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Emend (FOSAPREPITANT)
Emend blocks the action of substance P, a natural substance that can trigger nausea and vomiting.
Emend (FOSAPREPITANT) is a small molecule substance P/neurokinin-1 receptor antagonist developed by Merck and currently owned by Steriscience. It was FDA-approved in 2003 for the prevention of chemotherapy-induced nausea and vomiting. Emend works by blocking the action of substance P, a natural substance in the body that can trigger nausea and vomiting. The drug is available as a generic medication, with 18 generic manufacturers, and its commercial status is off-patent. Key safety considerations include its half-life of 2.2 hours.
At a glance
| Generic name | FOSAPREPITANT |
|---|---|
| Sponsor | Steriscience |
| Drug class | Substance P/Neurokinin-1 Receptor Antagonist |
| Target | Substance-P receptor |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2003 |
Mechanism of action
Fosaprepitant is prodrugof aprepitant and accordingly, its antiemetic effectsare attributable to aprepitant.Aprepitant is selectivehigh-affinity antagonist of human substanceP/neurokinin 1(NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapiesfor chemotherapy-induced nausea and vomiting(CINV). Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxicchemotherapeutic 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 humanstudies have shown that aprepitant augmentsthe antiemetic activityof the 5-HT3 -receptor antagonist ondansetron and the corticosteroid dexamethasone and inhibitsboth the acuteand delayed phasesof cisplatin-induced emesis.
Approved indications
- Chemotherapy-induced nausea and vomiting
Common side effects
- fatigue
- diarrhea
- neutropenia
- infusion-site pain
- infusion-site erythema
- infusion-site pruritus
- infusion-site induration
- infusion-site irritation
- vessel puncture-site pain
- infusion-site thrombophlebitis
- asthenia
- anemia
Drug interactions
- alfentanil
- carbamazepine
- dexamethasone
- fosphenytoin
- methylprednisolone
- phenytoin
- rifampicin
- vardenafil
Key clinical trials
- An Exploratory Study on Efficacy and Safety of Fosaprepitant and Palonosetron Hydrochloride for Injection in Preventing CINV From Multi-Agent HEC (PHASE4)
- A Prospective, Multicenter, Study of APF530 (Granisetron) SC for Prevention of CINV in Patients Receiving HEC (PHASE3)
- Prevention of Delayed CINV After Autologous Transplant: Olanzapine-Containing Regimen vs. Dexamethasone-Containing Regimen (PHASE3)
- Electroacupuncture for Chemotherapy-Induced GI Symptom Clusters in Breast Cancer (PHASE3)
- To Evaluate the Efficacy and Safety of QLM2010 for Prevention of Chemotherapy-induced Nausea and Vomiting After Highly Emetogenic Chemotherapy. (PHASE3)
- Broadening Antiemetics Research by Comparing the Effectiveness of Fosaprepitant and Metoclopramide (PHASE4)
- Antiemetic Fosaprepitant To Remedy Nausea and Vomiting (PHASE2,PHASE3)
- Nanocrystalline Megestrol for Managing Chemotherapy-Induced Nausea and Vomiting (PHASE3)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |