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Xenobiotica
the fate of foreign compounds in biological systems
Volume 47, 2017 - Issue 10
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Clinical Pharmacokinetics and Metabolism

An open-label, single-dose, phase 1 study of the absorption, metabolism and excretion of quizartinib, a highly selective and potent FLT3 tyrosine kinase inhibitor, in healthy male subjects, for the treatment of acute myeloid leukemia

Madhu SangaCovance Laboratories Inc, Madison, WI, USA,
,
Joyce JamesLyric Pharmaceuticals, Inc, South San Francisco, CA, USA,
,
Joseph MariniCovance Laboratories Inc, Madison, WI, USA,
,
Guy GammonDaiichi Sankyo, Inc, San Diego, CA, USA, and
,
Christine HaleCovance Clinical Research Unit, Madison, WI, USA
&
Jianke LiDaiichi Sankyo, Inc, San Diego, CA, USA, and Correspondence[email protected]
Pages 856-869 | Received 06 Jun 2016, Accepted 21 Jul 2016, Published online: 25 Jul 2017

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Alejandro Garcia-Horton & Karen Wl Yee. (2020) Quizartinib for the treatment of acute myeloid leukemia. Expert Opinion on Pharmacotherapy 21:17, pages 2077-2090.
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Fang Zhou, Zheng Ge & Baoan Chen. (2019) Quizartinib (AC220): a promising option for acute myeloid leukemia. Drug Design, Development and Therapy 13, pages 1117-1125.
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Samuel J. Taylor & Wallace Y. Langdon. (2017) Hitting the snooze button: Inducing quiescence with the FLT3 inhibitor quizartinib protects hematopoietic progenitors from chemotherapy. Molecular & Cellular Oncology 4:6.
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Tomoya Aikawa, Noriko Togashi, Koichi Iwanaga, Hiroyuki Okada, Yumi Nishiya, Shinichi Inoue, Mark J. Levis & Takeshi Isoyama. (2020) Quizartinib, a selective FLT3 inhibitor, maintains antileukemic activity in preclinical models of RAS-mediated midostaurin-resistant acute myeloid leukemia cells. Oncotarget 11:11, pages 943-955.
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Jianke Li, Denise Trone, Jeanne Mendell, Patrick O’Donnell & Natalie Cook. (2019) A drug–drug interaction study to assess the potential effect of acid-reducing agent, lansoprazole, on quizartinib pharmacokinetics. Cancer Chemotherapy and Pharmacology 84:4, pages 799-807.
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Jianke Li, Martin Kankam, Denise Trone & Guy Gammon. (2019) Effects of CYP3A inhibitors on the pharmacokinetics of quizartinib, a potent and selective FLT3 inhibitor, and its active metabolite. British Journal of Clinical Pharmacology 85:9, pages 2108-2117.
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Yu-Ting Chang, Daniela Hernandez, Salvador Alonso, Minling Gao, Meng Su, Gabriel Ghiaur, Mark J. Levis & Richard J. Jones. (2019) Role of CYP3A4 in bone marrow microenvironment–mediated protection of FLT3/ITD AML from tyrosine kinase inhibitors. Blood Advances 3:6, pages 908-916.
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Jing Wang, Changpei Gan, Irene A. Retmana, Rolf W. Sparidans, Wenlong Li, Maria C. Lebre, Jos H. Beijnen & Alfred H. Schinkel. (2019) P-glycoprotein (MDR1/ABCB1) and Breast Cancer Resistance Protein (BCRP/ABCG2) limit brain accumulation of the FLT3 inhibitor quizartinib in mice. International Journal of Pharmaceutics 556, pages 172-180.
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Kyriakos P. Papadopoulos, Eytan Ben-Ami, Amita Patnaik, Denise Trone, Jianke Li & George D. Demetri. (2018) Safety and tolerability of quizartinib, a FLT3 inhibitor, in advanced solid tumors: a phase 1 dose-escalation trial. BMC Cancer 18:1.
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Jaideep B. Bharate, Nicholas McConnell, Gunaganti Naresh, Lingtian Zhang, Naga Rajiv Lakkaniga, Lucky Ding, Neil P. Shah, Brendan Frett & Hong-yu Li. (2018) Rational Design, Synthesis and Biological Evaluation of Pyrimidine-4,6-diamine derivatives as Type-II inhibitors of FLT3 Selective Against c-KIT. Scientific Reports 8:1.
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Samuel J. Taylor, Johanna M. DuyvestynSamantha A. Dagger, Emma J. DishingtonCatherine A. RinaldiOliver M. Dovey, George S. Vassiliou, Carolyn S. Grove & Wallace Y. Langdon. (2017) Preventing chemotherapy-induced myelosuppression by repurposing the FLT3 inhibitor quizartinib. Science Translational Medicine 9:402.
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Irene A. Retmana, Jing Wang, Alfred H. Schinkel, Jan H.M. Schellens, Jos H. Beijnen & Rolf W. Sparidans. (2017) Liquid chromatography-tandem mass spectrometric assay for the quantitative determination of the tyrosine kinase inhibitor quizartinib in mouse plasma using salting-out liquid-liquid extraction.. Journal of Chromatography B.
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