Rolapitant is a neurokinin-1 (NK-1) receptor antagonist used in combination with other antiemetics for the prevention of delayed nausea and vomiting associated with emetogenic chemotherapy. 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.
- Mechanism
- Curator reviewed
Rolapitant is an orally active, highly selective Neurokinin-1 Receptor (NK1R) antagonist. NK1 receptors are located primarily in the gut and central nervous system and are activated by Substance P following chemotherapy administration. By binding to the NK1 receptor, rolapitant prevents binding of its ligand Substance P, which is released in the gut following chemotherapy administration.
- Primary indication
- This drug is indicated in adults in combination with other antiemetics for the prevention of delayed nausea and vomiting associated with emetogenic chemotherapy.Curator reviewed · 1 structured indication
- Formula / weight
- C25H26F6N2O2 · 500.485 g/mol (avg)
- First approval
- United States, 2015
- Brand names
Resolves to
FIVSJYGQAIEMOC-ZGNKEGEESA-NSMILESC[C@@H](OC[C@]1(CC[C@]2(CCC(=O)N2)CN1)C1=CC=CC=C1)C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)FWhat you can answer from here — as of October 02, 2026
Which drugs share a target with Rolapitant, and which of those have an active Phase 3 trial?
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