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Kayleigh L Brocklesby, Jennifer S Waby, Chris Cawthorne, Graham Smith
Vandetanib is an orally available tyrosine kinase inhibitor used in the treatment of cancer. The current synthesis proceeds via an unstable 4-chloroquinazoline, using harsh reagents, in addition to requiring sequential protection and deprotection steps. In the present work, use of the Dimroth rearrangement in the key quinazoline forming step enabled the synthesis of Vandetanib in nine steps (compared to the previously reported 12-14).
April 12, 2017: Tetrahedron Letters
Poupak Fallahi, Silvia Martina Ferrari, Enke Baldini, Marco Biricotti, Salvatore Ulisse, Gabriele Materazzi, Paolo Miccoli, Alessandro Antonelli
Traditional therapies for advanced or metastatic progressive medullary thyroid cancer (pMTC) are poor effective. Several TKIs have been tested in clinical trials in pMTC patients. Areas covered: This paper reviews efficacy and safety of vandetanib in the treatment of pMTC. Expert commentary: Vandetanib (trade name CAPRELSA® [Vandetanib]) has been shown to improve progression-free survival (30.5 vs 19.3 months in controls) in pMTC patients. Vandetanib is approved by FDA and EMA for metastatic MTC in adults; in adolescents and children with metastatic or locally advanced MTC, vandetanib seems to be effective...
November 2016: Expert Review of Anticancer Therapy
Jolanta Krajewska, Barbara Jarzab
INTRODUCTION: New therapeutic options for both differentiated thyroid cancer (DTC) and medullary thyroid cancer (MTC) have opened up during the past few years, as the key role of tyrosine kinases in the pathogenesis of thyroid carcinoma has been proved. Recently, two tyrosine kinase inhibitors (TKIs) targeting VEGFR vandetanib (Caprelsa) and cabozantinib (Cometriq) have been approved for advanced MTC, whereas, sorafenib (Nexavar) has been accepted to treat late-stage of DTC. Their efficacy was demonstrated in Phase III studies, compared to placebo; each of them significantly prolonged the progression-free survival...
December 2014: Expert Opinion on Pharmacotherapy
Amalia Azzariti, Letizia Porcelli, Anita Mangia, Concetta Saponaro, Anna E Quatrale, Ondina S Popescu, Sabino Strippoli, Gianni Simone, Angelo Paradiso, Michele Guida
Angiosarcomas are rare soft-tissue sarcomas of endothelial cell origin. They can be sporadic or caused by therapeutic radiation, hence secondary breast angiosarcomas are an important subgroup of patients. Assessing the molecular biology of angiosarcomas and identify specific targets for treatment is challenging. There is currently great interest in the role of angiogenesis and of angiogenic factors associated with tumor pathogenesis and as targets for treatment of angiosarcomas. A primary cell line derived from a skin fragment of a irradiation-induced angiosarcoma patient was obtained and utilized to evaluate cell biomarkers CD31, CD34, HIF-1 alpha and VEGFRs expression by immunocytochemistry and immunofluorescence, drugs cytotoxicity by cell counting and VEGF release by ELISA immunoassay...
February 15, 2014: Experimental Cell Research
Maryann R Cooper, Soo Yun Yi, Wael Alghamdi, Daniel J Shaheen, Michael Steinberg
OBJECTIVE: To review the place in therapy of vandetanib for medullary thyroid carcinoma (MTC). DATA SOURCES: Literature searches were performed in Ovid MEDLINE, EMBASE, and Google Scholar using the search terms ZD6474 OR vandetanib OR Caprelsa combined with medullary thyroid carcinoma. STUDY SELECTION AND DATA EXTRACTION: Two phase 2 trials and 1 phase 3 trial were identified. DATA SYNTHESIS: Vandetanib is approved for the treatment of unresectable, locally advanced or metastatic MTC in patients with symptomatic or progressive disease...
March 2014: Annals of Pharmacotherapy
Cosimo Durante, Alessandra Paciaroni, Katia Plasmati, Fabiana Trulli, Sebastiano Filetti
Medullary thyroid cancer (MTC) is frequently diagnosed in a locally advanced or metastatic stage, and 10-year survival rates in these cases are below 20 %. Cytotoxic chemotherapy has no significant impact on overall or progression-free survival. Vandetanib (Caprelsa(®), AstraZeneca) is a once-daily oral tyrosine kinase inhibitor that selectively inhibits signalling mediated by growth-factor receptor tyrosine kinase RET (constitutively activated in roughly 60 % of all MTCs), vascular endothelial growth-factor receptors 2 and 3, and epidermal growth-factor receptors...
