Aprepitant is a substance P/neurokinin 1 receptor antagonist used to treat nausea and vomiting caused by chemotherapy and surgery. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CI NV).
- Mechanism
- Curator reviewed
Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with Aprepitant have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies show that Aprepitant augments the antiemetic activity of the 5-HT3-receptor antagonist ondansetron and the corticosteroid ethasone and inhibits both the acute and delayed phases of cisplatin induced emesis.
- Primary indication
- For the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy, including high-dose cisplatin (in combination with other antiemetic agents).Curator reviewed · 10 structured indications
- Formula / weight
- C23H21F7N4O3 · 534.4267 g/mol (avg)
- First approval
- Canada, 2007 · United States, 2003 · European Union, 2016
- Code names
- L-754,030 · L-754939 · MK-0869 · MK-869
- Brand names
Resolves to
ATALOFNDEOCMKK-OITMNORJSA-NSMILESC[C@@H](O[C@H]1OCCN(CC2=NNC(=O)N2)[C@H]1C1=CC=C(F)C=C1)C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)FWhat you can answer from here — as of September 23, 2026
Which drugs share a target with Aprepitant, and which of those have an active Phase 3 trial?
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