Dasatinib: Is it all in the dose?

BioDrugs

Volumn 24, Issue 3, 2010, Pages 157-163

  Condorelli, Fabrizio ^a   Genazzani, Armando A ^a  

^a UNIVERSITY OF EASTERN PIEDMONT   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

3 BENZYL 7 CYANO 2,3,4,5 TETRAHYDRO 1 (1H IMIDAZOL 4 YLMETHYL) 4 (2 THIENYLSULFONYL) 1H 1,4 BENZODIAZEPINE; BCR ABL PROTEIN; CYCLIN DEPENDENT KINASE INHIBITOR 1A; DASATINIB; DRUG METABOLITE; ERLOTINIB; FLAVOPIRIDOL; HISTONE DEACETYLASE INHIBITOR; IMATINIB; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE 3; MITOGEN ACTIVATED PROTEIN KINASE P38; MULTIDRUG RESISTANCE PROTEIN; NILOTINIB; PROMYELOCYTIC LEUKEMIA PROTEIN; PROTEIN BAD; PROTEIN FARNESYLTRANSFERASE INHIBITOR; PROTEIN KINASE C BETA; PROTEIN TYROSINE KINASE; PROTEIN TYROSINE KINASE INHIBITOR;

ANTINEOPLASTIC ACTIVITY; APOPTOSIS; CANCER STEM CELL; CHRONIC MYELOID LEUKEMIA; CLINICAL TRIAL; DOSAGE SCHEDULE COMPARISON; DRUG DOSE ESCALATION; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG HALF LIFE; DRUG INTERMITTENT THERAPY; DRUG POTENCY; DRUG PULSE THERAPY; DRUG SAFETY; DRUG TOLERABILITY; HUMAN; LEUKEMIA CELL; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; OPTIMAL DRUG DOSE; PLEURA EFFUSION; PRIORITY JOURNAL; REVIEW; THROMBOCYTOPENIA;

ANIMALS; ANTINEOPLASTIC AGENTS; CLINICAL TRIALS AS TOPIC; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG ADMINISTRATION SCHEDULE; HUMANS; LEUKEMIA, MYELOGENOUS, CHRONIC, BCR-ABL POSITIVE; PIPERAZINES; PROTEIN KINASE INHIBITORS; PYRIMIDINES; THIAZOLES;

EID: 77952518004     PISSN: 11738804     EISSN: 1179190X     Source Type: Journal    
DOI: 10.2165/11535870-000000000-00000     Document Type: Review

References (54)

