Anlotinib: a novel multi-targeting tyrosine kinase inhibitor in clinical development

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Abstract

Anlotinib is a new, orally administered tyrosine kinase inhibitor that targets vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR), platelet-derived growth factor receptors (PDGFR), and c-kit. Compared to the effect of placebo, it improved both progression-free survival (PFS) and overall survival (OS) in a phase III trial in patients with advanced non-small-cell lung cancer (NSCLC), despite progression of the cancer after two lines of prior treatments. Recently, the China Food and Drug Administration (CFDA) approved single agent anlotinib as a third-line treatment for patients with advanced NSCLC. Moreover, a randomized phase IIB trial demonstrated that anlotinib significantly prolonged the median PFS in patients with advanced soft tissue sarcoma (STS). Anlotinib also showed promising efficacy in patients with advanced medullary thyroid carcinoma and metastatic renal cell carcinoma (mRCC). The tolerability profile of anlotinib is similar to that of other tyrosine kinase inhibitors that target VEGFR and other tyrosine kinase-mediated pathways; however, anlotinib has a significantly lower incidence of grade 3 or higher side effects compared to that of sunitinib. We review the rationale, clinical evidence, and future perspectives of anlotinib for the treatment of multiple cancers.

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Most cited references 67

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Author and article information

Contributors

Jiuda Zhao: jiudazhao@126.com

Journal

Journal ID (nlm-ta): J Hematol Oncol

Journal ID (iso-abbrev): J Hematol Oncol

Title: Journal of Hematology & Oncology

Publisher: BioMed Central (London )

ISSN (Electronic): 1756-8722

Publication date (Electronic): 19 September 2018

Publication date PMC-release: 19 September 2018

Publication date Collection: 2018

Volume: 11

Electronic Location Identifier: 120

Affiliations

[1 ]GRID grid.459333.b, Affiliated Hospital of Qinghai University, Affiliated Cancer Hospital of Qinghai University, ; Xining, 810000 China

[2 ]Shouguang Hospital of Traditional Chinese Medicine, Weifang, 262700 China

[3 ]ISNI 0000 0001 0027 0586, GRID grid.412474.0, Peking University Cancer Hospital and Institute, ; Beijing, 100142 China

[4 ]The Fifth People’s Hospital of Qinghai Province, Xining, 810000 China

Article

Publisher ID: 664

DOI: 10.1186/s13045-018-0664-7

PMC ID: 6146601

PubMed ID: 30231931

SO-VID: ced85a17-e2d2-418a-a02b-67192f1a40b9

License:

Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License ( http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver ( http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.

History

Date received : 9 July 2018

Date accepted : 6 September 2018

Funding

Funded by: the Thousand Talents of Program of High-end Innovation of Qinghai Province in China

Custom metadata

ScienceOpen disciplines: Oncology & Radiotherapy

Keywords: anlotinib,tyrosine kinase inhibitor,vegfr,nsclc,sts

Data availability:

ScienceOpen disciplines: Oncology & Radiotherapy

Keywords: anlotinib, tyrosine kinase inhibitor, vegfr, nsclc, sts

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