Page last updated: 2024-10-15

aprepitant

Description

Aprepitant: A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

aprepitant : A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID135413536
CHEMBL ID1471
CHEBI ID499361
SCHEMBL ID264924
MeSH IDM0447596

Synonyms (114)

Synonym
HY-10052
c23h21f7n4o3
AB01274775-01
AB01275535-01
ono-7436
aprepitant
mk-0869
mk-869
l-754030
emend
aprepitant (jan/usp/inn)
emend (tn)
170729-80-3
cinvanti (tn)
D02968
NCGC00181785-01
DB00673
3h-1,2,4-triazol-3-one, 5-(((2r,3s)-2-((1r)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)-4-morpholinyl)methyl)-1,2-dihydro-
3h-1,2,4-triazol-3-one, 5-((2-(1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)-4-morpholinyl)methyl)-1,2-dihydro-, (2r-(2alpha(r*),3alpha))-
l 754030
mk 869
aprepitant [usan]
mk 0869
3-(((2r,3s)-3-(p-fluorophenyl)-2-(((alphar)-alpha-methyl-3,5-bis(trifluoromethyl)benzyl)oxy)morpholino)methyl)-delta(sup 2)-1,2,4-triazolin-5-one
HMS2090N12
CHEMBL1471 ,
nsc-748825
l-754,030
5-(((2r,3s)-2-((r)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholino)methyl)-2h-1,2,4-triazol-3(4h)-one
5-[(2r,3s)-2-[(r)-1-(3,5-bis-trifluoromethyl-phenyl)-ethoxy]-3-(4-fluoro-phenyl)-morpholin-4-ylmethyl]-2,4-dihydro-[1,2,4]triazol-3-one
3-[2-{1-[3,5-di(trifluoromethyl)phenyl]ethoxy}-3-(4-fluorophenyl)-1,4-oxazinan-4-ylmethyl]-4,5-dihydro-1h-1,2,4-triazol-5-one
bdbm50220136
5-{[(2r,3s)-2-{(1r)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}-3-(4-fluorophenyl)morpholin-4-yl]methyl}-2,4-dihydro-3h-1,2,4-triazol-3-one
aprepitantum
3-(((2r,3s)-3-(p-fluorophenyl)-2-(((alphar)-alpha-methyl-3,5-bis(trifluoromethyl)benzyl)oxy)morpholino)methyl)-delta(2)-1,2,4-triazolin-5-one
chebi:499361 ,
3h-1,4-triazol-3-one, 5-[[(2r,3s)-2-[(1r)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-
nsc748825
3-[((2r,5-bis(trifluoromethyl)benzyl]oxy}morpholino)methyl]-.delta.2-1,2,4-triazolin-5-one
5-[[(2r,3s)-2-[(1r)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,2-dihydro-1,2,4-triazol-3-one
ono 7436
nsc 748825
aprepitant [usan:inn:jan]
cinvanti
mk0869
1nf15yr6uy ,
unii-1nf15yr6uy
3h-1,2,4-triazol-3-one, 5-(((2r,3s)-2-((1r)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)-4-morpholinyl)methyl)-2,4-dihydro-
cas-170729-80-3
dtxcid801021794
tox21_113595
dtxsid3049047 ,
BCP9000312
AKOS015969344
aprepitant,mk-0869, l-754030, emend
5-[[(2r,3s)-2-[(1r)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3h-1,2,4-triazol-3-one
CS-0487
S1189
AKOS015895498
BRD-K52827117-001-01-6
gtpl3490
aprepitant [usp-rs]
aprepitant [inn]
aprepitant [orange book]
aprepitant [usp monograph]
aprepitant [mi]
aprepitant [ep monograph]
aprepitant [mart.]
aprepitant [jan]
aponvie
aprepitant [ema epar]
3-(((2r,3s)-3-(p-fluorophenyl)-2-(((.alpha.r)-.alpha.-methyl-3,5-bis(trifluoromethyl)benzyl)oxy)morpholino)methyl)-.delta.(sup 2)-1,2,4-triazolin-5-one.
aprepitant [vandf]
aprepitant [who-dd]
CCG-220747
SCHEMBL264924
smr002530053
MLS006011068
NCGC00344566-01
tox21_113595_1
Q-200647
3-(((2r,3s)-2-((r)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholino)methyl)-1h-1,2,4-triazol-5(4h)-one
AB01274775_02
3-{[(2r,3s)-2-[(1r)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl}-4,5-dihydro-1h-1,2,4-triazol-5-one
3-[[(2r,3s)-2-[(1r)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,4-dihydro-1,2,4-triazol-5-one
C21555
EX-A212
aprepitant`
SR-05000001531-1
sr-05000001531
emende
HMS3714E16
5-(((2r,3s)-2-((r)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholino)methyl)-1h-1,2,4-triazol-3(2h)-one
aprepitant, united states pharmacopeia (usp) reference standard
aprepitant (mk-0869, l-754030)
321125-94-4
3h-1,2,4-triazol-3-one, 5-[[(2r,3s)-2-[(1r)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-, rel-
aprepitant, form i
aprepitant, form ii
aprepitant (mk-0869) ,
AS-14638
HMS3884G05
CCG-264854
NCGC00181785-11
aprepitant- bio-x
BA164216
aprepitant (usp monograph)
aprepitant (ep monograph)
a04ad12
aprepitant (mart.)
aprepitant (usp-rs)
EN300-761455
3h-1,2,4-triazol-3-one,5-[[(2r,3s)-2-[(1r)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-,rel-
Z2937147473

Research Excerpts

Overview

Aprepitant is an NK-1 antagonist used to treat nausea and vomiting. Fosaprepitant is a relevant alternative in preventing and treating PONV in patients who underwent bariatric/metabolic surgical procedures.

ExcerptReference
"Aprepitant is an NK-1 antagonist used to treat nausea and vomiting."( Aprepitant is a novel, selective activator of the K2P channel TRAAK.
Avkiran, T; Byrom, L; Gaffey, F; Jerman, J; Large, JM; Mathie, A; McCoull, D; Vaitone, E; Veale, EL; Walsh, Y; Wright, PD, 2022
)
"Aprepitant (Apr) is an effective antiemetic agent for chemotherapy-induced nausea and vomiting (CINV). "( Clinical interaction between dexamethasone and aprepitant in chemotherapy for lymphoma.
Ashizawa, M; Fujiwara, SI; Hatano, K; Ikeda, T; Ito, S; Kanda, Y; Kawaguchi, SI; Mashima, K; Minakata, D; Morita, K; Nagayama, T; Nakano, H; Ohmine, K; Sato, K; Toda, Y; Ueda, M; Umino, K; Yamamoto, C; Yamasaki, R, 2022
)
"Aprepitant is an important medication used to prevent chemotherapy-induced nausea and vomiting (CINV)."( Prolonged administration of aprepitant improves cisplatin-based chemotherapy-induced nausea and vomiting.
Chen, P; Li, Y; Liu, B; Sun, Y; Wang, Y; Xie, K; Zhu, J, 2022
)
"Aprepitant is a neurokinin-1 receptor antagonist, and recent guidelines by the American Neurogastoenterology and Motility Society recommend its use as prophylaxis in moderate-to severe cyclic vomiting syndrome (CVS). "( Efficacy of aprepitant as a prophylactic medication in adults with cyclic vomiting syndrome.
Garacchi, Z; Kovacic, K; Mooers, H; Partovi, O; Patel, M; Venkatesan, T, 2023
)
"Aprepitant is a safe and effective prophylactic medication in adults with refractory CVS. "( Efficacy of aprepitant as a prophylactic medication in adults with cyclic vomiting syndrome.
Garacchi, Z; Kovacic, K; Mooers, H; Partovi, O; Patel, M; Venkatesan, T, 2023
)
"Fosaprepitant is a relevant alternative in preventing and treating PONV in patients who underwent bariatric/metabolic surgical procedures."( Impact of Emend on Perioperative Bariatric Surgery Antiemetic Utilization, Patient Satisfaction, and Costs.
Aghazarian, GS; Ghanem, M; Jawad, MA; Lastrapes, L; Lind, R; Motola, D; Perry, M; Singletary, N; Teixeira, AF, 2023
)
"Aprepitant is a neurokinin-1 receptor blocker and has been shown to reduce chemotherapy-related nausea and vomiting and PONV."( The use of aprepitant for the prevention of postoperative nausea and vomiting in endoscopic transsphenoidal pituitary surgery.
Adappa, ND; Atkins, JH; Chang, J; Douglas, JE; Grady, MS; Jackson, C; Kohanski, MA; Lee, DJ; Lee, JYK; Palmer, JN; Wilensky, J; Yoshor, D, 2023
)
"Aprepitant is a kind of NK-1R antagonist."( The NK-1R Antagonist Aprepitant Prevents LPS-Induced Oxidative Stress and Inflammation in RAW264.7 Macrophages.
Bai, ZZ; Li, CH; Li, HY; Sheng, CL; Zhao, XN, 2020
)
"Aprepitant is a neurokinin-1 receptor antagonist approved for the treatment of chemotherapy-induced nausea. "( Aprepitant in the Treatment of Subacute Sclerosing Panencephalitis: A Randomized, Double-Blind, Placebo-Controlled Study.
Anlar, B; Arioz, F; Arman-Kandirmaz, E; Gumeler, E; Konuskan, B; Oncel, I; Parlak, S; Sancar, M; Tezcan, S, 2020
)
"Aprepitant is a selective SP/NK-1 receptor antagonist and used in postoperative and chemotherapeutics induced emesis and vomiting. "( Can aprepitant used for nausea and vomiting be good gastrointestinal complaints?
Bal Tastan, T; Cadirci, E; Halici, Z; Kose, D; Ugan, RA; Un, H; Yayla, M, 2020
)
"Aprepitant is a neurokinin-1 receptor antagonist approved for the prevention of chemotherapy-induced and postoperative nausea and vomiting (CINV, PONV)."( Aprepitant for the Treatment of Chronic Refractory Pruritus.
Alhariri, JM; He, A; Kwatra, MM; Kwatra, SG; Sweren, RJ, 2017
)
"Aprepitant is a NK-1 receptor antagonist."( Substance P Antagonist Aprepitant Shows no Additive Effect Compared with Standardized Topical Treatment Alone in Patients with Atopic Dermatitis.
Bradley, M; Hall, MA; Heilborn, J; Holmberg, J; Holst, M; Killasli, H; Lönndahl, L; Nordlind, K; Theodorsson, E, 2018
)
"Aprepitant is a selective high‑affinity antagonist of the human neurokinin‑1 (NK‑1) receptor (NK1R) with robust antitumor activity."( Antitumor activity of neurokinin-1 receptor antagonists in MG-63 human osteosarcoma xenografts.
Berger, M; Carranza, A; Coveñas, R; Gonzalez-Ortega, A; Muñoz, M; Rosso, M, 2014
)
"Aprepitant is a neurokinin-1 receptor antagonist affecting the substance P receptor."( Treatment of pruritus in early-stage hypopigmented mycosis fungoides with aprepitant.
Albarrán Planelles, C; Fernández Anguita, MJ; Jiménez Gallo, D; Linares Barrios, M; Márquez Enríquez, J; Rodríguez Mateos, ME,
)
"Fosaprepitant is an antiemetic used for chemotherapy-induced nausea and vomiting. "( An analysis of fosaprepitant-induced venous toxicity in patients receiving highly emetogenic chemotherapy.
Anderson, KJ; Grendahl, DC; Hegerova, LT; Hilger, CR; Leal, AD; Loprinzi, CL; Seisler, DK; Sorgatz, KM, 2015
)
"Aprepitant is a neurokinin 1 receptor antagonist approved for prevention of chemotherapy-induced and post-operative nausea and vomiting. "( Addition of an NK1 receptor antagonist to an SSRI did not enhance the antidepressant effects of SSRI monotherapy: results from a randomized clinical trial in patients with major depressive disorder.
Ball, WA; Hargreaves, RJ; Lines, C; Reines, SA; Snavely, DB; Szegedi, A, 2014
)
"Aprepitant is a P/neurokinin-1 receptor antagonist approved for the prevention of CINV in moderate emetic risk chemotherapy."( Phase II, open label, randomized comparative trial of ondansetron alone versus the combination of ondansetron and aprepitant for the prevention of nausea and vomiting in patients with hematologic malignancies receiving regimens containing high-dose cytara
Badar, T; Borthakur, G; Cortes, J; Ferrajoli, A; Garcia-Manero, G; Kadia, T; Kantarjian, H; Mattiuzzi, G; O'Brien, S; Poku, R; Wierda, W, 2015
)
"Aprepitant (APT) is a lipophilic, poorly water soluble drug with moderate permeability characteristic. "( Aprepitant loaded solid preconcentrated microemulsion for enhanced bioavailability: A comparison with micronized Aprepitant.
Kamboj, S; Rana, V; Sharma, R; Singh, K, 2015
)
"Aprepitant is a relatively new agent for this condition which may be superior to other treatment."( Aprepitant for postoperative nausea and vomiting: a systematic review and meta-analysis.
Borle, A; Goudra, B; Makkar, JK; Rewari, V; Singh, PM; Sinha, AC; Trikha, A, 2016
)
"Aprepitant acts as an inhibitor of the binding of substance P to the neurokinin-1 receptor and, consequently, may reduce the frequency of paclitaxel-induced HSR."( Efficacy of aprepitant for the prevention of chemotherapy-induced nausea and vomiting with a moderately emetogenic chemotherapy regimen: a multicenter, placebo-controlled, double-blind, randomized study in patients with gynecologic cancer receiving paclit
Hasuo, Y; Ichinoe, A; Kato, K; Kobayashi, H; Masuda, S; Nishida, M; Ogawa, S; Ohgami, T; Saito, T; Sakai, K; Shimokawa, M; Sonoda, K; Ueoka, Y; Yahata, H, 2016
)
"Aprepitant is a known inducer of CYP2C9, the main warfarin-metabolizing enzyme. "( Assessment of Drug-Drug Interaction between Warfarin and Aprepitant and Its Effects on PT-INR of Patients Receiving Anticancer Chemotherapy.
Hisaka, A; Ohno, Y; Suzuki, H; Takaki, J; Yamada, M; Yamaguchi, R, 2016
)
"Aprepitant is an FDA-approved medication for chemotherapy-induced nausea and vomiting. "( Aprepitant for refractory cutaneous T-cell lymphoma-associated pruritus: 4 cases and a review of the literature.
Chau, NG; Kupper, TS; LeBoeuf, NR; Song, JS; Tawa, M, 2017
)
"Aprepitant (AP) is a known inhibitor of cytochrome P450 3A4 which may affect tacrolimus metabolism. "( Effect of aprepitant on intravenous tacrolimus disposition in reduced intensity hematopoietic stem cell transplantation.
Abidi, MH; Ayash, LJ; Cadotte, C; Cronin, SM; Edwards, DJ; Ibrahim, RB; Jacobson, PA; Mulawa, J; Smith, DW; Uberti, JP, 2008
)
"Aprepitant is a selective NK-1 receptor antagonist approved as part of combination therapy with a corticosteroid and a 5-HT(3) receptor antagonist for the prevention of acute and delayed CINV in patients receiving moderately and highly emetogenic chemotherapy."( Fosaprepitant: a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.
Navari, RM, 2008
)
"Aprepitant is a selective high-affinity antagonist of human substance P (SP)/Neurokinin-1 (NK-1) receptors. "( The NK-1 receptor antagonist aprepitant as a broad spectrum antitumor drug.
Muñoz, M; Rosso, M, 2010
)
"Aprepitant (Emend) is a neurokinin-1 (NK(1)) receptor antagonist that is able to alleviate the emetic effects of substance P. "( Aprepitant: a review of its use in the prevention of nausea and vomiting.
Curran, MP; Robinson, DM, 2009
)
"Aprepitant is a selective high-affinity antagonist of the human NK-1 receptor."( The NK-1 receptor is expressed in human melanoma and is involved in the antitumor action of the NK-1 receptor antagonist aprepitant on melanoma cell lines.
Coveñas, R; González-Ortega, A; Muñoz, M; Robles-Frias, MJ; Rosso, M; Rosso, R; Salinas-Martín, MV, 2010
)
"Aprepitant is a new neurokinin-1 (NK(1) ) receptor antagonist developed as a treatment for chemotherapy-induced nausea and vomiting (CINV). "( Multicenter, phase II, placebo-controlled, double-blind, randomized study of aprepitant in Japanese patients receiving high-dose cisplatin.
Eguchi, K; Hoshi, E; Katsumata, N; Kawahara, M; Takagi, M; Takahashi, T, 2010
)
"Fosaprepitant is an intravenous prodrug of aprepitant that offers a new alternative to patients with CINV. "( Pharmacokinetic evaluation of fosaprepitant dimeglumine.
Colon-Gonzalez, F; Kraft, WK, 2010
)
"Aprepitant is a neurokin-1 receptor antagonist with a long duration of action and no sedative side effect."( A comparison of the combination of aprepitant and dexamethasone versus the combination of ondansetron and dexamethasone for the prevention of postoperative nausea and vomiting in patients undergoing craniotomy.
Borel, CO; Gan, TJ; Habib, AS; Keifer, JC; White, WD, 2011
)
"Aprepitant is a very active antiemetic drug for the prevention of delayed nausea and vomiting induced by mFOLFOX6 regimen."( [Clinical usefulness of oral aprepitant for alleviation of delayed nausea and vomiting induced by mFOLFOX6--report of a case].
Abe, T; Hachiro, Y; Kunimoto, M, 2010
)
"Fosaprepitant 150 mg is a weak inhibitor of CYP3A4."( Pharmacokinetics of oral dexamethasone and midazolam when administered with single-dose intravenous 150 mg fosaprepitant in healthy adult subjects.
Caro, L; Jin, B; Marbury, TC; Murphy, G; Ngo, PL; Panebianco, D; Shadle, CR; Valentine, J, 2011
)
"Aprepitant is a NK1R antagonist approved by FDA as an antiemetic."( A randomized, placebo controlled, double masked phase IB study evaluating the safety and antiviral activity of aprepitant, a neurokinin-1 receptor antagonist in HIV-1 infected adults.
Barrett, JS; Douglas, SD; Gonin, R; Kim, D; Korelitz, J; Tebas, P; Tuluc, F; Wagner, W; Zhao, H, 2011
)
"Aprepitant is a selective NK1 antagonist currently marketed for clinical use as an anti-emetic."( Effects of the NK1 antagonist, aprepitant, on response to oral and intranasal oxycodone in prescription opioid abusers.
Heilig, M; Henderson, P; Lofwall, MR; Nuzzo, PA; Walsh, SL, 2013
)
"Aprepitant (APR) is a water insoluble drug approved for the treatment of chemotherapy induced nausea and vomiting (CINV) and post-operative nausea and vomiting (PONV). "( Inclusion complex of aprepitant with cyclodextrin: evaluation of physico-chemical and pharmacokinetic properties.
Ansari, KA; Dhawan, S; Kaul, NS; Krishnamurthy, T; Kumar, D; Pillai, R; Ridhurkar, DN, 2013
)
"Aprepitant is a novel neurokinin 1 (NK(1)) antagonist that has been shown to improve control of chemotherapy-induced nausea and vomiting (CINV) when added to a standard antiemetic regimen of a 5-hydroxytriptamine-3 antagonist plus a corticosteroid. "( Addition of the neurokinin 1 receptor antagonist aprepitant to standard antiemetic therapy improves control of chemotherapy-induced nausea and vomiting. Results from a randomized, double-blind, placebo-controlled trial in Latin America.
Carides, AD; Eldridge, K; Evans, JK; Hipple, A; Horgan, KJ; Julie Ma, G; Lawson, F; Poli-Bigelli, S; Rodrigues-Pereira, J, 2003
)
"Aprepitant is a neurokinin(1) receptor antagonist that, in combination with a corticosteroid and a 5-hydroxytryptamine(3) receptor antagonist, has been shown to be very effective in the prevention of chemotherapy-induced nausea and vomiting. "( Effects of the neurokinin1 receptor antagonist aprepitant on the pharmacokinetics of dexamethasone and methylprednisolone.
Blum, RA; Deutsch, PJ; Gargano, C; Goldberg, MR; Goldwater, DR; Gottesdiener, KM; Hesney, M; Iwamoto, M; Lines, CR; Majumdar, AK; McCrea, JB; Murphy, MG; Panebianco, DL; Petty, KJ, 2003
)
"Aprepitant is a neurokinin(1) receptor antagonist that enhances prevention of chemotherapy-induced nausea and vomiting when added to conventional therapy with a corticosteroid and a 5-hydroxytryptamine(3) (5-HT(3)) antagonist. "( Effects of aprepitant on cytochrome P450 3A4 activity using midazolam as a probe.
Blum, RA; Constanzer, M; Dru, J; Goldberg, MR; Gottesdiener, KM; Hesney, M; Lines, CR; Majumdar, AK; McCrea, JB; Murphy, G; Panebianco, DL; Petty, KJ, 2003
)
"Aprepitant is a highly selective neurokinin-1 receptor antagonist that, in combination with a corticosteroid and a 5-hydroxytryptamine3 (5HT3) receptor antagonist, has been shown to be efficacious in the prevention of highly emetogenic chemotherapy-induced nausea and vomiting. "( Lack of effect of aprepitant on digoxin pharmacokinetics in healthy subjects.
Brackett, LE; De Smet, M; Feuring, M; Goldberg, MR; Gottesdiener, KM; Hesney, M; Lee, Y; Majumdar, AK; Michiels, N; Murphy, MG; Orlowski, LH; Petty, KJ; Wehling, M, 2003
)
"Aprepitant is an oral neurokinin-1 receptor antagonist which acts centrally to block chemotherapy-induced emesis. "( Aprepitant in antiemetic combinations to prevent chemotherapy-induced nausea and vomiting.
Olver, IN, 2004
)
"Aprepitant is a highly selective substance P (neurokinin 1 [NK(1)] receptor) antagonist that significantly improves the pharmacotherapy of acute and delayed highly emetogenic chemotherapy-induced nausea and vomiting, probably through an action in the brain stem region of the central nervous system. "( Human positron emission tomography studies of brain neurokinin 1 receptor occupancy by aprepitant.
Antoni, G; Battisti, WP; Bergström, M; Bradstreet, TE; Burns, HD; Constanzer, ML; Eskola, O; Gargano, C; Goldberg, MR; Hargreaves, RJ; Hietala, J; Långström, B; Majumdar, AK; Ogren, M; Petty, KJ; Reines, SA; Scheinin, M; Sciberras, D; Solin, O, 2004
)
"Aprepitant is a substrate, a moderate inhibitor and an inducer of cytochrome P450 (CYP)3A4 and CYP2C9."( Aprepitant: a neurokinin-1 receptor antagonist for the treatment of chemotherapy-induced nausea and vomiting.
Navari, RM, 2004
)
"Aprepitant is a selective neurokinin-1 receptor antagonist that is effective for the prevention of nausea and vomiting caused by highly emetogenic chemotherapy. "( Lack of effect of aprepitant on the pharmacokinetics of docetaxel in cancer patients.
Ahmed, T; Cocquyt, V; de Smet, M; Fedgchin, M; Gottesdiener, KM; Hande, K; Majumdar, A; Murphy, MG; Nygren, P; Panebianco, D; Petty, KJ; van Belle, S; van Dyck, K, 2005
)
"Aprepitant is a selective antagonist of substance P/neurokinin 1 that augments the benefit of 5-HT(3) receptor antagonists in the prevention of chemotherapy-induced nausea and vomiting."( Pharmacokinetics of palonosetron in combination with aprepitant in healthy volunteers.
Cullen, MT; Gallagher, SC; Hunt, TL; Shah, AK, 2005
)
"Aprepitant is a neurokinin-1 (NK1)-receptor antagonist developed as an antiemetic for chemotherapy-induced nausea and vomiting."( Effect of aprepitant on the pharmacokinetics and pharmacodynamics of warfarin.
Bergman, A; Crumley, T; de Hoon, JN; De Lepeleire, I; Depré, M; Laethem, T; Majumdar, A; Oeyen, M; Panebianco, D; Petty, KJ; Rothenberg, P; Van Hecken, A, 2005
)
"Aprepitant is a selective high-affinity human SP/NK1 receptor antagonist approved by the FDA in 2003."( [Neurokinin 1 receptor antagonists--between hope and disappointment].
Fleischer, F; Nieber, K; Rost, K, 2006
)
"Fosaprepitant is an intravenous formulation of aprepitant, an oral NK1 antagonist used to prevent chemotherapy-induced nausea and vomiting. "( Tolerability of fosaprepitant and bioequivalency to aprepitant in healthy subjects.
Bergman, A; Constanzer, M; Dru, J; Evans, JK; Gambale, J; Han, TH; Jin, B; Lasseter, KC; Majumdar, A; Murphy, MG, 2007
)
"Aprepitant is a selective NK-1 receptor antagonist approved as part of combination therapy with a corticosteroid and a 5-HT(3) receptor antagonist for the prevention of acute and delayed CINV."( Fosaprepitant (MK-0517): a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.
Navari, RM, 2007
)

Effects

Oral aprepitant has a large interindividual variation in clinical responses in advanced cancer. Aprepitant allows the majority of patients to complete their chemotherapies without significant morbidity.

Fosaprepitant 115 mg has been submitted for FDA approval as an alternative on day 1 of a 3-day oral aprepitant regimen. Aprepitant has been shown to reduce chemotherapy-induced nausea and vomiting in children receiving highly emetogenic chemotherapy (HEC)

ExcerptReference
"Oral aprepitant has a large interindividual variation in clinical responses in advanced cancer. "( Associations of plasma aprepitant and its N-dealkylated metabolite with cachexia status and clinical responses in head and neck cancer patients.
Hosokawa, S; Kawakami, J; Naito, T; Shibata, K; Suzuki, Y, 2023
)
"Aprepitant has a significant role in the management of CINV, as it allows the majority of patients to complete their chemotherapies without significant morbidity. "( Prevention of chemotherapy induced nausea and vomiting: a focus on aprepitant.
Chawla, SP; Giles, FJ; Pandya, DM; Sankhala, KK; Sarantopoulos, J; Soefje, SA, 2009
)
"Aprepitant has been shown to reduce chemotherapy-induced nausea and vomiting in children receiving highly emetogenic chemotherapy (HEC). "( Cost-effectiveness analysis of aprepitant-based anti-emetic regimen for children receiving highly emetogenic chemotherapy: Individual patient data analysis of a randomized trial.
Bakhshi, S; Ganguly, S; Giri, RK; Rasheed, AA; Sasi, A; Sharma, P; Sra, MS, 2022
)
"Aprepitant has been classified into BCS class IV, which has low permeability and poor water solubility, resulting in low bioavailability. "( Fabrication of an aprepitant nanosuspension using hydroxypropyl chitosan to increase the bioavailability.
Ao, W; Bai, M; Li, S; Li, Y; Liu, J; Xiao, Y, 2022
)
"fosaprepitant has been approved as an alternative to 3 day oral aprepitant, a neurokinin-1 receptor antagonist, and improves prevention of chemotherapy-induced nausea and vomiting (CINV)."( Evaluation of aprepitant and fosaprepitant in pediatric patients.
Arakawa, A; Arima, T; Hashimoto, H; Ishimaru, S; Kumamoto, T; Makino, Y; Nakajima, M; Ogawa, C; Saito, Y; Shirakawa, N; Sonoda, T; Sugiyama, M; Yamaguchi, M, 2019
)
"Aprepitant has shown to be effective for CINV in adults, but little is known on its effect in pediatrics."( Emesis control by aprepitant in children and adolescents with chemotherapy.
Bauters, TG; Benoit, Y; Laureys, G; Robays, H; Verlooy, J, 2013
)
"Aprepitant has been shown in small studies to be efficacious for treating chronic and malignancy-associated pruritus. "( Aprepitant for refractory cutaneous T-cell lymphoma-associated pruritus: 4 cases and a review of the literature.
Chau, NG; Kupper, TS; LeBoeuf, NR; Song, JS; Tawa, M, 2017
)
"Fosaprepitant 150 mg has been submitted to regulatory agencies for consideration of approval as a single-day alternative to the 3-day oral aprepitant antiemetic regimen currently marketed."( Pharmacokinetics of oral dexamethasone and midazolam when administered with single-dose intravenous 150 mg fosaprepitant in healthy adult subjects.
Caro, L; Jin, B; Marbury, TC; Murphy, G; Ngo, PL; Panebianco, D; Shadle, CR; Valentine, J, 2011
)
"Aprepitant has been noted to produce modest decreases in plasma S(-)-warfarin concentrations, suggesting potential induction of CYP2C9."( Evaluation of potential inductive effects of aprepitant on cytochrome P450 3A4 and 2C9 activity.
Blum, RA; Bradstreet, TE; Evans, JK; Gargano, C; Lee, Y; Majumdar, AK; Petty, KJ; Shadle, CR, 2004
)
"As aprepitant has been shown to be a moderate inhibitor of the cytochrome P450 (CYP) 3A4 isoenzyme, its effect on the pharmacokinetics and metabolism of cyclophosphamide and thiotepa was evaluated."( Aprepitant inhibits cyclophosphamide bioactivation and thiotepa metabolism.
Beijnen, JH; de Jonge, ME; Holtkamp, MJ; Huitema, AD; Rodenhuis, S; van Dam, SM, 2005
)
"Aprepitant has been approved for the prevention and treatment of acute (0-24 h after chemotherapy) and delayed (1-5 days after chemotherapy) emesis resulting from cisplatin-based chemotherapy and moderately emetogenic chemotherapy."( Neurokinin-1-receptor antagonists: a new approach in antiemetic therapy.
Jordan, K, 2006
)
"Fosaprepitant 115 mg has been submitted for FDA approval as an alternative on day 1 of a 3-day oral aprepitant regimen, with oral aprepitant administered on days 2 and 3."( Fosaprepitant (MK-0517): a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.
Navari, RM, 2007
)

Actions

Aprepitant did not lower incidence of post-ERCP pancreatitis in this preliminary human study. The drug did not increase severe adverse events.

ExcerptReference
"Aprepitant did not increase severe adverse events."( Aprepitant for Cough Suppression in Advanced Lung Cancer: A Randomized Trial.
Bhattacharjee, A; Ishi, S; Joshi, A; Kannan, S; Maske, K; Menon, N; Mukadam, SA; Noronha, V; Patil, VM; Prabhash, K; Shah, S, 2020
)
"Aprepitant did not lower incidence of post-ERCP pancreatitis in this preliminary human study. "( Pilot study of aprepitant for prevention of post-ERCP pancreatitis in high risk patients: a phase II randomized, double-blind placebo controlled trial.
Branch, MS; Jowell, P; Liddle, R; Obando, J; Poleski, M; Shah, TU, 2012
)

Treatment

Aprepitant treatment resulted in decreased plasma SP levels and affected 176 plasma proteins (56 after FDR) and several metabolic pathways, including inflammation and lipid metabolism. Treatment with aprepitant (P < 0.0001), older age, ethanol use, and no history of HIV were all significantly associated with improved complete response.

