Skip to main content

Advertisement

SpringerLink
Log in

Molecular-Genetic Basis of Gastrointestinal Stromal Tumor Personalized Therapy by Receptor Tyrosine Kinase Inhibitors (A Review)

  • MOLECULAR-BIOLOGICAL PROBLEMS OF DRUG DESIGN AND MECHANISM OF DRUG ACTION
  • Published:
Pharmaceutical Chemistry Journal Aims and scope

Studies of the pharmacotherapy of gastro-intestinal stromal tumor as examples of personalized medicine are reviewed. Peculiarities of the use of imatinib, sunitinib, and regorafenib, which inhibit the ATP-biding domain of tyrosine kinase KIT receptor, which largely determines the development of resistance to all three drugs, are considered. Characteristics of the recently approved drugs ripretinib (inhibiting the KIT receptor activation loop, which increases the sensitivity spectrum among various mutations) and avapritinib (inhibitor for PDGFRa mutant tumors) are also discussed. The new drugs together with the well-known three make it possible to offer patients an individual treatment scenario depending on the particular mutation.

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

Access this article

Log in via an institution

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

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1.
Fig. 2.
Fig. 3.
Fig. 4.
Fig. 5.
Fig. 6.
Fig. 7.
Fig. 8.

Similar content being viewed by others

References

  1. I. I. Dedov, A. N. Tyul’pakov, V. P. Chekhonin, et al., Vestn. Ross. Akad. Med. Nauk, 67(12), 4 – 12 (2012).

    Article  Google Scholar 

  2. R. A. Khvastunov, G. V. Skrypnikov, and A. A. Usachev, Lek. Vestn., 8, No. 4(56), 3 – 10 (2014).

  3. T. Hunter, Cell, 100(1), 113 – 127 (2000).

    Article  PubMed  CAS  Google Scholar 

  4. M. H. Cohen, G. Williams, J. R. Johnson, et al., Clin. Cancer Res., 8(5), 935 – 942 (2002).

    PubMed  CAS  Google Scholar 

  5. K. F. Croom and C. M. Perry, Drugs, 63(5), 513 – 522 (2003).

    Article  PubMed  CAS  Google Scholar 

  6. R. P. DeMatteo, J. J. Lewis, D. Leung, et al., Ann. Surg., 231(1), 51 – 63 (2000).

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  7. C. L. Corless, C. M. Barnett, and M. C. Heinrich, Nat. Rev. Cancer, 11(12), 865 – 878 (2011).

    Article  PubMed  CAS  Google Scholar 

  8. T. Niinuma, H. Suzuki, and T. Sugai, Transl. Gastroenterol. Hepatol., 3(1), 40 – 57 (2018).

    Google Scholar 

  9. T. Nishida, J.-Y. Blay, S. Hirota, et al., Gastric Cancer, 19(1), 3 – 14 (2016).

    Article  PubMed  CAS  Google Scholar 

  10. A. Chou, J. Chen, A. Clarkson, et al., Mod. Pathol., 25(9), 1307 – 1313 (2012).

    Article  PubMed  CAS  Google Scholar 

  11. K. S. Bhullar, N. O. Lagaron, E. M. McGowan, et al., Mol. Cancer, 11(1), 48 (2018).

    Article  CAS  Google Scholar 

  12. R. Roskoski, Pharmacol. Res., 144, 19 – 50 (2019).

    Article  PubMed  CAS  Google Scholar 

  13. R. Roskoski, Pharmacol. Res., 103, 26 – 48 (2016).

    Article  PubMed  CAS  Google Scholar 

  14. C.-H. Heldin, J. Lennartsson, and B. Westermark, J. Intern. Med., 283(1), 16 – 44 (2018).

    CAS  Google Scholar 

  15. A. Kazlauskas, Gene, 614, 1 – 7 (2017).

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  16. R. Bhatia, Chronic Myeloid Leukemia, Hematology (Seventh Ed.), R. Hoffman, E. J. Benz, Jr., and S. Ali Abutalib (eds.), Elsevier (2018), pp. 1055 – 1070.

  17. H.-Z. Ying, Q. Chen,W.-Y. Zhang, et al., Mol. Med. Rep., 16(6), 7879 – 7889 (2017).

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  18. M. P. Nikulin, P. P. Arkhiri, L. Yu. Vladimirova, et al., Practical Recommendations for Medical Treatment of Gastro-intestinal Stromal Tumors [in Russian], Moscow (2019), pp. 477 – 485.

