Influence of pharmacogenetic variability on the pharmacokinetics and toxicity of the aurora kinase inhibitor danusertib

Investigational New Drugs

Volumn 29, Issue 5, 2011, Pages 953-962

  Steeghs, Neeltje ^a   Mathijssen, Ron H J ^b   Wessels, Judith A M ^a   De Graan, Anne Joy ^b   Van Der Straaten, Tahar ^a   Mariani, Mariangela ^c   Laffranchi, Bernard ^c   Comis, Silvia ^c   De Jonge, Maja J A ^b   Gelderblom, Hans ^a   Guchelaar, Henk Jan ^a  

^a LEIDEN UNIVERSITY MEDICAL CENTER   (Netherlands)

^b ERASMUS MEDICAL CENTER   (Netherlands)

^c NERVIANO MEDICAL SCIENCES   (Italy)

Author keywords

Cancer: aurora kinase inhibitor; Danusertib; PHA 739358; Pharmacogenetics; Pharmacogenomics

Indexed keywords

DANUSERTIB; DRUG METABOLIZING ENZYME; HISTONE H3; ANTINEOPLASTIC AGENT; AURORA KINASE; BENZAMIDE DERIVATIVE; PROTEIN KINASE INHIBITOR; PROTEIN SERINE THREONINE KINASE; PYRAZOLE DERIVATIVE;

ABCB1 GENE; ABCG2 GENE; ADULT; AGED; ARTICLE; AURKA GENE; AURKB GENE; BREAST CANCER; CANCER PATIENT; COLORECTAL CANCER; CONTROLLED STUDY; DNA POLYMORPHISM; DOSAGE SCHEDULE COMPARISON; DRUG CLEARANCE; DRUG DOSE ESCALATION; DRUG TARGETING; ESOPHAGUS CANCER; FEBRILE NEUTROPENIA; FEMALE; FLT3 GENE; FLT4 GENE; FMO3 GENE; GENE; GENE FREQUENCY; GENETIC VARIABILITY; GENOTYPE; HAPLOTYPE; HETEROZYGOSITY; HOMOZYGOSITY; HUMAN; KDR GENE; MAJOR CLINICAL STUDY; MALE; MULTIPLE CYCLE TREATMENT; NEUTROPENIA; OVARY CANCER; PANCREAS CANCER; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; PROSTATE CANCER; PROTEIN PHOSPHORYLATION; RET GENE; SINGLE NUCLEOTIDE POLYMORPHISM; TREATMENT DURATION; ANALYSIS OF VARIANCE; CANCER GRADING; CLINICAL TRIAL; DRUG ANTAGONISM; GENETIC POLYMORPHISM; GENETICS; METABOLISM; MIDDLE AGED; PHARMACOGENETICS; PHASE 1 CLINICAL TRIAL; PHASE 2 CLINICAL TRIAL;

ADULT; AGED; ANALYSIS OF VARIANCE; ANTINEOPLASTIC AGENTS; BENZAMIDES; FEMALE; HAPLOTYPES; HUMANS; MALE; MIDDLE AGED; NEOPLASM GRADING; PHARMACOGENETICS; POLYMORPHISM, GENETIC; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; PYRAZOLES; YOUNG ADULT;

EID: 84856072919     PISSN: 01676997     EISSN: 15730646     Source Type: Journal    
DOI: 10.1007/s10637-010-9405-7     Document Type: Article

References (38)