ExcerptReference
"Aprepitant treatment normalized all parameters compared to cisplatin treated group."( A novel effect of Aprepitant: Protection for cisplatin-induced nephrotoxicity and hepatotoxicity.
Bayir, Y; Cadirci, E; Halici, Z; Kose, D; Selli, J; Ugan, RA; Un, H, 2020
)
"Aprepitant treatment offers an opportunity to target inflammation and mood disorders frequently co-existing in chronic HIV infection."( Effect of aprepitant on kynurenine to tryptophan ratio in cART treated and cART naïve adults living with HIV.
Douglas, SD; Evans, DL; Kinder, A; Pappa, V; Rappaport, J; Spitsin, S, 2021
)
"Aprepitant treatment resulted in decreased plasma SP levels and affected 176 plasma proteins (56 after FDR) and several metabolic pathways, including inflammation and lipid metabolism."( Antiinflammatory effects of aprepitant coadministration with cART regimen containing ritonavir in HIV-infected adults.
Barrett, JS; Douglas, SD; Evans, DL; Kim, D; Pappa, V; Spitsin, S; Taylor, D; Tebas, P, 2017
)
"Aprepitant treatment had no effect on PTSD symptoms or subjective or physiological responses to stress or alcohol cues. "( The neurokinin-1 receptor antagonist aprepitant in co-morbid alcohol dependence and posttraumatic stress disorder: a human experimental study.
Diamond, CA; George, DT; Heilig, M; Hommer, DW; Kwako, LE; Momenan, R; Schwandt, ML; Shaham, Y; Sinha, R; Spagnolo, PA, 2015
)
"Aprepitant treatment was associated with significant decreases of median within patient change in percentages of CD4(+) T cells expressing programmed death 1 (-4.8%; P = 0.04), plasma substance P (-34.0 pg/ml; P = 0.05) and soluble CD163 (-563 ng/ml; P = 0.02), with no significant changes in the placebo arm."( Reduction of soluble CD163, substance P, programmed death 1 and inflammatory markers: phase 1B trial of aprepitant in HIV-1-infected adults.
Barrett, JS; Catalano, R; Douglas, SD; Elci, O; Evans, DL; Kim, D; Korelitz, JJ; Spitsin, S; Tebas, P; Tuluc, F; Wagner, W; Winters, A, 2015
)
"Aprepitant-treated patients had decreased numbers of CD4(+) programmed death 1-positive cells and decreased plasma levels of substance P and soluble CD163, suggesting that blockade of the neurokinin 1 receptor pathway has a role in modulating monocyte activation in HIV infection."( Reduction of soluble CD163, substance P, programmed death 1 and inflammatory markers: phase 1B trial of aprepitant in HIV-1-infected adults.
Barrett, JS; Catalano, R; Douglas, SD; Elci, O; Evans, DL; Kim, D; Korelitz, JJ; Spitsin, S; Tebas, P; Tuluc, F; Wagner, W; Winters, A, 2015
)
"Pretreatment with aprepitant successfully ameliorated and improved all biochemical and molecular parameters induced by DIC."( Involvement of NOX-4/JAK/STAT pathway in the protective effect of aprepitant against diclofenac-induced renal toxicity.
Hafez, HM; Mohamed, MZ; Rifaai, RA; Waz, S, 2022
)
"Treatment with aprepitant and its vehicle alone resulted in a potentiating of the infiltration of nickel reactions compared with test reactions obtained after no treatment (1147 + 423 mm(3) and 1427 + 566 mm(3) vs 683 +202 mm(3)) (p = 0.03)."( Topical non-peptide antagonists of sensory neurotransmitters substance P and CGRP do not modify patch test and prick test reactions: a vehicle-controlled, double-blind pilot study.
Edvinsson, L; Wallengren, J, 2014
)
"Treatment with aprepitant (p < 0.0001), male gender (p = 0.023), cisplatin dose <80 mg/m(2) (p = 0.001), age >or=65 years (p = 0.021), and five or more alcoholic drinks per week (p = 0.027) were all significantly associated with improved complete response. "( Evaluation of risk factors predictive of nausea and vomiting with current standard-of-care antiemetic treatment: analysis of two phase III trials of aprepitant in patients receiving cisplatin-based chemotherapy.
Aapro, M; Carides, AD; Hesketh, PJ; Street, JC, 2010
)
"Treatment with aprepitant (P < 0.0001), older age (P = 0.006), ethanol use (P = 0.0048), and no history of morning sickness (P = 0.0007) were all significantly associated with reduced likelihood of emesis. "( Evaluation of risk factors predictive of nausea and vomiting with current standard-of-care antiemetic treatment: analysis of phase 3 trial of aprepitant in patients receiving adriamycin-cyclophosphamide-based chemotherapy.
Carides, AD; Street, JC; Warr, DG, 2011
)
"Pre-treatment with aprepitant did not increase adverse events including constipation and elevation of alanine transaminase."( [Efficacy and safety of aprepitant in patients with breast cancer].
Aogi, K; Eguchi, H; Hara, F; Kiyoto, S; Matsuhisa, T; Osumi, S; Oze, I; Tagashira, H; Takabatake, D; Takahashi, M; Takashima, S, 2011
)
"Pre-treatment with aprepitant (200 mg) significantly enhanced ratings of oxycodone subjective effects related to euphoria and liking and doubled the street value estimates for the highest test doses of oxycodone by both routes."( Effects of the NK1 antagonist, aprepitant, on response to oral and intranasal oxycodone in prescription opioid abusers.
Heilig, M; Henderson, P; Lofwall, MR; Nuzzo, PA; Walsh, SL, 2013
)
"Treatment with aprepitant (10(-6) M) inhibited infection of macrophages with the AZT-resistant viruses (A018, A012) by 0.7 log(10)."( Neurokinin-1 receptor antagonist (aprepitant) inhibits drug-resistant HIV-1 infection of macrophages in vitro.
Douglas, SD; Ho, WZ; Lai, JP; Tebas, P; Tuluc, F; Wang, X, 2007
)

Toxicity

Fosaprepitant is an intravenous neurokinin-1 receptor antagonist for chemotherapy-induced nausea and vomiting. It contains polysorbate 80, which is associated with infusion-site adverse events (ISAEs) and hypersensitivity systemic reactions (HSRs)

ExcerptReference
" A potential side effect is neurotoxicity, often manifesting as confusion, hallucination, or seizure."( Characterization of the occurrence of ifosfamide-induced neurotoxicity with concomitant aprepitant.
Hatfield Seung, A; Howell, JE; Nesbit, SA; Szabatura, AH, 2008
)
" In the previous five cycles of ifosfamide, carboplatin, and etoposide, the patient had no problems with the neurotoxic adverse effects associated with ifosfamide use."( Possible contribution of aprepitant to ifosfamide-induced neurotoxicity.
Jarkowski, A, 2008
)
" The literature review was performed using Medline with the following search terms: adverse events, aprepitant, chemotherapy, CYP3A4, MK-0869, neurokinin(1) receptor antagonist, safety and tolerability."( Safety evaluation of aprepitant for the prevention of chemotherapy-induced nausea and vomiting.
Herrstedt, J; Ruhlmann, CH, 2011
)
" Pre-treatment with aprepitant did not increase adverse events including constipation and elevation of alanine transaminase."( [Efficacy and safety of aprepitant in patients with breast cancer].
Aogi, K; Eguchi, H; Hara, F; Kiyoto, S; Matsuhisa, T; Osumi, S; Oze, I; Tagashira, H; Takabatake, D; Takahashi, M; Takashima, S, 2011
)
" The rates of adverse drug events (ADEs) did not significantly differ between groups."( Antiemetic effectiveness and safety of aprepitant in patients with hematologic malignancy receiving multiday chemotherapy.
Akashi, K; Egashira, N; Hiraiwa, H; Ichinose, K; Ikesue, H; Iwasaki, H; Kato, K; Miyamoto, T; Oishi, R; Sakurai, A; Takenaka, K; Teshima, T; Uchida, M, 2013
)
" The frequencies of adverse drug events (ADEs) were not significantly different between two groups."( Effectiveness and safety of antiemetic aprepitant in Japanese patients receiving high-dose chemotherapy prior to autologous hematopoietic stem cell transplantation.
Akashi, K; Egashira, N; Hiraiwa, H; Ichinose, K; Ikesue, H; Iwasaki, H; Kato, K; Miyamoto, T; Muta, T; Oishi, R; Sakurai, A; Shiratsuchi, M; Suetsugu, K; Takenaka, K; Teshima, T; Uchida, M, 2013
)
" In general, NK-1 receptor antagonists are safe and well tolerated."( Safety of neurokinin-1 receptor antagonists.
Coveñas, R; Muñoz, M, 2013
)
"A search was carried out in Medline using the following terms: adverse events, aprepitant, casopitant, clinical trials, CP-122,721, ezlopitant, fosaprepitant, NK-1 receptor antagonists, randomized, safety, side effects, tolerability and vofopitant."( Safety of neurokinin-1 receptor antagonists.
Coveñas, R; Muñoz, M, 2013
)
" Rates of other frequently observed adverse drug events were similar between groups."( Efficacy and safety of aprepitant in allogeneic hematopoietic stem cell transplantation.
Akashi, K; Egashira, N; Hiraiwa, H; Ichinose, K; Ikesue, H; Iwasaki, H; Kato, K; Miyamoto, T; Muta, T; Nagata, K; Oishi, R; Sakurai, A; Shiratsuchi, M; Suetsugu, K; Takenaka, K; Teshima, T; Uchida, M, 2013
)
" Of the 460 cycles, adverse events, drug-related adverse events, and serious adverse events occurred in 179 (38."( Safety and efficacy of aprepitant, ramosetron, and dexamethasone for chemotherapy-induced nausea and vomiting in patients with ovarian cancer treated with paclitaxel/carboplatin.
Bae, DS; Choi, CH; Kim, BG; Kim, HJ; Kim, MK; Kim, TJ; Lee, JW; Lee, YY; Park, JY; Yoon, A, 2014
)
"Triplet therapy using an increased-dose of DEX is suggested to be safe and effective for patients receiving HEC."( Efficacy and safety of an increased-dose of dexamethasone in patients receiving fosaprepitant chemotherapy in Japan.
Akashi, K; Arita, S; Ariyama, H; Baba, E; Komoda, M; Kumagai, H; Kusaba, H; Nagata, K; Nakano, M; Okumura, Y; Takaishi, S; Tamura, S; Uchida, M, 2014
)
" Incidence and severity of nausea were assessed based on the Common Terminology Criteria for Adverse Events (CTCAE) and a subjective rating scale completed by patients."( Antiemetic efficacy and safety of a combination of palonosetron, aprepitant, and dexamethasone in patients with testicular germ cell tumor receiving 5-day cisplatin-based combination chemotherapy.
Arai, Y; Habuchi, T; Hamada, S; Hinotsu, S; Kamba, T; Kawai, K; Kawakami, K; Narita, S; Nishiyama, H; Ogawa, O; Yamada, S, 2014
)
" The reported adverse drug reactions were hiccups (13."( Antiemetic efficacy and safety of a combination of palonosetron, aprepitant, and dexamethasone in patients with testicular germ cell tumor receiving 5-day cisplatin-based combination chemotherapy.
Arai, Y; Habuchi, T; Hamada, S; Hinotsu, S; Kamba, T; Kawai, K; Kawakami, K; Narita, S; Nishiyama, H; Ogawa, O; Yamada, S, 2014
)
" The most common adverse reactions were constipation and fatigue (reported by three patients each)."( Efficacy and safety of triple therapy with aprepitant, palonosetron, and dexamethasone for preventing nausea and vomiting induced by cisplatin-based chemotherapy for gynecological cancer: KCOG-G1003 phase II trial.
Abe, M; Furuya, K; Hasegawa, K; Hirashima, Y; Itamochi, H; Ito, K; Kai, K; Kuritani, K; Matoda, M; Nasu, K; Otsuki, T; Sato, S; Takano, M; Takeshima, N; Terao, K; Tsubamoto, H, 2014
)
" We recently reported increased infusion site adverse events (ISAE) in a cohort of breast cancer patients receiving chemotherapy with doxorubicin and cyclophosphamide (AC)."( An analysis of fosaprepitant-induced venous toxicity in patients receiving highly emetogenic chemotherapy.
Anderson, KJ; Grendahl, DC; Hegerova, LT; Hilger, CR; Leal, AD; Loprinzi, CL; Seisler, DK; Sorgatz, KM, 2015
)
"Chemotherapy-induced nausea and vomiting (CINV) is a common adverse event associated with anticancer treatment that can have a significant adverse impact on patient health-related quality of life and that can potentially undermine the effectiveness of chemotherapy."( Aprepitant and fosaprepitant: a 10-year review of efficacy and safety.
Aapro, M; Carides, A; Rapoport, BL; Schmoll, HJ; Warr, D; Zhang, L, 2015
)
" There were no grade 3 or 4 adverse events."( Efficacy and safety of olanzapine combined with aprepitant, palonosetron, and dexamethasone for preventing nausea and vomiting induced by cisplatin-based chemotherapy in gynecological cancer: KCOG-G1301 phase II trial.
Abe, M; Hihara, H; Hirakawa, T; Hirashima, Y; Ichikawa, Y; Ito, K; Itonaga, Y; Kado, N; Kasamatsu, Y; Komeda, S; Kuji, S; Miyagi, K; Murakami, J; Nasu, K; Takahashi, N; Takekuma, M; Tanaka, A, 2016
)
" The overall incidence of adverse events was similar between the two treatment groups (p > ."( Efficacy and safety of triple therapy with aprepitant, ondansetron, and prednisone for preventing nausea and vomiting induced by R-CEOP or CEOP chemotherapy regimen for non-Hodgkin lymphoma: a phase 2 open-label, randomized comparative trial.
Song, Z; Wang, H; Yang, F; Zhang, H; Zhang, M; Zhao, K, 2017
)
" The most common adverse event was constipation."( Efficacy and safety of fosaprepitant in the prevention of nausea and vomiting following highly emetogenic chemotherapy in Chinese people: A randomized, double-blind, phase III study.
Chen, YX; Chen, ZD; Cheng, Y; Dang, CX; Dong, J; Han, BH; Hu, B; Li, BL; Li, JL; Liu, B; Lu, JG; Qin, SK; Shi, JH; Shu, YQ; Sun, XC; Wang, D; Wang, HB; Wang, KM; Wang, QM; Wu, Q; Yang, LQ; Zhang, HL; Zhang, QY; Zhang, ZH, 2017
)
"An eight-year long case series follow-up study with pediatric bone cancer patients was conducted to compare the occurrence of adverse events associated with aprepitant with official sources of drug information (manufacturer's leaflet, clinical trials, and European Medicines Agency leaflet)."( Adverse events associated with aprepitant pediatric bone cancer patients.
da Silva Ries, SA; Ferreira, MAP; Meneses, CF; Michalowski, MB; Moreira, LB; Okumura, LM, 2019
)
"Two open-label, randomized, two-way crossover studies evaluated treatment-emergent adverse events (TEAEs) in 200 healthy subjects."( Safety of HTX-019 (intravenous aprepitant) and fosaprepitant in healthy subjects.
Clendeninn, N; Cravets, M; Keller, MR; Lauw, M; Manhard, K; Ottoboni, T; Quart, B, 2018
)
" No HTX-019 recipients had infusion-site adverse events, versus 15 (8%) fosaprepitant recipients."( Safety of HTX-019 (intravenous aprepitant) and fosaprepitant in healthy subjects.
Clendeninn, N; Cravets, M; Keller, MR; Lauw, M; Manhard, K; Ottoboni, T; Quart, B, 2018
)
"Fosaprepitant, an intravenous neurokinin-1 receptor antagonist for chemotherapy-induced nausea and vomiting, contains polysorbate 80, which is associated with infusion-site adverse events (ISAEs) and hypersensitivity systemic reactions (HSRs)."( Hypersensitivity and infusion-site adverse events with intravenous fosaprepitant after anthracycline-containing chemotherapy: a retrospective study.
Boccia, R; Clendeninn, N; Geller, RB; Ottoboni, T, 2019
)
" Electronic medical records of patients receiving HTX-019 were queried for nursing and medical documentation associated with infusion-site adverse events (ISAEs)."( Safety Profile of HTX-019 Administered as an Intravenous Push in Cancer Patients: A Retrospective Review.
Walton, GD, 2019
)
" No clinically significant ISAEs or adverse events associated with HTX-019 were reported."( Safety Profile of HTX-019 Administered as an Intravenous Push in Cancer Patients: A Retrospective Review.
Walton, GD, 2019
)
"Chemotherapy-induced nausea and vomiting (CINV) is a distressing treatment side-effect that could negatively affect children's quality of life (QoL)."( Single center experience on efficacy and safety of Aprepitant for preventing chemotherapy-induced nausea and vomiting (CINV) in pediatric Hodgkin Lymphoma.
Beneduce, G; Buffardi, I; Buffardi, S; Giagnuolo, G; Marra, N; Menna, G; Parasole, R; Petruzziello, F; Rossi, F; Tortora, C, 2019
)
" This retrospective analysis shows that HTX-019 administered via IV infusion has a favorable safety profile in patients with cancer, and no new treatment-emergent adverse events were identified."( Safety Profile of HTX-019 Administered as an Intravenous Infusion in Patients With Cancer: A Retrospective Analysis.
Calcanes, G; Vacirca, JL,
)
" These adverse events may be so severe that they impair the patient's compliance with the treatment or even cause its discontinuation."( Substance P receptor blocker, aprepitant, inhibited cutaneous and other neurogenic inflammation side effects of the EGFR1-TKI, erlotinib.
Chmielinska, JJ; Kramer, JH; Mak, IT; Spurney, CF; Weglicki, WB, 2020
)
" The standard treatment for newly diagnosed AML is chemotherapy consisting of cytosine arabinoside (Ara-C) and anthracyclines with disappointing clinical outcomes and severe adverse effects, such as symptomatic bradycardia, neurotoxicity."( Aprepitant Sensitizes Acute Myeloid Leukemia Cells to the Cytotoxic Effects of Cytosine Arabinoside in vitro and in vivo.
Cheng, X; Fu, C; Huang, F; Jia, X; Meng, Y; Shao, G; Wang, L; Wang, T; Wang, X; Wu, H; Yang, T, 2020
)
" The primary endpoint was the rate of adverse events (AEs), including drug related AEs and serious AEs (SAEs)."( Safety and efficacy of aprepitant as mono and combination therapy for the prevention of emetogenic chemotherapy-induced nausea and vomiting: post-marketing surveillance in China.
Cai, K; Cheng, G; Fang, J; Hu, X; Huang, J; Li, J; Li, W; Liao, W; Liu, H; Liu, X; Ouyang, Q; Wang, D; Wang, X; Wu, L; Xu, H; Xu, N; Yang, N; Yang, Y; Ye, S; Zhang, H; Zhang, L; Zhang, Y; Zhao, Q; Zheng, J; Zhong, D; Zhong, M; Zhong, W, 2020
)
"Especially as a combination treatment, aprepitant is safe and efficient for preventing CINV in patients receiving highly emetogenic chemotherapy."( Safety and efficacy of aprepitant as mono and combination therapy for the prevention of emetogenic chemotherapy-induced nausea and vomiting: post-marketing surveillance in China.
Cai, K; Cheng, G; Fang, J; Hu, X; Huang, J; Li, J; Li, W; Liao, W; Liu, H; Liu, X; Ouyang, Q; Wang, D; Wang, X; Wu, L; Xu, H; Xu, N; Yang, N; Yang, Y; Ye, S; Zhang, H; Zhang, L; Zhang, Y; Zhao, Q; Zheng, J; Zhong, D; Zhong, M; Zhong, W, 2020
)
" Aprepitant is administered as an anti-emetic agent in chemotherapy and regarding the inhibitory effect on CYP3A4, aprepitant can increase the risk of ifosfamide adverse effects."( Aprepitant, fosaprepitant and risk of ifosfamide-induced neurotoxicity: a systematic review.
Mohammadpour, AH; Rahimi, H; Sadeghi, M; Samadi, S; Vazirian, F, 2022
)

Pharmacokinetics

This review examines the chemical development of fosaprepitant. Standard pharmacokinetic parameters were calculated and nonparametric testing was applied. With and without aprepitant coadministration, respectively, mean plasma elimination half-life was 40 hours and 43 hours.

ExcerptReference
"Two studies were conducted to determine whether concomitant administration of aprepitant altered the pharmacokinetic profiles of ondansetron and granisetron, two 5-HT(3)-receptor antagonists commonly used as antiemetic therapy for CINV."( Effects of aprepitant on the pharmacokinetics of ondansetron and granisetron in healthy subjects.
Blum, RA; Busillo, J; Goldberg, MR; Gottesdiener, KM; Greenberg, HE; Hesney, M; Hustad, CM; Kraft, WK; Lates, C; Majumdar, A; McCrea, J; Murphy, MG; Orlowski, LH; Panebianco, D; Petty, KJ; Van Buren, S; Waldman, SA, 2003
)
" Individual plasma samples were used to estimate area under the plasma concentration-time curve from time zero to infinity (AUC(0- infinity )), peak plasma concentration, and apparent terminal elimination half-life (t(12)) of both ondansetron and granisetron."( Effects of aprepitant on the pharmacokinetics of ondansetron and granisetron in healthy subjects.
Blum, RA; Busillo, J; Goldberg, MR; Gottesdiener, KM; Greenberg, HE; Hesney, M; Hustad, CM; Kraft, WK; Lates, C; Majumdar, A; McCrea, J; Murphy, MG; Orlowski, LH; Panebianco, D; Petty, KJ; Van Buren, S; Waldman, SA, 2003
)
"019), with no significant effect on peak concentration at the end of the infusion (360."( Effects of aprepitant on the pharmacokinetics of ondansetron and granisetron in healthy subjects.
Blum, RA; Busillo, J; Goldberg, MR; Gottesdiener, KM; Greenberg, HE; Hesney, M; Hustad, CM; Kraft, WK; Lates, C; Majumdar, A; McCrea, J; Murphy, MG; Orlowski, LH; Panebianco, D; Petty, KJ; Van Buren, S; Waldman, SA, 2003
)
"Concomitant administration of aprepitant had no clinically significant effect on the mean pharmacokinetic characteristics of either ondansetron or granisetron in these healthy subjects."( Effects of aprepitant on the pharmacokinetics of ondansetron and granisetron in healthy subjects.
Blum, RA; Busillo, J; Goldberg, MR; Gottesdiener, KM; Greenberg, HE; Hesney, M; Hustad, CM; Kraft, WK; Lates, C; Majumdar, A; McCrea, J; Murphy, MG; Orlowski, LH; Panebianco, D; Petty, KJ; Van Buren, S; Waldman, SA, 2003
)
" The pharmacokinetic profile of docetaxel was assessed over 30 h following docetaxel infusion."( Lack of effect of aprepitant on the pharmacokinetics of docetaxel in cancer patients.
Ahmed, T; Cocquyt, V; de Smet, M; Fedgchin, M; Gottesdiener, KM; Hande, K; Majumdar, A; Murphy, MG; Nygren, P; Panebianco, D; Petty, KJ; van Belle, S; van Dyck, K, 2005
)
" The corresponding harmonic mean half-life values were 10."( Lack of effect of aprepitant on the pharmacokinetics of docetaxel in cancer patients.
Ahmed, T; Cocquyt, V; de Smet, M; Fedgchin, M; Gottesdiener, KM; Hande, K; Majumdar, A; Murphy, MG; Nygren, P; Panebianco, D; Petty, KJ; van Belle, S; van Dyck, K, 2005
)
" Blood for pharmacokinetic evaluations was collected through 168 hours after palonosetron administration on days 1 and 15; safety was monitored through day 22."( Pharmacokinetics of palonosetron in combination with aprepitant in healthy volunteers.
Cullen, MT; Gallagher, SC; Hunt, TL; Shah, AK, 2005
)
" With and without aprepitant coadministration, respectively, mean plasma elimination half-life was 40 hours and 43 hours (difference: -3."( Pharmacokinetics of palonosetron in combination with aprepitant in healthy volunteers.
Cullen, MT; Gallagher, SC; Hunt, TL; Shah, AK, 2005
)
"These results indicate no significant differences in pharmacokinetic parameters for palonosetron between the two treatments, and suggest that palonosetron can be safely coadministered with aprepitant with no alterations in the expected safety profile and no dosage adjustment necessary."( Pharmacokinetics of palonosetron in combination with aprepitant in healthy volunteers.
Cullen, MT; Gallagher, SC; Hunt, TL; Shah, AK, 2005
)
" Pharmacokinetic parameters after a single oral dose of aprepitant 240 mg were measured in eight patients with end-stage renal disease (ESRD) requiring haemodialysis, eight patients with severe renal insufficiency (SRI [24-hour creatinine clearance <30 mL/min/1."( Effect of impaired renal function and haemodialysis on the pharmacokinetics of aprepitant.
Aiyer, KJ; Bergman, AJ; Bradstreet, TE; Busillo, J; Constanzer, M; Fosbinder, T; Hickey, L; Huskey, SE; Majumdar, A; Marbury, T; Petty, KJ; Swan, S, 2005
)
" Aprepitant pharmacokinetic parameters in ESRD patients were clinically similar when haemodialysis was initiated at 4 hours or 48 hours after aprepitant administration."( Effect of impaired renal function and haemodialysis on the pharmacokinetics of aprepitant.
Aiyer, KJ; Bergman, AJ; Bradstreet, TE; Busillo, J; Constanzer, M; Fosbinder, T; Hickey, L; Huskey, SE; Majumdar, A; Marbury, T; Petty, KJ; Swan, S, 2005
)
" Complete pharmacokinetic data of vinorelbine administered alone and with the aprepitant antiemetic regimen were obtained in 12 patients."( Aprepitant when added to a standard antiemetic regimen consisting of ondansetron and dexamethasone does not affect vinorelbine pharmacokinetics in cancer patients.
de Bruijn, P; de Wit, R; Freedman, SJ; Gambale, JJ; Li, S; Loos, WJ; Murphy, GM; Van Dyck, K; van Noort, C; Verweij, J, 2007
)
"To develop a population pharmacokinetic model of aprepitant and dexamethasone in Japanese patients with cancer, explore the factors that affect the pharmacokinetics of aprepitant, and evaluate the effect of aprepitant on the clearance of intravenous dexamethasone."( Population pharmacokinetics of aprepitant and dexamethasone in the prevention of chemotherapy-induced nausea and vomiting.
Awata, H; Hashimoto, Y; Katayama, M; Kitagawa, J; Kodama, Y; Miyata, Y; Nakade, S; Ohno, T, 2008
)
"A pharmacokinetic model for aprepitant has been developed that incorporates body weight, age, ALT, BUN and aprepitant dose to predict the CL/F."( Population pharmacokinetics of aprepitant and dexamethasone in the prevention of chemotherapy-induced nausea and vomiting.
Awata, H; Hashimoto, Y; Katayama, M; Kitagawa, J; Kodama, Y; Miyata, Y; Nakade, S; Ohno, T, 2008
)
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
" Such data include physicochemical and in vitro drug properties, biorelevant solubility and dissolution, and in vivo pre-clinical and clinical pharmacokinetic data."( Predicting pharmacokinetics of drugs using physiologically based modeling--application to food effects.
Bolger, MB; Fraczkiewicz, G; Lukacova, V; Parrott, N, 2009
)
"This review examines the chemical development of fosaprepitant, its pharmacokinetic properties, approved uses and potential applications."( Pharmacokinetic evaluation of fosaprepitant dimeglumine.
Colon-Gonzalez, F; Kraft, WK, 2010
)
" 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."( Pharmacokinetic evaluation of fosaprepitant dimeglumine.
Colon-Gonzalez, F; Kraft, WK, 2010
)
" Standard pharmacokinetic parameters were calculated and nonparametric testing was applied to assess the differences between aprepitant and placebo treatment."( The NK₁ receptor antagonist aprepitant does not alter the pharmacokinetics of high-dose melphalan chemotherapy in patients with multiple myeloma.
Burhenne, J; Egerer, G; Eisenlohr, K; Gronkowski, M; Mikus, G; Riedel, KD, 2010
)
" In addition, AUC and terminal elimination half-life were not changed by aprepitant."( The NK₁ receptor antagonist aprepitant does not alter the pharmacokinetics of high-dose melphalan chemotherapy in patients with multiple myeloma.
Burhenne, J; Egerer, G; Eisenlohr, K; Gronkowski, M; Mikus, G; Riedel, KD, 2010
)
" No dosage adjustment was necessary, and administration of aprepitant in HSCT at the prescribed dosage of 125 mg orally on day 1 and 80 mg orally on each consecutive day through day +4 after HSCT was well tolerated with no significant changes in CY pharmacokinetic parameters."( Aprepitant pharmacokinetics and assessing the impact of aprepitant on cyclophosphamide metabolism in cancer patients undergoing hematopoietic stem cell transplantation.
Bubalo, JS; Cherala, G; Maziarz, R; McCune, JS; Munar, MY; Tse, S, 2012
)
" The half-life and clearance of dinaciclib were similar, with or without aprepitant."( Effect of aprepitant on the pharmacokinetics of the cyclin-dependent kinase inhibitor dinaciclib in patients with advanced malignancies.
Bannerji, R; Kantesaria, B; Mita, M; Poon, J; Shapiro, GI; Small, K; Statkevich, P; Tzontcheva, A; Zhang, D; Zhu, Y, 2012
)
" Due to the low aqueous solubility of the active substance the product development has been focused on decreasing the particle size of the active compound down to the submicron range in order to overcome this disadvantageous pharmacokinetic property."( Novel continuous flow technology for the development of a nanostructured aprepitant formulation with improved pharmacokinetic properties.
Angi, R; Darvas, F; Filipcsei, G; Glavinas, H; Heltovics, G; Ordasi, B; Ötvös, Z; Solymosi, T, 2014
)
" Subsequently, a pharmacokinetic study was performed using liquid chromatography-tandem mass spectrometry."( Preparation and pharmacokinetic study of aprepitant-sulfobutyl ether-β-cyclodextrin complex.
Chen, G; Li, M; Ren, L; Wei, P; Zhou, Y, 2014
)
" The solid dispersions were characterized by dissolution, FTIR, XRPD, DSC, SEM and pharmacokinetic studies in rats."( Characterization and Pharmacokinetic Study of Aprepitant Solid Dispersions with Soluplus®.
Cheng, G; Gao, Y; Liu, J; Liu, Y; Ma, N; Piao, H; Tang, B; Zou, M, 2015
)
" At a test dose of 20mg/kg, the pharmacokinetic study of APPT-Ms showed that it accorded with first-order kinetics in mice, and its AUC value was higher than the pure AAPT about 6 times."( 15-hydroxystearate micelles for the delivery of aprepitant: Preparation, characterization, pharmacokinetics and tissue distribution in mice.
Ge, J; Kong, H; Liu, H; Pan, H; Wang, M, 2021
)
" The current pharmacokinetic study was developed to investigate whether this extemporaneous oral suspension offers an appropriate treatment option."( A simple extemporaneous oral suspension of aprepitant yields sufficient pharmacokinetic exposure in children.
de Vos-Kerkhof, E; Enters-Weijnen, CF; Hanff, LM; Huitema, ADR; Lalmohamed, A; Lange, R; Nijstad, AL; Rosing, H; Tibben, MM; Tissing, WJE; van de Wetering, MD; Zwaan, CM, 2023
)
" Pharmacokinetic analyses were performed using nonlinear mixed effects modelling."( A simple extemporaneous oral suspension of aprepitant yields sufficient pharmacokinetic exposure in children.
de Vos-Kerkhof, E; Enters-Weijnen, CF; Hanff, LM; Huitema, ADR; Lalmohamed, A; Lange, R; Nijstad, AL; Rosing, H; Tibben, MM; Tissing, WJE; van de Wetering, MD; Zwaan, CM, 2023
)
" An integrated dexamethasone and aprepitant pharmacokinetic model was developed using non-linear mixed effects modelling in order to investigate the effect of aprepitant administration on dexamethasone CL."( Overestimation of the effect of (fos)aprepitant on intravenous dexamethasone pharmacokinetics requires adaptation of the guidelines for children with chemotherapy-induced nausea and vomiting.
de Vos-Kerkhof, E; Enters-Weijnen, CF; Huitema, ADR; Lalmohamed, A; Nijstad, AL; Rosing, H; Tibben, MM; Tissing, WJE; van de Wetering, MD; Zwaan, CM, 2022
)
"A population pharmacokinetic approach was applied to analyze data obtained in 42 patients at cycle 1 (without aprepitant) and cycle 2 (with aprepitant for 34 of them)."( Population pharmacokinetic analysis reveals no impact of aprepitant on the pharmacokinetics of ifosfamide, 2-dechloroifosfamide, and 3-dechloroifosfamide.
Allal, B; Chaltiel, L; Chatelut, E; Chevreau, C; Filleron, T; Firmin, N; Lambert, M; Mseddi, M; Toulmonde, M; Valentin, T; Yakoubi, M, 2023
)
"A previously published pharmacokinetic model including a time-dependency process well fit the data."( Population pharmacokinetic analysis reveals no impact of aprepitant on the pharmacokinetics of ifosfamide, 2-dechloroifosfamide, and 3-dechloroifosfamide.
Allal, B; Chaltiel, L; Chatelut, E; Chevreau, C; Filleron, T; Firmin, N; Lambert, M; Mseddi, M; Toulmonde, M; Valentin, T; Yakoubi, M, 2023
)

Compound-Compound Interactions

Aprepitant combined with palonosetron did not reduce the incidence of PONV. Moderate to no interactions were observed with ondansetron, aprepitant, rolapitant, and dexamethasone in combination with anticancer agents.

