Document Detail


Neuromuscular junction toxicity with tandutinib induces a myasthenic-like syndrome.
MedLine Citation:
PMID:  21242491     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
BACKGROUND: Tandutinib (MLN 518, Millennium Pharmaceuticals, Cambridge, MA) is an orally active multitargeted tyrosine kinase inhibitor that is currently under evaluation for the treatment of glioblastoma and has been used in the treatment of leukemia. In prior clinical and animal studies, a dose-dependent muscular weakness has been observed with this drug, though the etiology of the weakness has not been defined.
METHODS: Standard neurophysiologic techniques, including repetitive nerve stimulation, needle EMG, and single-fiber EMG, were used to evaluate patients who developed weakness while being treated with tandutinib and bevacizumab (Avastin, Genentech, South San Francisco, CA) for glioblastoma (NCT00667394).
RESULTS: Six patients were observed to develop a reversible weakness that correlated with the administration of the tandutinib. The onset of weakness after starting tandutinib occurred within 3 to 112 days and in less than 15 days in 3 patients. Electrophysiologic studies showed that all patients developed abnormal repetitive nerve stimulation studies. Four patients had short duration motor unit potentials. Two of these patients also had abnormal single-fiber EMG, as did a third patient who did not have standard needle EMG. The clinical and electrophysiologic abnormalities improved with the termination or reduction in the dose of tandutinib.
CONCLUSION: These observations suggest that tandutinib is toxic to the neuromuscular junction, possibly by reversibly binding to a molecule on the postsynaptic acetylcholine receptor complex. Classification of evidence: This study provides Class III evidence that tandutinib 500 mg twice daily induces reversible muscle weakness and electrophysiologic changes consistent with neuromuscular junction dysfunction.
Authors:
T J Lehky; F M Iwamoto; T N Kreisl; M K Floeter; H A Fine
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, N.I.H., Intramural    
Journal Detail:
Title:  Neurology     Volume:  76     ISSN:  1526-632X     ISO Abbreviation:  Neurology     Publication Date:  2011 Jan 
Date Detail:
Created Date:  2011-01-18     Completed Date:  2011-02-14     Revised Date:  2012-01-18    
Medline Journal Info:
Nlm Unique ID:  0401060     Medline TA:  Neurology     Country:  United States    
Other Details:
Languages:  eng     Pagination:  236-41     Citation Subset:  AIM; IM    
Affiliation:
EMG Section, NINDS, NIH, 8900 Wisconsin Ave., Bethesda, MD 20892-1404, USA. lehkyt@ninds.nih.gov
Data Bank Information
Bank Name/Acc. No.:
ClinicalTrials.gov/NCT00667394
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MeSH Terms
Descriptor/Qualifier:
Adult
Aged
Antibodies, Monoclonal / administration & dosage
Antibodies, Monoclonal, Humanized
Antineoplastic Combined Chemotherapy Protocols / adverse effects
Brain Neoplasms / drug therapy
Clinical Trials, Phase II as Topic
Drug Administration Schedule
Electromyography
Female
Glioblastoma / drug therapy
Humans
Male
Middle Aged
Myasthenia Gravis / chemically induced*,  physiopathology
Neuromuscular Diseases / chemically induced
Neuromuscular Junction / drug effects*,  physiopathology
Piperazines / administration & dosage,  adverse effects*
Protein Kinase Inhibitors / administration & dosage,  adverse effects*
Protein-Tyrosine Kinases / antagonists & inhibitors*
Quinazolines / administration & dosage,  adverse effects*
Syndrome
Chemical
Reg. No./Substance:
0/4-(6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-yl)piperazine-1-carboxylic acid (4-isopropoxyphenyl)amide; 0/Antibodies, Monoclonal; 0/Antibodies, Monoclonal, Humanized; 0/Piperazines; 0/Protein Kinase Inhibitors; 0/Quinazolines; 0/bevacizumab; EC 2.7.10.1/Protein-Tyrosine Kinases

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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