Principal Investigator
Drug Metabolism and Pharmacokinetics Research Center;Shanghai Research Center for Drug Metabolism & Pharmacokinetics
Personal Homepage
CONTACT
xxdiao@simm.ac.cn
021-50802321
201203
501 Haike Road, Suite 1705, Zhangjiang, Pudong, Shanghai, China
Xingxing Diao got his PhD degree from Shanghai Institute of Materia Medica, Chinese Academy of Sciences in 2014 and received his postdoctoral training in NIH (National Institutes of Health), USA between 2014 and 2016. In years 2016-2019, Dr. Diao worked in XenoBiotic Laboratories (Plainsboro, NJ, USA) and Celgene (Summit, NJ, USA), focusing on 14C-radiolabeled drug metabolism. Since Feb 2019, Dr. Diao started running an independent DMPK laboratory, focusing on 14C-radiolabeled drug metabolism.
Education
2005.9-2009.6, B.S., Wuhan University, Pharmaceutical Science
2009.9-2014.7, Ph.D., Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Medicinal Analysis
Work Experience
2014.7-2016.6, NIH (National Institutes of Health, USA), Postdoctoral Fellow, Chemistry and Drug Metabolism
2016.6-2018.8, XenoBiotic Laboratories (USA), Scientist I/II, DMPK Department
2018.8-2019.2, Celgene (USA), Scientist II, DMPK Department
2019.2-Present, Professor, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai Center of Drug Metabolism and Pharmacokinetics
1. 14C-radiolabeled DMPK research
2. Drug metabolism, mechanism for adverse drug reactions, new metabolic pathway, uncommon pharmacokinetics, new techniques in drug metabolism
1. Systemic investigation on human DMPK of 3-n-butylphthalide (Drug Metab Dispos, 2013; J Pharm Biomed Anal, 2013; J Chromatogr B, 2013); elucidated the metabolic bioactivation mechanism underlying the hepatotoxicity of 3-n-butylphthalide (Drug Metab Dispos, 2014); mechanism responsible for the isomer-selective distribution of 3-OH-NBP and 10-OH-NBP across blood-brain barrier (Acta Pharmacol Sin, 2015).
2. Set up human hepatocyte incubation platform for new synthetic cannabinoid in NIH/NIDA; proposed strategies on new synthetic cannabinoid metabolism – used for forensic investigation (Clin Chem, 2016; Clin Chem, 2017; Clin Pharmacol Ther, 2017; Forensic Toxicol, 2018).
3. High-quality radio-labeled drug metabolism services, including rat [14C] drug metabolism (mass balance, tissue distribution, radioactive PK, Radioprofiling, metabolite ID), human [14C] drug metabolism (mass balance, radioactive PK, B/P, Radioprofiling, metabolite ID) and metabolite ID (Acta Pharmacol Sin, 2020).
Full Publication List
Selected Publications
1.Zheng Y, Zhang H, Zhan Y, Bian Y, Ma Sheng, Gan H, Lai X, Liu Y, Gong Y, Liu X, Sun H, Li Y, Zhong D*, Miao L*, Diao X* (2020). Pharmacokinetics, Mass Balance, and Metabolism of [14C]Vicagrel, a Novel Irreversible P2Y12 Inhibitor in Humans. Acta Pharmacol Sin, Accepted (IF = 5.0)
2.Tian Q, Zhu Y, Diao X, Zhang X, Xu Y, Jiang X, Shen J, Wang Z*, Zhong D* (2019). Species differences in the CYP3A-catalyzed metabolism of TPN729, a novel PDE5 inhibitor. Acta Pharmacol Sin, In press (IF = 5.0)
3.Pan L, Yang Y, Hui M, Wang S, Li C, Zhang H, Ding Y*, Fu L*, Diao X*, Zhong D* (2020). Sulfation predominates the pharmacokinetics, metabolism, and excretion of forsythin in humans: major enzymes and transporters identified. Acta Pharmacol Sin, In press (IF = 5.0)
4.Liu X, Guo Z, Chen Z, Zhang Y, Zhou J, Jiang Y, Zhao Q, Diao X*, Zhong D* (2020). Alflutinib (AST2818), primarily metabolized by CYP3A4, is a potent CYP3A4 inducer. Acta Pharmacol Sin, 1-11 (IF = 4.0)
