Dasatinib in chronic myeloid leukemia: A review

Therapeutics and Clinical Risk Management

Volumn 5, Issue 1, 2009, Pages 281-289

  Aguilera, Dolly G ^a   Tsimberidou, Apostolia M ^b  

^a NORTHWESTERN UNIVERSITY   (United States)

^b UNIVERSITY OF TEXAS MD ANDERSON CANCER CENTER   (United States)

Author keywords

BCR ABL; Chronic myeloid leukemia; Dasatininb; Tyrosine kinase inhibitor

Indexed keywords

4 (3 DIMETHYLAMINO 1 PYRROLIDINYLMETHYL) 3 TRIFLUOROMETHYL N [4 METHYL 3 [[4 (5 PYRIMIDINYL) 2 PYRIMIDINYL]AMINO]PHENYL]BENZAMIDE; ANTIFUNGAL AGENT; ANTIRETROVIRUS AGENT; BCR ABL PROTEIN; BOSUTINIB; CHOLESTEROL; CREATININE; CYCLOPROPANECARBOXYLIC ACID [4 [4 (4 METHYL 1 PIPERAZINYL) 6 (5 METHYL 2H PYRAZOL 3 YLAMINO) 2 PYRIMIDINYLTHIO]PHENYL]AMIDE; DASATINIB; DIURETIC AGENT; IMATINIB; MACROLIDE; MOLECULAR MARKER; NILOTINIB; PROTEIN SERINE THREONINE KINASE; PROTEIN TYROSINE KINASE; PROTEIN TYROSINE KINASE INHIBITOR; STEROID; TRIACYLGLYCEROL;

ABDOMINAL PAIN; AMINO ACID SUBSTITUTION; ANEMIA; ANOREXIA; ANUS FISSURE; APPETITE DISORDER; ASCITES; BONE MARROW SUPPRESSION; BRAIN HEMORRHAGE; CARDIOTOXICITY; CHOLESTEROL BLOOD LEVEL; CHRONIC LEUKEMIA; CHRONIC MYELOID LEUKEMIA; COLITIS; CONSTIPATION; CREATININE BLOOD LEVEL; CYTOGENETICS; DIARRHEA; DIGESTIVE SYSTEM ULCER; DOSAGE SCHEDULE COMPARISON; DRUG APPROVAL; DRUG DOSE COMPARISON; DRUG DOSE ESCALATION; DRUG DOSE REDUCTION; DRUG EFFICACY; DRUG HYPERSENSITIVITY; DRUG TARGETING; DRUG WITHDRAWAL; DYSPHAGIA; EDEMA; ENZYME INHIBITION; ESOPHAGITIS; FATIGUE; FEBRILE NEUTROPENIA; FEVER; FLUID RETENTION; FOOD AND DRUG ADMINISTRATION; GASTROINTESTINAL HEMORRHAGE; GENE MUTATION; GYNECOMASTIA; HEMATOPOIETIC STEM CELL TRANSPLANTATION; HUMAN; HYPOCALCEMIA; HYPOPHOSPHATEMIA; LUNG EDEMA; MENSTRUATION DISORDER; MUCOSA INFLAMMATION; NAUSEA; NEUROTOXICITY; NEUTROPENIA; NONHUMAN; ONCOGENE; PANCREATITIS; PERICARDIAL EFFUSION; PERIPHERAL EDEMA; PLEURA EFFUSION; PROGRESSION FREE SURVIVAL; PULMONARY HYPERTENSION; RECOMMENDED DRUG DOSE; REVIEW; SIDE EFFECT; SKIN TOXICITY; STOMATITIS; THROMBOCYTOPENIA; TREATMENT FAILURE; TREATMENT RESPONSE; TRIACYLGLYCEROL BLOOD LEVEL; VERTIGO; VOMITING;

EID: 77949439646     PISSN: 11766336     EISSN: 1178203X     Source Type: Journal    
DOI: None     Document Type: Review

References (52)