1. Vardiman JW. Chronic myelogenous leukemia, BCR-ABL1+. Am J Clin Pathol 2009 Aug;132(2):250-60
2. McWhirter JR, Galasso DL, Wang JY. A coiled-coil oligomerization domain of Bcr is essential for the transforming function of Bcr-Abl oncoproteins. Mol Cell Biol 1993 Dec;13(12):7587-95
3. Mayer BJ, Baltimore D. Mutagenic analysis of the roles of SH2 and SH3 domains in regulation of the Abl tyrosine kinase. Mol Cell Biol 1994 May;14(5):2883-94
4. McWhirter JR, Wang JY. An actin-binding function contributes to transformation by the Bcr-Abl oncoprotein of Philadelphia chromosome-positive human leukemias. Embo J 1993 Apr;12(4):1533-46
5. Pendergast AM, Quilliam LA, Cripe LD, et al. BCR-ABL-induced oncogenesis is mediated by direct interaction with the SH2 domain of the GRB-2 adaptor protein. Cell 1993 Oct. 8;75(1):175-85
6. Amarante-Mendes GP, Jascur T, Nishioka WK, et al. Bcr-Abl-mediated resistance to apoptosis is independent of PI 3-kinase activity. Cell Death Differ 1997 Oct;4(7):548-54
7. Mandanas RA, Leibowitz DS, Gharehbaghi K, et al. Role of p21 RAS in p210 bcrabl transformation of murine myeloid cells. Blood 1993 Sep. 15;82(6):1838-47
8. Nichols GL, Raines MA, Vera JC, et al. Identification of CRKL as the constitutively phosphorylated 39-kD tyrosine phosphoprotein in chronic myelogenous leukemia cells. Blood 1994 Nov. 1;84(9):2912-8
9. Parada Y. BCR-ABL and interleukin 3 promote haematopoietic cell proliferation and survival through modulation of cyclin D2 and p27Kip1 expression. J Biol Chem 2001 Jun. 22;276(26):23572-80
10. Perrotti D, Cesi V, Trotta R, et al. BCR-ABL suppresses C/EBPalpha expression through inhibitory action of hnRNP E2. Nat Genet 2002 Jan;30(1):48-58
11. Salomoni P, Condorelli F, Sweeney SM, et al. Versatility of BCR/ABL-expressing leukemic cells in circumventing proapoptotic BAD effects. Blood 2000 Jul. 15;96(2):676-84
12. Bhatia R, Munthe HA, Forman SJ. Abnormal growth factor modulation of beta1-integrin-mediated adhesion in chronic myelogenous leukaemia haematopoietic progenitors. Br J Haematol 2001 Dec. 1;115(4):845-53
13. Chen Y-Y, Malik M, Tomkowicz BE, et al. BCR-ABL1 alters SDF-1alphamediated adhesive responses through the beta2 integrin LFA-1 in leukemia cells. Blood 2008 May 15;111(10):5182-6
14. Skorski T, Nieborowska-Skorska M, Wlodarski P, et al. The SH3 domain contributes to BCR/ABL-dependent leukemogenesis in vivo: role in adhesion, invasion, and homing. Blood 1998 Jan 15;91(2):406-18
15. Fernandes MS, Reddy MM, Gonneville JR, et al. BCR-ABL promotes the frequency of mutagenic single-strand annealing DNA repair. Blood 2009 Aug. 27;114(9):1813-9
16. Stoklosa T, Poplawski T, Koptyra M, et al. BCR/ABL inhibits mismatch repair to protect from apoptosis and induce point mutations. Cancer Res 2008 Apr. 15;68(8):2576-80
17. Fang G, Kim CN, Perkins CL, et al. CGP57148B (STI-571) induces differentiation and apoptosis and sensitizes Bcr-Abl-positive human leukemia cells to apoptosis due to antileukemic drugs. Blood 2000 Sep. 15;96(6):2246-53
18. Verweij J, Casali PG, Zalcberg J, et al. Progression-free survival in gastrointestinal stromal tumours with high-dose imatinib: randomised trial. Lancet 2004; 364: 1127-34
19. Larghero J, Leguay T, Mourah S, et al. Relationship between elevated levels of the alpha 1 acid glycoprotein in chronic myelogenous leukemia in blast crisis and pharmacological resistance to imatinib (Gleevec) in vitro and in vivo. Biochem Pharmacol 2003 Nov. 15;66(10):1907-13
20. Kantarjian HM, Talpaz M, Giles F, et al. New insights into the pathophysiology of chronic myeloid leukemia and imatinib resistance. Ann Intern Med 2006 Dec. 19;145(12):913-23 (Pubitemid 351639967)
21. Quintas-Cardama A, Kantarjian HM, Cortes JE. Mechanisms of primary and secondary resistance to imatinib in chronic myeloid leukemia. Cancer Control 2009 Apr;16(2):122-31
22. Li S. Src-family kinases in the development and therapy of Philadelphia chromosome-positive chronic myeloid leukemia and acute lymphoblastic leukemia. Leuk Lymphoma 2008 Jan 1;49(1):19-26
23. Cannell E. Dasatinib is effective inimatinib-resistant CML. Lancet Oncol 2007 Apr;8(4):286
24. Muller MC, Cortes JE, Kim DW, et al. Dasatinib treatment of chronic-phase chronic myeloid leukemia: analysis of responses according to preexisting BCR-ABL mutations. Blood 2009 Dec. 3;114(24):4944-53
25. Konig H, Copland M, Chu S, et al. Effects of dasatinib on Src kinase activity and downstream intracellular signaling in primitive chronic myelogenous leukemia hematopoietic cells. Cancer Res 2008 Dec. 1;68(23):9624-33
26. Steelman LS, Pohnert SC, Shelton JG, et al. JAK/STAT, Raf/MEK/ERK, PI3K/Akt and BCR-ABL in cell cycle progression and leukemogenesis. Leukemia 2004 Feb;18(2):189-218
27. Vajpai N, Strauss A, Fendrich G, et al. Solution conformations and dynamics of ABL kinase-inhibitor complexes determined by NMR substantiate the different binding modes of imatinib/nilotinib and dasatinib. J Biol Chem 2008 Jun. 27;283(26):18292-302