  19. J. Verweij, P. G. Casali, and J. Zalcbergetal, Lancet, 364(9440), 1127 – 1134 (2004).

    Article  PubMed  CAS  Google Scholar 

  20. S. Patel, Cancer Chemother. Pharmacol., 72(2), 277 – 286 (2013).

    Article  PubMed  CAS  Google Scholar 

  21. J. F. Emile, S. Brahimi, J. M. Coindre, et al., Med. Oncol., 29(3), 1765 – 1772 (2012).

    Article  PubMed  CAS  Google Scholar 

  22. H. Joensuu, M. Eriksson, K. S. Hall, et al., J. Am. Med. Assoc., 307(12), 1265 – 1272 (2012).

    Article  CAS  Google Scholar 

  23. R. P. DeMatteo, K. V. Ballman, C. R. Antonescu, et al., Lancet, 373(9669), 1097 – 1104 (2009).

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  24. G. D. Demetri, R. Benjamin, C. D. Blanke, et al., J. Natl. Compr. Cancer Network, 2 (suppl. 1), 27 – 30 (2004).

    Google Scholar 

  25. R. Chetty and S. Serra, J. Clin. Pathol., 69(9), 754 – 760 (2016).

    CAS  Google Scholar 

  26. M. A. Babaei, B. Kamalidehghan, M. Saleem, et al., Drug Des., Dev. Ther., 10, 2443 – 2459 (2016).

  27. M. von Mehren and H. Joensuu, J. Clin. Oncol., 36(2), 136 – 143 (2018).

    Google Scholar 

  28. Ph. A. Cassier, E. Fumagalli, P. Rutkowski, et al., Clin. Cancer Res., 18(16), 4458 – 4464 (2012).

    Article  PubMed  CAS  Google Scholar 

  29. D. A. Filonenko, B. M. Medvedeva, and A. A. Meshcheryakov, J. Mod. Oncol., 22(4), 96 – 100 (2021).

    Google Scholar 

  30. C. D. Blanke, G. D. Demetri, M. von Mehren, et al., J. Clin. Oncol., 26(4), 620 – 625 (2008).

    Article  PubMed  CAS  Google Scholar 

  31. G. D. Demetri, M. von Mehren, C. D. Blanke, et al., N. Engl. J. Med., 347(7), 472 – 480 (2002).

    Article  PubMed  CAS  Google Scholar 

  32. B. D. Smith, M. D. Kaufman, W.-P. Lu, et al., Cancer Cell, 35(5), 738 – 751 (2019).

    Article  PubMed  CAS  Google Scholar 

  33. G. D. Demetri, P. Reichardt, Y.-K. Kang, et al., Lancet, 381(9863), 295 – 302 (2013).

    Article  PubMed  CAS  Google Scholar 

  34. K. Ohshima, K. Fujiya, T. Nagashima, S. Ohnami, et al., Cancer Sci., 110(12), 3821 – 3833 (2019).

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  35. C. Serrano, A. Marino-Enriquez, D. L. Tao, et al., Br. J. Cancer, 120(6), 612 – 620 (2019).

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  36. A. W. Gramza, C. L. Corless, and M. C. Heinrich, Clin. Cancer Res., 15(24), 7510 – 7518 (2009).

    Article  PubMed  CAS  Google Scholar 

  37. V. L. Goodman, E. P. Rock, R. Dagher, et al., Clin. Cancer Res., 13(5), 1367 – 1373 (2007).

    Article  PubMed  CAS  Google Scholar 

  38. D. Ferraro and J. Zalcberg, Ther. Adv. Med. Oncol., 6(5), 222 – 228 (2014).

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  39. S. Patel, Curr. Oncol. Rep., 15(4), 386 – 395 (2013).