ExcerptReference
"The implications of chemotherapeutic drug-drug interactions can be serious and thus need to be addressed."( Aprepitant: drug-drug interactions in perspective.
Aapro, MS; Walko, CM, 2010
)
"Aprepitant or its prodrug fosaprepitant, in combination with a corticosteroid and a 5-HT(3) receptor antagonist, are used to prevent chemotherapy-induced nausea and vomiting."( Pharmacokinetics of oral dexamethasone and midazolam when administered with single-dose intravenous 150 mg fosaprepitant in healthy adult subjects.
Caro, L; Jin, B; Marbury, TC; Murphy, G; Ngo, PL; Panebianco, D; Shadle, CR; Valentine, J, 2011
)
" We conducted a double-blind, placebo-controlled phase III cross-over study that compared aprepitant to placebo combined with standard antiemetic prophylaxis (a 5HT3-RA and dexamethasone) in patients receiving 5 days of cisplatin combination chemotherapy for testicular cancer."( Randomized, double-blind, placebo-controlled, phase III cross-over study evaluating the oral neurokinin-1 antagonist aprepitant in combination with a 5HT3 receptor antagonist and dexamethasone in patients with germ cell tumors receiving 5-day cisplatin co
Albany, C; Brames, MJ; Einhorn, LH; Fausel, C; Johnson, CS; Picus, J, 2012
)
"There was a significant improvement in CR rate with aprepitant combined with a 5HT3-RA and dexamethasone."( Randomized, double-blind, placebo-controlled, phase III cross-over study evaluating the oral neurokinin-1 antagonist aprepitant in combination with a 5HT3 receptor antagonist and dexamethasone in patients with germ cell tumors receiving 5-day cisplatin co
Albany, C; Brames, MJ; Einhorn, LH; Fausel, C; Johnson, CS; Picus, J, 2012
)
" This study aimed to retrospectively evaluate the efficacy of repeated administrations of 3-day courses of aprepitant according to the cisplatin split regimen (20mg/m² day, days 1-4, 22-25, 43-46) in combination with radiation."( [Evaluation of aprepitant as a prophylactic antiemetic in the Cisplatin split regimen combined with radiation for patients with head and neck cancer].
Endo, K; Enokida, T; Ichida, Y; Ishiki, H; Izumi, K; Saitoh, S; Suzuki, S; Tahara, M; Yoshida, M, 2014
)
" Oral olanzapine (5 mg) was administered with triplet therapy a day prior to cisplatin administration and on days 1-5."( Efficacy and safety of olanzapine combined with aprepitant, palonosetron, and dexamethasone for preventing nausea and vomiting induced by cisplatin-based chemotherapy in gynecological cancer: KCOG-G1301 phase II trial.
Abe, M; Hihara, H; Hirakawa, T; Hirashima, Y; Ichikawa, Y; Ito, K; Itonaga, Y; Kado, N; Kasamatsu, Y; Komeda, S; Kuji, S; Miyagi, K; Murakami, J; Nasu, K; Takahashi, N; Takekuma, M; Tanaka, A, 2016
)
"Preventive use of olanzapine combined with triplet therapy gives better results than those from previously reported studies of triplet therapy."( Efficacy and safety of olanzapine combined with aprepitant, palonosetron, and dexamethasone for preventing nausea and vomiting induced by cisplatin-based chemotherapy in gynecological cancer: KCOG-G1301 phase II trial.
Abe, M; Hihara, H; Hirakawa, T; Hirashima, Y; Ichikawa, Y; Ito, K; Itonaga, Y; Kado, N; Kasamatsu, Y; Komeda, S; Kuji, S; Miyagi, K; Murakami, J; Nasu, K; Takahashi, N; Takekuma, M; Tanaka, A, 2016
)
" This article is aimed to provide pharmacists and other healthcare professionals with an updated summary of drug-drug interactions of aprepitant/fosaprepitant and implications for clinical practice."( Drug interactions with aprepitant or fosaprepitant: Review of literature and implications for clinical practice.
Carbone, A; Dushenkov, A; Jungsuwadee, P; Kalabalik, J, 2017
)
" In patients who receive highly emetogenic chemotherapy, aprepitant, an NK1-receptor antagonist, is combined with ondansetron and dexamethasone."( Drug-drug interactions with aprepitant in antiemetic prophylaxis for chemotherapy.
Desar, IME; Kramers, C; Lankheet, AG; Schoffelen, R; van der Hoeven, JJM; van Herpen, CML, 2018
)
"The aim of this study was to evaluate aprepitant in combination with palonosetron as compared to palonosetron alone for the prevention of postoperative nausea and vomiting (PONV) in female patients receiving fentanyl- based intravenous patient-controlled analgesia (IV-PCA)."( Aprepitant in combination with palonosetron for the prevention of postoperative nausea and vomiting in female patients using intravenous patient-controlled analgesia.
Chung, JW; Han, YM; Jun, MR; Kim, SI; Kim, YJ; Yoo, JH, 2018
)
"Aprepitant combined with palonosetron did not reduce the incidence of PONV as compared to palonosetron alone within 24 h of surgery in women receiving fentanyl-based IV-PCA."( Aprepitant in combination with palonosetron for the prevention of postoperative nausea and vomiting in female patients using intravenous patient-controlled analgesia.
Chung, JW; Han, YM; Jun, MR; Kim, SI; Kim, YJ; Yoo, JH, 2018
)
"Polypharmacy of elderly oncology patients and fragmented medication management are well-known risk factors for drug-drug interactions (DDIs)."( Nightmares and hallucinations with aprepitant and opium powder: a suspected drug-drug interaction.
Azzouz, B; Bouché, O; Clarenne, J; Narjoux, G; Slimano, F; Zeller, PS, 2019
)
"Preventive use of OLZ combined with standard triplet therapy had promising activity with manageable safety, suggesting that this combination could be an effective standard treatment option for patients with AUC ≥4 mg/mL/min CBDCA combination therapy."( Efficacy and safety of 5 mg olanzapine combined with aprepitant, granisetron and dexamethasone to prevent carboplatin-induced nausea and vomiting in patients with gynecologic cancer: A multi-institution phase II study.
Abe, M; Arai, T; Fujita, Y; Hayasaki, Y; Iihara, H; Kado, N; Mori, M; Morishige, KI; Murase, S; Nakamura, K; Sakurai, M; Shimaoka, R; Shimokawa, M; Suzuki, A; Takenaka, M; Yamamoto, S, 2020
)
"25 mg intravenously) D1, combined with APR (125 mg orally, D1 and 80 mg orally, D2-3) and DEX (12 mg orally or intravenously, D1 and 8 mg orally, D2-4)."( Ramosetron versus Palonosetron in Combination with Aprepitant and Dexamethasone for the Control of Highly-Emetogenic Chemotherapy-Induced Nausea and Vomiting.
Ahn, JS; An, HJ; Kang, JH; Kim, GM; Kim, HJ; Kim, JY; Koo, DH; Kwon, JH; Lee, H; Lee, YG; Park, KU; Seol, YM; Sohn, J; Song, H; Yang, JH; Yun, HJ, 2020
)
" This study aimed to evaluate the antiemetic efficacy of palonosetron (PALO) over granisetron (GRA) in combination with dexamethasone for multiple highly emetogenic chemotherapy drugs (HEC), especially in chemotherapy regimens in Egyptian breast cancer patients and cisplatin-based regimens in other diseases."( Evaluation of clinical outcomes and efficacy of palonosetron and granisetron in combination with dexamethasone in Egyptian patients receiving highly emetogenic chemotherapy.
A El-Azab, G; A Mahrous, M; A Tawfik, H, 2021
)
" All patients received dexamethasone in combination with the 5-HT3 receptor antagonist."( Evaluation of clinical outcomes and efficacy of palonosetron and granisetron in combination with dexamethasone in Egyptian patients receiving highly emetogenic chemotherapy.
A El-Azab, G; A Mahrous, M; A Tawfik, H, 2021
)
"Palonosetron, combined with dexamethasone, is more effective than granisetron and dexamethasone combination against both acute and delayed emesis induced by highly emetogenic chemotherapy (HEC) cisplatin-based protocols and the combination of cyclophosphamide and anthracyclines (AC)."( Evaluation of clinical outcomes and efficacy of palonosetron and granisetron in combination with dexamethasone in Egyptian patients receiving highly emetogenic chemotherapy.
A El-Azab, G; A Mahrous, M; A Tawfik, H, 2021
)
"The purpose of the present work was to evaluate in silico drug-drug interaction (DDI) potential between BCa chemotherapeutic drugs and antiemetic agents."( Simulation of drug-drug interactions between breast cancer chemotherapeutic agents and antiemetic drugs.
Deb, S; Hopefl, R, 2023
)
"The Drug-Drug Interaction™ module of GastroPlus™ was employed to assess CYP-related interactions between antiemetic and anticancer therapy combinations."( Simulation of drug-drug interactions between breast cancer chemotherapeutic agents and antiemetic drugs.
Deb, S; Hopefl, R, 2023
)
" Moderate to no interactions were observed with ondansetron, aprepitant, rolapitant, and dexamethasone in combination with anticancer agents."( Simulation of drug-drug interactions between breast cancer chemotherapeutic agents and antiemetic drugs.
Deb, S; Hopefl, R, 2023
)

Bioavailability

Relative bioavailability of the aprepitant suspension was 82%. This study focused on improving its permeability and solubility in order to improve the oral bioavailability.

ExcerptReference
" Study 1 evaluated the bioavailability of the capsules and estimated the effect of food."( Pharmacokinetics of aprepitant after single and multiple oral doses in healthy volunteers.
Bergman, AJ; Bradstreet, TE; Butler, K; Constanzer, M; Crumley, TM; De Lepeleire, I; Goldberg, MR; Greenberg, HE; Hickey, L; Howard, L; Knops, A; Majumdar, AK; Michiels, N; Panebianco, D; Petty, KJ; Rothenberg, PL; Waldman, SA, 2006
)
" This drug is well absorbed orally with a t max of about four hours."( Aprepitant: a substance P antagonist for chemotherapy induced nausea and vomiting.
Girish, C; Manikandan, S,
)
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
" The bioavailability of this formulation is unknown."( Stability of an extemporaneous oral liquid aprepitant formulation.
Dupuis, LL; Lingertat-Walsh, K; Walker, SE, 2009
)
" Although dissolution is the primary limitation to the rate of absorption for micronized aprepitant, some permeability restrictions are revealed for the nanosized formulation."( Forecasting in vivo oral absorption and food effect of micronized and nanosized aprepitant formulations in humans.
Dressman, JB; Jantratid, E; Kesisoglou, F; Reppas, C; Shono, Y, 2010
)
" The results indicate that aprepitant is well absorbed and does not auto-induce its metabolism."( Aprepitant pharmacokinetics and assessing the impact of aprepitant on cyclophosphamide metabolism in cancer patients undergoing hematopoietic stem cell transplantation.
Bubalo, JS; Cherala, G; Maziarz, R; McCune, JS; Munar, MY; Tse, S, 2012
)
" The innovator Emend® is a formulation incorporating drug nanoparticles with good bioavailability (~67%)."( Inclusion complex of aprepitant with cyclodextrin: evaluation of physico-chemical and pharmacokinetic properties.
Ansari, KA; Dhawan, S; Kaul, NS; Krishnamurthy, T; Kumar, D; Pillai, R; Ridhurkar, DN, 2013
)
"These studies established that cyclodextrin complexation may provide another viable and cost effective option for enhancing solubility and bioavailability of APR."( Inclusion complex of aprepitant with cyclodextrin: evaluation of physico-chemical and pharmacokinetic properties.
Ansari, KA; Dhawan, S; Kaul, NS; Krishnamurthy, T; Kumar, D; Pillai, R; Ridhurkar, DN, 2013
)
"The oral bioavailability of Aprepitant is limited by poor dissolution of the compound in the gastrointestinal tract which is more prominent in the fasted state resulting in significant positive food effect."( Novel continuous flow technology for the development of a nanostructured aprepitant formulation with improved pharmacokinetic properties.
Angi, R; Darvas, F; Filipcsei, G; Glavinas, H; Heltovics, G; Ordasi, B; Ötvös, Z; Solymosi, T, 2014
)
" The bioavailability of the drug complex was comparable to that of Emend."( Preparation and pharmacokinetic study of aprepitant-sulfobutyl ether-β-cyclodextrin complex.
Chen, G; Li, M; Ren, L; Wei, P; Zhou, Y, 2014
)
"Solid dispersions are a useful approach to improve the dissolution rate and bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs)."( Characterization and Pharmacokinetic Study of Aprepitant Solid Dispersions with Soluplus®.
Cheng, G; Gao, Y; Liu, J; Liu, Y; Ma, N; Piao, H; Tang, B; Zou, M, 2015
)
" Therefore, we aimed to improve solubility as well as permeability that could possibly improve oral bioavailability of APT."( Aprepitant loaded solid preconcentrated microemulsion for enhanced bioavailability: A comparison with micronized Aprepitant.
Kamboj, S; Rana, V; Sharma, R; Singh, K, 2015
)
" The data also suggested increase in absorption rate when APT incorporated into SCFG-SEP."( Formulation optimization of aprepitant microemulsion-loaded silicated corn fiber gum particles for enhanced bioavailability.
Kamboj, S; Rana, V, 2016
)
" The optimized ODF was evaluated for various physicochemical, mechanical, drug release kinetics and bioavailability studies."( Development of aprepitant loaded orally disintegrating films for enhanced pharmacokinetic performance.
Kamboj, S; Rana, V; Sharma, R; Singh, G, 2016
)
"32-fold, and the bioavailability was greatly decreased about 30."( Effects of aprepitant on the pharmacokinetics of imatinib and its main metabolite in rats.
Darbalaei, S; Han, X; Lu, Y; Qin, Y; Rang, Y; Wang, N; Zhai, X; Zhang, X, 2018
)
"The characterization of nanocrystalline active ingredients in multicomponent formulations for the design and manufacture of products with increased bioavailability is often challenging."( Detailed Morphological Characterization of Nanocrystalline Active Ingredients in Solid Oral Dosage Forms Using Atomic Force Microscopy.
Goda, Y; Izutsu, KI; Nanjo, K; Okuda, H; Sakai-Kato, K; Takechi-Haraya, Y, 2019
)
" While nano-sizing aprepitant improves its in vivo performance, intestinal solubility remains a barrier to its bioavailability and thus aprepitant should be classified as DCS IIb."( Combining biorelevant in vitro and in silico tools to simulate and better understand the in vivo performance of a nano-sized formulation of aprepitant in the fasted and fed states.
Box, KJ; Dressman, J; Kostewicz, E; Kuentz, M; Litou, C; Patel, N; Turner, DB, 2019
)
" We aimed to determine the bioavailability of this aprepitant suspension relative to the capsule."( Relative bioavailability of an extemporaneously prepared aprepitant oral suspension in healthy adults.
Dupuis, LL; Nathan, PC; Patel, P; Volpe, J; Walker, SE; Zupanec, S, 2019
)
" Relative bioavailability was defined as the geometric least squares mean ratio for area under the concentration versus time curve (AUC) from time zero to infinity of the aprepitant suspension versus the capsule."( Relative bioavailability of an extemporaneously prepared aprepitant oral suspension in healthy adults.
Dupuis, LL; Nathan, PC; Patel, P; Volpe, J; Walker, SE; Zupanec, S, 2019
)
"Relative bioavailability of the aprepitant suspension was 82."( Relative bioavailability of an extemporaneously prepared aprepitant oral suspension in healthy adults.
Dupuis, LL; Nathan, PC; Patel, P; Volpe, J; Walker, SE; Zupanec, S, 2019
)
"With a relative bioavailability of 82."( Relative bioavailability of an extemporaneously prepared aprepitant oral suspension in healthy adults.
Dupuis, LL; Nathan, PC; Patel, P; Volpe, J; Walker, SE; Zupanec, S, 2019
)
" The bioavailability of the extemporaneous oral suspension was not significantly different to that of the capsules (P = 0."( A simple extemporaneous oral suspension of aprepitant yields sufficient pharmacokinetic exposure in children.
de Vos-Kerkhof, E; Enters-Weijnen, CF; Hanff, LM; Huitema, ADR; Lalmohamed, A; Lange, R; Nijstad, AL; Rosing, H; Tibben, MM; Tissing, WJE; van de Wetering, MD; Zwaan, CM, 2023
)
" An adequate exposure to aprepitant in children was yielded and the bioavailability of the extemporaneous suspension was comparable to capsules."( A simple extemporaneous oral suspension of aprepitant yields sufficient pharmacokinetic exposure in children.
de Vos-Kerkhof, E; Enters-Weijnen, CF; Hanff, LM; Huitema, ADR; Lalmohamed, A; Lange, R; Nijstad, AL; Rosing, H; Tibben, MM; Tissing, WJE; van de Wetering, MD; Zwaan, CM, 2023
)
" This study focused on improving its permeability and solubility in order to improve the oral bioavailability of aprepitant."( Fabrication of an aprepitant nanosuspension using hydroxypropyl chitosan to increase the bioavailability.
Ao, W; Bai, M; Li, S; Li, Y; Liu, J; Xiao, Y, 2022
)

Dosage Studied

Multiple-day dosing of aprepitant was effective for prevention of nausea. No dosage adjustment was necessary. Repeated dosing over multiple cycles was generally well tolerated.

ExcerptReference
" dosing of I to rats and dogs."( Substance P receptor antagonist I: conversion of phosphoramidate prodrug after i.v. administration to rats and dogs.
Chiu, SH; Dean, BJ; Feeney, WP; Huskey, SE; Luffer-Atlas, D; McGowan, EM, 1999
)
" Continued dosing with MK-869 may enhance control of other measures of delayed emesis, such as the use of rescue medication, although confirmation is required before a definitive conclusion may be drawn."( Prevention of cisplatin-induced acute and delayed emesis by the selective neurokinin-1 antagonists, L-758,298 and MK-869.
Brestan, E; Bui, B; Carides, AD; De Smet, M; Decramer, ML; Eldridge, K; Evans, JK; Garin, AM; Gertz, BJ; Lichinitser, MR; Michiels, N; Navari, RM; Reinhardt, RR; Riviere, A; Thant, M; Van Belle, S, 2002
)
" An important objective of all neuroscience drug discovery and development programs is to establish the correlation between dose, receptor occupancy, and the observed clinical effect (the dose-response relationship)."( Imaging substance P receptors (NK1) in the living human brain using positron emission tomography.
Hargreaves, R, 2002
)
" Thus, aprepitant, when dosed as a 5-day regimen, did not interact with a known substrate of the P-glycoprotein transporter."( Lack of effect of aprepitant on digoxin pharmacokinetics in healthy subjects.
Brackett, LE; De Smet, M; Feuring, M; Goldberg, MR; Gottesdiener, KM; Hesney, M; Lee, Y; Majumdar, AK; Michiels, N; Murphy, MG; Orlowski, LH; Petty, KJ; Wehling, M, 2003
)
" Repeated dosing with aprepitant over multiple cycles was generally well tolerated."( The oral NK(1) antagonist, aprepitant, given with standard antiemetics provides protection against nausea and vomiting over multiple cycles of cisplatin-based chemotherapy: a combined analysis of two randomised, placebo-controlled phase III clinical trial
Carides, AD; de Wit, R; Elmer, M; Evans, JK; Guoguang-Ma, J; Herrstedt, J; Horgan, KJ; Rapoport, B; Schmidt, C, 2004
)
" Because metabolism of some chemotherapeutic agents may involve CYP3A4, the potential inductive effect of the CINV dosing regimen of aprepitant on this metabolic pathway was evaluated using intravenous midazolam, a sensitive probe substrate of CYP3A4."( Evaluation of potential inductive effects of aprepitant on cytochrome P450 3A4 and 2C9 activity.
Blum, RA; Bradstreet, TE; Evans, JK; Gargano, C; Lee, Y; Majumdar, AK; Petty, KJ; Shadle, CR, 2004
)
" The first study evaluated the plasma concentration-occupancy relationships for aprepitant dosed orally at 10, 30, 100, or 300 mg, or placebo (n = 12)."( Human positron emission tomography studies of brain neurokinin 1 receptor occupancy by aprepitant.
Antoni, G; Battisti, WP; Bergström, M; Bradstreet, TE; Burns, HD; Constanzer, ML; Eskola, O; Gargano, C; Goldberg, MR; Hargreaves, RJ; Hietala, J; Långström, B; Majumdar, AK; Ogren, M; Petty, KJ; Reines, SA; Scheinin, M; Sciberras, D; Solin, O, 2004
)
" Acute and delayed nausea may also be improved by aprepitant when used in combination with a 5-HT3 and dexamethasone prechemotherapy or with daily dosing for 3-5 days following chemotherapy."( Pathogenesis-based treatment of chemotherapy-induced nausea and vomiting--two new agents.
Navari, RM,
)
" In addition, the dog model was used for optimizing formulation processes in which the nanoparticles were incorporated into solid dosage forms, and for selecting excipients to effectively re-disperse the nanoparticles from the dosage units."( The role of biopharmaceutics in the development of a clinical nanoparticle formulation of MK-0869: a Beagle dog model predicts improved bioavailability and diminished food effect on absorption in human.
Batra, U; Chen, C; Hettrick, L; Higgins, R; Kwei, G; Landis, E; Loper, A; Lynn, K; Novak, L; Shelukar, S; Storey, D; Thompson, K; Wu, Y, 2004
)
"These results indicate no significant differences in pharmacokinetic parameters for palonosetron between the two treatments, and suggest that palonosetron can be safely coadministered with aprepitant with no alterations in the expected safety profile and no dosage adjustment necessary."( Pharmacokinetics of palonosetron in combination with aprepitant in healthy volunteers.
Cullen, MT; Gallagher, SC; Hunt, TL; Shah, AK, 2005
)
" Therefore, no dosage adjustment of aprepitant is warranted in SRI or ESRD patients."( Effect of impaired renal function and haemodialysis on the pharmacokinetics of aprepitant.
Aiyer, KJ; Bergman, AJ; Bradstreet, TE; Busillo, J; Constanzer, M; Fosbinder, T; Hickey, L; Huskey, SE; Majumdar, A; Marbury, T; Petty, KJ; Swan, S, 2005
)
" A positron emission tomography (PET) study was also performed in normal subjects to determine the relationship between neurokinin(1) receptor occupancy and aprepitant plasma concentrations in dosing regimens relevant to the trials."( Lack of efficacy of the substance p (neurokinin1 receptor) antagonist aprepitant in the treatment of major depressive disorder.
Ball, W; Beebe, K; Hargreaves, R; Hietala, J; Keller, M; Lines, C; Liu, G; Montgomery, S; Morrison, M; Reines, S; Snavely, D, 2006
)
" Results from the PET study indicated that the aprepitant dosing regimens provided continuously high levels of neurokinin(1) receptor blockade over 8 weeks."( Lack of efficacy of the substance p (neurokinin1 receptor) antagonist aprepitant in the treatment of major depressive disorder.
Ball, W; Beebe, K; Hargreaves, R; Hietala, J; Keller, M; Lines, C; Liu, G; Montgomery, S; Morrison, M; Reines, S; Snavely, D, 2006
)
" Further study is needed to clarify the use of fosaprepitant for the prevention of CINV, and to clarify optimal dosing regimens that may be appropriate substitutes for oral aprepitant."( Fosaprepitant (MK-0517): a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.
Navari, RM, 2007
)
" Multiple-day dosing of palonosetron plus dexamethasone was safe and effective for prevention of emesis induced by 5-day cisplatin-based chemotherapy."( Clinical update on palonosetron in the management of chemotherapy-induced nausea and vomiting.
Bajetta, E; Canova, S; Celio, L; Denaro, A; Gevorgyan, A,
)
" Further study is needed to clarify the utility of fosaprepitant in the prevention of CINV and to clarify optimal dosing regimens that may be appropriate substitutes for oral aprepitant."( Fosaprepitant: a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.
Navari, RM, 2008
)
" Pharmacokinetics suggest that the adult dosing regimen is appropriate for adolescents."( Aprepitant in adolescent patients for prevention of chemotherapy-induced nausea and vomiting: a randomized, double-blind, placebo-controlled study of efficacy and tolerability.
Carides, AD; Chawla, S; Chua, V; Devandry, S; Evans, JK; Gore, L; Hemenway, M; Oxenius, B; Petrilli, A; Schissel, D; Taylor, A; Valentine, J, 2009
)
" The lack of an oral liquid dosage form is one barrier to its use in children."( Stability of an extemporaneous oral liquid aprepitant formulation.
Dupuis, LL; Lingertat-Walsh, K; Walker, SE, 2009
)
" If such drugs reach clinical development and show undesirable variability when dosed with food, improved formulation can help to reduce the food effect and carefully designed in vivo studies in dogs can be a useful guide to clinical formulation development."( Predicting pharmacokinetics of drugs using physiologically based modeling--application to food effects.
Bolger, MB; Fraczkiewicz, G; Lukacova, V; Parrott, N, 2009
)
" GI parameters (gastric emptying rate and GI fluid volume) were varied according to the dosing conditions."( Forecasting in vivo oral absorption and food effect of micronized and nanosized aprepitant formulations in humans.
Dressman, JB; Jantratid, E; Kesisoglou, F; Reppas, C; Shono, Y, 2010
)
" The exact dosing regimen for ondansetron and dexamethasone was different in each study."( Differential time course of action of 5-HT3 and NK1 receptor antagonists when used with highly and moderately emetogenic chemotherapy (HEC and MEC).
Carides, AD; Hesketh, PJ; Street, JC; Warr, DG, 2011
)
" No dosage adjustment was necessary, and administration of aprepitant in HSCT at the prescribed dosage of 125 mg orally on day 1 and 80 mg orally on each consecutive day through day +4 after HSCT was well tolerated with no significant changes in CY pharmacokinetic parameters."( Aprepitant pharmacokinetics and assessing the impact of aprepitant on cyclophosphamide metabolism in cancer patients undergoing hematopoietic stem cell transplantation.
Bubalo, JS; Cherala, G; Maziarz, R; McCune, JS; Munar, MY; Tse, S, 2012
)
" Aprepitant plasma concentration profiles were comparable for the two dosage forms."( Equivalent dynamic human brain NK1-receptor occupancy following single-dose i.v. fosaprepitant vs. oral aprepitant as assessed by PET imaging.
Bormans, G; Butterfield, KL; De Hoon, J; De Lepeleire, I; Declercq, R; Derdelinckx, I; Hamill, T; Hargreaves, RJ; Koole, M; Liu, F; Liu, Y; Mahon, C; Mozley, PD; Murphy, MG; Rosen, LB; Sanabria Bohorquez, SM; Shadle, CR; Tatosian, D; Van Laere, K; Wagner, JA; Xie, W; Zappacosta, P, 2012
)
" During cycle 1 and cycle 2, subjects received dinaciclib with aprepitant in one cycle and dinaciclib without aprepitant in the other cycle; aprepitant was administered at a dose of 125 mg orally on day 1 and 80 mg orally on days 2 and 3, along with standard dosing regimens of ondansetron and dexamethasone."( Effect of aprepitant on the pharmacokinetics of the cyclin-dependent kinase inhibitor dinaciclib in patients with advanced malignancies.
Bannerji, R; Kantesaria, B; Mita, M; Poon, J; Shapiro, GI; Small, K; Statkevich, P; Tzontcheva, A; Zhang, D; Zhu, Y, 2012
)
"Patients scheduled to receive cisplatin (≥70 mg/m 2 ) were administered a single IV dose of fosaprepitant dimeglumine (150 mg) on day 1 or a 3-day dosing regimen of oral aprepitant (day 1:125 mg, days 2 and 3:80 mg) with standard doses of ondansetron and dexamethasone."( A phase 3, randomized, double-blind study of single-dose fosaprepitant for prevention of cisplatin-induced nausea and vomiting: results of an Indian population subanalysis.
Carides, AD; Desai, CJ; Gangadharan, VP; Maru, A; Mohapatra, RK,
)
" Plasma concentration of oxycodone and its metabolites were measured up to 8 hours after administration as follows: on day 1, CR oxycodone was administered alone; on day 2, CR oxycodone was administered with aprepitant (125 mg, at the same time of oxycodone dosing in the morning)."( Effects of aprepitant on the pharmacokinetics of controlled-release oral oxycodone in cancer patients.
Chayahara, N; Fujiwara, Y; Imamura, Y; Kiyota, N; Minami, H; Mukohara, T; Shimada, T; Toyoda, M, 2014
)
" Although warfarin dosage was steadily increased over the four subsequent cycles of chemotherapy, therapeutic target range was not recovered."( Persistent drug interaction between aprepitant and warfarin in patients receiving anticancer chemotherapy.
Hisaka, A; Ohno, Y; Suzuki, H; Yamada, M; Yamaguchi, R, 2014
)
" Ondansetron was dosed per the product label for paediatric use or local standard of care."( Aprepitant for the prevention of chemotherapy-induced nausea and vomiting in children: a randomised, double-blind, phase 3 trial.
DiCristina, C; Green, S; Kang, HJ; Loftus, S; Taylor, A; Zwaan, CM, 2015
)
"There were no significant changes in the plasma viremia or CD4(+) T cells during the dosing period."( Reduction of soluble CD163, substance P, programmed death 1 and inflammatory markers: phase 1B trial of aprepitant in HIV-1-infected adults.
Barrett, JS; Catalano, R; Douglas, SD; Elci, O; Evans, DL; Kim, D; Korelitz, JJ; Spitsin, S; Tebas, P; Tuluc, F; Wagner, W; Winters, A, 2015
)
" These alterations did not translate into adverse outcomes and/or necessitate dosing adjustments."( Drug interactions with aprepitant or fosaprepitant: Review of literature and implications for clinical practice.
Carbone, A; Dushenkov, A; Jungsuwadee, P; Kalabalik, J, 2017
)
" Aprepitant and ondansetron as dosed in this trial was not superior to standard ondansetron monotherapy."( Effectiveness of aprepitant in addition to ondansetron in the prevention of nausea and vomiting caused by fractionated radiotherapy to the upper abdomen (AVERT).
Ades, S; Ashikaga, T; Blackstock, W; Halyard, M; Heimann, R; Kumar, S; Wilson, K, 2017
)
" Solid-state nuclear magnetic resonance (ssNMR) spectroscopy plays a critical role in the characterization of solid dosage forms due to its capabilities of chemical identification, quantification, and structural elucidation at a molecular level."( Three-Dimensional NMR Spectroscopy of Fluorinated Pharmaceutical Solids under Ultrafast Magic Angle Spinning.
Lu, X; McNevin, MJ; Skomski, D; Su, Y; Thompson, KC; Xu, W, 2019
)
"Using patient-derived glioblastoma stem cell (GSC) cultures from 15 GBM patients, we described stem cell properties of individual cultures, determined the dose-response relationships of the drugs in the CUSP9, and assessed the efficacy the CUSP9 combination with TMZ in concentrations clinically achievable."( The efficacy of a coordinated pharmacological blockade in glioblastoma stem cells with nine repurposed drugs using the CUSP9 strategy.
Grieg, Z; Langmoen, IA; Sandberg, CJ; Skaga, E; Skaga, IØ; Vik-Mo, EO, 2019
)
" PONV incidence, complete response, 80 mg aprepitant combined with dexamethasone and ondansetron, vomiting, nausea, and analgesic dose-response were the main outcomes measured."( The efficacy of aprepitant for the prevention of postoperative nausea and vomiting: A meta-analysis.
Chen, X; He, H; Hu, W; Liao, Y; Liu, W; Liu, Y; Pan, Z; Wang, X; Zheng, F; Zhong, H, 2023
)
" No statistically significant difference between the dose-response of analgesics was identified (mean difference: -1."( The efficacy of aprepitant for the prevention of postoperative nausea and vomiting: A meta-analysis.
Chen, X; He, H; Hu, W; Liao, Y; Liu, W; Liu, Y; Pan, Z; Wang, X; Zheng, F; Zhong, H, 2023
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
antidepressantAntidepressants are mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions.
antiemeticA drug used to prevent nausea or vomiting. An antiemetic may act by a wide range of mechanisms: it might affect the medullary control centres (the vomiting centre and the chemoreceptive trigger zone) or affect the peripheral receptors.
peripheral nervous system drugA drug that acts principally at one or more sites within the peripheral neuroeffector systems, the autonomic system, and motor nerve-skeletal system.
neurokinin-1 receptor antagonistAn antagonist at the neurokinin-1 receptor.
substance P receptor antagonistAn antagonist at the substance P receptor.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
triazolesAn azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.
morpholinesAny compound containing morpholine as part of its structure.
cyclic acetalAn acetal in the molecule of which the acetal carbon and one or both oxygen atoms thereon are members of a ring.
(trifluoromethyl)benzenesAn organofluorine compound that is (trifluoromethyl)benzene and derivatives arising from substitution of one or more of the phenyl hydrogens.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (48)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency26.83253.189029.884159.4836AID1224846
RAR-related orphan receptor gammaMus musculus (house mouse)Potency26.60320.006038.004119,952.5996AID1159521; AID1159523
GALC proteinHomo sapiens (human)Potency0.631028.183828.183828.1838AID1159614
TDP1 proteinHomo sapiens (human)Potency19.98670.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency11.57080.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency29.05330.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743042; AID743054; AID743063
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency33.49150.013326.981070.7614AID1346978
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency26.60320.000657.913322,387.1992AID1259378
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency10.01510.001022.650876.6163AID1224838; AID1224893
progesterone receptorHomo sapiens (human)Potency22.04120.000417.946075.1148AID1346784; AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.69180.01237.983543.2770AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency27.18240.000214.376460.0339AID720691; AID720692; AID720719
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency29.60670.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency12.06520.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency25.84820.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency29.84700.375827.485161.6524AID743217
pregnane X nuclear receptorHomo sapiens (human)Potency9.43920.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency26.38280.000229.305416,493.5996AID1259244; AID1259248; AID743069; AID743078; AID743091
GVesicular stomatitis virusPotency11.98770.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency15.48710.00108.379861.1304AID1645840
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency31.66790.001024.504861.6448AID743215; AID743227
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency33.48890.001019.414170.9645AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency28.33980.023723.228263.5986AID743222; AID743223
caspase-3Homo sapiens (human)Potency33.49150.013326.981070.7614AID1346978
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency29.84930.001723.839378.1014AID743083
thyroid stimulating hormone receptorHomo sapiens (human)Potency29.84930.001628.015177.1139AID1259385
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency26.83250.057821.109761.2679AID1159526; AID1159528
Histone H2A.xCricetulus griseus (Chinese hamster)Potency61.93150.039147.5451146.8240AID1224845; AID1224896
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency10.07410.000323.4451159.6830AID743065; AID743066; AID743067
heat shock protein beta-1Homo sapiens (human)Potency33.48890.042027.378961.6448AID743210; AID743228
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency33.48890.000627.21521,122.0200AID743202
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency29.84930.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency11.98770.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency30.73370.002319.595674.0614AID651631; AID720552
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency29.84930.001551.739315,848.9004AID1259244
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)0.04600.00011.753610.0000AID301062
Substance-P receptorHomo sapiens (human)IC50 (µMol)0.00020.00000.09526.8130AID1817659; AID208406; AID208423; AID208440; AID208587; AID270514; AID271466; AID301059; AID342286; AID779964
Substance-P receptorHomo sapiens (human)Ki0.00130.00000.79368.7470AID1064184; AID715707; AID715708
Neuromedin-K receptorHomo sapiens (human)Ki0.45410.00020.05430.9250AID715706
Substance-P receptorMeriones unguiculatus (Mongolian gerbil)IC50 (µMol)0.00010.00010.00630.0126AID1237291
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Substance-P receptorHomo sapiens (human)Kd0.00830.00000.00540.0166AID715902
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (288)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
aggressive behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of leukocyte migrationSubstance-P receptorHomo sapiens (human)
angiotensin-mediated drinking behaviorSubstance-P receptorHomo sapiens (human)
inflammatory responseSubstance-P receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationSubstance-P receptorHomo sapiens (human)
tachykinin receptor signaling pathwaySubstance-P receptorHomo sapiens (human)
long-term memorySubstance-P receptorHomo sapiens (human)
associative learningSubstance-P receptorHomo sapiens (human)
detection of abiotic stimulusSubstance-P receptorHomo sapiens (human)
response to ozoneSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell migrationSubstance-P receptorHomo sapiens (human)
response to auditory stimulusSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell migrationSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, cholinergicSubstance-P receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicSubstance-P receptorHomo sapiens (human)
response to estradiolSubstance-P receptorHomo sapiens (human)
response to progesteroneSubstance-P receptorHomo sapiens (human)
response to nicotineSubstance-P receptorHomo sapiens (human)
operant conditioningSubstance-P receptorHomo sapiens (human)
sperm ejaculationSubstance-P receptorHomo sapiens (human)
eating behaviorSubstance-P receptorHomo sapiens (human)
positive regulation of vascular permeabilitySubstance-P receptorHomo sapiens (human)
response to ethanolSubstance-P receptorHomo sapiens (human)
positive regulation of action potentialSubstance-P receptorHomo sapiens (human)
positive regulation of blood pressureSubstance-P receptorHomo sapiens (human)
positive regulation of ossificationSubstance-P receptorHomo sapiens (human)
positive regulation of vasoconstrictionSubstance-P receptorHomo sapiens (human)
positive regulation of hormone secretionSubstance-P receptorHomo sapiens (human)
behavioral response to painSubstance-P receptorHomo sapiens (human)
regulation of smooth muscle cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of lymphocyte proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationSubstance-P receptorHomo sapiens (human)
positive regulation of stress fiber assemblySubstance-P receptorHomo sapiens (human)
response to electrical stimulusSubstance-P receptorHomo sapiens (human)
smooth muscle contraction involved in micturitionSubstance-P receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionSubstance-P receptorHomo sapiens (human)
positive regulation of flagellated sperm motilitySubstance-P receptorHomo sapiens (human)
tachykinin receptor signaling pathwayNeuromedin-K receptorHomo sapiens (human)
positive regulation of heart rateNeuromedin-K receptorHomo sapiens (human)
response to estradiolNeuromedin-K receptorHomo sapiens (human)
regulation of dopamine metabolic processNeuromedin-K receptorHomo sapiens (human)
response to cocaineNeuromedin-K receptorHomo sapiens (human)
positive regulation of blood pressureNeuromedin-K receptorHomo sapiens (human)
regulation of feeding behaviorNeuromedin-K receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionNeuromedin-K receptorHomo sapiens (human)
positive regulation of flagellated sperm motilityNeuromedin-K receptorHomo sapiens (human)
protein phosphorylationcGMP-dependent protein kinase 1 Homo sapiens (human)
neuron migrationcGMP-dependent protein kinase 1 Homo sapiens (human)
signal transductioncGMP-dependent protein kinase 1 Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationcGMP-dependent protein kinase 1 Homo sapiens (human)
spermatid developmentcGMP-dependent protein kinase 1 Homo sapiens (human)
negative regulation of inositol phosphate biosynthetic processcGMP-dependent protein kinase 1 Homo sapiens (human)
negative regulation of glutamate secretioncGMP-dependent protein kinase 1 Homo sapiens (human)
dendrite developmentcGMP-dependent protein kinase 1 Homo sapiens (human)
cGMP-mediated signalingcGMP-dependent protein kinase 1 Homo sapiens (human)
cerebellum developmentcGMP-dependent protein kinase 1 Homo sapiens (human)
actin cytoskeleton organizationcGMP-dependent protein kinase 1 Homo sapiens (human)
forebrain developmentcGMP-dependent protein kinase 1 Homo sapiens (human)
positive regulation of circadian rhythmcGMP-dependent protein kinase 1 Homo sapiens (human)
regulation of GTPase activitycGMP-dependent protein kinase 1 Homo sapiens (human)
collateral sproutingcGMP-dependent protein kinase 1 Homo sapiens (human)
relaxation of vascular associated smooth musclecGMP-dependent protein kinase 1 Homo sapiens (human)
cell growth involved in cardiac muscle cell developmentcGMP-dependent protein kinase 1 Homo sapiens (human)
negative regulation of platelet aggregationcGMP-dependent protein kinase 1 Homo sapiens (human)
negative regulation of vascular associated smooth muscle cell proliferationcGMP-dependent protein kinase 1 Homo sapiens (human)
negative regulation of vascular associated smooth muscle cell migrationcGMP-dependent protein kinase 1 Homo sapiens (human)
regulation of testosterone biosynthetic processcGMP-dependent protein kinase 1 Homo sapiens (human)
protein kinase A signalingcGMP-dependent protein kinase 1 Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (101)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
tachykinin receptor activitySubstance-P receptorHomo sapiens (human)
protein bindingSubstance-P receptorHomo sapiens (human)
substance P receptor activitySubstance-P receptorHomo sapiens (human)
protein bindingNeuromedin-K receptorHomo sapiens (human)
tachykinin receptor activityNeuromedin-K receptorHomo sapiens (human)
protein kinase activitycGMP-dependent protein kinase 1 Homo sapiens (human)
cGMP-dependent protein kinase activitycGMP-dependent protein kinase 1 Homo sapiens (human)
calcium channel regulator activitycGMP-dependent protein kinase 1 Homo sapiens (human)
protein bindingcGMP-dependent protein kinase 1 Homo sapiens (human)
ATP bindingcGMP-dependent protein kinase 1 Homo sapiens (human)
cGMP bindingcGMP-dependent protein kinase 1 Homo sapiens (human)
identical protein bindingcGMP-dependent protein kinase 1 Homo sapiens (human)
mitogen-activated protein kinase p38 bindingcGMP-dependent protein kinase 1 Homo sapiens (human)
protein serine kinase activitycGMP-dependent protein kinase 1 Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (57)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
plasma membraneSubstance-P receptorHomo sapiens (human)
cell surfaceSubstance-P receptorHomo sapiens (human)
dendriteSubstance-P receptorHomo sapiens (human)
sperm flagellumSubstance-P receptorHomo sapiens (human)
cell bodySubstance-P receptorHomo sapiens (human)
sperm headSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
plasma membraneSubstance-P receptorHomo sapiens (human)
sperm midpieceSubstance-P receptorHomo sapiens (human)
plasma membraneNeuromedin-K receptorHomo sapiens (human)
dendrite membraneNeuromedin-K receptorHomo sapiens (human)
neuronal cell body membraneNeuromedin-K receptorHomo sapiens (human)
sperm midpieceNeuromedin-K receptorHomo sapiens (human)
plasma membraneNeuromedin-K receptorHomo sapiens (human)
sperm midpieceNeuromedin-K receptorHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
acrosomal vesiclecGMP-dependent protein kinase 1 Homo sapiens (human)
nucleoplasmcGMP-dependent protein kinase 1 Homo sapiens (human)
cytoplasmcGMP-dependent protein kinase 1 Homo sapiens (human)
Golgi apparatuscGMP-dependent protein kinase 1 Homo sapiens (human)
cytosolcGMP-dependent protein kinase 1 Homo sapiens (human)
plasma membranecGMP-dependent protein kinase 1 Homo sapiens (human)
sarcolemmacGMP-dependent protein kinase 1 Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (180)

