OSI-420 Desmethyl Erlotinib Similar chemical structure as imatinib, but a form topographic improve ABL kinase pocket. Dasatinib a chemical structure v Llig other to imatinib and unlike imatinib and nilotinib BCR ABL binds in the active conformation. Bosutinib binds to an intermediate form of BCRABL. Three TKIs activity a t Against most mutant forms of BCR-ABL kinase have been associated with clinical resistance to imatinib in combination. Dasatinib 100 mg once t Possible and nilotinib 400 mg twice t Resembled approved in the United States and Europe as a treatment for patients with CML compared with imatinib resistant or intolerant. Dasatinib 100 mg once t Resembled and 300 mg of nilotinib were recently approved in the United States for patients with newly diagnosed CML CP. Bosutinib still in clinical trials.
Clinical trials to evaluate new TKI as first-line therapy in newly diagnosed CML CP are in progress and the results of studies of dasatinib and nilotinib were recently reported. To dasatinib clinical trials in CPCML ver ffentlicht newly diagnosed go Ren DASISION an international, multicenter, randomized, phase 3 trials of dasatinib t 100 mg once resembled vs. imatinib 400 mg once t possible, and a Phase Test 2 of Dasatinib 100 mg once t daily or 50 mg twice conducted by MD Anderson Cancer Center, Houston, TX. For nilotinib, clinical studies in newly diagnosed CML-CP are comparable ffentlicht: ENESTnd an international, multicenter, randomized Phase 3 nilotinib 300 mg bid vs. 400 mg BID nilotinib vs imatinib 400 mg once a day, a Phase 2 clinical trials of Tasigna 400 mg BID arm MDACC performed, and a second phase 2 single-arm study with nilotinib 400 mg of the Italian GIMEMA group made.
No data from an international, multicenter, randomized bosutinib vs imatinib ver Been ffentlicht. In this paper, the most recent data for the first-line treatment with dasatinib or nilotinib are discussed, with an emphasis on safety and reps Possibility. Compared the effectiveness of dasatinib and nilotinib with imatinib in the frontline in randomized trials, both dasatinib and nilotinib showed superior efficacy compared with imatinib as first-line therapy for patients with CP CML. The test reactions were DASISION h More frequently with dasatinib vs imatinib, including normal one hour Heren rates a completely Ndigen cytogenetic response 12 months and major molecular response.
Dasatinib showed the superiority of imatinib on the prime Ren test, the rate of the best Saturated complete cytogenetic response, be with 12-month rate of 77% vs. 66%. CCyR and MMR both occurred faster with dasatinib compared with imatinib. Median of 14 months of treatment had. 1.9% of patients AP / blast phase with dasatinib compared with 3.5% with imatinib No patient in the MMR AP / BP reached advanced. In the primary test ENESTnd Re endpoint was the rate of MMR at 12 months, and both nilotinib arms were significantly h Higher prices compared to the imatinib arm. Rates a completely Ndigen cytogenetic responses obtained 12 months were also significantly h Ago nilotinib vs imatinib and CCyR and MMR was faster in the nilotinib arm. Median of 14 months of treatment, patients treated with nilotinib less AP / BP phase progressed in relation to imatinib treated patients. How DASISION had no patient had an MMR progress .