Review : Third Generation Tyrosine Kinase Inhibitors and Their Development in Advanced Renal Cell Carcinoma
Angiogenesis in general and the VEGF signaling axis in particular is a validated target in renal cell carcinoma. Clear cell carcinoma of the kidney is now recognized as a malignancy that is sensitive to inhibitors of the vascular endothelial growth factor pathway. Treatment options for patients with...
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2012-02-01
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| Series: | Frontiers in Oncology |
| Subjects: | |
| Online Access: | http://journal.frontiersin.org/Journal/10.3389/fonc.2012.00013/full |
| _version_ | 1818553500095741952 |
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| author | Ronald M Bukowski |
| author_facet | Ronald M Bukowski |
| author_sort | Ronald M Bukowski |
| collection | DOAJ |
| description | Angiogenesis in general and the VEGF signaling axis in particular is a validated target in renal cell carcinoma. Clear cell carcinoma of the kidney is now recognized as a malignancy that is sensitive to inhibitors of the vascular endothelial growth factor pathway. Treatment options for patients with metastatic renal cell carcinoma have evolved in dramatic fashion over the past six years, and a new paradigm has developed. The cytokines interferon-α and interleukin-2 were previously utilized for therapy, but since December 2005, six new agents have been approved in the United States for the treatment of advanced RCC. Three are tyrosine kinase inhibitors (TKI’s) including sunitinib, sorafenib, and recently pazopanib. The current review examines the evolving data with the next generation of TKI’s, axitinib and tivozanib being developed for the treatment of advanced RCC. These agents were synthesized to provide increased target specificity and enhanced target inhibition. The preclinical and clinical data are examined, an overview of the development of these TKI’s is provided, and discussion plus speculation concerning their potential roles as RCC therapy is provided. |
| first_indexed | 2024-12-12T09:26:36Z |
| format | Article |
| id | doaj.art-7206f1f82ba148d3ba9c3bd4932d27c9 |
| institution | Directory Open Access Journal |
| issn | 2234-943X |
| language | English |
| last_indexed | 2024-12-12T09:26:36Z |
| publishDate | 2012-02-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Oncology |
| spelling | doaj.art-7206f1f82ba148d3ba9c3bd4932d27c92022-12-22T00:29:01ZengFrontiers Media S.A.Frontiers in Oncology2234-943X2012-02-01210.3389/fonc.2012.0001320973Review : Third Generation Tyrosine Kinase Inhibitors and Their Development in Advanced Renal Cell CarcinomaRonald M Bukowski0Cleveland Clinic FoundationAngiogenesis in general and the VEGF signaling axis in particular is a validated target in renal cell carcinoma. Clear cell carcinoma of the kidney is now recognized as a malignancy that is sensitive to inhibitors of the vascular endothelial growth factor pathway. Treatment options for patients with metastatic renal cell carcinoma have evolved in dramatic fashion over the past six years, and a new paradigm has developed. The cytokines interferon-α and interleukin-2 were previously utilized for therapy, but since December 2005, six new agents have been approved in the United States for the treatment of advanced RCC. Three are tyrosine kinase inhibitors (TKI’s) including sunitinib, sorafenib, and recently pazopanib. The current review examines the evolving data with the next generation of TKI’s, axitinib and tivozanib being developed for the treatment of advanced RCC. These agents were synthesized to provide increased target specificity and enhanced target inhibition. The preclinical and clinical data are examined, an overview of the development of these TKI’s is provided, and discussion plus speculation concerning their potential roles as RCC therapy is provided.http://journal.frontiersin.org/Journal/10.3389/fonc.2012.00013/fullTyrosineCancerkinaseinhibitorsRenal |
| spellingShingle | Ronald M Bukowski Review : Third Generation Tyrosine Kinase Inhibitors and Their Development in Advanced Renal Cell Carcinoma Frontiers in Oncology Tyrosine Cancer kinase inhibitors Renal |
| title | Review : Third Generation Tyrosine Kinase Inhibitors and Their Development in Advanced Renal Cell Carcinoma |
| title_full | Review : Third Generation Tyrosine Kinase Inhibitors and Their Development in Advanced Renal Cell Carcinoma |
| title_fullStr | Review : Third Generation Tyrosine Kinase Inhibitors and Their Development in Advanced Renal Cell Carcinoma |
| title_full_unstemmed | Review : Third Generation Tyrosine Kinase Inhibitors and Their Development in Advanced Renal Cell Carcinoma |
| title_short | Review : Third Generation Tyrosine Kinase Inhibitors and Their Development in Advanced Renal Cell Carcinoma |
| title_sort | review third generation tyrosine kinase inhibitors and their development in advanced renal cell carcinoma |
| topic | Tyrosine Cancer kinase inhibitors Renal |
| url | http://journal.frontiersin.org/Journal/10.3389/fonc.2012.00013/full |
| work_keys_str_mv | AT ronaldmbukowski reviewthirdgenerationtyrosinekinaseinhibitorsandtheirdevelopmentinadvancedrenalcellcarcinoma |