Assay IDTitleYearJournalArticle
AID715672Binding affinity to human NK1 receptor assessed as dissociation half life2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
AID222272Dose (ID50) for inhibition of SP-mediated vascular leakage was determined after intravenous administration followed by resiniferatoxin (RTX) challenge 1 hour before2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID25716Area under curve was determined after intravenous administration of compound as Bis(N-methyl-D-glucamine) salt in rat at a dose 1 mg/kg2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID72683compound was tested for antiemetic action in ferret at 3 mg/kg after peroral administration followed by emetogen (apomorphine) challenge at 0.25 mg/kg, sc1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID26988concentration in plasma after incubation in human blood after 120 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID271466Displacement of [125I]SP from human cloned NK1 receptor expressed in CHO cells2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
AID72562compound was tested for antiemetic action in ferret at 3 mg/kg after peroral administration followed by emetogen (morphine) challenge at 0.5 mg/kg, sc1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID26973concentration in human hepatic cytosolic subcellular fractions after 30 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID26991concentration in plasma after incubation in human blood after 60 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID270528Inhibition of foot tapping in iv dosed gerbil after 4 hrs by CNS assay2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID26990concentration in plasma after incubation in human blood after 30 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID77134Inhibition of resiniferatoxin-induced systemic vascular leakage in guinea pig (SYVAL) upon oral administration at 24 hr r1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID25482Area under curve (AUC) was determined after intravenous administration in dog at a dose of 0.5 mg/kg2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID26993concentration in plasma after incubation in rat after 120 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID25483Area under curve (AUC) was determined after intravenous administration in dog at a dose of 2 mg/kg2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID72687compound was tested for antiemetic action in ferret at 3 mg/kg after peroral administration followed by emetogen (apomorphine) challenge at 0.25 mg/kg, sc1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID26986concentration in plasma after incubation in dog after 60 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID26972concentration in human hepatic cytosolic subcellular fractions after 15 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID72559compound was tested for antiemetic action in ferret at 0.3 mg/kg after intravenous administration followed by emetogen (cisplatin) challenge at 10 mg/kg, iv after 3 min1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID342286Inhibition of NK1 receptor2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
The many roles for fluorine in medicinal chemistry.
AID75086Inhibition of GR-73632-induced Gerbil foot tapping after immediate pretreatment iv2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID270527Solubility in potassium hydrogen buffer at pH 52006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
AID270514Displacement of [125I]SP from human cloned NK1 receptor expressed in CHO cells2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID271473Solubility in potassium hydrogen phosphate buffer at pH 52006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
AID26984concentration in plasma after incubation in dog after 15 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID76983Inhibition of resiniferatoxin-induced systemic vascular leakage in guinea pig (SYVAL) upon oral administration at 1 hr1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID342287Inhibition of resiniferatoxin-induced systemic vascular leakage in po dosed guinea pig emesis model after 24 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
The many roles for fluorine in medicinal chemistry.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID25488Area under curve (AUC) was determined after intravenous administration of compound as Bis(N-methyl-D-glucamine) salt in dog at a dose of 32 mg/Kg2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID26975concentration in human hepatic microsomal subcellular fractions after 0 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID208406Displacement of [125I]-labeled SP from the human Tachykinin receptor 1 expressed in CHO cells1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1220560Fraction unbound in human occipital cortex at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1817621Selectivity index, ratio of IC50 for human MRC5 to IC50 for human A5492021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Carbohydrate-Based NK1R Antagonists with Broad-Spectrum Anticancer Activity.
AID25485Area under curve (AUC) was determined after intravenous administration in rat at a dose of 5 mg/kg2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID270515Solubility in acetate buffer at pH 52006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
AID1220558Fraction unbound in Beagle dog brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID26974concentration in human hepatic cytosolic subcellular fractions after 60 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID72568Dose-dependent reduction in cisplatin-induced vomiting in ferrets at 0.1 mg/kg iv dose2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1220556Fraction unbound in CD-1 mouse brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID715707Displacement of radioligand [3H]SP from human NK1 F264Y6.51 mutant expressed in HEK293 cells2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
AID26976concentration in human hepatic microsomal subcellular fractions after 120 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID270517Inhibition of SP-elicited plasma extravasation in esophagus of orally dosed guinea pig after 1 hr by SYVAL assay2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
AID72570Dose-dependent reduction in cisplatin-induced vomiting in ferrets at 1.0 mg/kg iv dose2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID1817619Anti-cancer activity against human MRC5 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Carbohydrate-Based NK1R Antagonists with Broad-Spectrum Anticancer Activity.
AID222274Dose (ID50) for inhibition of SP-mediated vascular leakage was determined after oral administration followed by resiniferatoxin (RTX) challenge 1 hour2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID222273Dose (ID50) for inhibition of SP-mediated vascular leakage was determined after intravenous administration followed by resiniferatoxin (RTX) challenge 24 hour before2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID26971concentration in human hepatic cytosolic subcellular fractions after 120 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID72686compound was tested for antiemetic action in ferret at 0.3 mg/kg after intravenous administration followed by emetogen (cisplatin) challenge at 10 mg/kg, iv after 3 min1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID72689compound was tested for antiemetic action in ferret at 3 mg/kg after peroral administration followed by emetogen (morphine) challenge at 0.5 mg/kg, sc1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID25487Area under curve (AUC) was determined after intravenous administration of compound as Bis(N-methyl-D-glucamine) salt in dog at a dose of 2 mg/Kg2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID72556compound was tested for antiemetic action in ferret at 3 mg/kg after peroral administration followed by emetogen (apomorphine) challenge at 0.25 mg/kg, sc1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID26996concentration in plasma after incubation in rat after 60 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID715705Displacement of radioligand [3H]osanetant at human NK3 Y315F6.51 mutant expressed in HEK293 cells2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
AID1220554Fraction unbound in Wistar Han rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID270525Solubility at pH 8.22006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
AID72558compound was tested for antiemetic action in ferret at 3 mg/kg after peroral administration followed by emetogen (morphine) challenge at 0.5 mg/kg, sc1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID26970concentration in human hepatic cytosolic subcellular fractions after 0 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID26994concentration in plasma after incubation in rat after 15 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID75084Inhibition of GR 73632-induced foot tapping in gerbils upon intravenous administration of compound after 4 hr1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID208440compounds were evaluated for inhibitory activity against human Tachykinin receptor 12000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID715902Competitive inhibition of human NK1 F264Y6.51 mutant expressed in HEK293 cells assessed as decrease in SP1-induced [3H]IP accumulation after 20 mins2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
AID1817620Anti-cancer activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Carbohydrate-Based NK1R Antagonists with Broad-Spectrum Anticancer Activity.
AID72684compound was tested for antiemetic action in ferret at 3 mg/kg after peroral administration followed by emetogen (cisplatin) challenge at 10 mg/kg, iv after 3 min1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID72682compound was tested for antiemetic action in ferret at 0.3 mg/kg after intravenous administration followed by emetogen (cisplatin) challenge at 10 mg/kg, iv after 3 min1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID715901Noncompetitive inhibition of wild type human NK1 receptor expressed in HEK293 cells assessed as decrease in SP1-induced [3H]IP accumulation after 20 mins2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
AID72688compound was tested for antiemetic action in ferret at 3 mg/kg after peroral administration followed by emetogen (cisplatin) challenge at 10 mg/kg, iv after 3 min1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID301059Displacement of [125I]SP from human NK1 receptor expressed in CHO cells2007Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.
AID301062Inhibition of human CYP3A42007Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.
AID715704Selectivity ratio of Ki for wild type human NK3 receptor expressed in HEK293 cells to Ki for human NK3 Y315F6.51 mutant expressed in HEK293 cells2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
AID25717Area under curve was determined after intravenous administration of compound as Bis(N-methyl-D-glucamine) salt in rat at a dose 8 mg/kg2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID1817661Anti-cancer activity against human A549 cells incubated for 96 hrs by Resazurin assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Carbohydrate-Based NK1R Antagonists with Broad-Spectrum Anticancer Activity.
AID72207inhibitory dose was determined after intravenous administration of the compound.2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID25489Area under curve (AUC) was determined after intravenous administration of compound as Bis(N-methyl-D-glucamine) salt in rat at a dose 25 mg/Kg2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID25486Area under curve (AUC) was determined after intravenous administration of compound as Bis(N-methyl-D-glucamine) salt in dog at a dose of 0.5 mg/Kg2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID72561compound was tested for antiemetic action in ferret at 3 mg/kg after peroral administration followed by emetogen (cisplatin) challenge at 10 mg/kg, iv after 3 min1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID75085Inhibition of GR-73632-induced Gerbil foot tapping after 24 hr pretreatment iv2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID1220559Fraction unbound in cynomolgus monkey brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID342288Inhibition of GR-73632-induced foot-tapping in iv dosed gerbils after 24 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
The many roles for fluorine in medicinal chemistry.
AID72557compound was tested for antiemetic action in ferret at 3 mg/kg after peroral administration followed by emetogen (cisplatin) challenge at 10 mg/kg, iv after 3 min1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID26978concentration in human hepatic microsomal subcellular fractions after 30 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID72569Dose-dependent reduction in cisplatin-induced vomiting in ferrets at 0.3 mg/kg iv dose2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1220555Fraction unbound in Sprague-Dawley rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1237291Displacement of [125I]-substance P from gerbil NK1 receptor expressed in HEK293 cell membranes incubated for 30 mins by liquid scintillation counting method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors.
AID1817660Antagonist activity at NK1R (unknown origin) assessed as decreased IP1 levels in presence of endogenous SP ligand preincubated for 10 mins followed by 30 min incubation with antagonist and SP by HTRF-FRET assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Carbohydrate-Based NK1R Antagonists with Broad-Spectrum Anticancer Activity.
AID72566Dose dependent reduction in cisplatin-induced retching in ferrets at 0.3 mg/kg iv dose2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID75083Inhibition of GR 73632-induced foot tapping in gerbils upon intravenous administration of compound after 24 hr1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID72567Dose dependent reduction in cisplatin-induced retching in ferrets at 1.0 mg/kg iv dose2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID208423In vitro inhibition of binding of [125I]-substance P to tachykinin receptor 12001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration.
AID270516Dissociation constant, pKa of the compound2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID271470Bioavailability in orally dosed dog2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
AID271468Dissociation constant, pKa of the compound2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
AID26995concentration in plasma after incubation in rat after 30 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID1064184Binding affinity to NK1 receptor (unknown origin)2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
Design and synthesis of potential dual NK(1)/NK(3) receptor antagonists.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID72555compound was tested for antiemetic action in ferret at 0.3 mg/kg after intravenous administration followed by emetogen (cisplatin) challenge at 10 mg/kg, iv after 3 min1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID270518Inhibition of SP-elicited plasma extravasation in esophagus of orally dosed guinea pig after 24 hrs by SYVAL assay2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
AID26992concentration in plasma after incubation in rat after 0 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID72560compound was tested for antiemetic action in ferret at 3 mg/kg after peroral administration followed by emetogen (apomorphine) challenge at 0.25 mg/kg, sc1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID715708Displacement of radioligand [3H]SP from wild type human NK1 receptor expressed in HEK293 cells2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID271469Bioavailability in orally dosed rat2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
AID208587Binding affinity against human Tachykinin receptor 1 expressed in CHO cells using [3H]-substance P as the radioligand2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives.
AID25484Area under curve (AUC) was determined after intravenous administration in rat at a dose of 2 mg/kg2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID72565Dose dependent reduction in cisplatin-induced retching in ferrets at 0.1 mg/kg iv dose2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID26989concentration in plasma after incubation in human blood after 15 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID72685compound was tested for antiemetic action in ferret at 3 mg/kg after peroral administration followed by emetogen (morphine) challenge at 0.5 mg/kg, sc1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID715706Displacement of [3H]osanetant from wild type human NK3 receptor expressed in HEK293 cells2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
AID26983concentration in plasma after incubation in dog after 120 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID270522Inhibition of foot tapping in iv dosed gerbil after 24 hrs by CNS assay2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
AID271471Solubility in isotonic saline at pH 8.22006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID26982concentration in plasma after incubation in dog after 0 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID26987concentration in plasma after incubation in human blood after 0 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID75082Inhibition of GR 73632-induced foot tapping in gerbils upon intravenous administration of compound1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID26985concentration in plasma after incubation in dog after 30 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID1817659Antagonist activity at NK1R (unknown origin) in presence of endogenous SP ligand preincubated for 10 mins followed by 30 min incubation with antagonist and SP by HTRF-FRET assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Carbohydrate-Based NK1R Antagonists with Broad-Spectrum Anticancer Activity.
AID1777610Activation of full length PKG1alpha (unknown origin) using Glass-tide peptide substrate incubated for 120 mins followed by addition of ADP-Glo max reagent incubated for 40 mins2021ACS medicinal chemistry letters, Aug-12, Volume: 12, Issue:8
Discovery of the First Non-cGMP Mimetic Small Molecule Activators of cGMP-Dependent Protein Kinase 1 α (PKG1α).
AID26979concentration in human hepatic microsomal subcellular fractions after 60 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID270521Inhibition of foot tapping in iv dosed gerbil after 5 mins by CNS assay2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Cyclopentane-based human NK1 antagonists. Part 2: development of potent, orally active, water-soluble derivatives.
AID26977concentration in human hepatic microsomal subcellular fractions after 15 min2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID779964Antagonist activity at NK1 receptor (unknown origin)2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.
AID1220557Fraction unbound in Hartley guinea pig brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID686947qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Identification of potent Yes1 kinase inhibitors using a library screening approach.
AID1346346Human NK1 receptor (Tachykinin receptors)1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.
AID1346346Human NK1 receptor (Tachykinin receptors)2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.
AID1745855NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (737)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (0.68)18.7374
1990's11 (1.49)18.2507
2000's174 (23.61)29.6817
2010's400 (54.27)24.3611
2020's147 (19.95)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials229 (29.78%)5.53%
Reviews115 (14.95%)6.00%
Case Studies33 (4.29%)4.05%
Observational15 (1.95%)0.25%
Other377 (49.02%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (197)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized, Double-Blind, Parallel-Group Study Conducted Under In-House Blinding Conditions to Determine the Efficacy and Tolerability of Aprepitant for the Prevention of Chemotherapy Induced Nausea and Vomiting (CINV) Associated With Moderately Emetoge[NCT00337727]Phase 3848 participants (Actual)Interventional2007-01-01Completed
Randomized, Placebo-controlled Trial of Olanzapine Versus Aprepitant Plus Ondansetron and Dexamethasone as Antiemetic Prophylaxis in Patients Receiving High Emetic Chemotherapy[NCT03876938]Phase 3147 participants (Anticipated)Interventional2019-03-01Recruiting
A Phase Ib, Randomized, Placebo Controlled, Double Blind Study to Determine the Safety, Viral Suppression, Pharmacokinetics and Immune Modulatory Effects of Treatment With Aprepitant (Emend®) in HIV Infected Individuals[NCT01300988]Phase 118 participants (Actual)Interventional2010-12-31Completed
Multicenter Randomized Controlled Trial of Combination Antiemetic Therapy With Aprepitant / Fosaprepitant in Patients With Colorectal Cancer Receiving Oxaliplatin-based Chemotherapy[NCT01344304]413 participants (Actual)Interventional2011-04-30Completed
Olanzapine With or Without Fosaprepitant for the Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)in Patients Receiving Highly Emetogenic Chemotherapy (HEC): A Phase III Randomized, Double Blind, Placebo-Controlled Trial[NCT03578081]Phase 3690 participants (Actual)Interventional2018-10-15Completed
A Pilot Study to Evaluate the Safety and Efficacy of Aprepitant in Combination With Dolasetron and Dexamethasone for the Prevention of Nausea and Vomiting Following Oxaliplatin-containing Regimen Which Includes 5-FU.[NCT02550119]19 participants (Actual)Interventional2006-04-19Terminated(stopped due to Insufficient accrual)
Designing Optimal Prevention and Management of Postoperative Nausea and Emesis for Patients Undergoing Laparoscopic Sleeve Gastrectomy[NCT03435003]Phase 4104 participants (Actual)Interventional2017-08-28Completed
A Phase 4, Open-label, Single Arm Study to Evaluate the Safety and Tolerability of a Three-day Fosaprepitant Regimen Administered for the Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV) in Pediatric Participants Receiving Emetogenic Chemothe[NCT04054193]Phase 4103 participants (Actual)Interventional2019-09-09Completed
Phase II, Double-blind, Placebo-controlled, Crossover Study Evaluating a 5HT3 Antagonist Plus Dexamethasone With or Without Fosaprepitant in Patients With Advanced NSCLC Receiving Carboplatin Based Chemotherapy[NCT02407600]Phase 2150 participants (Anticipated)Interventional2015-04-30Not yet recruiting
Effect of Fosaprepitant on Motor Evoked and Somatosensory Evoked Potentials Under General Anesthesia[NCT03197064]Phase 411 participants (Actual)Interventional2018-01-01Completed
Efficacy and Safety of Fosaprepitant in Preventing Chemotherapy-induced Vomiting in Children Treated With Medium and High Emetic Chemotherapeutic Drugs[NCT05230654]120 participants (Anticipated)Interventional2022-02-01Not yet recruiting
Triple Combination of Fosaprepitant, Dexamethasone and Palonosetron Versus Combination of Dexamethasone and Palonosetron for the Prevention of Postoperative Nausea and Vomiting in Patients Undergoing Laparoscopic Gastrointestinal Surgery[NCT04853147]Phase 31,154 participants (Actual)Interventional2021-04-27Completed
Relative Bioavailability of NXP001 Compared to Emend® in Healthy Volunteers[NCT03889366]Phase 112 participants (Actual)Interventional2019-03-20Completed
Aprepitant Versus Gabapentin Prophylaxis for Postoperative Nausea and Vomiting in Laparoscopic Gynecological Surgeries[NCT02525848]Phase 2/Phase 3150 participants (Actual)Interventional2015-08-31Completed
A Phase 2 Randomized, Double-Blind, Placebo-Controlled Study of Aprepitant Injectable Emulsion in Early Hospitalized Adult Patients With COVID-19[NCT04470622]Phase 227 participants (Actual)Interventional2020-07-20Terminated(stopped due to Study was terminated early by Heron, and was not terminated for safety reasons.)
Aprepitant for Prevention of Acute and Delayed Nausea and Vomiting: a Phase III, Double-blind, Randomized, Placebo-controlled Trial in Patients Receiving a High-emetogenic Dose of Cyclophosphamide for Peripheral Blood Stem Cells Harvesting[NCT01088022]Phase 3120 participants (Anticipated)Interventional2010-04-30Not yet recruiting
Efficacy and Safety of Intravenous Versus Oral 5-HT3 Antagonists Combined With NK-1 Receptor Antagonists for the Prevention of Breast Cancer Chemotherapy-induced Nausea and Vomiting: a Single-center, Randomized Controlled Clinical Trial[NCT05841849]Phase 41,028 participants (Anticipated)Interventional2023-07-31Not yet recruiting
Randomized, Embedded, Multifactorial Adaptive Platform for Perioperative Medicine at UPMC (UPMC REMAP): Core Protocol - Enhanced Recovery Protocols (ERP)[NCT04606264]Phase 32,500 participants (Anticipated)Interventional2023-05-15Recruiting
Aprepitant vs. Placebo for the Prevention of Postoperative Nausea and Vomiting: a Randomized, Double-blind Study in Patients Undergoing Laparoscopic Cholecystectomy[NCT01020903]200 participants (Actual)Interventional2009-11-30Completed
An Open Label Phase II Study of Aprepitant for Multi-day Moderately-high to Highly Emetogenic Chemotherapy Regimens[NCT00711555]Phase 222 participants (Actual)Interventional2005-11-30Completed
Safety and Efficacy of Aprepitant for Chemotherapy-Induced Nausea and Vomiting in Patients With Lung Cancer Receiving Multiple-day Cisplatin Chemotherapy[NCT02445872]Phase 280 participants (Anticipated)Interventional2015-12-31Not yet recruiting
Evaluation of Palonosetron and Palonosetron/Aprepitant in Post Operative Nausea and Vomiting Incidence in Oncological Patients[NCT02431286]Phase 490 participants (Anticipated)Interventional2014-10-31Recruiting
Phase II Randomized Trial to Evaluate Efficacy of Olanzapine With Short-acting 5HT3 Inhibitors in Chemotherapy-induced Nausea & Vomiting (CINV) Prophylaxis[NCT03478605]Phase 2130 participants (Anticipated)Interventional2018-05-25Recruiting
A Phase III, Randomized, Placebo-Controlled Clinical Trial to Study the Efficacy and Safety of MK-0517/Fosaprepitant and Ondansetron Versus Ondansetron for the Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV) in Pediatric Subjects Receiving E[NCT02519842]Phase 375 participants (Actual)Interventional2015-09-14Terminated(stopped due to Further data are no longer required to support an application for use in pediatric patients. The decision to terminate was not based on any new safety findings)
Phase II Randomized Study of Multiple Doses of Palonosetron Plus Aprepitant Versus Multiple Doses of Palonosetron Alone in Preventing CINV in Patients With Newly Diagnosed AML or High-risk MDS Receiving Multiple Days Chemotherapy[NCT02205164]Phase 2134 participants (Anticipated)Interventional2011-10-31Recruiting
The Optimization of Antiemetic Regimen for Chemoradiotherapy-induced Nausea and Vomiting (C-RINV) in Locally Advanced Head and Neck Squamous Cell Carcinoma (LA-HNSCCs): A Prospective Phase Ⅱ Trial[NCT05202275]Phase 243 participants (Anticipated)Interventional2020-12-01Recruiting
The Effects of Intravenous Fosaprepitant and Ondansetron for the Prevention of Postoperative Nausea and Vomiting in Thoracicsurgery Patients: A Single-center, Randomized, Double-Blinded Clinical Study[NCT05881486]234 participants (Anticipated)Interventional2023-06-30Not yet recruiting
See Detailed Description[NCT00169572]Phase 2492 participants Interventional2005-02-28Completed
A Phase IB, Open Label Study to Examine the Safety, Pharmacokinetic Characteristics and Anti-Inflammatory Effects of the NK-1R Antagonist, Aprepitant, In HIV-Infected Subjects Receiving Atazanavir/Ritonavir Or Darunavir/Ritonavir[NCT02154360]Phase 112 participants (Actual)Interventional2014-05-31Completed
A Prospective, Open-label, Single-arm Study for Efficacy and Safety of Three-drug Antiemetic Regimen to Prevent the Emesis During Radiotherapy With Concurrent Chemoradiotherapy in Locally Advanced HNSCC[NCT03572829]Phase 244 participants (Actual)Interventional2018-03-01Completed
Relative Bioavailability of an Extemporaneous Oral Suspension of Aprepitant in Healthy Adult Volunteers[NCT03245918]Phase 117 participants (Actual)Interventional2017-08-10Completed
A Randomized Controlled Study to Compare (EMEND®)to Standard Treatment as Prevention for Delayed Chemotherapy-induced Nausea and Vomiting (CINV) After Myeloablative Therapy for Patients Undergoing Autologous Stem Cell Transplantation.[NCT01101529]Phase 290 participants (Anticipated)Interventional2010-05-31Completed
A Comparison of the Combination of Aprepitant and Dexamethasone Versus the Combination of Ondansetron and Dexamethasone for the Prevention of Postoperative Nausea and Vomiting (PONV) in Patients Undergoing Craniotomy[NCT00734929]Phase 4115 participants (Actual)Interventional2007-09-30Completed
Phase II Trial Testing the Antiemetic Efficacy of a Single-day Low Dose Aprepitant (or Fosaprepitant) Added to a 5-HT3 Receptor Antagonist Plus Dexamethasone in Patients Receiving Carboplatin[NCT03237611]Phase 215 participants (Actual)Interventional2018-10-30Terminated(stopped due to Expired IRB approval on 2/11/21)
Medications Development for the Treatment of Cannabis Related Disorders[NCT01204723]Phase 163 participants (Actual)Interventional2009-08-31Completed
Evaluating the Effect of Aprepitant on Cyclophosphamide Pharmacokinetics[NCT00719173]Phase 119 participants (Actual)Interventional2005-08-31Completed
Prevention of Nausea and Vomitting Associated With Stem Cell Transplant: Results of a Prospective, Randomized Trial of Aprepitant Used With Highly Emetogenic Preparative Regimens[NCT00781768]Phase 4181 participants (Actual)Interventional2003-08-31Completed
A Randomized, 5-Part, Intravenous Study of the Safety, Tolerability, Bioequivalence, and Drug Interaction Potential of Final Market Image Formulation of MK0517 in Young Healthy Subjects[NCT00990821]Phase 1188 participants (Actual)Interventional2005-01-31Completed
A Multicenter, Open-Label, 5-Part Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of Aprepitant and Fosaprepitant Dimeglumine in Pediatric Patients Receiving Emetogenic Chemotherapy[NCT00818259]Phase 192 participants (Actual)Interventional2009-02-05Terminated(stopped due to Study terminated early prior to completing targeted enrollment of participants <6 months of age due to recruitment challenges.)
Clinical on the Safety and Effectiveness of Fosaprepitant Dimeglumine for Injection in the Prevention of Nausea and Vomiting Caused by Tumor Chemotherapy Drugs.[NCT05755659]3,000 participants (Anticipated)Interventional2022-07-15Recruiting
Aprepitant to Mitigate Opioids' Cognitive Side Effects[NCT02226601]50 participants (Anticipated)Interventional2014-10-31Recruiting
Comparative Trial Ondansetron Alone Versus Combination of Ondansetron Plus Aprepitant for Prevention of Nausea and Vomiting With Hematologic Malignancies Receiving Regimens Containing High-dose Cytarabine[NCT00954941]Phase 2100 participants (Actual)Interventional2009-11-30Completed
Randomized Phase 3 Study of Aprepitant Versus Placebo in Chinese Advanced Non-small Cell Lung Cancer Who Received Highly Emetogenic Chemotherapy[NCT02161991]Phase 3244 participants (Actual)Interventional2014-02-01Completed
A Phase III, Randomized, Double-Blind, Active Comparator-Controlled Clinical Trial, Conducted Under In-House Blinding Conditions, to Examine the Efficacy and Safety of Aprepitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV) in Ped[NCT01362530]Phase 3307 participants (Actual)Interventional2011-09-13Completed
An Open-Label, Randomized, 2-Period Crossover Study To Evaluate The Effect Of A Single Dose Of Aprepitant, A Moderate CYP3A Inhibitor On Bosutinib Administered Orally To Healthy Subjects[NCT02058277]Phase 120 participants (Actual)Interventional2014-05-31Completed
A Multi-central Perspective Randomized Controlled Study Evaluating the Efficacy and Safety of Aprepitant in Autologous Hematopoietic Stem Cell Transplantation[NCT02576327]Phase 4130 participants (Anticipated)Interventional2015-10-31Active, not recruiting
A Multinational, Randomized, Double-blind, Placebo-controlled Study to Investigate the Efficacy and Tolerability of Palonosetron and Dexamethasone Plus Fosaprepitant or Placebo in Patients Receiving Radiotherapy and Weekly Cisplatin.[NCT01074697]Phase 3246 participants (Actual)Interventional2010-04-30Completed
A Phase 2 Open-Label Study of HTX-011 Via Individualized Dosing Administration for Postoperative Analgesia Following Unilateral Simple Bunionectomy[NCT03718039]Phase 278 participants (Actual)Interventional2018-10-24Completed
Evaluation of Aprepitant's Effect on Drug Metabolism in Multi-Day Combination (CHOP/R-CHOP) Chemotherapy Regimen in Patients With Non-Hodgkin's Lymphoma[NCT00651755]23 participants (Actual)Interventional2008-03-31Completed
A Randomized, Double-blind, Placebo-controlled Clinical Study on Prevention and Treatment of CINV Induced by TC Regimen in Gynecological Malignant Tumors[NCT06007586]Phase 4138 participants (Anticipated)Interventional2024-02-10Not yet recruiting
Comparison of Dual Therapy of Dexamethasone and Palonosetron and Triple Therapy of Dexamethasone, Palonosetron, Fosaprepitant for Postoperative Nausea and Vomiting Prevention: A Randomized Controlled Trial[NCT05773950]144 participants (Anticipated)Interventional2023-08-18Enrolling by invitation
A Phase III Trial Comparing Dexamethasone, Aprepitant With or Without Mirtazapine in Delayed Emesis Control and Appetite Improvement[NCT02336750]Phase 3212 participants (Actual)Interventional2014-12-31Completed
Prevention of Postoperative Nausea and Vomiting in a Gynecologic Surgery Population: A Randomized Placebo Controlled Trial of Aprepitant NK-1-receptor Antagonist[NCT00888329]Phase 4256 participants (Actual)Interventional2007-07-31Terminated(stopped due to Slow accrual.)
A Randomized and Placebo-Controlled Evaluation of Aprepitant for Decreasing the Incidence of Post-Operative Nausea and Vomiting (PONV) in Bariatric Patients[NCT00956215]125 participants (Actual)Interventional2010-05-31Completed
MK0869 and MK0517 Time-on-Target PET Study[NCT01111851]Phase 116 participants (Actual)Interventional2010-04-30Completed
Comparison of Ramosetron, Aprepitant, and Dexamethasone (RAD) With Palonosetron, Aprepitant, and Dexamethasone (PAD) for Prevention of Nausea and Vomiting Induced by Highly Emetogenic Chemotherapy[NCT02532634]Phase 4292 participants (Actual)Interventional2015-08-19Completed
A Multi-center, 2-Part Study to Evaluate the Pharmacokinetics Safety and Tolerability of Aprepitant in Pediatric Patients Undergoing Surgery[NCT00819039]Phase 198 participants (Actual)Interventional2009-01-26Completed
Combined Use of Multi-Day Doses of Palonosetron and Aprepitant With Low Doses Dexamethasone in Prevention of Nausea and Emesis Among Patients With Multiple Myeloma and Lymphoma Undergoing Autologous Stem Cell Transplant: A Pilot Study[NCT00600353]Phase 220 participants (Actual)Interventional2007-10-31Completed
A Prospective, Open Label, Non-comparative Trial to Determine the Incidence of Chemotherapy-Induced Nausea and Vomiting (CINV) Associated With the Docetaxel-Cyclophosphamide Regimen in Early Breast Cancer Patients[NCT01298193]Phase 4212 participants (Actual)Interventional2011-05-31Completed
A Comparison of Combination Antiemetic Regimen for Prevention of PONV in Breast Surgery Patients[NCT00738621]Phase 4100 participants (Actual)Interventional2008-07-31Completed
Aprepitant- and Olanzapine- Containing Regimens for Prevention of Acute and Delayed Nausea and Vomiting Associated With High Dose Melphalan and BEAM in Autologous Stem Cell Transplant Patients[NCT02939287]Phase 3429 participants (Actual)Interventional2017-09-23Completed
Relative Bioavailability of an Extemporaneous Oral Suspension of Aprepitant in Adolescents[NCT01249001]Phase 24 participants (Actual)Interventional2010-10-31Terminated(stopped due to lack of eligible participants to enrol)
A Phase III, Randomized, Multi-center, Double-Blind, Placebo-Controlled, Parallel-Group Clinical Trial to Study the Safety, Tolerability and Efficacy of MK0869/Aprepitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV) Associated Wit[NCT00952341]Phase 3421 participants (Actual)Interventional2009-08-25Completed
Phase III, Double-Blind, Placebo-Controlled, Crossover Study Evaluating Aprepitant in Combination With a 5HT3 & Dexamethasone in Patients With Germ Cell Tumors Undergoing 5 Day Cisplatin-Based Chemotherapy Regimen[NCT00572572]Phase 369 participants (Actual)Interventional2007-12-31Completed
A Single-Dose Bioequivalence and Food Effect Study With Aprepitant and Fosaprepitant Dimeglumine in Healthy Young Adult Subjects[NCT00945321]Phase 142 participants (Actual)Interventional2009-02-28Completed
A Phase II Study to Evaluate the Efficacy and Tolerability of Ramosetron, Aprepitant and Dexamethasone (RAD) in Preventing Cisplatin-induced Nausea and Vomiting in Chemotherapy-naïve Patients With Solid Cancer[NCT01046461]Phase 241 participants (Actual)Interventional2010-01-31Active, not recruiting
A Randomized, Double-Blind Comparison of Oral Aprepitant and Lower Dose Dexamethasone vs Aprepitant Alone for Preventing Postoperative Nausea and Vomiting After Elective Laparoscopic Surgeries[NCT00835965]50 participants (Anticipated)Interventional2009-02-28Not yet recruiting
Effects of Aprepitant/Dexamethasone Versus Mertazepine /Dexamethasone on Postoperative Nausea and Vomiting After Laparoscopic Sleeve Surgery: a Randomized Controlled Trial[NCT04013386]Phase 490 participants (Actual)Interventional2019-07-15Completed
A Phase III, Randomized, Double-Blind, Active-Controlled, Parallel-Group Study, Conducted Under In-House Blinding Conditions, to Examine the Safety, Tolerability, and Efficacy of a Single Dose of Intravenous MK-0517 for the Prevention of Chemotherapy-Indu[NCT00619359]Phase 32,322 participants (Actual)Interventional2008-02-29Completed
Developing Individualized Strategies to Prevent Nausea and Vomiting[NCT01393288]0 participants (Actual)Interventional2013-11-30Withdrawn
A Study to Evaluate the Anti-emetic Effect of Aprepitant Versus Placebo as an Add-on Therapy in Children and Adolescent Receiving Chemotherapy: A Randomized, Doubly Blinded Controlled Trial[NCT01402024]Phase 396 participants (Actual)Interventional2011-08-31Completed
Aprepitant in the Prevention of Delayed Emesis Induced by Moderately Emetogenic Chemotherapy (Cyclophosphamide Plus Anthracyclines) in Breast Cancer Patients: a Double-blind Randomized Study[NCT00869973]Phase 3580 participants (Actual)Interventional2009-09-30Terminated(stopped due to We terminated the study after enrolling 580/900 patients due to a slow accrual)
FORESIGHT: Feasibility of Olanzapine at REduced doSe in hIGHly Emetogenic chemoTherapy: a Randomised Controlled Trial Against Aprepitant in Triple Therapy[NCT04075955]Phase 330 participants (Actual)Interventional2019-04-29Completed
A Phase II Clinical Trial Investigating the Efficacy of Single-Dose Fosaprepitant for the Prevention of Cisplatin-Induced Nausea and Vomiting (CINV) in Patients With Head & Neck Cancer Undergoing Concurrent Chemotherapy and Radiation[NCT00895245]Phase 26 participants (Actual)Interventional2009-02-28Terminated(stopped due to Study stopped due to lack of efficacy in first 6 patients)