October 2013: Endocrine
C Monneret
Among the 35 new molecular entities approved by the FDA in 2011, 17 were particularly notable for their significant contributions to the health of patients, including abiraterone acetate, vandetanib, belatacept and fidaxomicin. Thus, abiraterone acetate, namely Zytiga®, was included as the first in a new class of drugs to treat late-stage prostate cancer. The ability of Zytiga® to prolong survival in these patients was considered as significant because they have few other treatments options and the benefits of Zytiga® outweighed the risks of reported side-effects...
March 2013: Annales Pharmaceutiques Françaises
C Jovelet, A Deroussent, S Broutin, A Paci, R Farinotti, J M Bidart, S Gil
Efflux transporters play an important role in the resistance of tumor cells against anticancer agents. Interaction between these transporters, including P-glycoprotein (P-gp), and drugs might influence their pharmacological properties and toxicities. The aim of this study was to investigate whether vandetanib (Caprelsa(®)), a small tyrosine kinase inhibitor, could interact with the multidrug transporter P-gp. Interaction of vandetanib with the P-gp was investigated using the parental cell line (IGROV1) and the P-gp doxorubicin-resistant (IGROV1-DXR) cell line, derived from the parental drug-sensitive IGROV1 cells...
September 2013: European Journal of Drug Metabolism and Pharmacokinetics
Nicole G Chau, Robert I Haddad
Vandetanib (ZD6474, Caprelsa, AstraZeneca), an oral small-molecule tyrosine kinase inhibitor (TKI) that targets the rearranged during transfection receptor (RET), VEGF receptor (VEGFR2-3), and EGF receptor (EGFR), is the first systemic therapy approved by the U.S. Food and Drug Administration (FDA) for the treatment of symptomatic or progressive advanced medullary thyroid cancer (MTC). In a randomized phase III trial of patients with unresectable, locally advanced, or metastatic MTC, vandetanib improved progression-free survival compared with placebo [HR, 0...
February 1, 2013: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
(no author information available yet)
Treatment of medullary thyroid cancer is mainly based on surgery. Life expectancy exceeds 10 years in almost half of patients with inoperable advanced or metastatic disease. Cytotoxic chemotherapy is generally ineffective when this malignancy progresses. Vandetanib (Caprelsa, AstraZeneca), a multiple kinase inhibitor, is authorised in the European Union for use in this setting. Its clinical evaluation is mainly based on a double-blind, randomised, placebo-controlled trial in 331 patients, 70% of whom had progressed within the previous 6 months...
October 2012: Prescrire International
Gillian M Keating, Katherine A Lyseng-Williamson, James E Frampton
Vandetanib (Caprelsa™) provides an acceptable treatment option in patients with advanced medullary thyroid cancer for whom, historically, there have been no effective therapies. Vandetanib, an orally active, multitargeted tyrosine kinase inhibitor, improves progression-free survival and tumor response in patients with unresectable, locally advanced or metastatic medullary thyroid cancer. It has an acceptable tolerability profile in this patient population, although it does have the potential to prolong the corrected QT interval...
December 1, 2012: BioDrugs: Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy
Nils Degrauwe, Julie Ann Sosa, Sanziana Roman, Hari A Deshpande
Medullary thyroid cancer (MTC) represents an aggressive form of thyroid malignancy. Some may occur spontaneously or can be associated with Multiple Endocrine Neoplasia syndromes, or Familial Medullary Thyroid Cancer syndrome. In these patients, the protooncogene RET (rearranged during transfection) is mutated. In patients who have unresectable or metastatic disease, the long term prognosis is poor. New treatments for this disease have focused on the use of targeted agents that inhibit the receptor tyrosine kinase of RET...
2012: Clinical Medicine Insights. Oncology
Katherine Thornton, Geoffrey Kim, V Ellen Maher, Somesh Chattopadhyay, Shenghui Tang, Young Jin Moon, Pengfei Song, Anshu Marathe, Suchitra Balakrishnan, Hao Zhu, Christine Garnett, Qi Liu, Brian Booth, Brenda Gehrke, Robert Dorsam, Leigh Verbois, Debasis Ghosh, Wendy Wilson, John Duan, Haripada Sarker, Sarah Pope Miksinski, Lisa Skarupa, Amna Ibrahim, Robert Justice, Anthony Murgo, Richard Pazdur
On April 6, 2011, the U.S. Food and Drug Administration approved vandetanib (Caprelsa tablets; AstraZeneca Pharmaceuticals LP) for the treatment of symptomatic or progressive medullary thyroid cancer in patients with unresectable, locally advanced, or metastatic disease. Vandetanib is the first drug approved for this indication, and this article focuses on the basis of approval. Approval was based on the results of a double-blind trial conducted in patients with medullary thyroid carcinoma. Patients were randomized 2:1 to vandetanib, 300 mg/d orally (n = 231), or to placebo (n = 100)...
July 15, 2012: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
(no author information available yet)
No abstract text is available yet for this article.
January 9, 2012: Medical Letter on Drugs and Therapeutics
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