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Nilotinib (641571-10-0) is Available on LEAPChem.com

Nov. 2018/12/6 14:48:24 By LEAP Chem


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Basic Information of Nilotinib

Chemical Name: Nilotinib

Cas No.: 641571-10-0

Molecular Formula: C28H22F3N7O

Chemical Structure:

 641571-10-0.png

 

Nilotinib (AMN107, trade name Tasigna), in the form of the hydrochloride monohydrate salt, is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia. Structurally related to imatinib, it was developed based on the structure of the Abl-imatinib complex to address imatinib intolerance and resistance. Nilotinib is a selective Bcr-Abl kinase inhibitor that is 10–30 fold more potent than imatinib in inhibiting Bcr-Abl tyrosine kinase activity and proliferation of Bcr-Abl expressing cells. Nilotinib was developed by Novartis and is sold under the trade name Tasigna.

In June 2006, a phase I clinical trial found nilotinib has a relatively favorable safety profile and shows activity in cases of CML resistant to treatment with imatinib, another tyrosine kinase inhibitor currently used as a first-line treatment. In that study 92% of patients (already resistant or unresponsive to imatinib) achieved normal white blood cell counts after five months of treatment.

Novartis announced on April 11, 2011 that it was discontinuing a phase III trial of Tasigna (nilotinib) for investigational use in the first-line treatment of gastrointestinal stromal tumor (GIST) based on the recommendation of an independent data monitoring committee. Interim results showed Tasigna is unlikely to demonstrate superiority compared to Novartis's Gleevec (imatinib)*, the current standard of care in this setting.

The use of low doses of nilotinib is being investigated for use for Parkinson's, and Alzheimer's disease, as well as for ALS, dementia and Huntington's disease.

Beginning in 2015, nilotinib was being trialed in people with Parkinson's disease as it appeared to be able to halt progression of the disease and even improve their symptoms. The researchers behind the trial hypothesized that the drug blocks a protein that interferes with the action of lysosomes which normally destroy harmful proteins in the brain.

Nilotinib has a number of adverse effects typical of anti-cancer drugs. These include headache, fatigue, gastrointestinal problems such as nausea, vomiting, diarrhea and constipation, muscle and joint pain, rash and other skin conditions, flu-like symptoms, and reduced blood cell count. Less typical side effects are those of the cardiovascular system, such as hypertension (high blood pressure), various types of arrhythmia, and prolonged QT interval. Nilotinib can also affect the body's electrolyte and glucose balance. Though pulmonary-related adverse effects are rare when compared with imatinib and dasatinib, there is a case report of acute respiratory failure from diffuse alveolar hemorrhage in a patient taking nilotinib.

 

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References:

https://en.wikipedia.org/wiki/Nilotinib

https://www.ncbi.nlm.nih.gov/pubmed/18956997

https://www.ncbi.nlm.nih.gov/pubmed/21419934

 

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