Contribution of Substance P to Blood Pressure Regulation in the Setting of Dipeptidyl Peptidase IV (DPP4) and Angiotensin-Converting Enzyme (ACE) Inhibition[NCT02130687]106 participants (Actual)Interventional2014-06-30Completed
Effectiveness of Aprepitant in Addition to Ondansetron in the Prevention of Nausea and Vomiting Caused by Fractionated Radiotherapy to the Upper Abdomen[NCT00970905]Phase 252 participants (Actual)Interventional2009-10-31Completed
Pilot Study of the Action of the Substance P Antagonist Aprepitant on Aldosterone and Cortisol Secretion in Healthy Volunteers.[NCT00977223]Phase 420 participants (Actual)Interventional2009-06-30Completed
A Randomized, Double-Blind, Active Comparator-Controlled, Parallel-Group Study Conducted Under In-House Blinding Conditions, to Examine the Safety and Tolerability of IV MK0517 for the Prevention of Postoperative Nausea and Vomiting (PONV)[NCT00231777]Phase 3216 participants (Actual)Interventional2005-07-31Completed
Pilot Study Exploring the Efficacy of Prolonged Emend to Reduce Nausea and Vomiting During Treatment in a Phase II Study (NYU 03-67) of Oxaliplatin Combined With Continuous Infusion Topotecan for Patients With Previously Treated Ovarian Cancer[NCT01017809]0 participants (Actual)Interventional2010-12-31Withdrawn(stopped due to NYU 03-67 reached accrual prior to this study opening.)
Pilot Study Evaluating Aprepitant (MK-869) for Prevention of Nausea & Vomiting Secondary to High Dose Cyclophosphamide Administered to Patients Underging Undergoing Peripheral Hematopoietic Progenitor Cell Mobilization Prior to Autologous Transplantation[NCT00293384]40 participants (Actual)Interventional2004-10-31Completed
A Randomized, Phase IV Trial of Individualized Care Versus Standard Care, in the Prevention of Chemotherapy Induced Nausea and Vomiting in Breast Cancer Patients. The EPIC Study[NCT01913990]Phase 4323 participants (Anticipated)Interventional2011-09-30Active, not recruiting
Aprepitant for the Relief of Nausea in Patients With Chronic Nausea and Vomiting of Presumed Gastric Origin: A Multicenter, Randomized, Double-Masked, Placebo-Controlled Trial[NCT01149369]Phase 2126 participants (Actual)Interventional2013-04-30Completed
THE EFFECT OF THE COMBINATION OF DEXAMETHASONE WITH ONDANSETRON VERSUS DEXAMETHASONE WITH APREPITANT TO PREVENT POSTOPERATIVE NAUSEA AND VOMITING IN PATIENTS UNDERGOING LAPAROSCOPIC SURGERY[NCT02021851]Phase 467 participants (Actual)Interventional2011-07-31Completed
Olanzapine Plus Fosaprepitant Standard Antiemetic Therapy in the Prevention of Chemotherapy-induced Nausea and Vomiting in Patients Receiving High Emetic Risk Multi-day Chemotherapy: a Multicenter, Randomized, Double-blind, Placebo-controlled, Phase 3 Stu[NCT04536558]Phase 3352 participants (Anticipated)Interventional2020-10-01Not yet recruiting
Aprepitant in the Management of Biological Therapies-related Severe Pruritus: a Pilot Study in 45 Cancer Patients[NCT01683552]Phase 245 participants (Actual)Interventional2010-09-30Completed
Ondanstron Weekly vs Every 3 Weeks for Prevention of Nausea and Vomiting Induced by Chemotherapy Combined With PD-1 Blockade:an Randomized Clinical Trial[NCT06080880]98 participants (Anticipated)Interventional2023-11-30Not yet recruiting
A Pilot Study to Evaluate the Efficacy of Fosaprepitant and Granisetron Transdermal System for the Prevention of Acute and Delayed Nausea and Vomiting in Breast Cancer Patients and to Identify Predictors of Response[NCT01649258]Phase 129 participants (Actual)Interventional2012-09-04Terminated(stopped due to Lack of Efficacy)
Modulation of Opiate Reward by NK1 Antagonism: A Laboratory-Based Proof of Concept Study[NCT00726960]Phase 160 participants (Anticipated)Interventional2008-01-31Active, not recruiting
Aprepitant in the Prevention of Cisplatin-induced Delayed Emesis: a Double-blind Randomized Trial[NCT00869310]Phase 3303 participants (Actual)Interventional2009-09-30Terminated(stopped due to we terminated the study before enrolling 303/560 due to a slow accrual)
Aprepitant vs. Desloratadine in Non-small Cell Lung Cancer Patients With Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors Related Pruritus: A Prospective, Randomized Control, Double-blinded, Phase II Clinical Trial[NCT02646020]Phase 2138 participants (Actual)Interventional2015-12-31Completed
Comparison of Aprepitant PO and Ondansetron IV for Prevention of Postoperative Nausea and Vomiting (PONV) in Patients Undergoing Orthognathic Surgery and General Anesthesia.[NCT00699894]0 participants (Actual)Interventional2008-06-30Withdrawn(stopped due to Logistical difficulties running the study)
A Proof-of-concept Clinical Trial Assessing the Safety of the Coordinated Undermining of Survival Paths by 9 Repurposed Drugs Combined With Metronomic Temozolomide (CUSP9v3 Treatment Protocol) for Recurrent Glioblastoma[NCT02770378]Phase 1/Phase 210 participants (Actual)Interventional2016-11-30Completed
Re-examination Study For General Drug Use to Assess the Safety and Efficacy Profile of EMEND in Usual Practice[NCT01074255]3,546 participants (Actual)Observational2007-04-30Completed
Pilot Study of Aprepitant Effect on Aldosterone Secretion in Diabetic Patient (Diabetes Mellitus) With Hypertension Associated With Low Renin[NCT02811055]Phase 220 participants (Anticipated)Interventional2017-07-13Recruiting
Compared With Fosaprepitant Dimeglumine for Injection and Palonosetron Hydrochloride Injection, to Evaluate the Efficacy and Safety of HR20013 for Injection for Prevention of Chemotherapy-induced Nausea and Vomiting After Highly Emetogenic Chemotherapy[NCT05509634]Phase 3754 participants (Actual)Interventional2022-09-21Completed
A Phase 1 Dose-Escalation Study of the Safety, Pharmacokinetics, and Pharmacodynamics of the Cyclin-Dependent Kinase (CDK) Inhibitor SCH 727965 Administered Every 3 Weeks in Subjects With Advanced Malignancies[NCT00871910]Phase 181 participants (Actual)Interventional2006-10-11Completed
Steroid-free Regimen With Aprepitant in Preventing Chemotherapy-induced Nausea and Vomiting in Patients With Colorectal Cancer Receiving FOLFOX Chemotherapy: a Randomized Phase 3 Trial[NCT02909478]Phase 3315 participants (Actual)Interventional2017-09-01Completed
A Pilot Study of Aprepitant Versus Ondansetron for the Treatment of Opioid Induced Nausea and Vomiting[NCT00499668]0 participants (Actual)Interventional2007-08-31Withdrawn(stopped due to slow accrual)
The Effect of Aprepitant Reducing Postoperative Nausea and Vomiting in Patients Undergoing Laparoscopic Gastric Sleeve Surgery[NCT05772676]Phase 4400 participants (Actual)Interventional2022-12-01Active, not recruiting
Aprepitant for the Prevention of Chemotherapy-induced Nausea and Vomiting Following High-dose Cisplatin in Nasopharyngeal Carcinoma Patients:a Randomized Phase 3 Trial[NCT02933099]Phase 3300 participants (Anticipated)Interventional2016-10-31Not yet recruiting
Mechanisms Underlying Hypotensive Response to ARB/NEP Inhibition - Aim 3[NCT04649229]Phase 480 participants (Anticipated)Interventional2021-05-27Recruiting
Pharmacological Treatment of Cannabis Withdrawal and Dependence[NCT01611948]Phase 270 participants (Actual)Interventional2011-05-31Completed
COMPARATIVE STUDY BETWEEN PALONOSETRON AND FOSAPREPITANT IN THE PROFILAXIA OF POSTOPERATIVE NAUSEA AND VOMITING IN WOMEN SUBMITTED TO VIDEOLAPAROSCOPIC COLECISTECTOMIES[NCT03586817]Phase 4100 participants (Anticipated)Interventional2019-03-02Recruiting
Comparison of Aprepitant vs. Gabapentin in the Prevention of Delayed Nausea and Vomiting[NCT00250744]Phase 2200 participants (Actual)Interventional2004-12-31Completed
A Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study, Conducted Under In-House Blinding Conditions, to Examine the Safety, Tolerability, and Efficacy of Aprepitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting Associated W[NCT00080444]Phase 350 participants (Actual)Interventional2004-04-30Completed
A Randomized, Double-Blind, Parallel-Group Study Conducted Under In-House Blinding Conditions to Determine the Safety, Tolerability and Efficacy of Aprepitant Regimen Compared to Ondansetron Regimen for the Prevention of Chemotherapy Induced Nausea and Vo[NCT00090207]Phase 4477 participants (Actual)Interventional2004-01-13Completed
A Randomized, Double-Blind, Active Comparator-Controlled, Parallel-Group Study, Conducted Under In-House Blinding Conditions, to Examine the Safety, Tolerability, and Efficacy of 2 Doses of Aprepitant for the Prevention of Postoperative Nausea and Vomitin[NCT00090246]Phase 3922 participants (Actual)Interventional2004-05-13Completed
A Study Evaluating the Efficacy and Safety of the Oral Neurokinin-1 Antagonist, Aprepitant, in Combination With Ondansetron and Dexamethasone in Patients Undergoing Autologous Peripheral Blood Stem Cell Transplantation[NCT00314743]Early Phase 148 participants (Actual)Interventional2005-10-31Completed
Open-label Extension to: A Randomized, Double-Blind, Parallel-Group Study Conducted Under In-House Blinding Conditions to Determine the Efficacy and Tolerability of Aprepitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting Associated With [NCT00092196]Phase 3820 participants (Actual)Interventional2002-12-01Completed
Comparative Study of Fosaprepitant and Aprepitant for the Prevention of Chemotherapy-induced Nausea and Vomiting in Pediatric Cancer Patients:A Superiority Design, Phase III Randomized Trial[NCT04873284]120 participants (Anticipated)Interventional2021-05-01Not yet recruiting
A Randomized, Double-Blind, Active Comparator-Controlled, Parallel-Group Study, Conducted Under In-House Blinding Conditions, to Examine the Safety, Tolerability, and Efficacy of 2 Doses of Aprepitant for the Prevention of Postoperative Nausea and Vomitin[NCT00090155]Phase 3805 participants (Actual)Interventional2003-09-26Completed
A Randomized, Double-Blind, Parallel-Group Study Conducted Under In-House Blinding Conditions to Determine the Efficacy and Tolerability of Aprepitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting Associated With Moderately Emetogenic Che[NCT00092183]Phase 4866 participants (Actual)Interventional2002-10-10Completed
A Pharmacokinetic Evaluation of the Addition of Aprepitant to the Bleomycin -Etoposide - Cisplatin (BEP) Treatment of Patients With Testis Carcinoma (A-BEP)[NCT00429754]Phase 40 participants (Actual)InterventionalWithdrawn(stopped due to change of study population and chemotherapeutic regimen)
Prevention of Delayed Nausea A Phase III Double-Blind Placebo-Controlled Clinical Trial[NCT00475085]Phase 31,021 participants (Actual)Interventional2006-12-31Completed
The Effect of Combining Aprepitant With Ondansetron in High-risk Patients for Postoperative Nausea and Vomiting[NCT01897337]Phase 4125 participants (Actual)Interventional2012-06-30Completed
A Randomized, Double-blind Comparison of Oral Aprepitant Alone vs Oral Aprepitant and Transdermal Scopolamine for Preventing Postoperative Nausea and Vomiting[NCT00717054]115 participants (Actual)Interventional2008-02-29Completed
A Pharmacokinetic Evaluation of the Addition of Aprepitant to the Cisplatin - Etoposide (CE) Treatment of Patients With Metastatic Lung Carcinoma (ACE).[NCT00588835]Phase 420 participants (Anticipated)Interventional2008-03-31Terminated
New Neural Drug Targets: An Evaluation of the Effects of Aprepitant on the Response to Oxycodone[NCT00999544]9 participants (Actual)Interventional2009-10-31Completed
A Phase Ib, Randomized, Placebo Controlled, Double Blind Study to Determine the Safety, Viral Suppression, Pharmacokinetics and Immune Modulatory Effects of Treatment With Aprepitant (Emend®) in HIV Infected Individuals[NCT00428519]Phase 130 participants (Actual)Interventional2007-01-31Completed
Clinical Laboratory Evaluations of Aprepitant for the Treatment of Opioid Dependence: Inpatient Test[NCT01527994]Phase 164 participants (Actual)Interventional2012-01-31Completed
To Assess the Efficacy and Safety of Ramosetron, Aprepitant and Dexamethasone Therapy vs Ondansetron, Aprepitant and Dexamethasone Therapy for Preventing of Nausea and Vomiting in Highly Emetogenic Chemotherapy (ROAD Study)[NCT01536691]Phase 3338 participants (Anticipated)Interventional2011-06-30Recruiting
A Double-Blind, Multicenter, Placebo and Active-Controlled, Acute Extension Study of 2 Doses of MK-0869 in the Treatment of Patients With Major Depressive Disorder[NCT00048607]Phase 3600 participants (Actual)Interventional2002-07-30Completed
A Double-Blind, Multicenter, Placebo Controlled, Acute and Extension Study of 2 Doses of MK0869 in the Treatment of Patients With Major Depressive Disorder[NCT00034944]Phase 3495 participants (Actual)Interventional2002-01-24Completed
A Worldwide, Multicenter, Double-Blind, Parallel, Active-Controlled, Long-Term Safety Study of MK0869 in Outpatients With Major Depressive Disorder[NCT00034983]Phase 3900 participants (Actual)Interventional2001-10-29Completed
A Double-Blind, Multicenter, Placebo-and Active-Controlled Acute and Extension Study of 2 Doses of MK-0869 in the Treatment of Patients With Major Depressive Disorder[NCT00035295]Phase 3584 participants (Actual)Interventional2001-11-08Completed
A Double-Blind, Multicenter, Placebo- and Active-Controlled Acute and Extension Study of MK0869 in the Treatment of Patients With Major Depressive Disorder With Melancholic Features[NCT00035009]Phase 3468 participants (Actual)Interventional2001-09-20Completed
A Double-Blind, Placebo-Controlled, Multicenter Study of the Long-Term Efficacy of MK0869 in the Maintenance of Antidepressant Effect in Geriatric Outpatients With Major Depressive Disorder[NCT00035048]Phase 3540 participants (Actual)Interventional2001-11-21Completed
A Double-Blind, Placebo- and Active-Controlled Acute and Extension Study of MK0869 in the Treatment of Patients With Major Depressive Disorder[NCT00035282]Phase 3450 participants (Actual)Interventional2001-09-30Completed
ONO-7436 Phase II Study - A Multicenter, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study to Examine the Efficacy and Safety of ONO-7436 for the Prevention of Cancer Chemotherapy-Induced Nausea and Vomiting in Japan[NCT00212602]Phase 2420 participants Interventional2005-08-31Completed
A Double-Blind, Multicenter, Placebo-Controlled Study of MK0869 in the Treatment of Patients With Major Depressive Disorder[NCT00042029]Phase 3324 participants (Actual)Interventional2002-06-18Completed
Aprepitant Versus Ondansetron in Preoperative Triple-therapy Treatment of Nausea and Vomiting[NCT01474915]Phase 4122 participants (Actual)Interventional2007-06-30Completed
A Double-Blind, Placebo-Controlled, Multicenter Study of the Long-Term Efficacy of MK0869 in the Maintenance of Antidepressant Effect in Patients With Major Depressive Disorder[NCT00048594]Phase 3800 participants (Actual)Interventional2002-01-03Completed
A Randomized, Double-blind Comparison of Oral Aprepitant Alone Versus Oral Aprepitant and Transdermal Scopolamine for Preventing Postoperative Nausea and Vomiting[NCT00659737]115 participants (Actual)Interventional2008-04-30Completed
ApRepitant in Combination With Granisetron and Dexamethasone versUs Granisetron and dexamEthasone for the Prevention of Vomiting in Patients With HAIC Therapy for Hepatocellular Carcinoma: a Randomized Controlled Study (ARGUE)[NCT05711823]Phase 3300 participants (Anticipated)Interventional2023-07-01Not yet recruiting
Phase 1/2 Investigator Sponsored Study of Selinexor in Combination With High-Dose Melphalan Before Autologous Hematopoietic Cell Transplantation for Multiple Myeloma[NCT02780609]Phase 1/Phase 222 participants (Actual)Interventional2017-07-20Completed
Influence of Antipruritics on the Dermal Blood Flow Response After a Histamine Skin Prick as Well as After the Topical Application of Cinnamaldehyde and Capsaicin[NCT04399148]13 participants (Actual)Interventional2019-06-11Completed
A Randomized, Double-Blind, Prospective Trial of Oral Administration of Aprepitant For Prevention of Post-Endoscopic Retrograde Cholangiopancreatography (ERCP) Pancreatitis[NCT00736073]73 participants (Actual)Interventional2007-08-31Completed
Aprepitant Versus Hydroxyzine in Association With Cytoreductive Treatments for Patients With Myeloproliferative Neoplasia Suffering From Persistent Aquagenic Pruritus.[NCT03808805]Phase 380 participants (Anticipated)Interventional2019-04-16Recruiting
A Phase 3 Clinical Study Protocol: A Prospective, Randomized, Placebo-Controlled, Double-Blind, Multicenter, Phase 3 Study of APF530 500 mg SC, Fosaprepitant 150 mg IV, and Dexamethasone vs. Ondansetron 0.15 mg/kg IV, Fosaprepitant 150 mg IV, and Dexameth[NCT02106494]Phase 3942 participants (Actual)Interventional2014-03-31Completed
Pilot Study on the Efficacy of an Ondansetron Versus Palonosetron-containing Antiemetic Regimen Prior to Highly Emetogenic Chemotherapy(HEC).[NCT01640340]40 participants (Actual)Interventional2011-01-31Completed
Efficacy of Pre-operative Aprepitant Plus Ondansetron vs Ondansetron Plus Placebo in Patients at Moderate-to-High Risk Post-operative Nausea (PONV) Undergoing Ambulatory Plastic Surgery[NCT00659945]Phase 4150 participants (Actual)Interventional2008-06-30Completed
AMENO-2: Fase IV Study, National, Multiple Centers, Competitive, Randomized, Double Blind, Controlled With Parallel Groups to Determinate the Security, Tolerability and Efficacy of Aprepitant Plus Palonosetron Versus Granisetron in the Prevention of Nause[NCT00415103]Phase 4196 participants (Anticipated)Interventional2006-11-30Completed
Granisetron Transdermal Delivery System Versus Palonosetron in the Prevention of Delayed Chemotherapy-induced Nausea and Vomiting: a Phase 3 Non-inferiority Randomized Trial[NCT04912271]Phase 3140 participants (Anticipated)Interventional2021-06-10Not yet recruiting
"Olanzapine for Prevention of Nausea and Vomiting in Children and Adolescents Receiving Highly Emetogenic Chemotherapy (HEC): An Investigator Initiated, Randomized, Open-label Trial (PRaCTiCE Trial: PRevention of ChemoTherapy Induced Emesis in Children)"[NCT03219710]Phase 3240 participants (Actual)Interventional2017-07-01Completed
Efficacy of Aprepitant (Emend®) in Children Receiving Highly Emetogenic Chemotherapy[NCT01661335]Phase 319 participants (Actual)Interventional2012-06-01Completed
EMEND® IV In Salvage Treatment of Chemotherapy-Induced Vomiting[NCT01405924]Phase 2111 participants (Actual)Interventional2011-10-25Terminated(stopped due to Low enrollment)
A Single Arm Study to Evaluate the Control of Chemotherapy Induced Nausea and Vomiting in Non-Hodgkin Lymphoma Patients Receiving R-CHOP.[NCT01843868]130 participants (Anticipated)Interventional2013-05-31Not yet recruiting
A Study to Evaluate the Efficacy of Anti-emetic Drug Aprepitant Upon the Combination Chemotherapy of Nedaplatin and Docetaxel for Non-small Cell Lung Cancer[NCT02364804]10 participants (Anticipated)Observational2012-04-30Completed
Postoperative Nausea and Vomiting: Ramosetron Plus Aprepitant vs Palonosetron Plus Aprepitant[NCT02597907]88 participants (Actual)Interventional2014-07-31Completed
A Randomized Open Label Phase II Trial of Aprepitant (Emend) in Combination With Ondansetron Compared to Standard 5HT3 Serotonin Antagonist (Ondansetron) in the Prevention of Acute and Delayed Chemotherapy Induced Nausea and Vomiting (CINV) in Glioma Pati[NCT01450826]Phase 2136 participants (Actual)Interventional2014-06-24Completed
Topical Aprepitant in Prurigo Patients An Exploratory Phase IIa Trial With Topically Applied Aprepitant in Patients With Prurigo[NCT01963793]Phase 220 participants (Actual)Interventional2013-10-31Completed
Effect of Neurokinin-1 Receptor (NK1R) Antagonism on Pruritus in Patients With Sezary Syndrome[NCT01625455]Phase 47 participants (Actual)Interventional2012-02-29Terminated(stopped due to Difficulty recruiting.)
Retrospective Comparison of the Effects of Granisetron and Aprepitant in the Prevention of Postoperative Nausea and Vomiting in Laparoscopic Abdominal Surgery[NCT05632224]Phase 460 participants (Anticipated)Interventional2022-11-24Not yet recruiting
Weekly Fosaprepitant for the Prevention of Nausea and Emesis During Concurrent Chemoradiotherapy for Nasopharyngeal Carcinoma: a Prospective Pilot Study[NCT04636632]Phase 1100 participants (Actual)Interventional2020-11-24Completed
[NCT01440673]150 participants (Actual)Interventional2010-03-31Completed
Pilot Study of Fosaprepitant (MK-0517) for Breakthrough Chemotherapy Induced Nausea and Vomiting[NCT01031953]Phase 1/Phase 234 participants (Actual)Interventional2008-08-31Terminated(stopped due to Drug contract timelines and inadequate enrollment)
Study to Evaluate the Anti-emetic Effect of Aprepitant as an add-on Therapy in Children and Adolescents Receiving AML Remission Induction Chemotherapy: An Investigator-initiated, Randomized, Open Label Trial[NCT02979548]Phase 3116 participants (Anticipated)Interventional2016-11-30Recruiting
Fosaprepitant Combined With Tropisetron Plus Dexamethasone in Preventing Nausea and Emesis During Fractionated Radiotherapy With Weekly Cisplatin Chemotherapy in Cervical Cancer and Nasopharyngeal Cancer[NCT05564286]Phase 3206 participants (Anticipated)Interventional2021-07-01Recruiting
A Phase IV Study Comparing the Efficacy of Fosaprepitant to Aprepitant for Chemotherapy Induced Nausea and Vomiting in Patients Treated for Gynecological Cancer[NCT01432015]Phase 420 participants (Actual)Interventional2011-09-30Completed
Dual-dose Aprepitant to Reduce Postoperative Nausea and Vomiting After Laparoscopic Bariatric Surgery: a Prospective, Randomised, Placebo-controlled, Triple-blind, Single Centre Trial.[NCT05189756]Phase 4224 participants (Anticipated)Interventional2022-03-17Recruiting
Human Behavioral Pharmacology Laboratory (HBPL) Study of the Impact of the NK1 Antagonist Aprepitant (Emend®) on Stress-Induced Cocaine and Alcohol Craving[NCT01176591]Phase 213 participants (Actual)Interventional2010-09-30Completed
Importance of Substance P in Intracranial Pressure Elevation Following Traumatic Brain Injury[NCT03035838]Early Phase 10 participants (Actual)Interventional2021-11-30Withdrawn(stopped due to Alternate study commenced using different drug)
Evaluation of Fosaprepitant's Effect on Drug Metabolism in Sarcoma Patients Receiving Ifosfamide-based Multi-day Chemotherapy Regimen[NCT01490060]47 participants (Actual)Interventional2012-05-31Completed
A Single-Center, Placebo-Controlled, Double-Blind Study to Evaluate the Effects of Aprepitant on Satiation, Gastric Volume, Gastric Accommodation and Gastric Emptying in Healthy Volunteers[NCT02989467]Phase 127 participants (Actual)Interventional2017-01-27Completed
Differentiating the Effects of Substance P and Beta-endorphin in the Perception of Breathlessness During Resistive Load Breathing in Patients With Chronic Obstructive Pulmonary Disease (COPD)[NCT01854177]10 participants (Actual)Interventional2013-07-31Completed
Pharmacological Treatment of Comorbid Alcohol and Marijuana Withdrawal and Dependence[NCT02210195]Phase 220 participants (Actual)Interventional2014-09-04Completed
Real-time Decision Support for Postoperative Nausea and Vomiting (PONV) Prophylaxis[NCT02625181]27,034 participants (Actual)Interventional2016-07-31Completed
Pilot Study of Standard Therapy for Prevention of Nausea and Emesis Associated With First Line Post-Operative Intraperitoneal Chemotherapy[NCT01275664]4 participants (Actual)Interventional2011-06-30Terminated(stopped due to Study terminated due to no patient population available)
A Phase II Open Label Study of Aprepitant as Antiemetic Prophylaxis in Patients With Acute Myeloid Leukemia Undergoing Induction Chemotherapy[NCT01334086]Phase 241 participants (Actual)Interventional2011-09-30Completed
A Korean Multicenter, Randomized, Double-Blind, Clinical Trial to Evaluate the Efficacy and Tolerability of Aprepitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting in the First Cycle of Moderately Emetogenic Chemotherapies (MEC, Non-AC R[NCT01636947]Phase 4494 participants (Actual)Interventional2012-12-12Completed
Efficacy and Safety Addition of Low Dose Olanzapine to the Standard Prophylaxis of Nausea and Vomiting Induced by Highly-emetogenic Chemotherapy in Children and Adolescents (OZONE-V)[NCT05346731]Phase 3210 participants (Anticipated)Interventional2022-04-01Recruiting
Olanzapine for the Prevention of Chemotherapy Induced Nausea and Vomiting (CINV) in Patients Receiving Highly Emetogenic Chemotherapy (HEC): A Randomized, Double-Blind, Placebo-Controlled Trial[NCT02116530]Phase 3401 participants (Actual)Interventional2014-08-31Completed
Fosaprepitant , Tropisetron and Olanzapine for the Prevention of Nausea and Vomiting in Patients With Breast Cancer Receiving Anthracycline/Cyclophosphamide-containing Chemotherapy[NCT05242874]Phase 3403 participants (Anticipated)Interventional2022-01-01Recruiting
Phase 2B Double Blind Placebo Controlled Crossover Study Evaluating the Efficacy of IV Fosaprepitant for Chemo Induced N/V With High Dose Interleukin 2 for Metastatic Melanoma and Metastatic Renal Cell Carcinoma[NCT01874119]Phase 213 participants (Actual)Interventional2013-09-30Terminated(stopped due to Enrollment issues)
Efficacy of Aprepitant for the Prevention of Chemotherapy-induced Nausea and Vomiting in Nondrinking Women Younger Than 50 Years Who Received Moderately Emetogenic Chemotherapy: A Randomized, Double-blind, Phase Ⅲ Trial[NCT03674294]Phase 3248 participants (Actual)Interventional2015-08-04Completed
A Feasibility Study to Discern the Tolerability of 5-FU/Gemcitabine Based Chemotherapy Concurrent With Upper Abdominal Radiation and the Utility of Aprepitant/5HT-3 Antagonist (EMEND) for the Prevention of ChemoRadiation-Induced Nausea and Vomiting (CRINV[NCT01534637]Phase 222 participants (Actual)Interventional2006-08-31Completed
A Pilot Study of Aprepitant vs. Placebo Combined With Standard Antiemetics for the Control of Nausea and Vomiting During Hematopoietic Cell Transplatation(HCT)[NCT00248547]40 participants (Actual)Interventional2004-05-31Completed
Self-control Trial to Evaluate the Role of Aprepitant in the Prophylaxis of Post-lumbar-punture-headache (PLPH)[NCT02347878]Phase 485 participants (Anticipated)Interventional2015-04-30Not yet recruiting
A Phase III, Randomized, Double-Blind, Active Comparator-Controlled Parallel-Group Study, Conducted Under In-House Blinding Conditions, to Examine the Efficacy and Safety of a Single 150 mg Dose of Intravenous Fosaprepitant Dimeglumine for the Prevention [NCT01594749]Phase 31,015 participants (Actual)Interventional2012-09-24Completed
Effect of the Association of Neurokinin-1 Receptor Antagonist Aprepitant to Dexamethasone/Ondansetron in the Incidence of Postoperative Nausea and Vomiting in High Risk Apfel Score Patients[NCT02357693]Phase 490 participants (Actual)Interventional2015-02-28Completed
A Comparison Study to Determine the Increased Efficacy of Adding EMEND to the Treatment Regimen for Post-Discharge and Post-Operative Nausea and Vomiting[NCT01186029]0 participants (Actual)Interventional2010-10-31Withdrawn(stopped due to It didn't get IRB approval.)
Aprepitant and Granisetron for the Prophylaxis of Radiation Induced Nausea and Vomiting - A Pilot Study[NCT01183481]Phase 219 participants (Actual)Interventional2011-01-31Terminated(stopped due to Study was stopped due to inadequate accrual.)
The Role of Substance P on Perception of Breathlessness[NCT01580423]16 participants (Actual)Interventional2012-04-30Completed
A Multi-Center, Trial to Evaluate the Efficacy & Tolerability of Aprepitant and Palonosetron for the Prevention of CINV in Colorectal Cancer (CRC) Patients Receiving FOLFOX[NCT00381862]Phase 254 participants (Actual)Interventional2006-06-30Completed
Phase II Study of Fosaprepitant + 5HT3 Receptor Antagonists + Dexamethasone in Patients With Germ Cell Tumors Undergoing 5 Day Cisplatin-based Chemotherapy: Hoosier Oncology Group Study QL12-153[NCT01736917]Phase 265 participants (Actual)Interventional2013-01-31Completed
The Effect of NK1R Antagonism on Alcohol Craving and PTSD Symptoms in Alcohol Dependent Patients With PTSD[NCT00896038]Phase 258 participants (Actual)Interventional2009-05-31Completed
Safety and Efficacy of Aprepitant, Ramosetron, and Dexamethasone for Chemotherapy-Induced Nausea and Vomiting in Patients With Ovarian Cancer Treated With Taxane/Carboplatin[NCT01012336]Phase 289 participants (Actual)Interventional2010-05-31Completed
A Randomized Study to Determine the Efficacy and Tolerability of Olanzapine for the Prevention of Chemotherapy-Induced Nausea and Vomiting in Chinese Breast Cancer Patients[NCT03079219]Phase 3120 participants (Actual)Interventional2017-03-23Completed
Prevention of Nausea and Vomiting Secondary to FOLFIRINOX Chemotherapy in Gastrointestinal Cancer Patients[NCT01504711]30 participants (Actual)Interventional2012-06-30Completed
A Phase III, Multicenter, Randomized, Double-blind, Unbalanced (3:1) Active Control Study to Assess the Safety and Describe the Efficacy of Netupitant and Palonosetron for the Prevention of Chemotherapy-induced Nausea and Vomiting in Repeated Chemotherapy[NCT01376297]Phase 3413 participants (Actual)Interventional2011-07-31Completed
Efficacy, Safety and Feasibility of Fosaprepitant for the Prevention of Chemotherapy-induced Nausea and Vomiting in Pediatric Patients With Solid Tumors Receiving Moderately and Highly Emetogenic Chemotherapy[NCT04508400]Phase 2108 participants (Anticipated)Interventional2021-09-01Not yet recruiting
Randomised, Double-blind, Dose-finding Phase II Study to Assess the Efficacy of APD403 in the Prevention of Nausea and Vomiting Caused by Cisplatin- or Anthracycline/Cyclophosphamide (AC)-Based Chemotherapy[NCT01857232]Phase 2342 participants (Actual)Interventional2013-10-31Completed
A Phase IIb, Partially-Blinded, Randomized, Active Comparator-Controlled Study to Evaluate the Pharmacokinetics/Pharmacodynamics, Safety, and Tolerability of Aprepitant in Pediatric Patients for the Prevention of Post Operative Nausea and Vomiting[NCT01732458]Phase 2229 participants (Actual)Interventional2013-02-12Completed
Effects of Rolapitant on Nausea/Vomiting in Patients With Sarcoma Receiving Multi-Day Highly Emetogenic Chemotherapy (HEC) With Doxorubicin and Ifosfamide Regimen (AI)[NCT02732015]Phase 237 participants (Actual)Interventional2016-10-12Terminated(stopped due to Terminated per PI's request)
A Pilot Study Comparing Olanzapine and Aprepitant for the Prevention of Chemotherapy Induced Nausea and Vomiting in Pediatric Patients Receiving Highly Emetogenic Chemotherapy[NCT02097823]Phase 215 participants (Actual)Interventional2014-02-28Completed
A Phase IIb, Partially-Blinded, Randomized, Active Comparator-Controlled Study to Evaluate the Pharmacokinetics/Pharmacodynamics, Safety, and Tolerability of Fosaprepitant in Pediatric Patients for the Prevention of Chemotherapy-Induced Nausea and Vomitin[NCT01697579]Phase 2240 participants (Actual)Interventional2012-12-13Completed
Aprepitant ,Olanzapine,Palonosetron and Dexamethasone for the Prevention of Chemotherapy-induced Nausea and Vomiting---A Randomized Single Center Phase III Trial[NCT02484911]Phase 3120 participants (Actual)Interventional2015-05-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00231777 (4) [back to overview]Number of Patients With Clinical Adverse Experiences (CAEs)
NCT00231777 (4) [back to overview]Number of Patients With Drug-related CAEs
NCT00231777 (4) [back to overview]Number of Patients With Laboratory Adverse Experiences (LAEs)
NCT00231777 (4) [back to overview]Number of Patients With Serious CAEs
NCT00248547 (1) [back to overview]Number of Emesis Free Participants During the Study Period.
NCT00293384 (4) [back to overview]Overall Nausea Controlled
NCT00293384 (4) [back to overview]Delayed Vomiting Controlled
NCT00293384 (4) [back to overview]Proportion of Participants With Controlled Acute Vomiting
NCT00293384 (4) [back to overview]Toxicity Grade 3, 4, or 5
NCT00337727 (2) [back to overview]Number of Patients Who Reported No Vomiting
NCT00337727 (2) [back to overview]Number of Patients Who Reported Complete Response
NCT00381862 (1) [back to overview]Number of Participants With no Emesis and no Rescue Therapy Within 5 Days of Receiving FOLFOX and FOLFIRI in the First Cycle of Chemotherapy.
NCT00475085 (1) [back to overview]Home Record: Severity of Delayed Nausea
NCT00572572 (6) [back to overview]Proportion of Patients With no Emesis During the Acute CINV Time Period (Cycle Days 1-5)
NCT00572572 (6) [back to overview]Preferred Treatment Cycle
NCT00572572 (6) [back to overview]Visual Analouge (VAS) 100mm Scale Score
NCT00572572 (6) [back to overview]Proportion of Patients With no Emesis During the Delayed CINV Time Period (Cycle Days 6-8)
NCT00572572 (6) [back to overview]Complete Response.
NCT00572572 (6) [back to overview]MD Anderson Symptom Inventory Score
NCT00600353 (4) [back to overview]Overall Emetic Response
NCT00600353 (4) [back to overview]Overall Emetic Response: Acute
NCT00600353 (4) [back to overview]Overall Emetic Response: Extended
NCT00600353 (4) [back to overview]Overall Emetic Response: Delayed
NCT00619359 (3) [back to overview]No Vomiting Overall (in the 120 Hours Following Initiation of Cisplatin)
NCT00619359 (3) [back to overview]A Complete Response (no Vomiting and no Use of Rescue Therapy) Overall (in the 120 Hours Following Initiation of Cisplatin).
NCT00619359 (3) [back to overview]A Complete Response (no Vomiting and no Use of Rescue Therapy) in the Delayed Phase (25 to 120 Hours Following Initiation of Cisplatin).
NCT00651755 (6) [back to overview]Geometric Mean Area Under Curve (AUC) of Analyte, Vincristine (VC), in Aprepitant Treatment and Control Group
NCT00651755 (6) [back to overview]Geometric Mean Area Under Curve (AUC) of Analyte,Prednisone (PR), in Aprepitant Treatment and Control Group
NCT00651755 (6) [back to overview]Geometric Mean Area Under Curve (AUC) of Analyte, Prednisolone (PL), in Aprepitant Treatment and Control Group
NCT00651755 (6) [back to overview]Geometric Mean Area Under Curve (AUC) of Analyte, Cyclophosphamide (CP), in Aprepitant Treatment and Control Group
NCT00651755 (6) [back to overview]Geometric Mean Area Under Curve (AUC) of Analyte, 4-hydroxy-cyclophosphamide (4-OH-CP), in Aprepitant Treatment and Control Group
NCT00651755 (6) [back to overview]Geometric Mean Area Under Curve (AUC) of Analyte, 2-dechloro-cyclophosphamide(2-deCI-CP), in Aprepitant Treatment and Control Group
NCT00659737 (1) [back to overview]Number of Participants With Postoperative Nausea and Vomiting
NCT00659945 (1) [back to overview]Number of Participants Having Post-operative Emesis and Nausea.
NCT00711555 (5) [back to overview]Complete Protection
NCT00711555 (5) [back to overview]Complete Response (Percentage of Patients)
NCT00711555 (5) [back to overview]no Emesis
NCT00711555 (5) [back to overview]no Nausea
NCT00711555 (5) [back to overview]no Significant Nausea
NCT00717054 (4) [back to overview]Number of Participants With Nausea and Vomiting
NCT00717054 (4) [back to overview]Number of Participants With Nausea and Vomiting in PACU
NCT00717054 (4) [back to overview]Total Vomiting
NCT00717054 (4) [back to overview]Need for Antiemetic Medication
NCT00734929 (12) [back to overview]Cumulative Incidence of Emesis
NCT00734929 (12) [back to overview]Average Nausea Score
NCT00734929 (12) [back to overview]Incidence of Vomiting (Post OP)
NCT00734929 (12) [back to overview]"Number of Participants Who Rated Their Satisfaction With Antiemetic Management as Very Satisfied"
NCT00734929 (12) [back to overview]Number of Vomiting Episodes
NCT00734929 (12) [back to overview]Incidence of Vomiting (24 Hours)
NCT00734929 (12) [back to overview]Time to First Vomiting
NCT00734929 (12) [back to overview]Use of Rescue Antiemetics (24 Hours)
NCT00734929 (12) [back to overview]Use of Rescue Antiemetics (48 Hours)
NCT00734929 (12) [back to overview]Use of Rescue Antiemetics (Post OP)
NCT00734929 (12) [back to overview]Incidence of Nausea
NCT00734929 (12) [back to overview]Number of Participants With a Complete Response Rate
NCT00736073 (2) [back to overview]Number of Participants Who Were Hospitalized Within 7 Days Post-ERCP for Abdominal Pain That Did Not Meet Criteria for Acute Pancreatitis
NCT00736073 (2) [back to overview]Number of Post-ERCP Pancreatitis Cases in Participants Who Are Administered Aprepitant and Placebo Prior to ERCP and One Day After ERCP:Assess the Total Number of Incidents of Post-ERCP Pancreatitis in Each Group (Treatment and Control).
NCT00818259 (8) [back to overview]Number of Participants Discontinuing Study Drug Due to an AE
NCT00818259 (8) [back to overview]Apparent Terminal Half-life (t1/2) for Aprepitant
NCT00818259 (8) [back to overview]Area Under the Time-Concentration Curve From 0 to 24 Hours (AUC 0-24hr) for Aprepitant
NCT00818259 (8) [back to overview]Tmax for Fosaprepitant
NCT00818259 (8) [back to overview]Cmax for Fosaprepitant
NCT00818259 (8) [back to overview]Maximum Plasma Concentration (Cmax) for Aprepitant
NCT00818259 (8) [back to overview]Time to Cmax (Tmax) for Aprepitant
NCT00818259 (8) [back to overview]Number of Participants Experiencing Adverse Events (AEs)
NCT00819039 (12) [back to overview]Number of Participants Discontinuing Study Treatment Due to AEs
NCT00819039 (12) [back to overview]Number of Participants Experiencing Adverse Events (AEs)
NCT00819039 (12) [back to overview]Number of Participants With Complete Response Up to 24 Hours Following Surgery in Study Part 2
NCT00819039 (12) [back to overview]Number of Participants With No Vomiting Up to 24 Hours Following Surgery in Study Part 2
NCT00819039 (12) [back to overview]Number of Participants With No Vomiting Up to 48 Hours Following Surgery Ini Study Part 2
NCT00819039 (12) [back to overview]Area Under the Curve From 0-48 (AUC0-48) of Aprepitant Following a Single Oral Dose in Study Part 1
NCT00819039 (12) [back to overview]Maximum Plasma Concentration (Cmax) of Aprepitant Following a Single Oral Dose in Study Part 1
NCT00819039 (12) [back to overview]Number of Participants With Vomiting Frequency in Study Part 2
NCT00819039 (12) [back to overview]Plasma Concentration of Aprepitant at 24 Hours (C24 hr) Following a Single Oral Dose in Study Part 1
NCT00819039 (12) [back to overview]Plasma Concentration of Aprepitant at 48 Hours (C48 hr) Following a Single Oral Dose in Study Part 1
NCT00819039 (12) [back to overview]Time to Maximum Plasma Concentration (Tmax) of Aprepitant Following a Single Oral Dose in Study Part 1
NCT00819039 (12) [back to overview]Number of Participants With Complete Response Up to 48 Hours Following Surgery in Study Part 2
NCT00888329 (1) [back to overview]Number of Participants With Emesis
NCT00895245 (4) [back to overview]Rate of Complete Response to Anti-emetic Therapy in the Delayed Setting (25-120 Hours After Cisplatin Infusion)
NCT00895245 (4) [back to overview]Proportion of Patients With a Complete Response to the Anti-emetic Medication Regimen
NCT00895245 (4) [back to overview]Impact of Cisplatin-induced Nausea and Vomiting on Daily Life During the 5 Day Period Following Cisplatin Infusion for Multiple Cycles as Measured by the Functional Living Index-Emesis Questionnaire
NCT00895245 (4) [back to overview]Control of Nausea for 120 Hours Following Each Cisplatin Infusion for Multiple Cycles of Therapy as Measured by the Visual Analog Scale
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Stress Script
