Francheska Colon-Gonzalez1, Walter K Kraft. 1. Thomas Jefferson University, Department of Pharmacology and Experimental Therapeutics, 1170 Main Building, 132 S. 10th St., Philadelphia, PA 19107, USA.
Abstract
IMPORTANCE OF THE FIELD: 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. AREAS COVERED IN THIS REVIEW: This review examines the chemical development of fosaprepitant, its pharmacokinetic properties, approved uses and potential applications. WHAT THE READER WILL GAIN: 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. TAKE HOME MESSAGE: 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.
IMPORTANCE OF THE FIELD: Chemotherapy induced n class="Disease">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. AREAS COVERED IN THIS REVIEW: This review examines the chemical development of fosaprepitant, its pharmacokinetic properties, approved uses and potential applications. WHAT THE READER WILL GAIN: 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. TAKE HOME MESSAGE: 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 CINVpatients in the future.
Authors: J J Hale; S G Mills; M MacCoss; C P Dorn; P E Finke; R J Budhu; R A Reamer; S E Huskey; D Luffer-Atlas; B J Dean; E M McGowan; W P Feeney; S H Chiu; M A Cascieri; G G Chicchi; M M Kurtz; S Sadowski; E Ber; F D Tattersall; N M Rupniak; A R Williams; W Rycroft; R Hargreaves; J M Metzger; D E MacIntyre Journal: J Med Chem Date: 2000-03-23 Impact factor: 7.446
Authors: David G Warr; Paul J Hesketh; Richard J Gralla; Hyman B Muss; Jørn Herrstedt; Peter D Eisenberg; Harry Raftopoulos; Steven M Grunberg; Munir Gabriel; Anthony Rodgers; Norman Bohidar; George Klinger; Carolyn M Hustad; Kevin J Horgan; Franck Skobieranda Journal: J Clin Oncol Date: 2005-04-20 Impact factor: 44.544
Authors: V Cocquyt; S Van Belle; R R Reinhardt; M L Decramer; M O'Brien; J H Schellens; M Borms; L Verbeke; F Van Aelst; M De Smet; A D Carides; K Eldridge; B J Gertz Journal: Eur J Cancer Date: 2001-05 Impact factor: 9.162
Authors: M Depré; A Van Hecken; M Oeyen; I De Lepeleire; T Laethem; P Rothenberg; K J Petty; A Majumdar; T Crumley; D Panebianco; A Bergman; J N de Hoon Journal: Eur J Clin Pharmacol Date: 2005-06-28 Impact factor: 2.953
Authors: Paul J Hesketh; Steven M Grunberg; Richard J Gralla; David G Warr; Fausto Roila; Ronald de Wit; Sant P Chawla; Alexandra D Carides; Juliana Ianus; Mary E Elmer; Judith K Evans; Klaus Beck; Scott Reines; Kevin J Horgan Journal: J Clin Oncol Date: 2003-10-14 Impact factor: 44.544
Authors: Sergio Poli-Bigelli; Jose Rodrigues-Pereira; Alexandra D Carides; Guoguang Julie Ma; Krista Eldridge; Anita Hipple; Judith K Evans; Kevin J Horgan; Francesca Lawson Journal: Cancer Date: 2003-06-15 Impact factor: 6.860
Authors: Simon Van Belle; Michael R Lichinitser; Rudolph M Navari; August M Garin; Marc L A Decramer; Alain Riviere; Myo Thant; Elmer Brestan; Binh Bui; Krista Eldridge; Marina De Smet; Nicole Michiels; Rick R Reinhardt; Alexandra D Carides; Judith K Evans; Barry J Gertz Journal: Cancer Date: 2002-06-01 Impact factor: 6.860
Authors: Bernardo Rapoport; Daniel Chua; Allen Poma; Sujata Arora; Yan Wang; Luis Enrique Fein Journal: Support Care Cancer Date: 2015-05-05 Impact factor: 3.603
Authors: Anton G Henssen; Andrea Odersky; Annabell Szymansky; Marleen Seiler; Kristina Althoff; Anneleen Beckers; Frank Speleman; Simon Schäfers; Katleen De Preter; Kathy Astrahanseff; Joachim Struck; Alexander Schramm; Angelika Eggert; Andreas Bergmann; Johannes H Schulte Journal: Oncotarget Date: 2017-01-03