- Guide to PHARMACOLOGY
Synonyms: AMN 107 | AMN107 | Tasigna®
nilotinib is an approved drug (FDA & EMA (2007))
Compound class: Synthetic organic
Comment: Nilotinib is a Type-2 kinase inhibitor and was first approved by the FDA in 2007.
Preclinical studies in rodent Parkinson's disease models suggest that nilotinib has some potential to promote autophagic degradation of α-synuclein [4-6,9], a brain protein whose accumulation and aggregation contributes to the formation of toxic insoluble fibrils which cause pathological changes such as neuronal loss in Parkinson's disease and other synucleinopathies. This mechanism has been evaluated in a pilot, proof-of-concept and safety clinical trial in a small number of patients with Parkinson's disease- and diffuse Lewy body disease-associated cognitive impairment (see NCT02281474; note that this trial is not placebo controlled or blinded).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: nilotinib
|Compound class||Synthetic organic|
|Approved drug?||Yes (FDA & EMA (2007))|
|WHO Essential Medicine||WHO Essential Medicines List (EML) (23rd List, 2023). Access PDF version.
Click to view more information about the WHO Model Lists of Essential Medicines.
|International Nonproprietary Names|
|AMN 107 | AMN107 | Tasigna®|
|Reactome Reaction||R-HSA-9674430, R-HSA-9674095, R-HSA-9669868, R-HSA-9669854, R-HSA-9669900|
|CAS Registry No.||641571-10-0|
|GtoPdb PubChem SID||178102324|
|RCSB PDB Ligand||NIL|
|Search Google for chemical match using the InChIKey||HHZIURLSWUIHRB-UHFFFAOYSA-N|
|Search Google for chemicals with the same backbone||HHZIURLSWUIHRB|
|Search PubMed clinical trials||nilotinib|
|Search PubMed titles||nilotinib|
|Search PubMed titles/abstracts||nilotinib|
|SynPHARM||78747 (in complex with ABL proto-oncogene 1, non-receptor tyrosine kinase)|
|UniChem Compound Search for chemical match using the InChIKey||HHZIURLSWUIHRB-UHFFFAOYSA-N|
|UniChem Connectivity Search for chemical match using the InChIKey||HHZIURLSWUIHRB-UHFFFAOYSA-N|