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Stress Script
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Stress Script
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Stress Script
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Stress Script
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Stress Script
NCT00896038 (17) [back to overview]PTSD Total Symptom Severity Score
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Alcohol Cue Script
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Alcohol Cue Script
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Stress Script
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Stress Script
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Alcohol Cue Script
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Alcohol Cue Script
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Alcohol Cue Script
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Alcohol Cue Script
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Alcohol Cue Script
NCT00896038 (17) [back to overview]Alcohol Craving in Response to the Alcohol Cue Script
NCT00945321 (2) [back to overview]Area Under the Curve (AUC(0 to Infinity)) Following Single Dose Administration of Aprepitant 165 mg or 185 mg and Fosaprepitant 150 mg
NCT00945321 (2) [back to overview]Peak Plasma Concentration (Cmax) Following Single Dose Administration of Aprepitant 165 mg or 185 mg and Fosaprepitant 150 mg.
NCT00952341 (8) [back to overview]Time to First Vomiting Episode in Cycle 1
NCT00952341 (8) [back to overview]Proportion of Participants With Complete Response 120 Hours Following Initiation of High-dose Cisplatin Chemotherapy in the Overall Phase of Cycle 1
NCT00952341 (8) [back to overview]Proportion of Participants With Complete Response in the Acute Phase of Cycle 1
NCT00952341 (8) [back to overview]Proportion of Participants With Complete Response in the Delayed Phase of Cycle 1
NCT00952341 (8) [back to overview]Proportion of Participants With No Impact on Daily Life in Cycle 1
NCT00952341 (8) [back to overview]Proportion of Participants With No Vomiting in the Acute Phase of Cycle 1
NCT00952341 (8) [back to overview]Proportion of Participants With No Vomiting in the Delayed Phase of Cycle 1
NCT00952341 (8) [back to overview]Proportion of Participants With No Vomiting in the Overall Phase of Cycle 1
NCT00954941 (2) [back to overview]Treatment Success Rate
NCT00954941 (2) [back to overview]Participant Responses
NCT00990821 (1) [back to overview]Area Under the Plasma-Time Curve (AUC[0 to Infinity]) for Aprepitant and MK-0517 for Study Part V
NCT00999544 (2) [back to overview]Respiration Depression
NCT00999544 (2) [back to overview]Abuse Liability Proxy
NCT01012336 (1) [back to overview]Efficacy of the Aprepitant/Ramosetron/Dexamethasone Regimen in Terms of the Proportion of Patients With a Complete Response (CR) During the 120 Hour Following Initiation of Chemotherapy.
NCT01031953 (8) [back to overview]Participants With Specific Side Effects, Including Pain Sensation/Soreness at the Infusion Site, Headache, and Dizziness
NCT01031953 (8) [back to overview]Improvement in Nausea Score From 2 Hours to 24 Hours
NCT01031953 (8) [back to overview]Improvement in Nausea Score From Baseline to 2 Hours as Assessed by the Numerical Visual Analogue Scale
NCT01031953 (8) [back to overview]Number of Participants Who Experienced Vomiting Episodes From Baseline to 24 Hours
NCT01031953 (8) [back to overview]Participants Achieving a Complete Response (no Emesis, no Additional Rescue Medication Required)
NCT01031953 (8) [back to overview]Improvement in Nausea Score From Baseline to 12 Hours
NCT01031953 (8) [back to overview]Participants Who Required the Use of Second Rescue Drug (Time to Treatment Failure)
NCT01031953 (8) [back to overview]Participants With Increased Fatigue or Sedation Within 24 Hours After Receiving Fosaprepitant
NCT01074255 (1) [back to overview]Investigator Global Assessment of Participants' Response to Therapy With EMEND (Aprepitant) for the Prevention of Acute and Delayed Nausea Following Chemotherapy
NCT01111851 (4) [back to overview]Brain NK1-receptor Occupancy at 120 Hours Post Dose
NCT01111851 (4) [back to overview]Brain NK1-receptor Occupancy at 48 Hours Post Dose
NCT01111851 (4) [back to overview]Brain NK1-receptor Occupancy at 24 Hours Post Dose
NCT01111851 (4) [back to overview]Brain NK1-receptor Occupancy at the Time of the Maximum Concentration (Tmax)
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Heartburn During the Day Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Heartburn When Lying Down Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Loss of Appetite Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Lower Abdominal Discomfort Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Lower Abdominal Pain Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Nausea Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Nausea/Vomiting Severity Subscore
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Regurgitation During the Day Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Regurgitation When Lying Down Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Retching Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Stomach Distention Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Stomach Fullness Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Unable to Finish Meal Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Upper Abdominal Discomfort Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Upper Abdominal Pain Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Upper Abdominal Pain Subscore
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Vomiting Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity: Bitter Taste Severity
NCT01149369 (80) [back to overview]Platelet Count
NCT01149369 (80) [back to overview]Potassium
NCT01149369 (80) [back to overview]Red Blood Cell Count (RBC)
NCT01149369 (80) [back to overview]Satiety Test, Volume Consumed
NCT01149369 (80) [back to overview]Sodium
NCT01149369 (80) [back to overview]State-Trait Anxiety Inventory (STAI): State Anxiety Score
NCT01149369 (80) [back to overview]State-Trait Anxiety Inventory (STAI): Trait Anxiety Score
NCT01149369 (80) [back to overview]White Blood Cell Count (WBC)
NCT01149369 (80) [back to overview]Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Upper Abdominal Pain Severity
NCT01149369 (80) [back to overview]Beck Depression Inventory (BDI) Score
NCT01149369 (80) [back to overview]Blood Urea Nitrogen (BUN)
NCT01149369 (80) [back to overview]Brief Pain Inventory: Interference Score
NCT01149369 (80) [back to overview]Brief Pain Inventory: Severity Score
NCT01149369 (80) [back to overview]Calcium
NCT01149369 (80) [back to overview]Carbon Dioxide
NCT01149369 (80) [back to overview]Chloride
NCT01149369 (80) [back to overview]Clinical Global Patient Impression Score (Patient-rated)
NCT01149369 (80) [back to overview]Creatinine
NCT01149369 (80) [back to overview]Electrogastrography (EGG): Bradygastria (1-<2.5 Cpm) at 4 Weeks, 0-30 Post-satiety Measurement
NCT01149369 (80) [back to overview]Electrogastrography (EGG): Bradygastria (1-<2.5 Cpm) at 4 Weeks, Baseline Measurement
NCT01149369 (80) [back to overview]Electrogastrography (EGG): Duodenal (>10-15 Cpm) at 4 Weeks, 0-30 Post-satiety Measurement
NCT01149369 (80) [back to overview]Electrogastrography (EGG): Duodenal (>10-15 Cpm) at 4 Weeks, Baseline Measurement
NCT01149369 (80) [back to overview]Electrogastrography (EGG): Normogastria (2.5-<3.8 Cpm) at 4 Weeks, 0-30 Post-satiety Measurement
NCT01149369 (80) [back to overview]Electrogastrography (EGG): Normogastria (2.5-<3.8 Cpm) at 4 Weeks, Baseline Measurement
NCT01149369 (80) [back to overview]Electrogastrography (EGG): Tachygastria (3.8-10 Cpm) at 4 Weeks, 0-30 Post-satiety Measurement
NCT01149369 (80) [back to overview]Electrogastrography (EGG): Tachygastria (3.8-10 Cpm) at 4 Weeks, Baseline Measurement
NCT01149369 (80) [back to overview]Gastrointestinal Symptom Rating Scale (GSRS): Abdominal Pain Score
NCT01149369 (80) [back to overview]Gastrointestinal Symptom Rating Scale (GSRS): Constipation Score
NCT01149369 (80) [back to overview]Gastrointestinal Symptom Rating Scale (GSRS): Diarrhea Score
NCT01149369 (80) [back to overview]Gastrointestinal Symptom Rating Scale (GSRS): Indigestion Score
NCT01149369 (80) [back to overview]Gastrointestinal Symptom Rating Scale (GSRS): Reflux Score
NCT01149369 (80) [back to overview]Gastrointestinal Symptom Rating Scale (GSRS): Total Score
NCT01149369 (80) [back to overview]Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Bloating Severity
NCT01149369 (80) [back to overview]Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Early Satiety Severity
NCT01149369 (80) [back to overview]Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Excessive Fullness Severity
NCT01149369 (80) [back to overview]Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): GCSI Total Score
NCT01149369 (80) [back to overview]Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Nausea (Hours)
NCT01149369 (80) [back to overview]Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Nausea Severity
NCT01149369 (80) [back to overview]Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Overall Symptom Severity
NCT01149369 (80) [back to overview]Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Retching (No. Episodes)
NCT01149369 (80) [back to overview]Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Vomiting (No. Episodes)
NCT01149369 (80) [back to overview]Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Vomiting Severity
NCT01149369 (80) [back to overview]Glucose
NCT01149369 (80) [back to overview]Hematocrit
NCT01149369 (80) [back to overview]Hemoglobin
NCT01149369 (80) [back to overview]Hemoglobin A1c (HbA1c)
NCT01149369 (80) [back to overview]Liver Enzymes and Proteins: Alanine Aminotransferase (ALT)
NCT01149369 (80) [back to overview]Liver Enzymes and Proteins: Albumin
NCT01149369 (80) [back to overview]Liver Enzymes and Proteins: Aspartate Aminotransferase (AST)
NCT01149369 (80) [back to overview]Liver Enzymes and Proteins: Total Protein
NCT01149369 (80) [back to overview]Magnesium
NCT01149369 (80) [back to overview]Number of Participants With Improvement in Nausea
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Bloating Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Bloating Subscore
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Chest Discomfort During Sleep Time Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Chest Discomfort During the Day Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Constipation Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Diarrhea Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Excessive Fullness Severity
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Fullness/Early Satiety Subscore
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: Gastroparesis Cardinal Symptom Index (GCSI) Score
NCT01149369 (80) [back to overview]PAGI-SYM Severity Index: GERD Subscore
NCT01176591 (6) [back to overview]Alcohol Craving as Measured by the Visual Analog Scale (VAS) 1
NCT01176591 (6) [back to overview]Alcohol Craving as Measured by the Visual Analog Scale (VAS) 2
NCT01176591 (6) [back to overview]Cocaine Craving as Measured on the Visual Analog Scale (VAS) 1
NCT01176591 (6) [back to overview]Cocaine Craving as Measured on the Visual Analog Scale (VAS) 2
NCT01176591 (6) [back to overview]Multiple Choice Procedure (MCP) 1
NCT01176591 (6) [back to overview]Multiple Choice Procedure (MCP) 2
NCT01183481 (5) [back to overview]Control Rate of Delayed Phase Nausea, Vomiting, and Retching in Patients Undergoing Multiple Fraction Radiotherapy
NCT01183481 (5) [back to overview]Control Rate of Delayed Phase Nausea, Vomiting, and Retching in Patients Undergoing Single Fraction Radiotherapy
NCT01183481 (5) [back to overview]Control Rate of Acute Phase Nausea, Vomiting, and Retching in Patients Undergoing Single Fraction Radiotherapy
NCT01183481 (5) [back to overview]Control Rate of Acute Phase Nausea, Vomiting, and Retching in Patients Undergoing Multiple Fraction Radiotherapy
NCT01183481 (5) [back to overview]The Proportion of Patients Experiencing no Vomiting and no Nausea, Without Use of Any Rescue Antiemetic Medication(s), From Days 2-10 Following the Radiation Therapy (Delayed RINV).
NCT01275664 (2) [back to overview]Frequency of Adverse Effects as Assessed by the NCI CTCAE v 4.0
NCT01275664 (2) [back to overview]Number of Participants With Complete Control Defined as no Vomiting and no Use of Rescue Medications (for Nausea or Emesis)
NCT01298193 (9) [back to overview]Number of Participants With Complete Response (CR) in Cycle 2 for Patient Without Complete Response in Cycle 1
NCT01298193 (9) [back to overview]Total Impact of Chemotherapy-Induced Nausea and Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2
NCT01298193 (9) [back to overview]Impact of Chemotherapy-Induced Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2
NCT01298193 (9) [back to overview]Total Impact of Chemotherapy-Induced Nausea and Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1
NCT01298193 (9) [back to overview]Impact of Chemotherapy-Induced Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1
NCT01298193 (9) [back to overview]Impact of Chemotherapy-Induced Nausea on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2
NCT01298193 (9) [back to overview]Impact of Chemotherapy-Induced Nausea on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1
NCT01298193 (9) [back to overview]Number of Participants With Treatment Related Adverse Events (AE) at Cycle 2
NCT01298193 (9) [back to overview]Number of Participants With Complete Response (CR)
NCT01334086 (5) [back to overview]Percentage of Participants With Incidence of Vomiting/Retching From Day 1 Through End of Day 5
NCT01334086 (5) [back to overview]Percentage of Patients' Use of Supplemental Anti-emetics as Determined by the Total Number of Doses Per Day and in Total, From Days 1-8.
NCT01334086 (5) [back to overview]Daily Number of Vomiting or Retching Incidents From Days 1-8
NCT01334086 (5) [back to overview]Percentage of Patients Experiencing Nausea From Days 1-8.
NCT01334086 (5) [back to overview]Percentage of Participants Experiencing Vomiting or Retching From Days 1-8.
NCT01362530 (4) [back to overview]Percentage of Participants With a Complete Response in the Overall Phase of Cycle 1
NCT01362530 (4) [back to overview]Percentage of Participants With a Complete Response in the Delayed Phase of Cycle 1
NCT01362530 (4) [back to overview]Percentage of Participants With No Vomiting in the Overall Phase of Cycle 1
NCT01362530 (4) [back to overview]Percentage of Participants With a Complete Response in the Acute Phase of Cycle 1
NCT01376297 (1) [back to overview]Percentage of Patients With Adverse Events
NCT01405924 (6) [back to overview]Percentage of Participants With No Vomiting and No Retching During Cycle 2 of Chemotherapy
NCT01405924 (6) [back to overview]Percentage of Participants With No Significant Nausea During Cycle 2 of Chemotherapy
NCT01405924 (6) [back to overview]Percentage of Participants With a Complete Response During Cycle 2 of Chemotherapy
NCT01405924 (6) [back to overview]Percentage of Participants Who Used No Rescue Medication During Cycle 2 of Chemotherapy
NCT01405924 (6) [back to overview]Percentage of Participants With No Vomiting and No Retching During Cycle 2 of Chemotherapy Per Type of Chemotherapy
NCT01405924 (6) [back to overview]Functional Living Index - Emesis (FLIE) Total Score During Cycle 2 of Chemotherapy
NCT01432015 (2) [back to overview]Overall Complete Response Rate
NCT01432015 (2) [back to overview]Impact on Daily Living Activities
NCT01450826 (4) [back to overview]Patient's Global Satisfaction With the Antiemetic Regimen
NCT01450826 (4) [back to overview]Proportion of Patients Achieving Complete Control (CC)
NCT01450826 (4) [back to overview]Time to Treatment Failure
NCT01450826 (4) [back to overview]Proportion of Patients Achieving an Acute and Delayed Complete Response (CR)
NCT01474915 (2) [back to overview]Post Operative Nausea and Vomiting (PONV) Scores on a Verbal Response Scale
NCT01474915 (2) [back to overview]Proportion of Patients With a Complete Response/Complete Control During the First 24 Hours After Neurological Surgery Under General Anesthesia
NCT01490060 (1) [back to overview]Complete Response
NCT01504711 (4) [back to overview]Overall Survival
NCT01504711 (4) [back to overview]Percentage of Participants With Control of Vomiting and Rescue Medication Control
NCT01504711 (4) [back to overview]Percentage of Participants With Control of Both Acute and Delayed Vomiting
NCT01504711 (4) [back to overview]Percentage of Participants With Control of Both Acute and Delayed Nausea
NCT01534637 (3) [back to overview]Number of Patients With Gastrointestinal Toxicities (Grade 3 and 4 Nausea and Vomiting) Associated With Delivering Fluorouracil/Gemcitabine Hydrochloride-based Chemotherapy With Upper Abdominal Radiation
NCT01534637 (3) [back to overview]Impact of Aprepitant/5HT-3 Antagonist Therapy on the Patient Quality of Life as Measured by the Number of Patients Taking Anti Nausea Drugs
NCT01534637 (3) [back to overview]Impact of Aprepitant/5HT-3 Antagonist Therapy on the Patient Quality of Life as Measured by the Number of Patients Using Anti Nausea Drugs
NCT01580423 (3) [back to overview]Intensity of Breathlessness
NCT01580423 (3) [back to overview]Intensity of Pain
NCT01580423 (3) [back to overview]Unpleasantness of Breathlessness
NCT01594749 (6) [back to overview]Percentage of Participants With Severe Infusion-site Reactions
NCT01594749 (6) [back to overview]Percentage of Participants With Complete Response From 0 to 120 Hours After Initiation of MEC
NCT01594749 (6) [back to overview]Percentage of Participants With No Vomiting From 0 to 120 Hours After Initiation of MEC
NCT01594749 (6) [back to overview]Percentage of Participants With Infusion-site Thrombophlebitis
NCT01594749 (6) [back to overview]Percentage of Participants With Complete Response From 0 to 24 Hours After Initiation of MEC
NCT01594749 (6) [back to overview]Percentage of Participants With Complete Response From 25 to 120 Hours After Initiation of Moderately Emetogenic Chemotherapy (MEC)
NCT01611948 (1) [back to overview]Change From Week 0 in Cannabis Use Using Urinary CN-THCCOOH Levels at Week 8
NCT01625455 (2) [back to overview]Quality of Life
NCT01625455 (2) [back to overview]Severity of Pruritus
NCT01636947 (8) [back to overview]Number of Participants With No Use of a Rescue Therapy - Overall, Acute, and Delayed Stages
NCT01636947 (8) [back to overview]Percentage of Participants With a Complete Response - Overall, Acute, and Delayed Stages
NCT01636947 (8) [back to overview]Percentage of Participants With No Vomiting - Acute and Delayed Stages
NCT01636947 (8) [back to overview]Number of Emetic Events - Overall Stage
NCT01636947 (8) [back to overview]Percentage of Participants With No Impact on Daily Life - Overall Stage
NCT01636947 (8) [back to overview]Percentage of Participants With No Vomiting and No Significant Nausea - Overall Stage
NCT01636947 (8) [back to overview]Percentage of Participants With One or More Clinical Adverse Event
NCT01636947 (8) [back to overview]The Percentage of Participants With No Vomiting - Overall Stage
NCT01640340 (6) [back to overview]Delayed CR (Complete Response)
NCT01640340 (6) [back to overview]Use of Rescue Medication for Each Treatment Arm
NCT01640340 (6) [back to overview]Acute CR (Complete Response)
NCT01640340 (6) [back to overview]Overall CR(Complete Response)After the First Course of HEC, Defined as no Emesis and no Use of Rescue Medication
NCT01640340 (6) [back to overview]Percentage of Patients Who Experienced Grade 1, 2 or 3 Nausea From Time 0 to 120 Hours
NCT01640340 (6) [back to overview]Percentage of Patients Who Experienced Grade 1, 2 or 3 Vomiting From Time 0 to 120 Hours
NCT01697579 (33) [back to overview]Area Under the Concentration-time Curve of Aprepitant From Time 0 to Infinity (AUC 0-∞) in Participants 0 to <2 Years of Age
NCT01697579 (33) [back to overview]Area Under the Concentration-time Curve of Aprepitant From Time 0 to 24 Hours (AUC 0-24hr) in Participants 0 to <2 Years of Age
NCT01697579 (33) [back to overview]Apparent Total Body Clearance (CL/F) of Aprepitant in Participants 0 to <2 Years of Age
NCT01697579 (33) [back to overview]Apparent Terminal Half-life (t1/2) of Aprepitant in Participants 0 to <2 Years of Age
NCT01697579 (33) [back to overview]C24hr of Aprepitant in Participants 6 to <12 Years of Age
NCT01697579 (33) [back to overview]AUC 0-24hr of Aprepitant in Participants 6 to <12 Years of Age
NCT01697579 (33) [back to overview]C24hr of Aprepitant in Participants 12 to 17 Years of Age
NCT01697579 (33) [back to overview]Cmax of Aprepitant in Participants 2 to <6 Years of Age
NCT01697579 (33) [back to overview]C48hr of Aprepitant in Participants 2 to <6 Years of Age
NCT01697579 (33) [back to overview]Cmax of Aprepitant in Participants 6 to <12 Years of Age
NCT01697579 (33) [back to overview]Concentration of Aprepitant After 24 Hours (C24hr) in Participants 0 to <2 Years of Age
NCT01697579 (33) [back to overview]Concentration of Aprepitant After 48 Hours (C48hr) in Participants 0 to <2 Years of Age
NCT01697579 (33) [back to overview]CL/F of Aprepitant in Participants 12 to 17 Years of Age
NCT01697579 (33) [back to overview]Maximum Concentration (Cmax) of Aprepitant in Participants 0 to <2 Years of Age
NCT01697579 (33) [back to overview]Percentage of Participants Who Experienced at Least One Adverse Event (AE) in Cycle 1
NCT01697579 (33) [back to overview]Percentage of Participants Who Experienced at Least One Adverse Event (AE) in Cycles 2-6
NCT01697579 (33) [back to overview]t1/2 of Aprepitant in Participants 12 to 17 Years of Age Hours
NCT01697579 (33) [back to overview]t1/2 of Aprepitant in Participants 2 to <6 Years of Age
NCT01697579 (33) [back to overview]C24hr of Aprepitant in Participants 2 to <6 Years of Age
NCT01697579 (33) [back to overview]AUC 0-24hr of Aprepitant in Participants 12 to 17 Years of Age
NCT01697579 (33) [back to overview]AUC 0-∞ of Aprepitant in Participants 6 to <12 Years of Age
NCT01697579 (33) [back to overview]AUC 0-∞ of Aprepitant in Participants 2 to <6 Years of Age
NCT01697579 (33) [back to overview]t1/2 of Aprepitant in Participants 6 to <12 Years of Age
NCT01697579 (33) [back to overview]Time to Maximum Concentration (Tmax) of Aprepitant in Participants 0 to <2 Years of Age
NCT01697579 (33) [back to overview]Tmax of Aprepitant in Participants 12 to 17 Years of Age
NCT01697579 (33) [back to overview]C48hr of Aprepitant in Participants 6 to <12 Years of Age
NCT01697579 (33) [back to overview]Tmax of Aprepitant in Participants 6 to <12 Years of Age
NCT01697579 (33) [back to overview]AUC 0-∞ of Aprepitant in Participants 12 to 17 Years of Age
NCT01697579 (33) [back to overview]AUC 0-24hr of Aprepitant in Participants 2 to <6 Years of Age
NCT01697579 (33) [back to overview]CL/F of Aprepitant in Participants 2 to <6 Years of Age
NCT01697579 (33) [back to overview]CL/F of Aprepitant in Participants 6 to <12 Years of Age
NCT01697579 (33) [back to overview]Cmax of Aprepitant in Participants 12 to 17 Years of Age
NCT01697579 (33) [back to overview]Tmax of Aprepitant in Participants 2 to <6 Years of Age
NCT01732458 (38) [back to overview]Cmax of Aprepitant Following Administration of 125 mg Dose Equivalent in Birth to <2 Year Age Group
NCT01732458 (38) [back to overview]Cmax of Aprepitant Following Administration of 40 mg Dose Equivalent in 2 to <6 Year Age Group
NCT01732458 (38) [back to overview]Cmax of Aprepitant Following Administration of 40 mg Dose Equivalent in 6 to <12 Year Age Group
NCT01732458 (38) [back to overview]Cmax of Aprepitant Following Administration of 40 mg Dose Equivalent in Birth to <2 Year Age Group
NCT01732458 (38) [back to overview]Maximum Concentration (Cmax) of Aprepitant Following Administration of 125 mg Dose Equivalent in 12 to 17 Year Age Group
NCT01732458 (38) [back to overview]Percentage of Participants Discontinuing Study Due to an AE
NCT01732458 (38) [back to overview]Time to Maximum Concentration (Tmax) of Aprepitant Following Administration of 125 mg Dose Equivalent in 12 to 17 Year Age Group
NCT01732458 (38) [back to overview]Tmax Following Administration of 40 mg Dose Equivalent in 12 to 17 Year Age Group
NCT01732458 (38) [back to overview]Tmax of Aprepitant Following Administration of 10 mg Dose Equivalent in 12 to 17 Year Age Group
NCT01732458 (38) [back to overview]Tmax of Aprepitant Following Administration of 10 mg Dose Equivalent in 2 to <6 Year Age Group
NCT01732458 (38) [back to overview]Tmax of Aprepitant Following Administration of 10 mg Dose Equivalent in 6 to <12 Year Age Group
NCT01732458 (38) [back to overview]Tmax of Aprepitant Following Administration of 125 mg Dose Equivalent in 2 to <6 Year Age Group
NCT01732458 (38) [back to overview]Tmax of Aprepitant Following Administration of 125 mg Dose Equivalent in 6 to <12 Year Age Group
NCT01732458 (38) [back to overview]Tmax of Aprepitant Following Administration of 125 mg Dose Equivalent in Birth to <2 Year Age Group
NCT01732458 (38) [back to overview]Tmax of Aprepitant Following Administration of 40 mg Dose Equivalent in 2 to <6 Year Age Group
NCT01732458 (38) [back to overview]Tmax of Aprepitant Following Administration of 40 mg Dose Equivalent in 6 to <12 Year Age Group
NCT01732458 (38) [back to overview]Tmax of Aprepitant Following Administration of 40 mg Dose Equivalent in Birth to <2 Year Age Group
NCT01732458 (38) [back to overview]Percentage of Participants Experiencing at Least One Adverse Event (AE)
NCT01732458 (38) [back to overview]Tmax of Aprepitant Following Administration of 10 mg Dose Equivalent in Birth to <2 Year Age Group
NCT01732458 (38) [back to overview]Area Under the Concentration-time Curve of Aprepitant From Time 0 to the Last Measurable Concentration (AUC0-last) Following Administration of 125 mg Dose Equivalent in 12 to 17 Year Age Group
NCT01732458 (38) [back to overview]AUC0-last Following Administration of 10 mg Dose Equivalent in 12 to 17 Year Age Group
NCT01732458 (38) [back to overview]AUC0-last Following Administration of 40 mg Dose Equivalent in 12 to 17 Year Age Group
NCT01732458 (38) [back to overview]AUC0-last of Aprepitant Following Administration of 10 mg Dose Equivalent in 2 to <6 Year Age Group
NCT01732458 (38) [back to overview]AUC0-last of Aprepitant Following Administration of 10 mg Dose Equivalent in 6 to <12 Year Age Group
NCT01732458 (38) [back to overview]AUC0-last of Aprepitant Following Administration of 10 mg Dose Equivalent in Birth to <2 Year Age Group
NCT01732458 (38) [back to overview]AUC0-last of Aprepitant Following Administration of 125 mg Dose Equivalent in 2 to <6 Year Age Group
NCT01732458 (38) [back to overview]AUC0-last of Aprepitant Following Administration of 125 mg Dose Equivalent in 6 to <12 Year Age Group
NCT01732458 (38) [back to overview]AUC0-last of Aprepitant Following Administration of 125 mg Dose Equivalent in Birth to <2 Year Age Group
NCT01732458 (38) [back to overview]AUC0-last of Aprepitant Following Administration of 40 mg Dose Equivalent in 2 to <6 Year Age Group
NCT01732458 (38) [back to overview]AUC0-last of Aprepitant Following Administration of 40 mg Dose Equivalent in 6 to <12 Year Age Group
NCT01732458 (38) [back to overview]AUC0-last of Aprepitant Following Administration of 40 mg Dose Equivalent in Birth to <2 Year Age Group
NCT01732458 (38) [back to overview]Cmax Following Administration of 40 mg Dose Equivalent in 12 to 17 Year Age Group
NCT01732458 (38) [back to overview]Cmax of Aprepitant Following Administration of 10 mg Dose Equivalent in 12 to 17 Year Age Group
NCT01732458 (38) [back to overview]Cmax of Aprepitant Following Administration of 10 mg Dose Equivalent in 2 to <6 Year Age Group
NCT01732458 (38) [back to overview]Cmax of Aprepitant Following Administration of 10 mg Dose Equivalent in 6 to <12 Year Age Group
NCT01732458 (38) [back to overview]Cmax of Aprepitant Following Administration of 10 mg Dose Equivalent in Birth to <2 Year Age Group
NCT01732458 (38) [back to overview]Cmax of Aprepitant Following Administration of 125 mg Dose Equivalent in 2 to <6 Year Age Group
NCT01732458 (38) [back to overview]Cmax of Aprepitant Following Administration of 125 mg Dose Equivalent in 6 to <12 Year Age Group
NCT01736917 (4) [back to overview]Self-Reported Assessment of Nausea
NCT01736917 (4) [back to overview]Percentage of Participants With Complete Response of Acute and Delayed Chemotherapy Induced Nausea and Vomiting
NCT01736917 (4) [back to overview]Use of Rescue Medications.
NCT01736917 (4) [back to overview]Total Number of Emetic Episodes
NCT01854177 (2) [back to overview]Intensity of Breathlessness
NCT01854177 (2) [back to overview]Unpleasantness of Breathlessness
NCT01857232 (2) [back to overview]Number of Participants With CR in the Overall Phase.
NCT01857232 (2) [back to overview]Number of Participants With Delayed Phase Complete Response(CR)
NCT01874119 (1) [back to overview]Number of Patients With Complete Response During Inpatient Admission
NCT01963793 (16) [back to overview]Clinical Score Assessment of Infiltration
NCT01963793 (16) [back to overview]Lesional Erythema by Mexameter
NCT01963793 (16) [back to overview]Daily Assessments of Duration of Pruritus (Preceding 12 Hours)
NCT01963793 (16) [back to overview]Pruritus by VAS (Visual Analogue Scale)
NCT01963793 (16) [back to overview]Non-lesional Melanin by Mexameter
NCT01963793 (16) [back to overview]Daily Assessments of Maximum Intensity of Pruritus by Use of a VAS
NCT01963793 (16) [back to overview]Clinical Score Assessment of Crusting
NCT01963793 (16) [back to overview]Melanin by Mexameter
NCT01963793 (16) [back to overview]Non-lesional Erythema by Mexameter
NCT01963793 (16) [back to overview]Percent Change From Baseline in Pruritis Assessed by VAS at End of Treatment
NCT01963793 (16) [back to overview]Pruritus by VAS (Visual Analogue Scale)
NCT01963793 (16) [back to overview]Change From Baseline in Participants' Global Assessment on Treatment Areas
NCT01963793 (16) [back to overview]Transepidermal Water Loss (TEWL)
NCT01963793 (16) [back to overview]Clinical Score Assessment of Erythema
NCT01963793 (16) [back to overview]Clinical Score Assessment of Scratch Artefacts
NCT01963793 (16) [back to overview]Daily Assessments of Average Pruritus by Use of a VAS
NCT02097823 (6) [back to overview]Number of Participants With Adverse Events.
NCT02097823 (6) [back to overview]Feasibility of Recruitment and Data Collection.
NCT02097823 (6) [back to overview]Complete Response in Overall Phase
NCT02097823 (6) [back to overview]Complete Response in Delayed Phase
NCT02097823 (6) [back to overview]Good Control of Nausea
NCT02097823 (6) [back to overview]Complete Response in Acute Phase
NCT02106494 (5) [back to overview]Delayed Complete Control (CC) Rate
NCT02106494 (5) [back to overview]Delayed Phase Complete Response (CR) Rate
NCT02106494 (5) [back to overview]Overall Complete Control Rate
NCT02106494 (5) [back to overview]Rate of No Emetic Episodes
NCT02106494 (5) [back to overview]Overall Complete Response Rate
NCT02116530 (5) [back to overview]Frequency of Rescue Medication
NCT02116530 (5) [back to overview]Proportion of Patients With Complete Response
NCT02116530 (5) [back to overview]Proportion of Patients With no Nausea
NCT02116530 (5) [back to overview]Mean Scores of Potential Toxicities Related to Olanzapine as Measured by the Nausea and Vomiting Daily Diary/Questionnaire
NCT02116530 (5) [back to overview]Median Nausea Scores
NCT02130687 (12) [back to overview]Norepinephrine (NE) Concentrations
NCT02130687 (12) [back to overview]Neuropeptide Y
NCT02130687 (12) [back to overview]Mean Arterial Blood Pressure
NCT02130687 (12) [back to overview]Dipeptidyl Peptidase IV (DPP4) Activity
NCT02130687 (12) [back to overview]Glucose
NCT02130687 (12) [back to overview]Heart Rate
NCT02130687 (12) [back to overview]Heart Rate
NCT02130687 (12) [back to overview]Low Frequency Variability of Blood Pressure Activity
NCT02130687 (12) [back to overview]24hr Urinary Testing for Sodium
NCT02130687 (12) [back to overview]Mean Arterial Blood Pressure
NCT02130687 (12) [back to overview]Insulin
NCT02130687 (12) [back to overview]Angiotensin Converting Enzyme (ACE) Activity
NCT02210195 (2) [back to overview]Change From Week 0 in Drinking Quantity and Frequency Using Drinks Per Week at Week 8
NCT02210195 (2) [back to overview]Change From Week 0 in Cannabis Use Using Urinary CN-THCCOOH Levels at Week 8
NCT02484911 (12) [back to overview]Proportion of Participants Receiving MEC With No Vomiting in the Overall Phase
NCT02484911 (12) [back to overview]Proportion of Participants Receiving HEC With Complete Response in Overall Phase
NCT02484911 (12) [back to overview]Proportion of Participants Receiving HEC With Complete Response in the Acute Phase
NCT02484911 (12) [back to overview]Proportion of Participants Receiving HEC With Complete Response in the Delayed Phase
NCT02484911 (12) [back to overview]Proportion of Participants Receiving HEC With No Vomiting in the Acute Phase
NCT02484911 (12) [back to overview]Proportion of Participants Receiving HEC With No Vomiting in the Delayed Phase
NCT02484911 (12) [back to overview]Proportion of Participants Receiving HEC With No Vomiting in the Overall Phase
NCT02484911 (12) [back to overview]Proportion of Participants Receiving MEC With Complete Response in Overall Phase
NCT02484911 (12) [back to overview]Proportion of Participants Receiving MEC With Complete Response in the Acute Phase
NCT02484911 (12) [back to overview]Proportion of Participants Receiving MEC With Complete Response in the Delayed Phase
NCT02484911 (12) [back to overview]Proportion of Participants Receiving MEC With No Vomiting in the Acute Phase
NCT02484911 (12) [back to overview]Proportion of Participants Receiving MEC With No Vomiting in the Delayed Phase
NCT02519842 (6) [back to overview]Percentage of Participants Who Experienced a Complete Response During the Acute Phase (0 to 24 Hours Post Initiation of Chemotherapy) in Cycle 1
NCT02519842 (6) [back to overview]Percentage of Participants Who Discontinued Study Drug Due to an Adverse Event
NCT02519842 (6) [back to overview]Percentage of Participants Who Experienced a Complete Response During the Delayed Phase (>24 to 120 Hours Post Initiation of Chemotherapy) in Cycle 1
NCT02519842 (6) [back to overview]Percentage of Participants Who Experienced a Complete Response During the Overall Phase (0 to 120 Hours Post Initiation of Chemotherapy) in Cycle 1
NCT02519842 (6) [back to overview]Percentage of Participants Who Experienced One or More Adverse Events
NCT02519842 (6) [back to overview]Percentage of Participants Who Experienced No Vomiting, Regardless of Rescue Medication Use, During the Overall Phase (0 to 120 Hours Post Initiation of Chemotherapy) in Cycle 1
NCT02597907 (1) [back to overview]The Incidence of Postoperative Nausea and Vomiting
NCT02625181 (4) [back to overview]PONV Incidence: Number of Participants With Postoperative Nausea and Vomiting
NCT02625181 (4) [back to overview]Adherence to PONV Guidelines
NCT02625181 (4) [back to overview]Time to Discharge From the Postanesthesia Care Unit (PACU)
NCT02625181 (4) [back to overview]The Number of Prophylactic Interventions for PONV
NCT02732015 (1) [back to overview]Number of Participants With Complete Response (CR) of Rolapitant Hydrochloride Administered as a Single-dose
NCT02780609 (5) [back to overview]Phase I: Recommended Phase II Dose (RPh2D)
NCT02780609 (5) [back to overview]Rate of Minimal Residual Disease (MRD)
NCT02780609 (5) [back to overview]Phase 1 and Phase 2 Percentage of Participants Treated at Dose Level 3/RP2D With Progression Free Survival (PFS)
NCT02780609 (5) [back to overview]Overall Survival (OS)
NCT02780609 (5) [back to overview]Complete Response (CR)
NCT03197064 (5) [back to overview]Somatosensory Evoked Potentials (SEPs), Extremity Amplitude (Right Upper Extremity)
NCT03197064 (5) [back to overview]Somatosensory Evoked Potentials (SEPs), Extremity Amplitude (Right Lower Extremity)
NCT03197064 (5) [back to overview]Somatosensory Evoked Potentials (SEPs), Extremity Amplitude (Left Upper Extremity)
NCT03197064 (5) [back to overview]Somatosensory Evoked Potentials (SEPs), Extremity Amplitude (Left Lower Extremity)
NCT03197064 (5) [back to overview]Motor Evoked Potentials Amplitude (Left Upper Extremity)
NCT03237611 (4) [back to overview]Complete Control Rate of Chemotherapy-induced Nausea and Vomiting (CINV) Following 2nd Cycle of Chemotherapy
NCT03237611 (4) [back to overview]Complete Control Rate of Chemotherapy-induced Nausea and Vomiting (CINV) Following 1st Cycle of Chemotherapy
NCT03237611 (4) [back to overview]Complete Control Rate of Chemotherapy-induced Nausea and Vomiting (CINV) Following 1st Cycle of Chemotherapy
NCT03237611 (4) [back to overview]Complete Control Rate of Chemotherapy-induced Nausea and Vomiting (CINV) Following 2nd Cycle of Chemotherapy
NCT03578081 (5) [back to overview]Complete Response (CR) (no Emetic Episodes and no Use of Rescue Medication) During the Acute, Delayed and the Overall Periods as Measured by the Nausea and Vomiting Daily Diary/Questionnaire
NCT03578081 (5) [back to overview]Potential Toxicities as Ascribed to Olanzapine as Measured by the Nausea and Vomiting Daily Diary/Questionnaire
NCT03578081 (5) [back to overview]Total Frequency of Rescue Medication as Measured by the Nausea and Vomiting Daily Diary/Questionnaire
NCT03578081 (5) [back to overview]Average Nausea Scores (0-10) Repeatedly Measured by the Nausea and Vomiting Daily Diary/Questionnaire
NCT03578081 (5) [back to overview]No Nausea Rate Defined as a Response of 0 in the Nausea Item of Nausea and Vomiting Daily Diary/Questionnaire in the Overall (0-120 Hours), Acute (0-24 Hours), and Delayed (24-120 Hours) Periods
NCT03718039 (5) [back to overview]Mean Area Under the Curve (AUC) of the NRS-R (Windowed Worst Observation Carried Forward) Pain Intensity Scores
NCT03718039 (5) [back to overview]Mean Total Postoperative Opioid Consumption (in Morphine Equivalents) Through 72 Hours
NCT03718039 (5) [back to overview]Percentage of Subjects Receiving no Opioid Rescue
NCT03718039 (5) [back to overview]Mean Area Under the Curve (AUC) of the NRS-A (Windowed Worst Observation Carried Forward) Pain Intensity Scores
NCT03718039 (5) [back to overview]Percentage of Subjects Receiving no Opioid Rescue
NCT04054193 (2) [back to overview]Percentage of Participants in Cycle 1 Who Discontinued Study Drug Due to an Adverse Event (AE)
NCT04054193 (2) [back to overview]Percentage of Participants in Cycle 1 Who Experienced One or More Adverse Events (AEs)
NCT04470622 (5) [back to overview]Time to Discharge From Hospital.
NCT04470622 (5) [back to overview]Incidence of Treatment-emergent Adverse Events.
NCT04470622 (5) [back to overview]Time to Death or Respiratory Failure, Defined as Any of the Following: Endotracheal Intubation and Mechanical Ventilation; Oxygen Delivered by High-flow Nasal Cannula; Noninvasive Positive Pressure Ventilation; Extracorporeal Membrane Oxygenation (ECMO).
NCT04470622 (5) [back to overview]Proportion of Subjects Alive and Discharged From the Hospital.
NCT04470622 (5) [back to overview]Change From Baseline in Interleukin 6 (IL-6).

