Synonyms: Example 2 [WO2013108809] | FGFR-IN-1 | Lytgobi® | TAS 120 | TAS-120 | TAS120
futibatinib is an approved drug (FDA (2022), EMA (2023))
Compound class:
Synthetic organic
Comment: Futibatinib (TAS-120) is a covalent (irreversible), non-selective FGFR inhibitor that was developed for anti-tumour activity [5]. It is claimed as Example 2 in patent WO2013108809 [4]. It can overcome acquired resistance to ATP-competitive FGFR inhibitors (such as infigratinib and zoligratinib) in intrahepatic cholangiocarcinomas that harbour FGFR2 kinase domain mutations [2]. A case study in a patient with metastatic cholangiocarcinoma, whose tumour had a FGFR2-CORO2B gene fusion and a pemigatinib-induced resistance mutation, demonstrated tumour shrinkage in response to futibatinib treatment [3].
Ligand Activity Visualisation ChartsThese 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. ✖ |
|
Classification | |
Compound class | Synthetic organic |
Approved drug? | Yes (FDA (2022), EMA (2023)) |
IUPAC Name |
1-[(3S)-3-[4-amino-3-[2-(3,5-dimethoxyphenyl)ethynyl]pyrazolo[3,4-d]pyrimidin-1-yl]pyrrolidin-1-yl]prop-2-en-1-one |
International Nonproprietary Names | |
INN number | INN |
10879 | futibatinib |
Synonyms |
Example 2 [WO2013108809] | FGFR-IN-1 | Lytgobi® | TAS 120 | TAS-120 | TAS120 |
Database Links | |
BindingDB Ligand | 161389 |
CAS Registry No. | 1448169-71-8 (source: WHO INN record) |
ChEMBL Ligand | CHEMBL3701238 |
GtoPdb PubChem SID | 354702259 |
PubChem CID | 71621331 |
RCSB PDB Ligand | TZ0 |
Search Google for chemical match using the InChIKey | KEIPNCCJPRMIAX-HNNXBMFYSA-N |
Search Google for chemicals with the same backbone | KEIPNCCJPRMIAX |
Search PubMed clinical trials | futibatinib |
Search PubMed titles | futibatinib |
Search PubMed titles/abstracts | futibatinib |
UniChem Compound Search for chemical match using the InChIKey | KEIPNCCJPRMIAX-HNNXBMFYSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | KEIPNCCJPRMIAX-HNNXBMFYSA-N |