5.Pan L, Guo S, Chen X, Jiang X, Shen J, Diao X*, Wang Z*, Zhong D* (2019). Characterization of TPN171 metabolism in humans via ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry. J Pharm Biomed Anal, 172: 302-310 (IF = 3.3)
6.Diao X, Huestis MA (2019). New Synthetic Cannabinoids Metabolism and Strategies to Best Identify Optimal Marker Metabolites. Frontiers in Chemistry, 7: 109 (IF = 4.2)
7.Diao X, Carlier J, Zhu M, Huestis MA (2018). Metabolism of the new synthetic cannabinoid EG-018 in human hepatocytes by high-resolution mass spectrometry. Forensic Toxicol, 36:304-312 (IF = 3.7)
8.Carlier J#, Diao X#, Huestis MA (2018). Synthetic cannabinoid BB-22 (QUCHIC): Human hepatocytes metabolism with liquid chromatography-high-resolution mass spectrometry detection. J Pharm Biomed Anal, 157: 27-35 (IF = 3.3)
9.Lee MR, Scheidweiler KB, Diao X, Akhlaghi F, Cummins A, Huestis MA, Leggio L, Averbeck BB (2018) Oxytocin by intranasal and intravenous routes reaches the cerebrospinal fluid in rhesus macaques: determination using a novel oxytocin assay. Mol Psychiatry, 23: 115-122 (IF = 13.2)
10.Diao X#, Carlier J#, Zhu M, Huestis MA (2017). Human hepatocyte metabolism of novel synthetic cannabinoids MN-18 and its 5-fluoro analog 5F-MN-18. Clin Chem, 63: 1753-1763 (IF = 8.0)
11.Diao X#, Carlier J#, Scheidweiler KB, Huestis MA (2017). In vitro metabolism of new synthetic cannabinoid SDB-006 in human hepatocytes by high-resolution mass spectrometry. Forensic Toxicol, 35: 252-262 (IF = 3.7)
12.Carlier J, Diao X, Scheidweiler KB, Huestis MA (2017) Distinguishing intake of new synthetic cannabinoids, ADB-PINACA and 5F-ADB-PINACA, with human hepatocyte metabolites and high resolution mass spectrometry. Clin Chem, 63: 1008-1021 (IF = 8.0)
13.Diao X, Huestis MA (2017). Approaches, challenges and advances in metabolism of new synthetic cannabinoids and identification of optimal urinary marker metabolites. Clin Pharmacol Ther, 101: 239-253. Invited Review (IF = 7.3)
14.Carlier J#, Diao X#, Sempio C, Baumann MH, Huestis MA (2017) Identification of new synthetic cannabinoid ADB-CHMINACA (MAB-CHMINACA) metabolites in human hepatocytes. AAPS J, 19: 568-577 (IF = 3.4)
15.Wohlfarth A, Roman M, Andersson M, Kugelberg FC, Diao X, Carlier J, Eriksson C, Wu X, Konradsson P, Josefsson M, Huestis MA, Kronstrand R (2017). 25C-NBOMe and 25I-NBOMe metabolite studies in human hepatocytes, in vivo mouse and human urine with high-resolution mass spectrometry. Drug Test Anal, 9: 680-698 (IF = 3.5)
16.Diao X, Carlier J, Zhu M, Pang S, Kronstrand R, Scheidweiler KB, Huestis MA (2017). In vitro and in vivo human metabolism of a new synthetic cannabinoid NM-2201 (CBL-2201). Forensic Toxicol, 35: 20-32 (IF = 3.7)
17.Carlier J, Diao X, Wohlfarth A, Scheidweiler KB, Huestis MA (2017). In vitro metabolite profiling of ADB-FUBINACA, a new synthetic cannabinoid. Curr Neuropharmacol, 15: 682-691 (IF = 3.4)
18.Zhu Y, Li L, Zhang G, Wan H, Yang C, Diao X, Chen X, Zhang L, Zhong D (2016). Metabolic characterization of pyrotinib in humans by ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry. J Chromatogr B, 1033: 117-127 (IF = 2.6)
19.Diao X, Scheidweiler KB, Wohlfarth A, Zhu M, Pang S, Huestis MA (2016). Strategies to distinguish new synthetic cannabinoid FUBIMINA (BIM-2201) intake from its isomer THJ-2201: metabolism of FUBIMINA in human hepatocytes. Forensic Toxicol, 34: 256-267 (IF = 3.7)
20.Jiang J, Pang X, Li L, Dai X, Diao X, Chen X, Zhong D, Wang Y, Chen Y (2016). Effect of N-methyl deuteration on metabolism and pharmacokinetics of enzalutamide. Drug Des Devel Ther, 10: 2181–2191 (IF = 2.8)