Number of Patients With Clinical Adverse Experiences (CAEs)

An adverse experience (AE) is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR'S product, whether or not considered related to the use of the product (NCT00231777)
Timeframe: Baseline and 24 hours

InterventionParticipants (Number)
MK0517 Intravenous (IV) 40 mg125
Ondansetron IV 4 mg32

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Number of Patients With Laboratory Adverse Experiences (LAEs)

A laboratory adverse experience (LAE) is defined as any unfavorable and unintended change in the chemistry of the body temporally associated with the use of the SPONSOR'S product, whether or not considered related to the use of the product. (NCT00231777)
Timeframe: Baseline and 24 hours

InterventionParticipants (Number)
MK0517 Intravenous (IV) 40 mg9
Ondansetron IV 4 mg2

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Number of Patients With Serious CAEs

Serious CAEs are any AEs occurring at any dose that; Results in death; or Is life threatening; or Results in a persistent or significant disability/incapacity; or Results in or prolongs an existing inpatient hospitalization; or Is a congenital anomaly/birth defect; or Is a cancer; or Is an overdose (NCT00231777)
Timeframe: Baseline and 24 hours

InterventionParticipants (Number)
MK0517 Intravenous (IV) 40 mg15
Ondansetron IV 4 mg3

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Number of Emesis Free Participants During the Study Period.

To compare the efficacy of aprepitant plus standard therapy to placebo plus standard therapy in control of nausea and vomiting during conditioning therapy for autologous or allogeneic hematopoietic stem cell transplantation (HSCT) as defined by the number of retch/emesis free days during the study period (NCT00248547)
Timeframe: Up to three weeks

InterventionParticipants (Number)
Aprepitant13
Placebo (Sugar Pill)5

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Overall Nausea Controlled

(NCT00293384)
Timeframe: at 0-120 hours

Interventionparticipants (Number)
Aprepitant, Dexamethasone, Cytoxan & Kytril31

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Delayed Vomiting Controlled

(NCT00293384)
Timeframe: at 25-120 hours

Interventionparticipants (Number)
Aprepitant, Dexamethasone, Cytoxan & Kytril22

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Proportion of Participants With Controlled Acute Vomiting

No episodes of vomiting and no rescue medication during first 24 hours after cyclophosphamide administration. (NCT00293384)
Timeframe: at 0-24 hours

Interventionparticipants (Number)
Aprepitant, Dexamethasone, Cytoxan & Kytril20

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Toxicity Grade 3, 4, or 5

(NCT00293384)
Timeframe: at 0-120 hours

Interventionparticipants (Number)
Aprepitant, Dexamethasone, Cytoxan & Kytril2

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Number of Patients Who Reported No Vomiting

"The number of patients who reported No Vomiting in the overall phase in Cycle~1" (NCT00337727)
Timeframe: Overall phase (0-120 hours post initiation of MEC) in Cycle 1.

InterventionParticipants (Number)
Aprepitant Regimen324
Standard Regimen252

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Number of Patients Who Reported Complete Response

The number of patients who reported Complete Response (no vomiting and no use of rescue medication) in the overall phase in Cycle 1. (NCT00337727)
Timeframe: Overall phase (0-120 hours post initiation of MEC) in Cycle 1

InterventionParticipants (Number)
Aprepitant Regimen292
Standard Regimen229

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Number of Participants With no Emesis and no Rescue Therapy Within 5 Days of Receiving FOLFOX and FOLFIRI in the First Cycle of Chemotherapy.

(NCT00381862)
Timeframe: Up to 24 weeks

InterventionParticipants (Number)
Aprepitant and Palonosetron54

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Home Record: Severity of Delayed Nausea

1=not at all nauseated to 7=extremely nauseated, therefore higher values are worse (NCT00475085)
Timeframe: average of day 1 afternoon, evening and night, and all of days 2 and 3

Interventionunits on a scale (Mean)
Arm II1.88
Arm III1.65
Arm I1.87
Arm IV1.68

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Proportion of Patients With no Emesis During the Acute CINV Time Period (Cycle Days 1-5)

Proportion of patients with no emesis regardless of use of rescue medication during cycle days 1-5. (NCT00572572)
Timeframe: Participants were evaluated from cycle days 1-5.

Interventionpercentage of evaluable subjects (Number)
Aprepitant80
Placebo52

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Preferred Treatment Cycle

Participants were asked which treatment cycles was preferable - aprepitant or placebo cycle. (NCT00572572)
Timeframe: 2 months

Interventionpercentage of subjects with a preference (Number)
Aprepitant78
Placebo22

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Visual Analouge (VAS) 100mm Scale Score

The Visual Analouge (VAS) 100mm Scale Score for Chemotherapy Induced Nausea and Vomiting (CINV). Participants were asked to mark a linear scale 100mm in length representing their level of nausea with 0mm indicating no nausea and 100mm indicating severe nausea. The mean VAS scores for days 1-8 combined, by treatment (Aprepitant vs. Placebo) were reported. (NCT00572572)
Timeframe: Days 1-8

Interventionmm (Mean)
Aprepitant22.6
Placebo27.1

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Proportion of Patients With no Emesis During the Delayed CINV Time Period (Cycle Days 6-8)

Proportion of patients with no emesis regardless of use of rescue medication during cycle days 6-8. (NCT00572572)
Timeframe: Participants were evaluated from cycle days 6-8.

Interventionpercentage of evaluable subjects (Number)
Aprepitant92
Placebo78

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Complete Response.

Participants were followed for chemotherapy induced nausea and vomiting (CINV) through day 8 of cycle 2. Complete response is defined as no emetic episodes and no use of rescue medication. (NCT00572572)
Timeframe: Participants were evaluated from start of treatment through day 8 of cycle 2.

Interventionpercentage of evaluable subjects (Number)
Aprepitant47
Placebo15

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MD Anderson Symptom Inventory Score

The MD Anderson Symptom Inventory (MDASI) is a brief measure of the severity and impact of cancer-related symptoms. Thirteen core items measure the severity of symptoms and six additional items measure the impact of symptoms. All items are rated on a scale from 0 (not present or did not interfere) to 10 (maximal severity or interference). The mean value of the total nineteen items ranges from 0 to 10. (NCT00572572)
Timeframe: Days 1-8

Interventionunits on a scale (Mean)
Aprepitant3.2
Placebo2.9

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Overall Emetic Response

Clinical responses were summarized using frequencies and percentages by phase, disease group, and overall. To compute emetic response by phase, the previously defined criteria were applied to each day of the three phases independently. The worst response was used to represent the response in each of these phases and overall emetic response. Overall emetic response was computed by applying the same definitions of emetic response to the entire study period. (NCT00600353)
Timeframe: At leaset 24 hours to more than 72 hours after chemotherapy

,
InterventionParticipants (Count of Participants)
CCCRMRFailureNSN
Group A - Subjects With Multiple Myeloma008106
Group B - Subjects With Relpased Lymphoma106205

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Overall Emetic Response: Acute

"Complete Control (CC) - no emetic episode in 24 hours, no rescue medications and nausea visual scale (NVS) of ≤ 2.5, Complete Emetic Response (CR) - 0 emetic episodes, no rescue medications. Major Emetic Response (MR) - 0 to 2 emetic episodes within 24 hour period with or without rescue medications.~Minor Emetic Response (mR) - 3 to 5 emetic episodes within 24 hour period with or without rescue medications.~Failure - >5 emetic episodes within 24 hour period. No Significant Nausea (NSN) - maximum NVS ≤ 5." (NCT00600353)
Timeframe: 24 hours after chemotherapy

,
InterventionParticipants (Count of Participants)
CCCRMRFailureNSN
Group A - Subjects With Multiple Myeloma513009
Group B - Subjects With Relpased Lymphoma900009

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Overall Emetic Response: Extended

"Complete Control (CC) - no emetic episode in 24 hours, no rescue medications and nausea visual scale (NVS) of ≤ 2.5, Complete Emetic Response (CR) - 0 emetic episodes, no rescue medications. Major Emetic Response (MR) - 0 to 2 emetic episodes within 24 hour period with or without rescue medications.~Minor Emetic Response (mR) - 3 to 5 emetic episodes within 24 hour period with or without rescue medications.~Failure - >5 emetic episodes within 24 hour period. No Significant Nausea (NSN) - maximum NVS ≤ 5." (NCT00600353)
Timeframe: 72 hours after chemotherapy

,
InterventionParticipants (Count of Participants)
CCCRMRFailureNSN
Group A - Subjects With Multiple Myeloma107000
Group B - Subjects With Relpased Lymphoma207005

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Overall Emetic Response: Delayed

"Complete Control (CC) - no emetic episode in 24 hours, no rescue medications and nausea visual scale (NVS) of ≤ 2.5, Complete Emetic Response (CR) - 0 emetic episodes, no rescue medications. Major Emetic Response (MR) - 0 to 2 emetic episodes within 24 hour period with or without rescue medications.~Minor Emetic Response (mR) - 3 to 5 emetic episodes within 24 hour period with or without rescue medications.~Failure - >5 emetic episodes within 24 hour period. No Significant Nausea (NSN) - maximum NVS ≤ 5." (NCT00600353)
Timeframe: 24 to 72 hours after chemotherapy

,
InterventionParticipants (Count of Participants)
CCCRMRFailureNSN
Group A - Subjects With Multiple Myeloma216000
Group B - Subjects With Relpased Lymphoma405008

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No Vomiting Overall (in the 120 Hours Following Initiation of Cisplatin)

The number of patients who reported No Vomiting in the 120 hours following initiation of cisplatin chemotherapy. (NCT00619359)
Timeframe: Overall (the 120 hours following initiation of cisplatin chemotherapy)

InterventionParticipants (Number)
Fosaprepitant806
Aprepitant844

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A Complete Response (no Vomiting and no Use of Rescue Therapy) Overall (in the 120 Hours Following Initiation of Cisplatin).

The number of patients who reported No Vomiting and No Use of Rescue Therapy in the 120 hours following initiation of cisplatin chemotherapy. (NCT00619359)
Timeframe: Overall (in the 120 hours following initiation of cisplatin chemotherapy).

InterventionParticipants (Number)
Fosaprepitant795
Aprepitant820

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A Complete Response (no Vomiting and no Use of Rescue Therapy) in the Delayed Phase (25 to 120 Hours Following Initiation of Cisplatin).

The number of patients who reported No Vomiting and No Use of Rescue Therapy in the 25 to 120 hours following initiation of cisplatin chemotherapy. (NCT00619359)
Timeframe: Delayed phase (25 to 120 hours following initiation of cisplatin).

InterventionParticipants (Number)
Fosaprepitant822
Aprepitant841

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Geometric Mean Area Under Curve (AUC) of Analyte, Vincristine (VC), in Aprepitant Treatment and Control Group

Pharmacokinetic (PK) blood sampling to determine the geometric mean AUC of VC, during & post chemotherapy infusion, baseline, at 30, 60, 75, 90 minutes, and 2 , 4, 6, 8, and 24 hours from start of cyclophosphamide infusion. The absence of PK drug interactions was determined if the 90% Confidence Intervals (CI) of the geometric mean AUC ratio between 2 groups is within 0.80 to 1.25. Measurements reported as concentrate times the time, i.e. nanograms (ng)/milliliters (mL) times hour (hr). (NCT00651755)
Timeframe: Time points over 24 hours of cyclophosphamide infusion for both cycles (21 day cycle)

Interventionng/mL*hr (Geometric Mean)
Aprepitant41
Control39

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Geometric Mean Area Under Curve (AUC) of Analyte,Prednisone (PR), in Aprepitant Treatment and Control Group

Pharmacokinetic (PK) blood sampling to determine the geometric mean AUC of PR, during & post chemotherapy infusion, baseline, at 30, 60, 75, 90 minutes, and 2 , 4, 6, 8, and 24 hours from start of cyclophosphamide infusion. The absence of PK drug interactions was determined if the 90% Confidence Intervals (CI) of the geometric mean AUC ratio between 2 groups is within 0.80 to 1.25. Measurements reported as concentrate times the time, i.e. nanograms (ng)/milliliters (mL) times hour (hr). (NCT00651755)
Timeframe: Time points over 8 hours of cyclophosphamide infusion for both cycles (21 day cycle)

Interventionng/mL*hr (Geometric Mean)
Aprepitant287
Control265

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Geometric Mean Area Under Curve (AUC) of Analyte, Prednisolone (PL), in Aprepitant Treatment and Control Group

Pharmacokinetic (PK) blood sampling to determine the geometric mean AUC of PL, during & post chemotherapy infusion, baseline, at 30, 60, 75, 90 minutes, and 2 , 4, 6, 8, and 24 hours from start of cyclophosphamide infusion. The absence of PK drug interactions was determined if the 90% Confidence Intervals (CI) of the geometric mean AUC ratio between 2 groups is within 0.80 to 1.25. Measurements reported as concentrate times the time, i.e. nanograms (ng)/milliliters (mL) times hour (hr). (NCT00651755)
Timeframe: Time points over 8 hours of cyclophosphamide infusion for both cycles (21 day cycle)

Interventionng/mL*hr (Geometric Mean)
Aprepitant4416
Control3817

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Geometric Mean Area Under Curve (AUC) of Analyte, Cyclophosphamide (CP), in Aprepitant Treatment and Control Group

Pharmacokinetic (PK) blood sampling to determine the geometric mean AUC of Cyclophosphamide (CP) during & post chemotherapy infusion, baseline, at 30, 60, 75, 90 minutes, and 2 , 4, 6, 8, and 24 hours from start of cyclophosphamide infusion. The absence of PK drug interactions was determined if the 90% Confidence Intervals (CI) of the geometric mean AUC ratio between 2 groups is within 0.80 to 1.25. Measurements reported as concentrate times the time, i.e. micrograms (ug)/milliliters (mL) times hour (hr). (NCT00651755)
Timeframe: Time points over 24 hours of cyclophosphamide infusion for both cycles (21 day cycle)

Interventionug/mL*hr (Geometric Mean)
Aprepitant300
Control Group250

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Geometric Mean Area Under Curve (AUC) of Analyte, 4-hydroxy-cyclophosphamide (4-OH-CP), in Aprepitant Treatment and Control Group

Pharmacokinetic (PK) blood sampling to determine the geometric mean AUC of 4-hydroxy-cyclophosphamide (4-OH-CP), during & post chemotherapy infusion, baseline, at 30, 60, 75, 90 minutes, and 2 , 4, 6, 8, and 24 hours from start of cyclophosphamide infusion. The absence of PK drug interactions was determined if the 90% Confidence Intervals (CI) of the geometric mean AUC ratio between 2 groups is within 0.80 to 1.25. Measurements reported as concentrate times the time, i.e. micrograms (ug)/milliliters (mL) times hour (hr). (NCT00651755)
Timeframe: Time points over 24 hours of cyclophosphamide infusion for both cycles (21 day cycle)

Interventionug/mL*hr (Geometric Mean)
Aprepitant3.9
Control4.0

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Geometric Mean Area Under Curve (AUC) of Analyte, 2-dechloro-cyclophosphamide(2-deCI-CP), in Aprepitant Treatment and Control Group

Pharmacokinetic (PK) blood sampling to determine the geometric mean AUC of 2-deCI-CP, during & post chemotherapy infusion, baseline, at 30, 60, 75, 90 minutes, and 2 , 4, 6, 8, and 24 hours from start of cyclophosphamide infusion. The absence of PK drug interactions was determined if the 90% Confidence Intervals (CI) of the geometric mean AUC ratio between 2 groups is within 0.80 to 1.25. Measurements reported as concentrate times the time, i.e. micrograms (ug)/milliliters (mL) times hour (hr). (NCT00651755)
Timeframe: Time points over 24 hours of cyclophosphamide infusion for both cycles (21 day cycle)

Interventionug/mL*hr (Geometric Mean)
Aprepitant4.5
Control6.0

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Number of Participants With Postoperative Nausea and Vomiting

(NCT00659737)
Timeframe: 0-24 hours

Interventionparticipants (Number)
Aprepitant and Placebo Transdermal Patch28
Aprepitant and Scopolamine Transdermal Patch34

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Number of Participants Having Post-operative Emesis and Nausea.