1. Jones SF, Cohen RB, Dees EC, Lee Y, Papas JA, Cooper MR et al. (2007). Phase I clinical trial of MLN8054, a selective inhibitor of Aurora A kinase. J Clin Oncol 25:18s (suppl; abstr 3577)
2. Renshaw S, Patnaik A, Gordon M, Beeram M, Fischer D, Gianella-Borradori A et al. (2007). A phase I two arm trial of AS703569(R763), an orally available aurora kinase inhibitor, in subjects with solid tumors: preliminary results. J Clin Oncol 25:18s (suppl; abstr 14130)
3. Rubin EH, Shapiro GI, Stein MN, Watson P, Bergstrom D, Xiao A et al. (2006) A phase I clinical and pharmacokinetic (PK) trial of the aurora kinase (AK) inhibitor MK-0457 in cancer patients. J Clin Oncol 24:18s (suppl; abstr 3009).
4. Schellens JH, Boss D, Witteveen PO, Zandvliet A, Beijnen JH, Voogel-Fuchs M et al. (2006). Phase I and pharmacological study of the novel aurora kinase inhibitor AZD1152. J Clin Oncol 24:18s (suppl; abstr 3008).
5. Foran JM, Ravandi F, O'Brien SM, Borthakur G, Rios M, Boone P et al. (2008). Phase I and pharmacodynamic trial of AT9283, an aurora kinase inhibitor, in patients with refractory leukemia. J Clin Oncol 26:18s (suppl; abstr 2518).
6. Jones SF, Burris HA, Dumez H, Infante JR, Fowst C, Gerletti P et al. (2008). Phase I accelerated dose-escalation, pharmacokinetic (PK) and pharmacodynamic study of PF-03814735, an oral aurora kinase inhibitor, in patients with advanced solid tumors: Preliminary results. J Clin Oncol 26:18s (suppl; abstr 2517)
7. Robert F, Hurwitz H, Verschraegen CF, Advani R, Berman C, Taverna P et al. (2008). Phase 1 trial of SNS-314, a novel selective inhibitor of aurora kinases A, B, and C, in advanced solid tumor patients. J Clin Oncol 26:18s (suppl; abstr 14642).
8. Cohen RB, Jones SF, von Mehren M, Cheng J, Spiegel DM, Laffranchi B et al. (2008). Phase I study of the pan aurora kinases (AKs) inhibitor PHA-739358 administered as a 24 h infusion without/with G-CSF in a 14-day cycle in patients with advanced solid tumors. J Clin Oncol 26:18s (suppl; abstr 2520).
9. Plummer ER, Calvert H, Arkenau H, Mallett KH, Squires M, Smith D et al. (2008). A dose-escalation and pharmacodynamic study of AT9283 in patients with refractory solid tumours. J Clin Oncol 26:18s (suppl; abstr 2519)
10. Carpinelli P, Ceruti R, Giorgini ML, Cappella P, Gianellini L, Croci V, Degrassi A, Texido G, Rocchetti M, Vianello P, Rusconi L, Storici P, Zugnoni P, Arrigoni C, Soncini C, Alli C, Patton V, Marsiglio A, Ballinari D, Pesenti E, Fancelli D, Moll J (2007) PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer. Mol Cancer Ther 6:3158-3168
11. Fancelli D, Moll J, Varasi M, Bravo R, Artico R, Berta D, Bindi S, Cameron A, Candiani I, Cappella P, Carpinelli P, Croci W, Forte B, Giorgini ML, Klapwijk J, Marsiglio A, Pesenti E, Rocchetti M, Roletto F, Severino D, Soncini C, Storici P, Tonani R, Zugnoni P, Vianello P (2006) 1, 4, 5, 6-tetrahydropyrrolo[3, 4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. J Med Chem 49:7247-7251
12. Warner SL, Gray PJ, Von Hoff DD (2006) Tubulin-associated drug targets: Aurora kinases, Polo-like kinases, and others. Semin Oncol 33:436-448
13. Carvajal RD, Tse A, Schwartz GK (2006) Aurora kinases: new targets for cancer therapy. Clin Cancer Res 12:6869-6875
14. Carpinelli P, Ceruti R, Giorgini ML, Cappella P, Gianellini L, Croci V, Degrassi A, Texido G, Rocchetti M, Vianello P, Rusconi L, Storici P, Zugnoni P, Arrigoni C, Soncini C, Alli C, Patton V, Marsiglio A, Ballinari D, Pesenti E, Fancelli D, Moll J (2007) PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer. Mol Cancer Ther 6:3158-3168