21.Swortwood MJ, Ellefsen KN, Wohlfarth A, Diao X, Concheiro-Guisan M, Kronstrand R, Huestis MA (2016). First metabolic profile of PV8, a novel synthetic cathinone, in human hepatocytes and urine by high-resolution mass spectrometry. Anal Bioanal Chem, 408: 4845-4856 (IF = 3.4)
22.Andersson M, Diao X, Wohlfarth A, Scheidweiler KB, Huestis MA (2016). Metabolic profiling of new synthetic cannabinoids AMB and 5F-AMB by human hepatocyte and liver microsome incubations and high-resolution mass spectrometry. Rapid Commun Mass Spectrom, 30: 1067-1078 (IF = 2.0)
23.Diao X, Scheidweiler KB, Wohlfarth A, Pang S, Kronstrand R, Huestis MA (2016). In vitro and in vivo human metabolism of synthetic cannabinoids FDU-PB-22 and FUB-PB-22. AAPS J, 18: 455-464 (IF = 3.4)
24.Swortwood MJ, Carlier J, Ellefsen KN, Wohlfarth A, Diao X, Concheiro M, Kronstrand R, Huestis MA (2016). In vitro, in vivo and in silico metabolic profiling of α-pyrrolidinopentiothiophenone, a novel thiophene stimulant. Bioanalysis, 8: 65-82 (IF = 2.7)
25.Diao X, Wohlfarth A, Pang S, Scheidweiler KB, Huestis MA (2016). High-resolution mass spectrometry for characterizing the metabolism of synthetic cannabinoids THJ-018 and its 5-fluoro analog THJ-2201 after incubation in human hepatocytes. Clin Chem, 62: 157-169 (IF = 8.0)
26.Ellefsen KN, Wohlfarth A, Swortwood MJ, Diao X, Concheiro M, Huestis MA (2016). 4-Methoxy-a-PVP: in silico prediction, metabolic stability, and metabolite identification by human hepatocyte incubation and high-resolution mass spectrometry. Forensic Toxicol, 34:61–75 (IF = 3.7)
27.Diao X, Zhong K, Li X, Zhong D, Chen X (2015). Isomer-selective distribution of 3-n-butylphthalide (NBP) hydroxylated metabolites, 3-OH-NBP and 10-OH-NBP, across the rat blood-brain barrier. Acta Pharmacol Sin, 36: 1520-1527 (IF = 5.0)
28.Diao X, Pang X, Xie C, Guo Z, Zhong D, Chen X (2014). Bioactivation of 3-n-butylphthalide via the sulfation of its major metabolite 3-hydroxy-NBP: mediated mainly by sulfotransferase1A1. Drug Metab Dispos, 42: 774-781 (IF = 4.2)
29.Diao X, Chen X (2014). The role of aldehyde oxidase in drug metabolism. Journal of Baoji University of Arts and Sciences (Natural Science) (in Chinese), 34: 26-38. Invited Review
30.Diao X, Ma Z, Wang H, Zhong D, Zhang Y, Jin J, Fan Y, Chen X (2013). Simultaneous quantitation of 3-n-butylphthalide (NBP) and its four major metabolites in human plasma by LC–MS/MS using deuterated internal standards. J Pharm Biomed Anal, 78: 19-26 (IF = 3.3)
31.Diao X, Ma Z, Lei P, Zhong D, Zhang Y, Chen X (2013). Enantioselective determination of 3-n-butylphthalide (NBP) in human plasma by liquid chromatography on a teicoplanin-based chiral column coupled with tandem mass spectrometry. J Chromatogr B, 939: 67-72 (IF = 2.6)
32.Xie C, Zhou J, Guo Z, Diao X, Gao Z, Zhong D, Chen X (2013). Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Brit J Pharmacol, 168: 1687-1706 (IF = 5.5)
33.Diao X, Deng P, Xie C, Li X, Zhong D, Zhang Y, Chen X (2013). Metabolism and pharmacokinetics of 3-n-butylphthalide (NBP) in humans: the role of cytochrome P450s and alcohol dehydrogenase in biotransformation. Drug Metab Dispos, 41: 430-444 (IF = 4.2)
34.Gao R, Li L, Xie C, Diao X, Zhong D, Chen X (2012). Metabolism and pharmacokinetics of morinidazole in humans: Identification of diastereoisomeric morpholine N+-glucuronides catalyzed by UDP glucuronosyltransferase. Drug Metab Dispos, 40: 556-567 (IF = 4.2)
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