusertib was generally well tolerated; the most common grade 3 and 4 drug-related adverse event was neutropenia which occurred in 37.2% (arm A) and 15.8% (arm B) of the patients. "
10/20/2009 - "Dose-limiting toxicity of danusertib is neutropenia, which was short lasting and generally uncomplicated; danusertib administration had limited nonhematologic toxicity. "
10/01/2011 - "Association analyses between neutropenia and drug target receptors, including KDR, RET, FLT3, FLT4, AURKB and AURKA, were performed in 30 patients treated at recommended phase II dose-levels in three danusertib phase I or phase II trials. "

07/01/2015 - "A phase 1 dose escalation study of danusertib was conducted in patients with accelerated or blastic phase chronic myeloid leukemia or Philadelphia chromosome-positive acute lymphoblastic leukemia. "
07/01/2015 - "A phase I study of danusertib (PHA-739358) in adult patients with accelerated or blastic phase chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia resistant or intolerant to imatinib and/or other second generation c-ABL therapy."
06/21/2012 - "Treatment of human pre-B acute lymphoblastic leukemia with the Aurora kinase inhibitor PHA-739358 (Danusertib)."