Skip to main content
Log in

Cabozantinib: A Review in Advanced Renal Cell Carcinoma

  • Adis Drug Evaluation
  • Published:
Drugs Aims and scope Submit manuscript

Abstract

The multiple tyrosine kinase inhibitor (TKI) cabozantinib (Cabometyx™) is approved in the USA for the treatment of patients with advanced renal cell carcinoma (RCC) who have received prior antiangiogenic therapy. In the EU, cabozantinib is indicated for the treatment of advanced RCC in adults following prior vascular endothelial growth factor (VEGF)-targeted therapy. In adults with advanced or metastatic clear-cell RCC who had previously received VEGF receptor (VEGFR) TKIs, progression-free survival (PFS) and overall survival (OS) were significantly prolonged in patients who received oral cabozantinib versus oral everolimus in the pivotal METEOR trial. Objective response was achieved in a significantly higher proportion of patients receiving cabozantinib than those receiving everolimus. Cabozantinib had a manageable adverse events profile in patients with advanced RCC. Thus, cabozantinib is an important new option for use in patients with advanced RCC who have previously received antiangiogenic therapy.

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.

Fig. 1

Reproduced from Choueiri et al. [17] with permission

Similar content being viewed by others

References

  1. Chow WH, Dong LM, Devesa SS. Epidemiology and risk factors for kidney cancer. Nat Rev Urol. 2010;7(5):245–57.

    Article  PubMed  PubMed Central  Google Scholar 

  2. Escudier B, Porta C, Schmidinger M, et al. Renal cell carcinoma: ESMO clinical practice guidelines for diagnosis, treatment and follow-up. Ann Oncol. 2014;25 (Suppl 3):iii49–56.

  3. Grassi P, Verzoni E, Ratta R, et al. Cabozantinib in the treatment of advanced renal cell carcinoma: design, development, and potential place in the therapy. Drug Des Devel Ther. 2016;10:2167–72.

    Article  PubMed  PubMed Central  Google Scholar 

  4. National Comprehensive Cancer Network. NCCN clinical practice guidelines in oncology: kidney cancer (version 3.2016). 2016. http://www.nccn.org. Accessed 2 Nov 2016.

  5. Malouf GG, Flippot R, Khayat D. Therapeutic strategies for patients with metastatic renal cell carcinoma in whom first-line vascular endothelial growth factor receptor-directed therapies fail. J Oncol Pract. 2016;12(5):412–20.

    Article  PubMed  Google Scholar 

  6. Yakes FM, Chen J, Tan J, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther. 2011;10(12):2298–308.

    Article  CAS  PubMed  Google Scholar 

  7. Exelixis Inc. Cabometyx™ (cabozantinib) tablets for oral use: US prescribing information. 2016. http://www.accessdata.fda.gov. Accessed 2 Nov 2016.

  8. European Medicines Agency. Cabometyx (cabozantinib) film-coated tablets: EU summary of product characteristics. 2016. http://ec.europa.eu/. Accessed 2 Nov 2016.

  9. Hoy SM. Cabozantinib: a review of its use in patients with medullary thyroid cancer. Drugs. 2014;74(12):1435–44.

    Article  CAS  PubMed  Google Scholar 

  10. Xie Z, Lee YH, Boeke M, et al. MET inhibition in clear cell renal cell carcinoma. J Cancer. 2016;7(10):1205–14.

    Article  PubMed  PubMed Central  Google Scholar 

  11. Zhou L, Liu XD, Sun M, et al. Targeting MET and AXL overcomes resistance to sunitinib therapy in renal cell carcinoma. Oncogene. 2016;35(21):2687–97.

    Article  CAS  PubMed  Google Scholar 

  12. Nguyen L, Benrimoh N, Xie Y, et al. Pharmacokinetics of cabozantinib tablet and capsule formulations in healthy adults. Anticancer Drugs. 2016;27(7):669–78.

