Pharmacokinetic evaluation of fosaprepitant dimeglumine.
BACKGROUND
Chemotherapy induced nausea and vomiting (CINV) is a common complication in the treatment of patients with cancer. The introduction of the first in class neurokinin-1 receptor antagonist aprepitant provided additive control on CINV in combination to existing antiemetics. Due to formulation issues, aprepitant is only available for oral administration. Fosaprepitant, a prodrug of aprepitant, was introduced to the market in 2008 as an intravenous bioequivalent to aprepitant.


METHODS
This review examines the chemical development of fosaprepitant, its pharmacokinetic properties, approved uses and potential applications.


RESULTS
The reader will get up-to-date information on the pharmacology and clinical uses of fosaprepitant. Clinical studies have demonstrated pharmacokinetic bioequivalence of aprepitant 125 mg to fosaprepitant 115 mg, as well as comparable efficacy in prevention of acute and delayed emesis following the first day of chemotherapy regimens.


CONCLUSIONS
Fosaprepitant is an intravenous prodrug of aprepitant that offers a new alternative to patients with CINV. Currently, fosaprepitant can substitute oral aprepitant in day 1 of a 3-day regimen. Current studies show that a single-day fosaprepitant regimen is also bioequivalent to the 3-day aprepitant regimen; this could significantly simplify the care for CINV patients in the future.
Colon-Gonzalez
Francheska
F
Thomas Jefferson University, Department of Pharmacology and Experimental Therapeutics, 1170 Main Building, 132 S. 10th St., Philadelphia, PA 19107, USA.
Kraft
Walter K
WK
D000818:Animals; D000932:Antiemetics / Q000493:pharmacokinetics* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000627:therapeutic use; D000077608:Aprepitant; D006801:Humans; D009025:Morpholines / Q000493:pharmacokinetics* / Q000494:pharmacology; D009325:Nausea / Q000139:chemically induced / Q000517:prevention & control; D009369:Neoplasms / Q000188:drug therapy; D064729:Neurokinin-1 Receptor Antagonists; D011355:Prodrugs; D013810:Therapeutic Equivalency; D014839:Vomiting / Q000139:chemically induced / Q000517:prevention & control
D000932:Antiemetics; D000970:Antineoplastic Agents; D009025:Morpholines; D064729:Neurokinin-1 Receptor Antagonists; D011355:Prodrugs; D000077608:Aprepitant; C579707:fosaprepitant
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