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Development of 2 Bromodomain and Extraterminal Inhibitors With Distinct Pharmacokinetic and Pharmacodynamic Profiles for the Treatment of Advanced Malignancies.

著者 Falchook GS , Rosen S , LoRusso PM , Watts JM , Gupta S , Coombs CC , Talpaz M , Kurzrock R , Mita MM , Cassaday RD , Harb W , Peguero JA , Smith DC , Piha-Paul SA , Szmulewitz RZ , Noel MS , Yeleswaram S , Liu P , Switzky J , Zhou G , Zheng F , Mehta AN
Clin Cancer Res.2019 Sep 16 ; ():.
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Bromodomain and extraterminal (BET) proteins are key epigenetic transcriptional regulators, inhibition of which may suppress oncogene expression. We report results from 2 independent first-in-human phase 1/2 dose-escalation and expansion, safety and tolerability studies of BET inhibitors INCB054329 (study INCB 54329-101; NCT02431260) and INCB057643 (study INCB 57643-101; NCT02711137).
PMID: 31527168 [PubMed - as supplied by publisher]
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