1. Goldman JM, Melo JV. Chronic myeloid leukemia-advances in biology and new approaches to treatment. N Engl J Med. 2003;349:1451-1464.
2. Kurzrock R, Gutterman JU, Talpaz M. The molecular genetics of Philadelphia chromosome-positive leukemias. N Engl J Med. 1988;319: 990-998.
3. Calabretta B, Perrotti D. The biology of CML blast crisis. Blood. 2004;103:4010-4022.
4. Druker BJ, Tamura S, Buchdunger E, et al. Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells. Nat Med. 1996;2:561-566.
5. Sawyers CL. Chronic myeloid leukemia. N Engl J Med. 1999;340: 1330-1340.
6. Cohen MH, Williams G, Johnson JR, et al. Approval summary for imatinib mesylate capsules in the treatment of chronic myelogenous leukemia. Clin Cancer Res. 2002;8:935-942.
7. Gambacorti-Passerini C, le Coutre P, Mologni L, et al. Inhibition of the ABL kinase activity blocks the proliferation of BCR/ABL+ leukemic cells and induces apoptosis. Blood Cells Mol Dis. 1997;23: 380-394.
8. Druker J, O'Brien S, Larson RA. Long-term benefits of imatinib (IM) for patients newly diagnosed with chronic myelogenous leukemia in chronic phase (CML-CP): The 5-year update from the IRIS study. J Clin Oncol. (Meeting Abstracts) 2006;24(18S P1): Abstract 6506.
9. Hochhaus A, Druker BJ, Larson R, O'Brien SG, Gathmann I, Guilhot F. IRIS 6-year follow-up: Sustained survival and declining annual rate of transformation in patients with newly diagnosed chronic myeloid leukemia in chronic phase (CML-CP) treated with imatinib (abstract 25). Blood. 2007;110. p. 16a.
10. O'Brien SG, Guilhot F, Larson RA, et al. Imatinib compared with interferon and low-dose cytarabine for newly diagnosed chronic-phase chronic myeloid leukemia. N Engl J Med. 2003;348:994-1004.
11. Baccarani M, Saglio G, Goldman J, et al. Evolving concepts in the management of chronic myeloid leukemia: recommendations from an expert panel on behalf of the European LeukemiaNet. Blood. 2006;108:1809-1820.
12. Shah NP, Sawyers CL. Mechanisms of resistance to STI571 in Philadelphia chromosome-associated leukemias. Oncogene. 2003;22:7389-7395.
13. Gorre ME, Mohammed M, Ellwood K, et al. Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science. 2001;293:876-880.
14. Soverini S, Martinelli G, Rosti G, et al. ABL mutations in late chronic phase chronic myeloid leukemia patients with up-front cytogenetic resistance to imatinib are associated with a greater likelihood of progression to blast crisis and shorter survival: a study by the GIMEMA Working Party on Chronic Myeloid Leukemia. J Clin Oncol. 2005;23:4100-4109.
15. Cowan-Jacob SW, Guez V, Fendrich G, et al. Imatinib (STI571) resistance in chronic myelogenous leukemia: molecular basis of the underlying mechanisms and potential strategies for treatment. Mini Rev Med Chem. 2004;4:285-299.
16. Hochhaus A, Kreil S, Corbin AS, et al. Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy. Leukemia. 2002;16:2190-2196.
17. Illmer T, Schaich M, Platzbecker U, et al. P-glycoprotein-mediated drug efflux is a resistance mechanism of chronic myelogenous leukemia cells to treatment with imatinib mesylate. Leukemia. 2004;18:401-408.
18. Thomas J, Wang L, Clark RE, Pirmohamed M. Active transport of imatinib into and out of cells: implications for drug resistance. Blood. 2004;104:3739-3745.
19. Gambacorti-Passerini C, Barni R, le Coutre P, et al. Role of alpha1 acid glycoprotein in the in vivo resistance of human BCR-ABL(+) leukemic cells to the abl inhibitor STI571. J Natl Cancer Inst. 2000;92:1641-1650.
20. Burger H, van Tol H, Boersma AW, et al. Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004;104:2940-2942.
21. Rix U, Hantschel O, Durnberger G, et al. Chemical proteomic profiles of the BCR-ABL inhibitors imatinib, nilotinib, and dasatinib reveal novel kinase and nonkinase targets. Blood. 2007;110: 4055-4063.
22. Shah NP, Tran C, Lee FY, Chen P, Norris D, Sawyers CL. Overriding imatinib resistance with a novel ABL kinase inhibitor. Science. 2004;305:399-401.
23. O'Hare T, Walters DK, Stoffregen EP, et al. In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res. 2005;65:4500-4505.
24. Muller MC, Cortes J, Kim D-W, et al. Dasatinib efficacy in patients with chronic myeloid leukemia in chronic phase and preexisting BCR-ABL mutations (abstract 449). Blood. 2008;112(11):171.
25. Redaelli S, Piazza R, Rostagno R, et al. Activity of bosutinib, dasatinib, and nilotinib against 18 imatinib-resistant BCR/ABL mutants. J Clin Oncol. 2009;27:469-471.
26. Apperley JF. Part I: mechanisms of resistance to imatinib in chronic myeloid leukaemia. Lancet Oncol. 2007;8:1018-1029.
27. Tokarski JS, Newitt JA, Chang CY, et al. The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants. Cancer Res. 2006;66:5790-5797.
28. Brave M, Goodman V, Kaminskas E, et al. Sprycel for chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia resistant to or intolerant of imatinib mesylate. Clin Cancer Res. 2008;14:352-359.