15. Carpinelli P, Ceruti R, Giorgini ML, Cappella P, Gianellini L, Croci V, Degrassi A, Texido G, Rocchetti M, Vianello P, Rusconi L, Storici P, Zugnoni P, Arrigoni C, Soncini C, Alli C, Patton V, Marsiglio A, Ballinari D, Pesenti E, Fancelli D, Moll J (2007) PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer. Mol Cancer Ther 6:3158-3168
16. Steeghs N, Eskens FA, Gelderblom H, Verweij J, Nortier JW, Ouwerkerk J, van Noort C, Mariani M, Spinelli R, Carpinelli P, Laffranchi B, de Jonge MJ (2009) Phase I pharmacokinetic and pharmacodynamic study of the aurora kinase inhibitor danusertib in patients with advanced or metastatic solid tumors. J Clin Oncol 27:5094-5101
17. Steeghs N, Eskens FA, Gelderblom H, Verweij J, Nortier JW, Ouwerkerk J, van Noort C, Mariani M, Spinelli R, Carpinelli P, Laffranchi B, de Jonge MJ (2009) Phase I pharmacokinetic and pharmacodynamic study of the aurora kinase inhibitor danusertib in patients with advanced or metastatic solid tumors. J Clin Oncol 27:5094-5101
18. Steeghs N, Eskens FA, Gelderblom H, Verweij J, Nortier JW, Ouwerkerk J, van Noort C, Mariani M, Spinelli R, Carpinelli P, Laffranchi B, de Jonge MJ (2009) Phase I pharmacokinetic and pharmacodynamic study of the aurora kinase inhibitor danusertib in patients with advanced or metastatic solid tumors. J Clin Oncol 27:5094-5101
19. Therasse P, Arbuck SG, Eisenhauer EA, Wanders J, Kaplan RS, Rubinstein L, Verweij J, Van GM, van Oosterom AT, Christian MC, Gwyther SG (2000) New guidelines to evaluate the response to treatment in solid tumors. European Organization for Research and Treatment of Cancer, National Cancer Institute of the United States, National Cancer Institute of Canada. J Natl Cancer Inst 92:205-216
20. Steeghs N, Eskens FA, Gelderblom H, Verweij J, Nortier JW, Ouwerkerk J, van Noort C, Mariani M, Spinelli R, Carpinelli P, Laffranchi B, de Jonge MJ (2009) Phase I pharmacokinetic and pharmacodynamic study of the aurora kinase inhibitor danusertib in patients with advanced or metastatic solid tumors. J Clin Oncol 27:5094-5101
21. Steeghs N, Eskens FA, Gelderblom H, Verweij J, Nortier JW, Ouwerkerk J, van Noort C, Mariani M, Spinelli R, Carpinelli P, Laffranchi B, de Jonge MJ (2009) Phase I pharmacokinetic and pharmacodynamic study of the aurora kinase inhibitor danusertib in patients with advanced or metastatic solid tumors. J Clin Oncol 27:5094-5101
22. Steeghs N, Eskens FA, Gelderblom H, Verweij J, Nortier JW, Ouwerkerk J, van Noort C, Mariani M, Spinelli R, Carpinelli P, Laffranchi B, de Jonge MJ (2009) Phase I pharmacokinetic and pharmacodynamic study of the aurora kinase inhibitor danusertib in patients with advanced or metastatic solid tumors. J Clin Oncol 27:5094-5101
23. Carpinelli P, Ceruti R, Giorgini ML, Cappella P, Gianellini L, Croci V, Degrassi A, Texido G, Rocchetti M, Vianello P, Rusconi L, Storici P, Zugnoni P, Arrigoni C, Soncini C, Alli C, Patton V, Marsiglio A, Ballinari D, Pesenti E, Fancelli D, Moll J (2007) PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer. Mol Cancer Ther 6:3158-3168
24. Soncini C, Carpinelli P, Gianellini L, Fancelli D, Vianello P, Rusconi L, Storici P, Zugnoni P, Pesenti E, Croci V, Ceruti R, Giorgini ML, Cappella P, Ballinari D, Sola F, Varasi M, Bravo R, Moll J (2006) PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity. Clin Cancer Res 12:4080-4089
