Bosutinib: a dual SRC/ABL kinase inhibitor for the treatment of chronic myeloid leukemia

References

• Sattler M, Scheijen B, Weisberg E, Griffin JD. Mutated tyrosine kinases as therapeutic targets in myeloid leukemias. Adv. Exp. Med. Biol.532, 121–140(2003).
   PubMed Web of Science ®Google Scholar
• Buchdunger E, Zimmermann J, Mett H et al. Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative. Cancer Res.56(1), 100–104(1996).
   PubMed Web of Science ®Google Scholar
• Deininger MW, O’Brien SG, Ford JM, Druker BJ. Practical management of patients with chronic myeloid leukemia receiving imatinib. J. Clin. Oncol.21(8), 1637–1647(2003).
   PubMed Web of Science ®Google Scholar
• O’Brien SG, Guilhot F, Goldman JM et al. International Randomized Study of Interferon Versus STI571 (IRIS) 7-year follow-up: sustained survival, low rate of transformation and increased rate of major molecular response (MMR) in patients (pts) with newly diagnosed chronic myeloid leukemia in chronic phase (CML-CP) treated with imatinib (IM). Proc. Am. Soc. Hematol.(2008) (Abstract 186).
   Google Scholar
• Sawyers CL, Hochhaus A, Feldman E et al. Imatinib induces hematologic and cytogenetic responses in patients with chronic myelogenous leukemia in myeloid blast crisis: results of a Phase II study. Blood99(10), 3530–3539(2002).
   PubMed Web of Science ®Google Scholar
• Deininger M, Buchdunger E, Druker BJ. The development of imatinib as a therapeutic agent for chronic myeloid leukemia. Blood105(7), 2640–2653(2005).
   PubMed Web of Science ®Google Scholar
• Corbin AS, La Rosee P, Stoffregen EP, Druker BJ, Deininger MW. Several Bcr–Abl kinase domain mutants associated with imatinib mesylate resistance remain sensitive to imatinib. Blood101(11), 4611–4614(2003).
   PubMed Web of Science ®Google Scholar
• Shah NP, Tran C, Lee FY, Chen P, Norris D, Sawyers CL. Overriding imatinib resistance with a novel ABL kinase inhibitor. Science305(5682), 399–401(2004).
   PubMed Web of Science ®Google Scholar
• Kantarjian HM, Giles F, Gattermann N et al. Nilotinib (formerly AMN107), a highly selective BCR–ABL tyrosine kinase inhibitor, is effective in patients with Philadelphia chromosome-positive chronic myelogenous leukemia in chronic phase following imatinib resistance and intolerance. Blood110(10), 3540–3546(2007).
   PubMed Web of Science ®Google Scholar
• 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. Blood109(12), 5143–5150(2007).
   PubMed Web of Science ®Google Scholar
• 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.14(2), 352–359(2008).
   PubMed Web of Science ®Google Scholar
• 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. Blood109(6), 2303–2309(2007).
   PubMed Web of Science ®Google Scholar
• 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.26(19), 3204–3212(2008).
   PubMed Web of Science ®Google Scholar
• Boschelli DH, Ye F, Wang YD et al. Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J. Med. Chem.44(23), 3965–3977(2001).
   PubMed Web of Science ®Google Scholar
• Boschelli DH. Exploitation of the 3-quinolinecarbonitrile template for SRC tyrosine kinase inhibitors. Curr. Top. Med. Chem.8(10), 922–934(2008).
   PubMed Web of Science ®Google Scholar
• Puttini M, Coluccia AM, Boschelli F et al.in vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells. Cancer Res.66(23), 11314–11322(2006).
   PubMed Web of Science ®Google Scholar
• Thomas SM, Brugge JS. Cellular functions regulated by Src family kinases. Annu. Rev. Cell. Dev. Biol.13, 513–609(1997).
   PubMed Web of Science ®Google Scholar
• Summy JM, Gallick GE. Src family kinases in tumor progression and metastasis. Cancer Metastasis Rev.22(4), 337–358(2003).
   PubMed Web of Science ®Google Scholar
• Johnson FM, Gallick GE. SRC family nonreceptor tyrosine kinases as molecular targets for cancer therapy. Anticancer Agents Med. Chem.7(6), 651–659(2007).
   PubMed Web of Science ®Google Scholar
• Li S. Src-family kinases in the development and therapy of Philadelphia chromosome-positive chronic myeloid leukemia and acute lymphoblastic leukemia. Leuk. Lymphoma49(1), 19–26(2008).
   PubMed Web of Science ®Google Scholar
• Golas JM, Lucas J, Etienne C et al. SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models. Cancer Res.65(12), 5358–5364(2005).
   PubMed Web of Science ®Google Scholar
• Laneuville P. Abl tyrosine protein kinase. Semin. Immunol.7(4), 255–266(1995).
   PubMedGoogle Scholar
• Pendergast AM. Nuclear tyrosine kinases: from Abl to WEE1. Curr. Opin. Cell Biol.8(2), 174–181(1996).
