Phase I Population Pharmacokinetic Assessment of the Oral Bromodomain Inhibitor OTX015 in Patients with Haematologic Malignancies

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• 作者：Elodie Odore ; François Lokiec ; Esteban Cvitkovic…
• 刊名：Clinical Pharmacokinetics
• 出版年：2016
• 出版时间：March 2016
• 年：2016
• 卷：55
• 期：3
• 页码：397-405
• 全文大小：1,151 KB
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• 作者单位：Elodie Odore (1) (2)
  François Lokiec (1)
  Esteban Cvitkovic (2) (3)
  Mohamed Bekradda (2)
  Patrice Herait (2) (3)
  Fabrice Bourdel (2)
  Carmen Kahatt (2)
  Emmanuel Raffoux (4)
  Anastasios Stathis (5)
  Catherine Thieblemont (4)
  Bruno Quesnel (6)
  David Cunningham (7)
  Maria E. Riveiro (2)
  Keyvan Rezaï (1)
  
  1. Department of Radio-Pharmacology, Institut Curie-Hôpital René Huguenin, 35 Rue Dailly, 92210, Saint-Cloud, France
  2. Oncology Therapeutic Development, Clichy, France
  3. Oncoethix GmbH, Lucerne, Switzerland
  4. Hôpital Saint Louis, Paris, France
  5. Oncology Institute of Southern Switzerland, Bellinzona, Switzerland
  6. CHRU Lille, Lille, France
  7. The Royal Marsden Hospital, London, UK
  
• 刊物主题：Pharmacotherapy; Pharmacology/Toxicology; Internal Medicine;
• 出版者：Springer International Publishing
• ISSN：1179-1926

文摘

Background and Objectives OTX015 (MK-8628) is a novel inhibitor of the bromodomain and extraterminal (BET)-bromodomain (BRD) protein family, binding specifically to bromodomains BRD2/3/4 and impacting the epigenetic regulation of several oncogenes. We characterized the pharmacokinetics of this first-in-class BET-BRD inhibitor administered as a single agent, including population pharmacokinetic modelling.