rolapitant
Sign in to saveAlso known as (5S,8S)-8- { [(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]}-8-phenyl-1,7-diazaspiro[4.5]decan-2-one
Rolapitant (INN, trade name Varubi in the US and Varuby in the European Union) is a drug originally developed by Schering-Plough and licensed for clinical development by Tesaro, which acts as a selective NK1 receptor antagonist (antagonist for the NK1 receptor). It has been approved as a medication for the treatment of chemotherapy-induced nausea and vomiting (CINV) after clinical trials showed it to have similar or improved efficacy and some improvement in safety over existing drugs for this application.
Wikidata facts
- Mass
- 500.189847
Show 4 more facts
- isomeric SMILES
- C[C@H](C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OC[C@]2(CC[C@]3(CCC(=O)N3)CN2)C4=CC=CC=C4
- chemical formula
- C₂₅H₂₆F₆N₂O₂
- canonical SMILES
- CC(C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OCC2(CCC3(CCC(=O)N3)CN2)C4=CC=CC=C4
- Commons category
- Rolapitant
via Wikidata · CC0
~6 min read
Article
11 sectionsContents
- Medical uses
- Contraindications
- Side effects
- Overdose
- Interactions
- Pharmacology
- Pharmacodynamics
- Pharmacokinetics
- Chemistry
- References
- External links
{{Drugbox | IUPAC_name = (5S,8S)-8-({(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}methyl)- 8-phenyl-1,7-diazaspiro[4.5]decan-2-one | image = Rolapitant (Patent Verified).svg | image_class = skin-invert-image | width = 225
| pronounce = | tradename = Varubi (US), Varuby (EU) | Drugs.com = | MedlinePlus = a615041 | DailyMedID = Rolapitant | pregnancy_AU = | pregnancy_US = N | pregnancy_category = | licence_EU = yes | legal_AU = | legal_CA = | legal_UK = | legal_US = Rx-only | legal_US_comment = | legal_EU = Rx-only | routes_of_administration = By mouth (tablets), intravenous | ATC_prefix = A04 | ATC_suffix = AD14 | class = NK1 receptor antagonists, antiemetics