Fosaprepitant
- Atc Codes:A04AD12
- CAS Codes:265121-04-8
- PHARMGKB ID:265121-04-8
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Ivemend; Bulgaria: Ivemend; Czech Republic: Ivemend; Denmark: Ivemend; Estonia: Ivemend; Finland: Ivemend; France: Ivemend; Germany: Ivemend; Greece: Ivemend; Hungary: Ivemend; Italy: Ivemend; Ireland: Ivemend; Latvia: Ivemend; Lithuania: Ivemend; Luxembourg: Ivemend; Malta: Ivemend; Netherlands: Ivemend; Poland: Ivemend; Portugal: Ivemend; Romania: Ivemend; Slovakia: Ivemend; Slovenia: Ivemend; Spain: Ivemend; Sweden: Ivemend; UK: Ivemend.
North America
USA: Emend.
Drug combinations
Chemistry
Fosaprepitant Dimeglumine: C~23~H~22~F~7~N~4~O~6~P 2(C~7~H~17~NO~5~). Mw: 1004.83. 1-Deoxy-1-(methylamino)-D-glucitol[3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]phosphonate (2:1)(salt). CAS-265121-04-8.
Pharmacologic Category
Antiemetics, Miscellaneous; Substance P/Neurokinin 1 Receptor Antagonist. (ATC-Code: A04AD12, as aprepitant).
Mechanism of action
Fosaprepitant is a prodrug of aprepitant and accordingly, its antiemetic effects are attributable to aprepitant. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT~3~), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting. Animal and human studies have shown that aprepitant crosses the blood-brain barrier and occupies brain NK1 receptors, augments the antiemetic activity of the 5-HT~3~-receptor antagonist ondansetron and the corticosteroid dexamethasone, and inhibits both the acute and delayed phases of cisplatin-induced emesis.
Therapeutic use
Prevention of acute and delayed nausea and vomiting associated with moderately- and highly-emetogenic chemotherapy (in combination with other antiemetics).
Pregnancy and lactiation implications
In pregnancy, use only if clearly needed. Not recommended during lactation.
Unlabeled use
Contraindications
Hypersensitivity to fosaprepitant, aprepitant, polysorbate 80, or any component of the formulation. Since fosaprepitant is rapidly converted to aprepitant, do not use concurrently with pimozide, terfenadine, astemizole, or cisapride, since inhibition of CYP3A4 by aprepitant may result in elevated plasma concentrations of these drugs, potentially causing serious or life-threatening reactions.
Warnings and precautions
Not intended for treatment of existing nausea and vomiting or for chronic continuous therapy. Fosaprepitant should be used with caution in patients receiving concomitant medications that are primarily metabolized through CYP3A4. Immediate hypersensitivity reactions may occur during infusion. Co-administration of fosaprepitant or aprepitant with warfarin (a CYP2C9 substrate) may result in a clinically significant decrease in International Normalized Ratio (INR) of prothrombin time. The efficacy of hormonal contraceptives during and for 28 days following the last dose of fosaprepitant or aprepitant may be reduced.