<unk>  was filed as Investigational New Drug (IND) number 76431. Initial Phase I studies with<unk>  involved determination of pharmacokinetic parameters following a single dose in healthy volunteers. Next, safety and tolerability were investigated in a Phase I trial involving 30 volunteers with advanced solid tumors or lymphoma. Although there were no notable tumor responses, a strong correlation was noted between dose and adverse events, with the primary adverse event reported being gastrointestinal reaction. A Phase II study in 18 patients with pancreatic cancer was initiated for combination treatment with<unk>  and gemcitabine, but efficacy of<unk>  was not observed. In 2004, a Phase I/II study involved 17 patients at 2 locations with relapsed, refractory poor-risk AML with FLT3 mutations; this study demonstrated effective FLT3 inhibition by<unk> . A multi-center Phase II study of 29 patients above the age of 60 was initiated for treatment with<unk>  alone; the results, reported in 2006, indicated that the primary endpoint of complete remission was not achieved in any participants. Despite this failure, another multi-center Phase II trial involving 42 patients combined<unk>  with conventional chemotherapy; the results, reported in 2005, indicated that twice as many patients showed a clinical response when treated with<unk>  as compared to those not treated. Consequently, a Phase III trial was initiated with 224 patients for<unk>  following chemotherapy; no significant difference in cancer remission was seen between patients treated with chemotherapy alone and with<unk>  and chemotherapy, according to results in a 2011 report. Additional clinical trials have been initiated since this Phase III trial. These include a multi-center Phase II trial involving 37 patients with V617F JAK2 positive polycythemia vera and essential thrombocytosis; results published in 2014 indicate that the trial did not achieve the endpoint of 15% reduction of V617F JAK2 allele burden in 15% of patients. A Phase I study of 47 patients reported in 2010 that treatment of refractory neuroblastoma was well tolerated at the recommended doses, and an additional Phase I study in children with refractory neuroblastoma was completed in 2011. Phase I results were reported in 2015 for a<unk>  trial involving patients with V617F JAK2 positive myelofibrosis.
Lestaurtinib
Mobocertinib
Osimertinib
Selpercatinib
Upadacitinib
Brigatinib
Baricitinib
Axitinib