    Article  PubMed  CAS  Google Scholar 

  40. S. Boichuk, P. Dunaev, A. Galembikova, et al., Anti-Cancer Drugs, 29(6), 549 – 559 (2018).

    Article  PubMed  CAS  Google Scholar 

  41. Y. Duan, J. Haybaeck, and Z. Yang, Cancers, 12(10), 1 – 21 (2018).

    Google Scholar 

  42. Ph. Zook, H. B. Pathak, M. G. Belinsky, et al., Clin. Cancer Res., 23(1), 171 – 180 (2017).

    Article  PubMed  CAS  Google Scholar 

  43. S. Dhillon, Drugs, 80(4), 433 – 439 (2020).

    Article  PubMed  CAS  Google Scholar 

  44. J.-Y. Blay, C. Serrano, M. C. Heinrich, et al., Lancet Oncol., 21(7), 923 – 934 (2020).

    Article  PubMed  CAS  PubMed Central  Google Scholar 

  45. C. P. Joseph, S. N. Abaricia, M. A. Angelis, et al., Oncologist, 25(1), 1 – 10 (2021).

    Google Scholar 

  46. M. C. Heinrich, R. L. Jones, M. von Mehren, et al., Lancet Oncol., 21(7), 935 – 946 (2020).

    Article  PubMed  CAS  Google Scholar 

  47. R. L. Jones, C. Serrano, M. von Mehren, et al., Eur. J. Cancer., 145, 132 – 142 (2021).

    Article  PubMed  CAS  Google Scholar 

  48. S. George, R. L. Jones, S. Bauer, et al., Oncologist, online (2021).

    Google Scholar 

  49. P. G. Casali, N. Abecassis, H. T. Aro, et al., Ann. Oncol., 29 (suppl 4), 68 – 78 (2018).

    Article  Google Scholar 

  50. B. Peng, P. Lloyd, and H. Schran, Clin. Pharmacokinet., 44(9), 879 – 894 (2005).

    Article  PubMed  CAS  Google Scholar 

  51. J. B. Rey, V. Launay-Vacher, and C. Tournigand, Target. Oncol., 10(2), 199 – 213 (2015).

    Article  PubMed  Google Scholar 

  52. B. I. Rin, Expert. Opin. Pharmacother., 8(14), 2359 – 2369 (2007).

    Article  Google Scholar 

  53. J. Nemunaitis, S. Bauer, J.-Y. Blay, et al., Future Oncol., 16(1), 4251 – 4264 (2019).

    Article  PubMed  CAS  Google Scholar 

  54. F. Janku, A. R. A. Razak, P. Chi, et al., J. Clin. Oncol., 38(28), 3294 – 3303 (2020).

    Article  PubMed  CAS  PubMed Central  Google Scholar 

  55. FDA, Highlights of Prescribing Information: QINLOCK, pp. 1 – 18 (2020).

  56. J. Falkenhorst, R. Hamacher, and S. Bauer, Curr. Opin. Oncol., 31(4), 322 – 328 (2019).

    Article  PubMed  CAS  Google Scholar 

  57. A. Mazzocca, A. Napolitano, M. Silletta, et al., Ther. Adv. Med. Oncol., 11 (2019).

  58. C. Serrano, S. George, C. Valverde, et al., Target. Oncol., 12(3), 277 – 288 (2017).

    Article  PubMed  Google Scholar 

  59. L. V. Ektova, V. A. Eremina, N. I. Tikhonova, et al., Khim.-farm. Zh., 54(5), 26 – 29 (2020); Pharm. Chem. J., 54(5), 455 – 458 (2020).

Download references

Author information

Authors and Affiliations

  1. N. I. Pirogov National Research Medical University, Ministry of Health of Russia, 1 Ostrovityanova St, Moscow, 117997, Russia

    M. T. Kozinova & N. L. Shimanovsky

  2. Fox Chase Cancer Center, 333 Kottman Ave, Philadelphia, PA, 19111, USA

    M. T. Kozinova, G. A. Abalakov & D. V. Sharipova

Authors
  1. M. T. Kozinova
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. G. A. Abalakov
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. D. V. Sharipova
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. N. L. Shimanovsky
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to M. T. Kozinova.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 55, No. 4, pp. 3 – 10, April, 2021.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Kozinova, M.T., Abalakov, G.A., Sharipova, D.V. et al. Molecular-Genetic Basis of Gastrointestinal Stromal Tumor Personalized Therapy by Receptor Tyrosine Kinase Inhibitors (A Review). Pharm Chem J 55, 315–322 (2021). https://doi.org/10.1007/s11094-021-02419-8

Download citation

  • Received:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s11094-021-02419-8

Keywords

Search

Navigation