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Aprepitant (Emend) was the first of a new class of anti-sickness drugs. Taken with a 5-HT3 blocker and dexamethasone, it prevents the delayed nausea and vomiting that follow strongly emetogenic chemotherapy such as cisplatin.
Aprepitant capsules were approved by the FDA in March 2003 for prevention of acute and delayed nausea and vomiting with highly emetogenic chemotherapy, extended to moderately emetogenic regimens in 2005, with the intravenous prodrug fosaprepitant (Emend for injection) approved in 2008 and a paediatric oral suspension from 6 months of age in 2015; Cinvanti (2017) is an intravenous aprepitant emulsion. In the pivotal cisplatin trials, adding aprepitant to ondansetron and dexamethasone raised complete response rates by roughly 20 percentage points, establishing triple therapy as the standard that every guideline (ASCO, MASCC/ESMO, NCCN) now recommends for highly emetogenic chemotherapy. The EU authorised Emend in 2003 and Ivemend in 2008. It is a moderate CYP3A4 inhibitor, so dexamethasone doses are halved and interactions with some chemotherapy and warfarin need attention.
Selective high-affinity antagonist of substance P at NK1 receptors in the brainstem vomiting centre; fosaprepitant is an intravenous prodrug converted to aprepitant within minutes.
1.Aprepitant (and fosaprepitant) slips into a pocket on its target.
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| Region | Year | Indication |
|---|---|---|
| US | 2003 | Prevention of acute and delayed nausea and vomiting with highly emetogenic chemotherapy (moderately emetogenic added 2005; paediatric suspension 2015) |
| US | 2008 | Fosaprepitant intravenous prodrug for the same indications |
| EU | 2003 | Prevention of chemotherapy-induced nausea and vomiting (Emend); Ivemend 2008 |
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Query for this drug: (TITLE:"Aprepitant" OR ABSTRACT:"Aprepitant" OR TITLE:"and fosaprepitant" OR ABSTRACT:"and fosaprepitant" OR TITLE:"Emend" OR ABSTRACT:"Emend" OR TITLE:"Cinvanti" OR ABSTRACT:"Cinvanti" OR TITLE:"Fosaprepitant" OR ABSTRACT:"Fosaprepitant" OR TITLE:"Ivemend" OR ABSTRACT:"Ivemend") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Aprepitant (and fosaprepitant), not a curated reading list.
Shares Heron Therapeutics, Ondansetron, Palonosetron, Antiemetics for chemotherapy-induced nausea and vomiting and the tag supportive.
Shares Antiemetics for chemotherapy-induced nausea and vomiting and the tag supportive.
Shares Antiemetics for chemotherapy-induced nausea and vomiting and the tag supportive.
Shares Netupitant and palonosetron, Palonosetron, Dexamethasone.
Shares NK1 receptor (TACR1), Ondansetron, Palonosetron.
Shares Study With IV NEPA (Fosnetupitant/Palonosetron) for the Prevention of Chemotherapy-induced Nausea and Vomiting in Paediatric Cancer Patients Undergoing Highly Emetogenic Chemotherapy (HEC), Netupitant and palonosetron, Palonosetron.
Shares Ondansetron, Palonosetron.
Shares Netupitant and palonosetron, Dexamethasone.