Lenvatinib: First Global Approval

Scott, Lesley J.

doi:10.1007/s40265-015-0383-0

Cited by 62 publications

(35 citation statements)

References 33 publications

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“…Landmark preclinical research implicating tyrosine kinase receptors (TKRs) and their downstream signaling cascades as drivers in the proliferation of MTC and DTC led to the development of numerous small molecule competitive inhibitors, the tyrosine kinase inhibitors (TKIs) [11,17,18]. Four of these agents are now approved by regulatory agencies for use in advanced thyroid cancer (Table 1) [20].…”

Section: Approved Tkis In Advanced Thyroid Cancermentioning

confidence: 99%

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The Treatment of Advanced Thyroid Cancer in the Age of Novel Targeted Therapies

Lirov

Worden

Cohen

2017

Drugs

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Until recently, patients with advanced thyroid cancers had limited options for systemic treatment. With the introduction of tyrosine kinase inhibitors (TKIs) as a promising new class of targeted therapies for thyroid cancer, suddenly patients with advanced disease were given new options to extend survival. Guidelines worldwide have been updated to include general indications for these newer agents, but questions remain regarding which agent(s) to select, when to begin treatment, and how long therapy should continue. Additionally, the true impact of TKIs on overall survival and quality-of-life in thyroid cancer patients needs further clarification. As familiarity with approved agents and longer-term data become available, better strategies for implementation of these targeted drugs will evolve to optimize benefit for patients living with metastatic disease.

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Section: Approved Tkis In Advanced Thyroid Cancermentioning

confidence: 99%

“…In 2015, Lenvatinib became the latest TKI to obtain regulatory approval for use in RAIR DTC [20,96]. This approval stems from the promising results reported in the SELECT trial [27].…”

Section: Approved Tkis In Advanced Thyroid Cancermentioning

confidence: 99%

The Treatment of Advanced Thyroid Cancer in the Age of Novel Targeted Therapies

Lirov

Worden

Cohen

2017

Drugs

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“…Selection of such targets was based on the reported inhibitory activity of many quinoline‐derived anticancer agents toward one or more of these enzymes, such as camptothecin , topotecan and irinotecan, which exert their anticancer activity throughout inhibition of Topo I. Besides, lenvatinib, tivozanib and cabozantinib are quinoline derivatives that proved to have considerable inhibitory activity against VEGFR. Furthermore, many other quinoline‐based derivatives and quinoline isosteres are well known to exhibit anticancer activity via inhibition of EGFR.…”

Section: Resultsmentioning

confidence: 99%

“…Literature surveys have revealed the importance of quinoline derivatives as potent anticancer agents, either from natural source like camptothecin ( A ) (MCF7: IC 50 = 0.23 µM), or synthetic compounds as bosutinib ( B ) (MDA‐MB‐231: IC 50 = 0.25 µM), lenvatinib, cabozantinib, topotecan, and irinotecan …”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, and docking study of new quinoline derivatives as antitumor agents

Nasr

Mostafa

El‐Sayed

et al. 2019

Archiv der Pharmazie

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New quinolines substituted with various heterocycles and chalcone moieties were synthesized and evaluated as antitumor agents. All the synthesized compounds were in vitro screened against 60 human cancer cell lines. Compound 13 showed the highest cytotoxicity toward 58 cell lines, exhibiting distinct growth inhibition values (GI 50 ) against the majority of them, including SR, HL-60 (TB) strains (leukemia), and MDA-MB-435 strains (melanoma), with GI 50 values of 0.232, 0.260, and 0.300 µM, respectively. It exhibited great selectivity toward cancer cell lines, with less toxic effect against normal cells represented by skin fibroblast (BJ) and breast epithelial cell lines (MCF-10F). The enzyme inhibitory activity of compound 13 was evaluated against topoisomerase 1 (Topo 1), epidermal growth factor receptor and vascular endothelial growth factor receptor 2, where it displayed worthy Topo 1 inhibition activity with an IC 50 value of 0.278 µM compared with camptothecin as a reference drug (IC 50 0.224 µM). Docking studies were performed to investigate the recognition profile of compound 13 with the Topo 1 enzyme binding site. K E Y W O R D S antitumor activity, chalcones, docking, EGFR, quinolone, Topo 1, VEGFR2

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“…Lenvatinib, a new molecular-targeted anticancer drug, is a multi-targeted receptor tyrosine kinase inhibitor that inhibits the activities of vascular endothelial growth factor receptors, fibroblast growth factor receptors, platelet-derived growth factor receptors, KIT, and RET [7,8]. Lenvatinib exerts its anticancer activity via the suppression of tumor angiogenesis, and it is generally indicated for unresectable radioiodine-refractory differentiated thyroid cancers [9].…”

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confidence: 99%

Anaplastic Thyroid Carcinoma Treated with Lenvatinib

et al. 2017

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Anaplastic thyroid carcinoma (ATC), which accounts for 1%-2% of all malignant tumors of the thyroid, is known to be highly resistant to any therapy and has a 1-year survival rate of 5%-20% [1][2][3]. ATC patients are limited in number, and most die within 6 months after diagnosis, making it difficult to establish a standard treatment protocol. Multimodal therapy including surgery, radiotherapy and chemotherapy has been introduced, but survival times remain poor [4][5][6].The use of molecular-targeted drugs as cancer therapy has been rapidly increasing over the past decade. Lenvatinib, a new molecular-targeted anticancer drug, is a multi-targeted receptor tyrosine kinase inhibitor that inhibits the activities of vascular endothelial growth factor receptors, fibroblast growth factor receptors, platelet-derived growth factor receptors, KIT, and RET [7,8]. Lenvatinib exerts its anticancer activity via the suppression of tumor angiogenesis, and it is generally indicated for unresectable radioiodine-refractory differentiated thyroid cancers [9]. However, the evidence of the clinical effect of this drug on ATC is very limited. We herein report a case of ATC with local recur- Kurume Medical Journal, 64, 00-00, 2017 Summary: Objective: We report a case of anaplastic thyroid carcinoma (ATC) with local recurrence and distant metastasis that responded very well to treatment with lenvatinib, a new molecular-targeted anticancer drug. Case Report: A 91-year-old Japanese woman presented with a 5-month history of a painless mass in her left anterior neck. She had a past history of total thyroidectomy and neck dissection for papillary carcinoma of the thyroid. Here she underwent neck dissection, and the histopathological diagnosis was lymph node metastasis of papillary carcinoma with anaplastic transformation. Five months later, a cervical lymph node swelled up again.Computed tomography demonstrated an enhanced mass in the neck and multiple nodules in both lungs. Recurrent ATC with multiple lung metastases was diagnosed, and molecular-targeted therapy with lenvatinib was initiated. The neck tumor reduced in 1 week, and the pulmonary nodules became completely hollow within 1 month. However, we had to discontinue lenvatinib because of severe side effects including high blood pressure, hypocalcemia, and hypoalbuminemia. Soon after discontinuation, the side effects subsided, but the tumor rapidly regrew. The patient died of lymphangiosis carcinomatosa 6 days after discontinuation. Conclusion: Although recent advances in molecular-targeted therapy have provided powerful cancer therapy tools, the negative side of this therapy must be addressed.

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Lenvatinib: First Global Approval

Cited by 62 publications

References 33 publications

The Treatment of Advanced Thyroid Cancer in the Age of Novel Targeted Therapies

The Treatment of Advanced Thyroid Cancer in the Age of Novel Targeted Therapies

Design, synthesis, and docking study of new quinoline derivatives as antitumor agents

Anaplastic Thyroid Carcinoma Treated with Lenvatinib

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