Synonyms: NMS-E628 | Rozlytrek® | RXDX-101
entrectinib is an approved drug (Japan and FDA (2019), EMA (2020))
Compound class:
Synthetic organic
Comment: Entrectinib is an oral, brain penetrant, receptor tyrosine kinase (RTK) inhibitor that targets solid tumours that harbour activating alterations in NTRK1, NTRK2, NTRK3 (the Trk family RTKs), ROS1 or ALK [6]. NTRK1 fusion proteins are becoming recognised as oncogenic-drivers in NSCLC [3], so the ability of the compound to target these and ALK- and ROS1-rearrangements suggests it has the potential to become a useful oncology agent.
More recently entrectinib has been shown to inhibit NLRP3 inflammasome assembly and activation via a direct interaction with NIMA related kinase 7 (NEK7) that disrupts the NLRP3-NEK7 interaction [5]. This discovery suggests a role for entrectinib as an intervention for inflammasome-related diseases. |
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Classification ![]() |
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Compound class | Synthetic organic |
Approved drug? | Yes (Japan and FDA (2019), EMA (2020)) |
Approved drug? | Yes. FDA (2019) | Japan (2019) | EMA (2020) |
IUPAC Name ![]() |
N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-2-(oxan-4-ylamino)benzamide |
International Nonproprietary Names ![]() |
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INN number | INN |
10132 | entrectinib |
Synonyms ![]() |
NMS-E628 | Rozlytrek® | RXDX-101 |
Database Links ![]() |
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CAS Registry No. | 1108743-60-7 |
ChEMBL Ligand | CHEMBL1983268 |
DrugCentral Ligand | 5345 |
GtoPdb PubChem SID | 252166502 |
PubChem CID | 25141092 |
RCSB PDB Ligand | YMX |
Search Google for chemical match using the InChIKey | HAYYBYPASCDWEQ-UHFFFAOYSA-N |
Search Google for chemicals with the same backbone | HAYYBYPASCDWEQ |
Search PubMed clinical trials | entrectinib |
Search PubMed titles | entrectinib |
Search PubMed titles/abstracts | entrectinib |
UniChem Compound Search for chemical match using the InChIKey | HAYYBYPASCDWEQ-UHFFFAOYSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | HAYYBYPASCDWEQ-UHFFFAOYSA-N |