   PubMed Web of Science ®Google Scholar
• Chung SW, Daniel R, Wong BY, Wong PM. The ABL genes in normal and abnormal cell development. Crit. Rev. Oncog.7(1–2), 33–48(1996).
   PubMed Web of Science ®Google Scholar
• Golas JM, Arndt K, Etienne C et al. SKI-606, a 4-anilino-3-quinolinecarbonitrile dual inhibitor of Src and Abl kinases, is a potent antiproliferative agent against chronic myelogenous leukemia cells in culture and causes regression of K562 xenografts in nude mice. Cancer Res.63(2), 375–381(2003).
   PubMed Web of Science ®Google Scholar
• Remsing Rix LL, Rix U, Colinge J et al. Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia23(3), 477–485(2009).
   PubMed Web of Science ®Google Scholar
• Mancini M, Brusa G, Zuffa E et al. Persistent Cdk2 inactivation drives growth arrest of BCR–ABL-expressing cells in response to dual inhibitor of SRC and ABL kinases SKI606. Leuk. Res.31(7), 979–987(2007).
   PubMed Web of Science ®Google Scholar
• Redaelli S, Piazza R, Rostagno R et al. Activity of bosutinib, dasatinib, and nilotinib against 18 imatinib-resistant BCR/ABL mutants. J. Clin. Oncol.27(3), 469–471(2009).
   PubMed Web of Science ®Google Scholar
• Cortes J, Kantarjian HM, Kim DW et al. Efficacy and safety of bosutinib (SKI-606) in patients with chronic phase (CP) Ph+ chronic myelogenous leukemia (CML) with resistance or intolerance to imatinib. Proc. Am. Soc. Hematol. (2008) (Abstract 1098).
   Google Scholar
• Gambacorti-Passerini C, Pogliani EM, Baccarani M et al. Bosutinib (SKI-606) Demonstrates clinical activity and is well tolerated in patients with AP and BP CML and Ph+ ALL. Proc .Am. Soc. Hematol. (2008) (Abstract 1101).
   Google Scholar
• Quintas-Cardama A, Cortes J. Management of patients with resistant or refractory chronic myelogenous leukemia. Oncology (Williston Park)22(4), 430–437(2008).
   PubMed Web of Science ®Google Scholar
• Quintas-Cardama A, Cortes J. Tailoring tyrosine kinase inhibitor therapy to tackle specific BCR–ABL1 mutant clones. Leuk. Res.32(8), 1313–1316(2008).
   PubMed Web of Science ®Google Scholar
• Bartolovic K, Balabanov S, Hartmann U et al. Inhibitory effect of imatinib on normal progenitor cells in vitro. Blood103(2), 523–529(2004).
   PubMed Web of Science ®Google Scholar
• Konig H, Holyoake TL, Bhatia R. Effective and selective inhibition of chronic myeloid leukemia primitive hematopoietic progenitors by the dual Src/Abl kinase inhibitor SKI-606. Blood111(4), 2329–2338(2008).
   PubMed Web of Science ®Google Scholar
• Hu Y, Swerdlow S, Duffy TM, Weinmann R, Lee FY, Li S. Targeting multiple kinase pathways in leukemic progenitors and stem cells is essential for improved treatment of Ph+ leukemia in mice. Proc. Natl Acad. Sci. USA103(45), 16870–16875(2006).
   PubMed Web of Science ®Google Scholar
• Ptasznik A, Nakata Y, Kalota A, Emerson SG, Gewirtz AM. Short interfering RNA (siRNA) targeting the Lyn kinase induces apoptosis in primary, and drug-resistant, BCR–ABL1(+) leukemia cells. Nat. Med.10(11), 1187–1189(2004).
   PubMed Web of Science ®Google Scholar
• 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. Blood107(11), 4532–4539(2006).
   PubMed Web of Science ®Google Scholar
• Gleixner KC, Remsing LL, Baumgartner C et al. Effects of bosutinib (SKI-606) in CML: kinase target profile, effects on bcr/abl mutants, and synergism with dasatinib in T315I+ cells. Proc. Am. Soc. Hematol. (2008) (Abstract 3195).
   Google Scholar
• Gontarewicz A, Balabanov S, Keller G et al. Simultaneous targeting of Aurora kinases and BCR–Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR–ABL mutations including T315I. Blood111(8), 4355–4364(2008).
   PubMed Web of Science ®Google Scholar
• O’Hare T, Eide CA, Deininger MW. New BCR–Abl inhibitors in chronic myeloid leukemia: keeping resistance in check. Expert Opin. Investig. Drugs17(6), 865–878(2008).
   PubMed Web of Science ®Google Scholar
• Essers MA, Offner S, Blanco-Bose WE et al. IFNα activates dormant haematopoietic stem cells in vivo. Nature458(7240), 904–908(2009).
   PubMed Web of Science ®Google Scholar