28. Shah NP, Tran C, Lee FY, et al. Overriding imatinib resistance with a novel ABL kinase inhibitor. Science 2004 Jul. 16;305(5682):399-401
29. Tanaka R, Kimura S. Abl tyrosine kinase inhibitors for overriding Bcr-Abl/T315I: from the second to third generation. Expert Rev Anticancer Ther 2008 Sep;8(9):1387-98
30. Luo FR, Yang Z, Camuso A, et al. Dasatinib (BMS-354825) pharmacokinetics and pharmacodynamic biomarkers in animal models predict optimal clinical exposure. Clin Cancer Res 2006 Dec. 1;12(23):7180-6
31. Kamath A, Wang J, Lee F, et al. Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL. Cancer Chemother Pharmacol 2008 Mar;61(3):365-76
32. Kindler T, Breitenbuecher F, Kasper S, et al. In BCR-ABL-positive cells, STAT-5 tyrosine-phosphorylation integrates signals induced by imatinib mesylate and Ara-C. Leukemia 2003 Jun;17(6):999-1009
33. Nam S, Williams A, Vultur A, et al. Dasatinib (BMS-354825) inhibits Stat5 signaling associated with apoptosis in chronic myelogenous leukemia cells. Mol Cancer Ther 2007 Apr. 1;6(4):1400-5
34. Dumka D, Puri P, Carayol N, et al. Activation of the p38 Map kinase pathway is essential for the antileukemic effects of dasatinib. Leuk Lymphoma 2009 Aug. 11; 1-13
35. Nguyen TK, Rahmani M, Harada H, et al. MEK1/2 inhibitors sensitize Bcr/Abl+ human leukemia cells to the dual Abl/Src inhibitor BMS-354/825. Blood 2007 May 1;109(9):4006-15
36. Jørgensen HG, Holyoake TL. Characterization of cancer stem cells in chronic myeloid leukaemia. Biochem Soc Trans 2007 Nov. 1; 35 (Pt 5):1347-51
37. Barnes DJ, Melo JV. Primitive, quiescent and difficult to kill: the role of nonproliferating stem cells in chronic myeloid leukemia. Cell Cycle 2006 Dec;5(24):2862-6
38. Ito K, Bernardi R, Morotti A, et al. PML targeting eradicates quiescent leukaemia-initiating cells. Nature 2008 Jun. 19;453(7198):1072-8
39. Viale A, De Franco F, Orleth A, et al. Cell-cycle restriction limits DNA damage and maintains self-renewal of leukaemia stem cells. Nature 2009 Jan 1;457(7225):51-6
40. Copland M, Pellicano F, Richmond L, et al. BMS-214662 potently induces apoptosis of chronic myeloid leukemia stem and progenitor cells and synergizes with tyrosine kinase inhibitors. Blood 2008 Mar. 1;111(5):2843-53
41. Pellicano F, Copland M, Jorgensen HG, et al. BMS-214662 induces mitochondrial apoptosis in chronic myeloid leukemia (CML) stem/progenitor cells, including CD34+38- cells, through activation of protein kinase Cbeta. Blood 2009 Nov. 5;114(19):4186-96
42. Bornhauser M, Pursche S, BoninM, et al. Elimination of imatinib mesylate and its metabolite N-desmethyl-imatinib [letter]. J Clin Oncol 2005 Jun;23(16):3855-6; author reply 7-8
43. Christopher L, Cui D, Li W, et al. Biotransformation of [14C] dasatinib: in vitro studies in rat, monkey, and human and disposition after administration to rats and monkeys. Drug Metab Dispos 2008 Jul;36(7):1341-56
44. Nicaise C, Wang S, Roy A, et al. Dasatinib pharmacokinetics and exposure-response (E-R): relationships to efficacy and safety in patients with chronic myelogenous leukemia in chronic phase (CML-CP) [abstract no. 1098]. 13th EHA Congress; 2008 Jun. 12-15; Copenhagen
45. Talpaz M, Shah N, Kantarjian H, et al. Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. N Engl J Med 2006 Jun;354(24):2531-41 (Pubitemid 43882349)
46. Shah NP, Kantarjian HM, Kim D-W, et al. Intermittent target inhibition with dasatinib 100mg once daily preserves efficacy and improves tolerability in imatinib-resistant and -intolerant chronic-phase chronic myeloid leukemia. J Clin Oncol 2008 May 12;26(19):3204-12
47. US FDA. FDA grants accelerated approval of a new dosing regimen of dasatinib (Sprycel) 2007 [online]. Available from URL: http://www.fda. gov/AboutFDA/CentersOffices/CDER/ucm129236.htm#at [Accessed 2009 Nov. 20]
48. EMEA. Sprycel summary of product characteristics [online]. Available from URL: http://www.emea.europa.eu/humandocs/PDFs/EPAR/sprycel/H-709-PI-en. pdf [Accessed 2009 Nov. 20]
49. Guilhot F, Roy L. Hematology: dasatinib regimens for patients with chronic myeloid leukemia. Nat Rev Clin Oncol 2009 Dec;6(12):680-2
50. Kantarjian H, Cortes J, Kim DW, et al. Phase 3 study of dasatinib 140mg once daily versus 70mg twice daily in patients with chronic myeloid leukemia in accelerated phase resistant or intolerant to imatinib: 15-month median follow-up. Blood 2009 Jun. 18;113(25):6322-9
51. Nicolau D, Wu A, Finocchiaro S, et al. Once-daily aminoglycoside dosing: impact on requests and costs for therapeutic drug monitoring. Ther Drug Monit 1996 Jun;18(3):263-6
52. Snead JL, O'hare T, Adrian LT, et al. Acute dasatinib exposure commits Bcr-Abl dependent cells to apoptosis. Blood 2009 Aug. 25; 1-24
53. Hiwase DK, White DL, Saunders VA, et al. Short-term intense Bcr-Abl kinase inhibition with nilotinib is adequate to trigger cell death in BCR-ABL (+) cells. Leukemia 2009 Jun;23(6):1205-6
54. Shah NP, Kasap C, Weier C, et al. Transient potent BCR-ABL inhibition is sufficient to commit chronic myeloid leukemia cells irreversibly to apoptosis. Cancer Cell 2008 Dec. 9;14(6):485-93