| Pharmaceutical Information |
| Drug Name |
Rolapitant |
| Drug ID |
BADD_D01963 |
| Description |
Rolapitant is a potent, highly selective, long-acting Neurokinin-1 (NK-1) receptor antagonist approved for the prevention of delayed chemotherapy-induced nausea and vomiting (CINV) in adults. Delayed-phase CINV typically occurs >24 hours after chemotherapy treatment and is principally mediated by Neurokinin-1 and its ligand Substance P, which is released in the gut following chemotherapy administration. Neurokinin-1 is also known as Tachykinin Receptor 1 (TACR1), Neurokinin 1 Receptor (NK1R), and Substance P Receptor (SPR).
By blocking Substance P from interacting with NK-1 receptors in the gut and the central nervous system, rolapitant prevents late-phase CINV. Unlike other available NK-1 receptor antagonists, rolapitant is not an inhibitor of Cytochrome P450 enzyme CYP3A4 and has a long elimination half-life, allowing a single dose to prevent both acute and late-phase CINV during the first 120 hours post-chemotherapy. |
| Indications and Usage |
This drug is indicated in adults in combination with other antiemetics for the prevention of delayed nausea and vomiting associated with emetogenic chemotherapy. |
| Marketing Status |
approved; investigational |
| ATC Code |
A04AD14 |
| DrugBank ID |
DB09291
|
| KEGG ID |
D10742
|
| MeSH ID |
C578834
|
| PubChem ID |
10311306
|
| TTD Drug ID |
D0CF0Y
|
| NDC Product Code |
70720-101; 47848-053 |
| UNII |
NLE429IZUC
|
| Synonyms |
rolapitant | (5S,8S)-8-(((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro(4.5)decan-2-one | Varubi | SCH 619734 | 8-((1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro(4,5)decan-2-one |
|
| Chemical Information |
| Molecular Formula |
C25H26F6N2O2 |
| CAS Registry Number |
552292-08-7 |
| SMILES |
CC(C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OCC2(CCC3(CCC(=O)N3)CN2)C4=CC=CC=C4 |
| Chemical Structure |
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| ADRs Induced by Drug |
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