| 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 |
Rolapitant is indicated in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy. |
| Marketing Status |
Not Available |
| ATC Code |
A04AD14 |
| DrugBank ID |
DB09291
|
| KEGG ID |
D10742
|
| MeSH ID |
C578834
|
| PubChem ID |
10311306
|
| TTD Drug ID |
D0CF0Y
|
| NDC Product Code |
47848-053; 70720-101 |
| 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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| ADR Related Proteins Induced by Drug |
| ADR Term |
Protein Name |
UniProt AC |
TTD Target ID |
PMID |
| Not Available | Not Available | Not Available | Not Available | Not Available |
|
| ADRs Induced by Drug |
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