25. Camidge DR, Pemberton MN, Growcott JW, Johnstone D, Laud PJ, Foster JR, Randall KJ, Hughes AM (2005) Assessing proliferation, cell-cycle arrest and apoptotic end points in human buccal punch biopsies for use as pharmacodynamic biomarkers in drug development. Br J Cancer 93:208-215
26. Carpinelli P, Ceruti R, Giorgini ML, Cappella P, Gianellini L, Croci V, Degrassi A, Texido G, Rocchetti M, Vianello P, Rusconi L, Storici P, Zugnoni P, Arrigoni C, Soncini C, Alli C, Patton V, Marsiglio A, Ballinari D, Pesenti E, Fancelli D, Moll J (2007) PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer. Mol Cancer Ther 6:3158-3168
27. Carpinelli P, Ceruti R, Giorgini ML, Cappella P, Gianellini L, Croci V, Degrassi A, Texido G, Rocchetti M, Vianello P, Rusconi L, Storici P, Zugnoni P, Arrigoni C, Soncini C, Alli C, Patton V, Marsiglio A, Ballinari D, Pesenti E, Fancelli D, Moll J (2007) PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer. Mol Cancer Ther 6:3158-3168
28. Fancelli D, Moll J, Varasi M, Bravo R, Artico R, Berta D, Bindi S, Cameron A, Candiani I, Cappella P, Carpinelli P, Croci W, Forte B, Giorgini ML, Klapwijk J, Marsiglio A, Pesenti E, Rocchetti M, Roletto F, Severino D, Soncini C, Storici P, Tonani R, Zugnoni P, Vianello P (2006) 1, 4, 5, 6-tetrahydropyrrolo[3, 4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. J Med Chem 49:7247-7251
29. Purcell S, Neale B, Todd-Brown K, Thomas L, Ferreira MA, Bender D, Maller J, Sklar P, de Bakker PI, Daly MJ, Sham PC (2007) PLINK: a tool set for whole-genome association and population-based linkage analyses. Am J Hum Genet 81:559-575
30. Swen JJ, Huizinga TW, Gelderblom H, de Vries EG, Assendelft WJ, Kirchheiner J, Guchelaar HJ (2007) Translating pharmacogenomics: challenges on the road to the clinic. PLoS Med 4:e209
31. Ridge SA, Sludden J, Wei X, Sapone A, Brown O, Hardy S, Canney P, Fernandez-Salguero P, Gonzalez FJ, Cassidy J, McLeod HL (1998) Dihydropyrimidine dehydrogenase pharmacogenetics in patients with colorectal cancer. Br J Cancer 77:497-500
32. Goetz MP, Kamal A, Ames MM (2008) Tamoxifen pharmacoge-nomics: the role of CYP2D6 as a predictor of drug response. Clin Pharmacol Ther 83:160-166
33. Iyer L, Das S, Janisch L, Wen M, Ramirez J, Karrison T, Fleming GF, Vokes EE, Schilsky RL, Ratain MJ (2002) UGT1A1*28 polymorphism as a determinant of irinotecan disposition and toxicity. Pharmacogenomics J 2:43-47
34. Zwaveling J, Press RR, Bredius RG, van Derstraaten TR, den HJ B, IH BJJ, Guchelaar HJ (2008) Glutathione S-transferase polymorphisms are not associated with population pharmaco-kinetic parameters of busulfan in pediatric patients. Ther Drug Monit 30:504-510
35. Mandema JW, Verotta D, Sheiner LB (1992) Building population pharmacokinetic-pharmacodynamic models. I. Models for covariate effects. J Pharmacokinet Biopharm 20:511-528
36. Zandvliet AS, Schellens JH, Beijnen JH, Huitema AD (2008) Population pharmacokinetics and pharmacodynamics for treatment optimization in clinical oncology. Clin Pharmacokinet 47:487-513
37. Zwaveling J, Press RR, Bredius RG, van Derstraaten TR, den HJ B, IH BJJ, Guchelaar HJ (2008) Glutathione S-transferase polymorphisms are not associated with population pharmaco-kinetic parameters of busulfan in pediatric patients. Ther Drug Monit 30:504-510
38. Mandema JW, Verotta D, Sheiner LB (1992) Building population pharmacokinetic-pharmacodynamic models. I. Models for covariate effects. J Pharmacokinet Biopharm 20:511-528