    Article  CAS  PubMed  Google Scholar 

  13. Lacy S, Hutmacher MM, Yang B, et al. Population pharmacokinetic (PopPK) and exposure-response (ER) modeling of cabozantinib (C) in patients (pts) with renal cell carcinoma (RCC) in the phase 3 METEOR study [abstract no. 2565 plus poster]. J Clin Oncol. 2016;34(Suppl).

  14. Nguyen LP, Holland JR, Ramies DMD, et al. Effect of renal and hepatic impairment on the pharmacokinetics of cabozantinib. J Clin Pharmacol. 2016;56(9):1130–40.

    Article  CAS  PubMed  Google Scholar 

  15. Choueiri TK, Escudier B, Powles T, et al. Cabozantinib versus everolimus in advanced renal-cell carcinoma. N Engl J Med. 2015;373(19):1814–23.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  16. Motzer RJ, Bacik J, Schwartz LH, et al. Prognostic factors for survival in previously treated patients with metastatic renal cell carcinoma. J Clin Oncol. 2004;22(3):454–63.

    Article  PubMed  Google Scholar 

  17. Choueiri TK, Escudier B, Powles T, et al. Cabozantinib versus everolimus in advanced renal cell carcinoma (METEOR): final results from a randomised, open-label, phase 3 trial. Lancet Oncol. 2016;17(7):917–27.

    Article  CAS  PubMed  Google Scholar 

  18. Cella D, Escudier B, Tannir N, et al. Quality of life (QoL) in the phase 3 METEOR trial of cabozantinib vs everolimus for advanced renal cell carcinoma (RCC) [abstract no. 816P]. Ann Oncol. 2016;27(Suppl 6):vi282.

  19. Powles T, Motzer RJ, Escudier BJ, et al. Outcomes based on prior VEGFR TKI and PD-1 checkpoint inhibitor therapy in METEOR, a randomized phase 3 trial of cabozantinib (C) vs everolimus (E) in advanced renal cell carcinoma (RCC) [abstract no. 4557 plus poster]. J Clin Oncol. 2016;34(Suppl).

  20. Escudier BJ, Powles T, Motzer RJ, et al. Efficacy of cabozantinib (C) vs everolimus (E) in patients (pts) with advanced renal cell carcinoma (RCC) and bone metastases (mets) from the phase III METEOR study [abstract no. 4558 plus poster]. J Clin Oncol. 2016;34(Suppl).

  21. Eisen T, Sternberg CN, Robert C, et al. Targeted therapies for renal cell carcinoma: review of adverse event management strategies. J Natl Cancer Inst. 2012;104(2):93–113.

    Article  CAS  PubMed  Google Scholar 

  22. Powles T, Staehler M, Ljungberg B, et al. European Association of Urology guidelines for clear cell renal cancers that are resistant to vascular endothelial growth factor receptor-targeted therapy. Eur Urol. 2016. doi:10.1016/j.eururo.2016.06.009.

    Google Scholar 

Download references

Acknowledgements

During the peer review process, the manufacturer of cabozantinib was also offered an opportunity to review this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Zaina T. Al-Salama.

Ethics declarations

Funding

The preparation of this review was not supported by any external funding.

Conflict of interest

Z T. Al-Salama and G.M. Keating are salaried employees of Adis/Springer, are responsible for the article content and declare no relevant conflicts of interest.

Additional information

The manuscript was reviewed by: M. Fukudo, Department of Hospital Pharmacy and Pharmacology, Asahikawa Medical University, Asahikawa, Japan; P. Marchetti, Medical Oncology, Sapienza University of Rome and IDI-IRCCS, Rome, Italy; U. Vaishampayan, Division of Haematology/Oncology, Department of Medicine, Wayne State University School of Medicine, Detroit, MI, USA.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Al-Salama, Z.T., Keating, G.M. Cabozantinib: A Review in Advanced Renal Cell Carcinoma. Drugs 76, 1771–1778 (2016). https://doi.org/10.1007/s40265-016-0661-5

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s40265-016-0661-5

Keywords

Navigation