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Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients.

Xie C, Zhou J, Guo Z, Diao X, Gao Z, Zhong D, Jiang H, Zhang L, Chen X.

Br J Pharmacol. 2013 Apr;168(7):1687-706. doi: 10.1111/bph.12047.


Metabolism and disposition of [14C]BMS-690514, an ErbB/vascular endothelial growth factor receptor inhibitor, after oral administration to humans.

Christopher LJ, Hong H, Vakkalagadda BJ, Clemens PL, Su H, Roongta V, Allentoff A, Sun H, Heller K, Harbison CT, Iyer RA, Humphreys WG, Wong T, Zhang S.

Drug Metab Dispos. 2010 Nov;38(11):2049-59. doi: 10.1124/dmd.110.034850. Epub 2010 Jul 28.


Phase I study of the safety, pharmacokinetics and antitumor activity of famitinib.

Zhou A, Zhang W, Chang C, Chen X, Zhong D, Qin Q, Lou D, Jiang H, Wang J.

Cancer Chemother Pharmacol. 2013 Nov;72(5):1043-53. doi: 10.1007/s00280-013-2282-y. Epub 2013 Sep 17.


Metabolism and pharmacokinetics of allitinib in cancer patients: the roles of cytochrome P450s and epoxide hydrolase in its biotransformation.

Lin L, Xie C, Gao Z, Chen X, Zhong D.

Drug Metab Dispos. 2014 May;42(5):872-84. doi: 10.1124/dmd.113.056341. Epub 2014 Mar 5.


In vitro metabolism studies of nomifensine monooxygenation pathways: metabolite identification, reaction phenotyping, and bioactivation mechanism.

Yu J, Brown DG, Burdette D.

Drug Metab Dispos. 2010 Oct;38(10):1767-78. doi: 10.1124/dmd.110.033910. Epub 2010 Jul 1.


In vitro metabolism of BIIB021, an inhibitor of heat shock protein 90, in liver microsomes and hepatocytes of rats, dogs, and humans and recombinant human cytochrome P450 isoforms.

Xu L, Woodward C, Khan S, Prakash C.

Drug Metab Dispos. 2012 Apr;40(4):680-93. doi: 10.1124/dmd.111.043000. Epub 2012 Jan 4.


Metabolism and pharmacokinetics of 3-n-butylphthalide (NBP) in humans: the role of cytochrome P450s and alcohol dehydrogenase in biotransformation.

Diao X, Deng P, Xie C, Li X, Zhong D, Zhang Y, Chen X.

Drug Metab Dispos. 2013 Feb;41(2):430-44. doi: 10.1124/dmd.112.049684. Epub 2012 Nov 20.


Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans.

Speed B, Bu HZ, Pool WF, Peng GW, Wu EY, Patyna S, Bello C, Kang P.

Drug Metab Dispos. 2012 Mar;40(3):539-55. doi: 10.1124/dmd.111.042853. Epub 2011 Dec 16.


In vitro studies on the oxidative metabolism of 20(s)-ginsenoside Rh2 in human, monkey, dog, rat, and mouse liver microsomes, and human liver s9.

Li L, Chen X, Zhou J, Zhong D.

Drug Metab Dispos. 2012 Oct;40(10):2041-53. doi: 10.1124/dmd.112.046995. Epub 2012 Jul 24.


[Predicting pharmacokinetics of anti-cancer drug, famitinib in human using physiologically based pharmacokinetic model].

Yu MM, Gao ZW, Chen XY, Zhong DF.

Yao Xue Xue Bao. 2014 Dec;49(12):1684-8. Chinese.


Metabolic map and bioactivation of the anti-tumour drug noscapine.

Fang ZZ, Krausz KW, Li F, Cheng J, Tanaka N, Gonzalez FJ.

Br J Pharmacol. 2012 Nov;167(6):1271-86. doi: 10.1111/j.1476-5381.2012.02067.x.


Evaluation of metabolism and disposition of GDC-0152 in rats using 14C labeling strategy at two different positions: a novel formation of hippuric acid from 4-phenyl-5-amino-1,2,3-thiadiazole.

Yue Q, Mulder T, Rudewicz PJ, Solon E, Budha N, Ware JA, Lyssikatos J, Hop CE, Wong H, Khojasteh SC.

Drug Metab Dispos. 2013 Feb;41(2):508-17. doi: 10.1124/dmd.112.047019. Epub 2012 Dec 4.


In vitro metabolism of oxymetazoline: evidence for bioactivation to a reactive metabolite.

Mahajan MK, Uttamsingh V, Daniels JS, Gan LS, LeDuc BW, Williams DA.

Drug Metab Dispos. 2011 Apr;39(4):693-702. doi: 10.1124/dmd.110.036004. Epub 2010 Dec 21.


Bioactivation of phencyclidine in rat and human liver microsomes and recombinant P450 2B enzymes: evidence for the formation of a novel quinone methide intermediate.

Driscoll JP, Kornecki K, Wolkowski JP, Chupak L, Kalgutkar AS, O'Donnell JP.

Chem Res Toxicol. 2007 Oct;20(10):1488-97. Epub 2007 Sep 25.


Metabolism of capsaicin by cytochrome P450 produces novel dehydrogenated metabolites and decreases cytotoxicity to lung and liver cells.

Reilly CA, Ehlhardt WJ, Jackson DA, Kulanthaivel P, Mutlib AE, Espina RJ, Moody DE, Crouch DJ, Yost GS.

Chem Res Toxicol. 2003 Mar;16(3):336-49.


Bioactivation of the nontricyclic antidepressant nefazodone to a reactive quinone-imine species in human liver microsomes and recombinant cytochrome P450 3A4.

Kalgutkar AS, Vaz AD, Lame ME, Henne KR, Soglia J, Zhao SX, Abramov YA, Lombardo F, Collin C, Hendsch ZS, Hop CE.

Drug Metab Dispos. 2005 Feb;33(2):243-53. Epub 2004 Nov 2. Erratum in: Drug Metab Dispos. 2005 May;33(5):696.


Studies on the role of metabolic activation in tyrosine kinase inhibitor-dependent hepatotoxicity: induction of CYP3A4 enhances the cytotoxicity of lapatinib in HepaRG cells.

Hardy KD, Wahlin MD, Papageorgiou I, Unadkat JD, Rettie AE, Nelson SD.

Drug Metab Dispos. 2014 Jan;42(1):162-71. doi: 10.1124/dmd.113.054817. Epub 2013 Nov 4.


Delineation of the interactions between the chemotherapeutic agent eribulin mesylate (E7389) and human CYP3A4.

Zhang ZY, King BM, Pelletier RD, Wong YN.

Cancer Chemother Pharmacol. 2008 Sep;62(4):707-16. doi: 10.1007/s00280-008-0755-1. Epub 2008 Apr 23.


Bioactivation of glafenine by human liver microsomes and peroxidases: identification of electrophilic iminoquinone species and GSH conjugates.

Wen B, Moore DJ.

Drug Metab Dispos. 2011 Sep;39(9):1511-21. doi: 10.1124/dmd.111.039396. Epub 2011 May 31.

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