29. Lombardo LJ, Lee FY, Chen P, et al. Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4-ylamino) thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem. 2004;47:6658-6661.
30. Konig H, Copland M, Chu S, Jove R, Holyoake TL, Bhatia R. Effects of dasatinib on Src kinase activity and downstream intracellular signaling in primitive chronic myelogenous leukemia hematopoietic cells. Cancer Res. 2008;68:9624-9633.
31. 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;14:485-493.
32. Copland M, Hamilton A, Elrick LJ, et al. Dasatinib (BMS-354825) targets an earlier progenitor population than imatinib in primary CML but does not eliminate the quiescent fraction. Blood. 2006;107: 4532-4539.
33. Kim DH, Kamel-Reid S, Chang H, et al. Natural killer or natural killer/T cell lineage large granular lymphocytosis associated with dasatinib therapy for Philadelphia chromosome positive leukemia. Haematologica. 2009;94:135-139.
34. Porkka K, Koskenvesa P, Lundan T, et al. Dasatinib crosses the blood-brain barrier and is an ef. cient therapy for central nervous system Philadelphia chromosome-positive leukemia. Blood. 2008;112: 1005-1012.
35. Kamath AV, Wang J, Lee FY, Marathe PH. 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;61:365-376.
36. Brendel C, Scharenberg C, Dohse M, et al. Imatinib mesylate and nilotinib (AMN107) exhibit high-affinity interaction with ABCG2 on primitive hematopoietic stem cells. Leukemia. 2007;21:1267-1275.
37. Talpaz M, Shah NP, Kantarjian H, et al. Dasatinib in imatinibresistant Philadelphia chromosome-positive leukemias. N Engl J Med. 2006;354:2531-2541.
38. Guilhot F, Apperley J, Kim DW, et al. Dasatinib induces significant hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in accelerated phase. Blood. 2007;109:4143-4150.
39. Cortes J, Rousselot P, Kim DW, et al. Dasatinib induces complete hematologic and cytogenetic responses in patients with imatinib-resistant or -intolerant chronic myeloid leukemia in blast crisis. Blood. 2007;109:3207-3213.
40. Hochhaus A, Kantarjian HM, Baccarani M, et al. Dasatinib induces notable hematologic and cytogenetic responses in chronic-phase chronic myeloid leukemia after failure of imatinib therapy. Blood. 2007;109:2303-2309.
41. Kantarjian H, Pasquini R, Hamerschlak N, et al. Dasatinib or high-dose imatinib for chronic-phase chronic myeloid leukemia after failure of first-line imatinib: a randomized phase 2 trial. Blood. 2007;109:5143-5150.
42. Ottmann O, Dombret H, Martinelli G, et al. Dasatinib induces rapid hematologic and cytogenetic responses in adult patients with Philadelphia chromosome positive acute lymphoblastic leukemia with resistance or intolerance to imatinib: interim results of a phase 2 study. Blood. 2007;110:2309-2315.
43. Shah NP, Kantarjian HM, Kim DW, et al. Intermittent target inhibition with dasatinib 100 mg once daily preserves efficacy and improves tolerability in imatinib-resistant and -intolerant chronic-phase chronic myeloid leukemia. J Clin Oncol. 2008;26:3204-3212.
44. Quintas-Cardama A, Kantarjian H, Jones D, et al. Dasatinib (BMS-354825) is active in Philadelphia chromosome-positive chronic myelogenous leukemia after imatinib and nilotinib (AMN107) therapy failure. Blood. 2007;109:497-499.
45. Cang S, Liu D. P-loop mutations and novel therapeutic approaches for imatinib failures in chronic myeloid leukemia. J Hematol Oncol. 2008;1:15.
46. Jones D, Kamel-Reid S, Bahler D, et al. Laboratory practice guidelines for detecting and reporting BCR-ABL drug resistance mutations in chronic myelogenous leukemia and acute lymphoblastic leukemia: a report of the Association for Molecular Pathology. J Mol Diagn. 2009;11:4-11.
47. Hughes T, Deininger M, Hochhaus A, et al. Monitoring CML patients responding to treatment with tyrosine kinase inhibitors: review and recommendations for harmonizing current methodology for detecting BCR-ABL transcripts and kinase domain mutations and for expressing results. Blood. 2006;108:28-37.
48. Soverini S, Martinelli G, Colarossi S, et al. Presence or the emergence of a F317L BCR-ABL mutation may be associated with resistance to dasatinib in Philadelphia chromosome-positive leukemia. J Clin Oncol. 2006;24:e51-e2.
49. Melo J, Chuah C. Novel agents in CML therapy: tyrosine kinase inhibitors and beyond. Am Soc Hematol. 2008:427-435.
50. 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;111:2843-2853.
51. Hochhaus A, Baccarani M, Deininger M, et al. Dasatinib induces durable cytogenetic responses in patients with chronic myelogenous leukemia in chronic phase with resistance or intolerance to imatinib. Leukemia. 2008;22:1200-1206.
52. Cortes J, Kim DW, Raffoux E, et al. Efficacy and safety of dasatinib in imatinib-resistant or -intolerant patients with chronic myeloid leukemia in blast phase. Leukemia. 2008;22:2176-2183.