Skip to main content

Advertisement

Log in

Dasatinib

  • Fresh from the Pipeline
  • Published:

From Nature Reviews Drug Discovery

View current issue Sign up to alerts

In June 2006, the tyrosine kinase inhibitor dasatinib (Sprycel; Bristol-Myers Squibb) was approved by the US FDA for the treatment of adults with chronic myeloid leukaemia and Philadelphia-chromosome-positive acute lymphoblastic leukaemia with resistance or intolerance to previous therapy, including the kinase inhibitor imatinib (Gleevec; Novartis).

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Figure 1

References

  1. Sawyers, C. L. Chronic myeloid leukemia. N. Engl. J. Med. 340, 1330–1340 (1999).

    Article  CAS  Google Scholar 

  2. Capdeville, R. et al. Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug. Nature Rev. Drug Discov. 1, 493–502 (2002).

    Article  CAS  Google Scholar 

  3. Shah, N. P. et al. Multiple BCR–ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell 2, 117–125 (2002).

    Article  CAS  Google Scholar 

  4. Shah, N. P. et al. Overriding imatinib resistance with a novel ABL kinase inhibitor. Science 305, 399–401 (2004).

    Article  CAS  Google Scholar 

  5. Lombardo, L. J. 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. 47, 6658–6661 (2004).

    Article  CAS  Google Scholar 

  6. Tokarski, J. S. 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. 66, 5790–5797 (2006).

    Article  CAS  Google Scholar 

  7. Talpaz, M. et al. Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. N. Engl. J. Med. 354, 2531–2541 (2006).

    Article  CAS  Google Scholar 

  8. FDA labelling information, [online] (2006).

  9. Ptasznik, A. et al. Short interfering RNA (siRNA) targeting the Lyn kinase induces apoptosis in primary, and drug-resistant, BCR–ABL1(+) leukemia cells. Nature Med. 10, 1187–1189 (2004).

    Article  CAS  Google Scholar 

  10. Donato, N. J. et al. BCR–ABL independence and LYN kinase overexpression in chronic myelogenous leukemia cells selected for resistance to STI571. Blood 101, 690–698 (2003).

    Article  CAS  Google Scholar 

  11. Druker, B. J. et al. Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of BCR–ABL positive cells. Nature Med. 2, 561–566 (1996).

    Article  CAS  Google Scholar 

  12. Kantarjian, H. et al. Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL. N. Engl. J. Med. 354, 2542–2551 (2006).

    Article  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Kantarjian, H., Jabbour, E., Grimley, J. et al. Dasatinib. Nat Rev Drug Discov 5, 717–718 (2006). https://doi.org/10.1038/nrd2135

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1038/nrd2135

  • Springer Nature Limited

This article is cited by

Navigation