Postoperative emesis was measured as present or not present (nominal data) and analyzed with Chi-square; Comparison of nausea severity was performed in two ways. In those patients who exhibited nausea VRS>0, a worst nausea score for each patient was defined as the highest nausea score recorded over the 48 hours. Mann-Whitney rank sum test was used to compare worst nausea scores. Multivariate Analysis of Variance (MANOVA) was used to determine if the mean VRS (Verbal Rating Scale) score over time was significant between the two groups. (NCT00659945)
Timeframe: 48 hours post surgery

Interventionparticipants (Number)
Group A(Oral Aprepitant+iv Ondansetron)7
Group B(Oral Placebo+iv Ondansetron)22

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Complete Protection

defined as no emesis, no use of rescue medications, and a maximum nausea severity < 25 mm (100 mm visual analog scale, 0 = no nausea, 100 = worst nausea) (NCT00711555)
Timeframe: cycle 1, day 1

Interventionpercentage of participants (Number)
Aprepitant, Dexamethasone, Ondansetron, Multiple Days74

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Complete Response (Percentage of Patients)

defined as a no emetic episodes and no use of rescue therapy (NCT00711555)
Timeframe: cycle 1, day 1

Interventionpercentage of participants (Number)
Aprepitant, Dexamethasone, Ondansetron, Multiple Days84

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no Emesis

(NCT00711555)
Timeframe: cycle 1, day 1

Interventionpercentage of participants (Number)
Aprepitant, Dexamethasone, Ondansetron, Multiple Days100

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no Nausea

defined as maximum nausea severity < 5 mm (100 mm visual analog scale, 0 = no nausea, 100 = worst nausea) (NCT00711555)
Timeframe: cycle 1, day 1

Interventionpercentage of participants (Number)
Aprepitant, Dexamethasone, Ondansetron, Multiple Days74

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no Significant Nausea

defined as a maximum nausea severity < 25 mm (100 mm visual analog scale, 0 = no nausea, 100 = worst nausea) (NCT00711555)
Timeframe: cycle 1, day 1

Interventionpercentage of participants (Number)
Aprepitant, Dexamethasone, Ondansetron, Multiple Days79

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Number of Participants With Nausea and Vomiting

(NCT00717054)
Timeframe: 24 hours postoperatively

Interventionparticipants (Number)
Aprepitant and Scopolamine Group24
Aprepitant and Placebo Scopolamine Group29

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Number of Participants With Nausea and Vomiting in PACU

(NCT00717054)
Timeframe: Postoperatively, up to 2 hours

Interventionparticipants (Number)
Aprepitant and Scopolamine Group35
Aprepitant and Placebo Scopolamine Group39

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Total Vomiting

(NCT00717054)
Timeframe: 24 hours postoperatively

Interventionparticipants (Number)
Aprepitant and Scopolamine Group5
Aprepitant and Scopolamine Placebo Group2

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Need for Antiemetic Medication

(NCT00717054)
Timeframe: 24 hours postoperatively

Interventionparticipants (Number)
Aprepitant and Scopolamine Group23
Aprepitant and Scopolamine Placebo Group21

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Cumulative Incidence of Emesis

Any vomiting or retching (NCT00734929)
Timeframe: 48 h

Interventionparticipants (Number)
Aprepitant8
Ondansetron20

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Average Nausea Score

Participants verbally rated their nausea on a scale of 0-10. 0 = No nausea, 10 = worst nausea imaginable (NCT00734929)
Timeframe: Post OP hours 0-2, 24 h, 48 h

,
Interventionunits on a scale (Mean)
0-2 hours post op24 hours post op48 hours post op
Aprepitant0.40.80.9
Ondansetron0.61.31.1

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Incidence of Vomiting (Post OP)

(NCT00734929)
Timeframe: Post OP (0 - 2 hours)

Interventionparticipants (Number)
Aprepitant3
Ondansetron11

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"Number of Participants Who Rated Their Satisfaction With Antiemetic Management as Very Satisfied"

Participants rated their satisfaction with antiemetic management on a 5 points scale: very satisfied, somewhat satisfied, neither satisfied nor dissatisfied, somewhat dissatisfied, very dissatisfied) (NCT00734929)
Timeframe: 48 hour

Interventionparticipants (Number)
Aprepitant36
Ondansetron32

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Number of Vomiting Episodes

(NCT00734929)
Timeframe: 48 hours

Interventionvomiting episodes (Mean)
Aprepitant0
Ondansetron0

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Incidence of Vomiting (24 Hours)

Any vomiting or retching (NCT00734929)
Timeframe: 24 h

Interventionparticipants (Number)
Aprepitant7
Ondansetron19

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Time to First Vomiting

(NCT00734929)
Timeframe: 48 h

Interventionhours (Median)
Aprepitant + Dexamethasone13.5
Ondansetron + Dexamethasone2

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Use of Rescue Antiemetics (24 Hours)

(NCT00734929)
Timeframe: 24 h

Interventionparticipants (Number)
Aprepitant31
Ondansetron30

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Use of Rescue Antiemetics (48 Hours)

(NCT00734929)
Timeframe: 48 hour

Interventionparticipants (Number)
Aprepitant33
Ondansetron32

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Use of Rescue Antiemetics (Post OP)

(NCT00734929)
Timeframe: Post OP (0 - 2 hours)

Interventionparticipants (Number)
Aprepitant20
Ondansetron24

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Incidence of Nausea

operative procedure (NCT00734929)
Timeframe: Post operative procedure (OP) hours (0-2, 24, 48)

,
Interventionparticipants (Number)
0-2 hours Post OP24 Hours Post Op48 Hours Post Op
Aprepitant273335
Ondansetron273032

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Number of Participants With a Complete Response Rate

complete response rate: defined as no Postoperative nausea and vomiting (PONV) and no need for rescue antiemetics. (NCT00734929)
Timeframe: 24 hours Post OP, 48 hours Post OP

,
Interventionparticipants (Number)
24 Hours Post OP48 Hours Post OP
Aprepitant1411
Ondansetron2119

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Number of Participants Who Were Hospitalized Within 7 Days Post-ERCP for Abdominal Pain That Did Not Meet Criteria for Acute Pancreatitis

(NCT00736073)
Timeframe: 7 days

Interventionparticipants (Number)
Arm 1-medication Pre and Post Procedure6
Arm 2-Randomized to Placebo9

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Number of Post-ERCP Pancreatitis Cases in Participants Who Are Administered Aprepitant and Placebo Prior to ERCP and One Day After ERCP:Assess the Total Number of Incidents of Post-ERCP Pancreatitis in Each Group (Treatment and Control).

(NCT00736073)
Timeframe: 48 hours

Interventioncases of ERCP in participants (Number)
Arm 1-medication Pre and Post Procedure7
Arm 2-Randomized to Placebo7

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Number of Participants Discontinuing Study Drug Due to an AE

An AE is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to the use of the product. The number of participants who discontinued from the study due to an AE are summarized. (NCT00818259)
Timeframe: Day 1 up to Day 3

InterventionParticipants (Number)
Part IA-fosaprepitant 115 mg/Aprepitant0
Part IB-fosaprepitant 150 mg0
Part IIA-aprepitant 80 mg Equiv.0
Part IIB-aprepitant 125 mg Equiv.0
Part III-ondansetron0
Part IV-aprepitant Regimen0
Part V-fosaprepitant Regimen1

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Apparent Terminal Half-life (t1/2) for Aprepitant

t1/2 is the amount of time from dosing until half of the aprepitant was metabolized from the body. Fosaprepitant is a prodrug for aprepitant and is rapidly converted to aprepitant after IV administration. Blood samples for PK assessment were collected at the following time points: Part IA - Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 3, 4, 6, 8 and 24 hr post fosaprepitant dose; Part IB - Pre-dose and -0.75, -0.5, 0, 0.5, 1.5, 3, 4, 6, 8, 24, 48 and 72 hr post start of chemotherapy; Parts II and IV - Pre-dose and 1.5, 3, 4, 6, 8, 24, 48 and 72 hr post aprepitant dose; Part V - Pre-dose and -0.75, -0.5, 0, 1.5, 3, 4, 6, 8, 24, 48 and 72 hr post start of chemotherapy. (NCT00818259)
Timeframe: Up to 72 hours post fosaprepitant/aprepitant dose

,,,,,
Interventionhr (Mean)
6 months to <2 years (n=0, 0, 5, 3, 0, 3, 6)2 years to <6 years (n=0, 0, 6, 4, 0, 5, 7)6 years to <12 years (n=0, 0, 5, 6, 0, 4, 8)12 years to 17 years (n=6 11, 0, 0, 0, 0, 0)
Part IA-fosaprepitant 115 mg/AprepitantNANANA11.0
Part IB-fosaprepitant 150 mgNANANA22.2
Part IIA-aprepitant 80 mg Equiv.7.288.279.17NA
Part IIB-aprepitant 125 mg Equiv.8.096.066.89NA
Part IV-aprepitant Regimen6.189.2110.8NA
Part V-fosaprepitant Regimen7.716.448.76NA

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Area Under the Time-Concentration Curve From 0 to 24 Hours (AUC 0-24hr) for Aprepitant

AUC is a measure of the amount of aprepitant in the plasma. Fosaprepitant is a prodrug for aprepitant and is rapidly converted to aprepitant after IV administration. Blood samples for pharmacokinetic (PK) assessment were collected at the following time points: Part IA - Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 3, 4, 6, 8 and 24 hours (hr) post fosaprepitant dose; Part IB - Pre-dose and -0.75, -0.5, 0, 0.5, 1.5, 3, 4, 6, 8 and 24 hr post start of chemotherapy; Parts II and IV - Pre-dose and 1.5, 3, 4, 6, 8 and 24 hr post aprepitant dose; Part V - Pre-dose and -0.75, -0.5, 0, 1.5, 3, 4, 6, 8 and 24 hr post start of chemotherapy. (NCT00818259)
Timeframe: Up to 24 hours post fosaprepitant/aprepitant dose

,,,,,
Interventionhr*ng/mL (Mean)
6 months to <2 years (n=0, 0, 5, 5, 0, 6, 6)2 years to <6 years (n=0, 0, 8, 7, 0, 6, 7)6 years to <12 years (n=0, 0, 6, 6, 0, 6, 8)12 years to 17 years (n=8, 11, 0, 0, 0, 0, 0)
Part IA-fosaprepitant 115 mg/AprepitantNANANA19500
Part IB-fosaprepitant 150 mgNANANA30800
Part IIA-aprepitant 80 mg Equiv.200001640016000NA
Part IIB-aprepitant 125 mg Equiv.63102300022000NA
Part IV-aprepitant Regimen211001730024400NA
Part V-fosaprepitant Regimen117001830019500NA

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Tmax for Fosaprepitant

Tmax is a measure of the amount of time after dosing to when the maximum concentration of fosaprepitant was achieved. Blood samples for PK assessment were collected at the following time points: Part IA - Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 3, 4, 6, 8 and 24 hr post fosaprepitant dose; Part V - Pre-dose and -0.75, -0.5, 0, 0.5, 1.5, 3, 4, 6, 8, 24, 48 and 72 hr post start of chemotherapy. (NCT00818259)
Timeframe: Up to 72 hours post fosaprepitant dose

,
Interventionhr (Mean)
6 months to <2 years (n=0, 0, 0, 0, 0, 0, 7)2 years to <6 years (n=0, 0, 0, 0, 0, 0, 7)6 years to <12 years (n=0, 0, 0, 0, 0, 0, 8)12 years to 17 years (n=0, 11, 0, 0, 0, 0, 0)
Part IB-fosaprepitant 150 mgNANANA0.614
Part V-fosaprepitant Regimen1.131.051.04NA

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Cmax for Fosaprepitant

Cmax is a measure of the maximum amount of fosaprepitant in the plasma. Blood samples for PK assessment were collected at the following time points: Part IA - Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 3, 4, 6, 8 and 24 hr post fosaprepitant dose; Part V - Pre-dose and -0.75, -0.5, 0, 0.5, 1.5, 3, 4, 6, 8, 24, 48 and 72 hr post start of chemotherapy. (NCT00818259)
Timeframe: Up to 72 hours post fosaprepitant dose

,
Interventionng/mL (Mean)
6 months to <2 years (n=0, 0, 0, 0, 0, 0, 7)2 years to <6 years (n=0, 0, 0, 0, 0, 0, 8)6 years to <12 years (n=0, 0, 0, 0, 0, 0, 8)12 years to 17 years (n=0, 11, 0, 0, 0, 0, 0)
Part IB-fosaprepitant 150 mgNANANA1310
Part V-fosaprepitant Regimen275630341654NA

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Maximum Plasma Concentration (Cmax) for Aprepitant

Cmax is a measure of the maximum amount of aprepitant in the plasma. Fosaprepitant is a prodrug for aprepitant and is rapidly converted to aprepitant after IV administration. Blood samples for PK assessment were collected at the following time points: Part IA - Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 3, 4, 6, 8 and 24 hr post fosaprepitant dose; Part IB - Pre-dose and -0.75, -0.5, 0, 0.5, 1.5, 3, 4, 6, 8, 24, 48 and 72 hr post start of chemotherapy; Parts II and IV - Pre-dose and 1.5, 3, 4, 6, 8, 24, 48 and 72 hr post aprepitant dose; Part V - Pre-dose and -0.75, -0.5, 0, 1.5, 3, 4, 6, 8, 24, 48 and 72 hr post start of chemotherapy. (NCT00818259)
Timeframe: Up to 72 hours post fosaprepitant/aprepitant dose

,,,,,
Interventionng/mL (Mean)
6 months to <2 years (n=0, 0, 5, 5, 0, 6, 7)2 years to <6 years (n=0, 0, 8, 7, 0, 6, 7)6 years to <12 years (n=0, 0, 6, 6, 0, 7, 8)12 years to 17 years (n=12, 11, 0, 0, 0, 0, 0)
Part IA-fosaprepitant 115 mg/AprepitantNANANA3240
Part IB-fosaprepitant 150 mgNANANA5870
Part IIA-aprepitant 80 mg Equiv.193013001300NA
Part IIB-aprepitant 125 mg Equiv.65921001930NA
Part IV-aprepitant Regimen181018401800NA
Part V-fosaprepitant Regimen170024302850NA

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Time to Cmax (Tmax) for Aprepitant

Tmax is a measure of the amount of time after dosing to when the maximum concentration of aprepitant was achieved. Fosaprepitant is a prodrug for aprepitant and is rapidly converted to aprepitant after IV administration. Blood samples for PK assessment were collected at the following time points: Part IA - Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 3, 4, 6, 8 and 24 hr post fosaprepitant dose; Part IB - Pre-dose and -0.75, -0.5, 0, 0.5, 1.5, 3, 4, 6, 8, 24, 48 and 72 hr post start of chemotherapy; Parts II and IV - Pre-dose and 1.5, 3, 4, 6, 8, 24, 48 and 72 hr post aprepitant dose; Part V - Pre-dose and -0.75, -0.5, 0, 1.5, 3, 4, 6, 8, 24, 48 and 72 hr post start of chemotherapy. (NCT00818259)
Timeframe: Up to 72 hours post fosaprepitant/aprepitant dose

,,,,,
Interventionhr (Mean)
6 months to <2 years (n=0, 0, 5, 5, 0, 6, 7)2 years to <6 years (n=0, 0, 8, 7, 0, 6, 7)6 years to <12 years (n=0, 0, 6, 6, 0, 7, 8)12 years to 17 years (n=12, 11, 0, 0, 0, 0, 0)
Part IA-fosaprepitant 115 mg/AprepitantNANANA0.41
Part IB-fosaprepitant 150 mgNANANA0.64
Part IIA-aprepitant 80 mg Equiv.2.333.785.17NA
Part IIB-aprepitant 125 mg Equiv.3.455.283.08NA
Part IV-aprepitant Regimen7.344.926.42NA
Part V-fosaprepitant Regimen1.131.411.07NA

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Number of Participants Experiencing Adverse Events (AEs)

An AE is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to the use of the product. Participants were monitored for the occurrence AEs for up to 14 days after last dose of study drug. (NCT00818259)
Timeframe: Up to 14 days after last dose of study drug (Up to 17 days)

InterventionParticipants (Number)
Part IA-fosaprepitant 115 mg/Aprepitant11
Part IB-fosaprepitant 150 mg6
Part IIA-aprepitant 80 mg Equiv.18
Part IIB-aprepitant 125 mg Equiv.16
Part III-ondansetron15
Part IV-aprepitant Regimen13
Part V-fosaprepitant Regimen17

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Number of Participants Discontinuing Study Treatment Due to AEs

(NCT00819039)
Timeframe: Day 1

InterventionParticipants (Number)
Part 1: Oral Aprepitant0
Part 2: Oral Aprepitant0
Part 2: Intravenous Ondansetron0

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Number of Participants Experiencing Adverse Events (AEs)

(NCT00819039)
Timeframe: Up to 21 Days Post-Surgery

InterventionParticipants (Number)
Part 1: Oral Aprepitant20
Part 2: Oral Aprepitant12
Part 2: Intravenous Ondansetron7

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Number of Participants With Complete Response Up to 24 Hours Following Surgery in Study Part 2

Complete response was defined as no vomiting and no use of rescue medication in 0-24 hours post-surgery. (NCT00819039)
Timeframe: Up to 24 Hours

InterventionParticipants (Number)
Part 2: Oral Aprepitant19
Part 2: Intravenous Ondansetron20

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Number of Participants With No Vomiting Up to 24 Hours Following Surgery in Study Part 2

(NCT00819039)
Timeframe: Up to 24 Hours

InterventionParticipants (Number)
Part 2: Oral Aprepitant20
Part 2: Intravenous Ondansetron20

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Number of Participants With No Vomiting Up to 48 Hours Following Surgery Ini Study Part 2

(NCT00819039)
Timeframe: Up to 48 Hours

InterventionParticipants (Number)
Part 2: Oral Aprepitant18
Part 2: Intravenous Ondansetron20

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Area Under the Curve From 0-48 (AUC0-48) of Aprepitant Following a Single Oral Dose in Study Part 1

Blood samples of 0.5 mL were collected from participants for the analysis of AUC0-48 at specified time points: pre-dose, and 1, 2, 3, 4, 8, 12, 24, and 48 hours post aprepitant single dose. (NCT00819039)
Timeframe: Pre-dose, and 1, 2, 3, 4, 8, 12, 24, and 48 hours post-dose

Interventionhr*ug/ml (Mean)
6 months to <2 years (n=11)2 years to <6 years (n=11)6 years to <12 years (n=11)12 years to 17 years (n=10)
Part 1: Oral Aprepitant5.974.766.166.01

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Maximum Plasma Concentration (Cmax) of Aprepitant Following a Single Oral Dose in Study Part 1

Blood samples were collected from participants for the analysis of Cmax up to 48 hours after dosing. (NCT00819039)
Timeframe: 48 Hours Post-Dose

Interventionng/mL (Mean)
6 months to <2 years (n=11)2 years to <6 years (n=11)6 years to <12 years (n=11)12 years to 17 years (n=10)
Part 1: Oral Aprepitant715586913520

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Number of Participants With Vomiting Frequency in Study Part 2

(NCT00819039)
Timeframe: Up to 24 Hours

,
InterventionParticipants (Number)
No Vomiting1 Vomiting Episode2 Vomiting Episodes3 Vomiting Episodes>3 Vomiting Episodes
Part 2: Intravenous Ondansetron203101
Part 2: Oral Aprepitant205000

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Plasma Concentration of Aprepitant at 24 Hours (C24 hr) Following a Single Oral Dose in Study Part 1

Blood samples were collected from participants for the analysis of C24 hr at 24 hours after dosing. N/A indicates that >50% of measurements were below the lower level of quantitaion (LLOQ). (NCT00819039)
Timeframe: 24 Hours Post-Dose

Interventionng/mL (Mean)
6 months to <2 years (n=11)2 years to <6 years (n=11)6 years to <12 years (n=11)12 years to 17 years (n=10)
Part 1: Oral Aprepitant31.058.651.181.1

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Plasma Concentration of Aprepitant at 48 Hours (C48 hr) Following a Single Oral Dose in Study Part 1

The mean plasma concentration of aprepitant was evaluated in participants at 48 hours following a single oral dose. (NCT00819039)
Timeframe: 48 Hours Post-Dose

Interventionng/mL (Mean)
6 months to <2 years (n=11)2 years to <6 years (n=11)6 years to <12 years (n=11)12 years to 17 years (n=10)
Part 1: Oral AprepitantNANANA7.25

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Time to Maximum Plasma Concentration (Tmax) of Aprepitant Following a Single Oral Dose in Study Part 1

Blood samples were collected from participants for the analysis of Tmax up to 48 hours after dosing. (NCT00819039)
Timeframe: 48 Hours Post-Dose

InterventionHours (Median)
6 months to <2 years (n=11)2 years to <6 years (n=11)6 years to <12 years (n=11)12 years to 17 years (n=10)
Part 1: Oral Aprepitant3.003.002.003.50

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Number of Participants With Complete Response Up to 48 Hours Following Surgery in Study Part 2

Complete response was defined as no vomiting and no use of rescue medication in 0-48 hours post-surgery. (NCT00819039)
Timeframe: Up to 48 Hours

InterventionParticipants (Number)
Part 2: Oral Aprepitant17
Part 2: Intravenous Ondansetron20

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Number of Participants With Emesis

This is the number of participants who had an episode of vomiting within 24 hours after emergence from anesthesia. (NCT00888329)
Timeframe: 24 hours after emergence from anesthesia

Interventionparticipants (Number)
Aprepitant6
Placebo17

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Rate of Complete Response to Anti-emetic Therapy in the Delayed Setting (25-120 Hours After Cisplatin Infusion)

(NCT00895245)
Timeframe: 25-120 hours following cisplatin infusion

InterventionParticipants (Count of Participants)
Arm I0

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Proportion of Patients With a Complete Response to the Anti-emetic Medication Regimen

Complete response is defined as no emesis or rescue nausea medications needed in the first 120 hours following cisplatin infusion. (NCT00895245)
Timeframe: 120 hours following cisplatin infusion

InterventionParticipants (Count of Participants)
Arm I0

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Impact of Cisplatin-induced Nausea and Vomiting on Daily Life During the 5 Day Period Following Cisplatin Infusion for Multiple Cycles as Measured by the Functional Living Index-Emesis Questionnaire

"FLIE is a patient-completed quality of life assessment modified from the original Functional Living Index - Cancer questionnaire. FLIE contains two domains: nausea and vomiting with nine items in each domain. The first item asks the patient to rate how much nausea (or vomiting) has occurred over a 5 day period. The remaining eight items ask patients to rate the impact of nausea (or vomiting) on various aspects of a patient's life (for example, ability to enjoy meals/liquids). Each item is answered using a 7 point visual analog scale with 7 being none /not at all and 1 being a great deal. The two domains are summed for a total score with a possible range of 18-126. Higher scores indicate a more favorable quality of life. A total score of >108 defines those patients who had a minimal impact of CINV on quality of life. All particpants discontinued the trial after one cycle of cisplatin." (NCT00895245)
Timeframe: 5 days following cisplatin infusion

Interventionunits on a scale (Mean)
Arm I83.98

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Control of Nausea for 120 Hours Following Each Cisplatin Infusion for Multiple Cycles of Therapy as Measured by the Visual Analog Scale

"The visual analog scale ranges from 0-100. 0 is labeled as no nausea and 100 is labeled as nausea as bad as it could be A score of < 25 is considered to indicate no significant nausea. All patients discontinued trial after only one cisplatin infusion." (NCT00895245)
Timeframe: 120 hours following cisplatin infusion

Interventionmillimeters (Mean)
Arm I45.2

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Alcohol Craving in Response to the Stress Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 30 minutes after the beginning of stress script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant18.0
Placebo18.0

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Alcohol Craving in Response to the Stress Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 5 minutes after the beginning of stress script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant20.9
Placebo25.0

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Alcohol Craving in Response to the Stress Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 60 minutes after the beginning of stress script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant15.9
Placebo17.0

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Alcohol Craving in Response to the Stress Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 45 minutes after the beginning of stress script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant18.1
Placebo18.3

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Alcohol Craving in Response to the Stress Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 75 minutes after the beginning of stress script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant15.9
Placebo16.8

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Alcohol Craving in Response to the Stress Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 90 minutes after the beginning of stress script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant15.9
Placebo14.1

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PTSD Total Symptom Severity Score

PTSD total symptom severity was measured using the Clinician-Administered PTSD Scale (CAPS). This is a 30-item interview-based questionnaire that measures symptom severity during the past week. The total symptom severity score ranges from 0 (lowest symptom severity) to 136 (highest symptom severity). (NCT00896038)
Timeframe: Day 29 of the treatment period, 2 days after the final script presentation

Interventionunits on a scale (Mean)
Aprepitant53.0
Placebo54.2

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Alcohol Craving in Response to the Alcohol Cue Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 15 minutes prior to the beginning of alcohol script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant13.8
Placebo14.0

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Alcohol Craving in Response to the Alcohol Cue Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 15 minutes after the beginning of alcohol script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant16.7
Placebo16.3

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Alcohol Craving in Response to the Stress Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 15 minutes prior to the beginning of stress script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant11.9
Placebo12.9

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Alcohol Craving in Response to the Stress Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 15 minutes after the beginning of stress script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant19.2
Placebo21.7

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Alcohol Craving in Response to the Alcohol Cue Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 90 minutes after the beginning of alcohol script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant14.8
Placebo13.6

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Alcohol Craving in Response to the Alcohol Cue Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 75 minutes after the beginning of alcohol script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant15.6
Placebo13.6

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Alcohol Craving in Response to the Alcohol Cue Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 60 minutes after the beginning of alcohol script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant14.3
Placebo14.4

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Alcohol Craving in Response to the Alcohol Cue Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 5 minutes after the beginning of alcohol script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant19.7
Placebo20.7

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Alcohol Craving in Response to the Alcohol Cue Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 45 minutes after the beginning of alcohol script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant14.7
Placebo15.1

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Alcohol Craving in Response to the Alcohol Cue Script

Alcohol craving was measured using the Alcohol Urges Questionnaire (AUQ). The AUQ is an 8-item self-administered instrument that assesses craving for alcohol among alcohol users in the current context (i.e., right now). The score ranges from 8 (lowest craving value) to 56 (highest craving value). (NCT00896038)
Timeframe: 30 minutes after the beginning of alcohol script presentation, which occurred on Day 25, 26, or 27 of the treatment period

Interventionunits on a scale (Mean)
Aprepitant16.5
Placebo14.4

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Area Under the Curve (AUC(0 to Infinity)) Following Single Dose Administration of Aprepitant 165 mg or 185 mg and Fosaprepitant 150 mg

(NCT00945321)
Timeframe: Through 72 Hours Postdose

Interventionng•hr/mL (Mean)
165 mg Aprepitant (Fasted State)34589
185 mg Aprepitant (Fasted State)39053
150 mg Fosaprepitant Dimeglumine (Fasted State)37375
165 mg Aprepitant (Light)37795
165 mg Aprepitant (High-Fat)50172
185 mg Aprepitant (Light)51146
185 mg Aprepitant (High-Fat)60578

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Peak Plasma Concentration (Cmax) Following Single Dose Administration of Aprepitant 165 mg or 185 mg and Fosaprepitant 150 mg.

(NCT00945321)
Timeframe: Through 72 Hours Postdose

Interventionng/mL (Mean)
165 mg Aprepitant (Fasted State)1738
185 mg Aprepitant (Fasted State)1636
165 mg Aprepitant (Light)1870
165 mg Aprepitant (High-Fat)2362
185 mg Aprepitant (Light)2116
185 mg Aprepitant (High-Fat)1995

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Time to First Vomiting Episode in Cycle 1

Time from administration of chemotherapy to first vomiting episode. (NCT00952341)
Timeframe: 0 to 120 hours

InterventionHours (Mean)
Aprepitant (MK-0869)77.0
Placebo76.0

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Proportion of Participants With Complete Response 120 Hours Following Initiation of High-dose Cisplatin Chemotherapy in the Overall Phase of Cycle 1

"Overall phase was defined as 0 to 120 hours following initiation of chemotherapy.~Complete response was defined as no vomiting with no rescue therapy." (NCT00952341)
Timeframe: 0 to 120 hours

InterventionProportion of participants (Number)
Aprepitant (MK-0869)0.696
Placebo0.570

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Proportion of Participants With Complete Response in the Acute Phase of Cycle 1

"Acute phase was defined as 0 to 24 hours following initiation of chemotherapy.~Complete response was defined as no vomiting with no rescue therapy." (NCT00952341)
Timeframe: 0 to 24 hours

InterventionProportion of participants (Number)
Aprepitant (MK-0869)0.794
Placebo0.793

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Proportion of Participants With Complete Response in the Delayed Phase of Cycle 1

"Delayed phase was defined as 25 to 120 hours following initiation of chemotherapy.~Complete response was defined as no vomiting with no rescue therapy." (NCT00952341)
Timeframe: 25 to 120 hours

InterventionProportion of participants (Number)
Aprepitant (MK-0869)0.740
Placebo0.594

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Proportion of Participants With No Impact on Daily Life in Cycle 1

"The Functional Living Index-Emesis is a self-administered, validated emesis & nausea-specific questionnaire. Participants completed the questionnaire 5 days post chemotherapy. It had 9 questions each on nausea and vomiting. No impact of chemotherapy-induced nausea & vomiting (CINV) on daily life was defined as an average item score of >6 on the 7-point scale (i.e., >108 total score). The scale was in the opposite direction for questions 3, 6, 11, 15 & 18. For each question: score ranged from 1 (worst) to 7 (best, i.e., no CINV). Total score range was 7 (worst) to 126 (best)." (NCT00952341)
Timeframe: 0 to 120 hours

InterventionProportion of participants (Number)
Aprepitant (MK-0869)0.705
Placebo0.683

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Proportion of Participants With No Vomiting in the Acute Phase of Cycle 1

Acute Phase was defined as 0 to 24 hours following initiation of chemotherapy. (NCT00952341)
Timeframe: 0 to 24 hours

InterventionProportion of participants (Number)
Aprepitant (MK-0869)0.804
Placebo0.798

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Proportion of Participants With No Vomiting in the Delayed Phase of Cycle 1

Delayed Phase was defined as 25 to 120 hours following initiation of chemotherapy (NCT00952341)
Timeframe: 25 to 120 hours

InterventionProportion of participants (Number)
Aprepitant (MK-0869)0.740
Placebo0.594

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Proportion of Participants With No Vomiting in the Overall Phase of Cycle 1

"Overall Phase was defined as 0 to 120 hours following initiation of chemotherapy.~No vomiting was defined as no vomiting or retching or dry heaves (included participants who received rescue therapy)." (NCT00952341)
Timeframe: 0 to 120 hours

InterventionProportion of participants (Number)
Aprepitant (MK-0869)0.706
Placebo0.570

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Treatment Success Rate

Treatment success is defined as no nausea, no vomiting and no need for rescue medication (or complete response) within the first 6 treatment days. Treatment success rate defined as percentage of participants achieving treatment success. (NCT00954941)
Timeframe: First 6 treatment days

Interventionpercentage of participants (Number)
Group 1: Ondansetron48
Group 2: Ondansetron + Aprepitant51

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Participant Responses

Participant response defined as: Complete response - no emetic episode, no nausea and no rescue medication during the administration of chemotherapy; Partial response - less than or equal to one episode of emesis in 24 hours, no rescue medication, and no more than moderate nausea (grade 2 National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE)) during chemotherapy. Vomit was defined as expulsion of stomach contents through the mouth, nausea as stomach distress with distaste for food and an urge to vomit, and rescue medication as antiemetic medications given to treat nausea and/or vomit that did not respond to the initial prophylactic regimen. Treatment success was defined as no nausea, no vomiting and no need for rescue medication within the first 6 treatment days with continuous monitoring. (NCT00954941)
Timeframe: First 6 treatment days

,
Interventionparticipants (Number)
Complete ResponsePartial ResponseNo Response
Group 1: Ondansetron20913
Group 2: Ondansetron + Aprepitant21128

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Area Under the Plasma-Time Curve (AUC[0 to Infinity]) for Aprepitant and MK-0517 for Study Part V

AUC (0-inf) is the area under the plasma concentration-time curve from time zero extrapolated to infinite time. The AUC(0-inf) bioequivalence was evaluated for single doses of 100 and 115 mg MK-0517 PS80, IV and that of an oral 125-mg capsule of aprepitant. Period I to IV populations are not included in the outcome analysis because those were formulation and dose-finding/dose confirmation arms. (NCT00990821)
Timeframe: Up to 72 Hours Post Dose

Interventionng*hr/mL (Least Squares Mean)
Aprepitant (125 mg)29215
MK-0517 (100 mg)24961
MK-0517 (115 mg)31724

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Respiration Depression

Respiration rate measured over 60 seconds. Data were collected across multiple time points, but the peak minimum score was used for this outcome measure. (NCT00999544)
Timeframe: 42 days

Interventionnumber of breaths per minute (Mean)
Placebo Aprepitant/0 mg Oxycodone IN PO13.75
Placebo Aprepitant/ Oxycodone 15 IN 0 PO11.63
Placebo Aprepitant/ Oxycodone 30 IN 0 PO11.25
Placebo Aprepitant/ Oxycodone 0 IN 20 PO12.13
Placebo Aprepitant/ Oxycodone 0 IN 40 PO10.25
Aprepitant 40 mg/ Oxycodone 0 IN 0 PO12.25
Aprepitant 40 mg/ Oxycodone 0 IN 20 PO12.25
Aprepitant 40 mg/ Oxycodone 0 IN 40 PO11.00
Aprepitant 40 mg/ Oxycodone 15 IN 0 PO12.38
Aprepitant 40 mg/ Oxycodone 30 IN 0 PO11.63
Aprepitant 200 mg/ Oxycodone 0 IN 0 PO14.00
Aprepitant 200 mg/ Oxycodone 0 IN 20 PO14.00
Aprepitant 200 mg/ Oxycodone 0 IN 40 PO12.13
Aprepitant 200 mg/ Oxycodone 15 IN 0 PO12.00
Aprepitant 200 mg/ Oxycodone 30 IN 0 PO11.38

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Abuse Liability Proxy

"Visual analog scale ratings (from 0-100) on the subject-rated measure of How much do you like the drug? with higher scores indicating greater abuse liability (and 100 anchored with extremely and zero indicating none anchored with none at all. Data were collected across multiple time points but the peak maximum score was used for the primary outcome measure." (NCT00999544)
Timeframe: 42 days

Interventionunits on a scale (points 0-100) (Mean)
Placebo-Placebo (in and po)0.197
Aprepitant 40 mg - Placebo0.483
Aprepitant 200 mg- Placebo0.159
Placebo- 15 mg Oxycodone Intranasal7.678
Placebo- 30 mg Oxycodone Intranasal17.450
Placebo- 20 mg Oxycodone Oral9.850
Placebo - 40 mg Oxycodone Oral16.646
Aprepitant 40 mg- 15 mg Oxycodone Intranasal8.543
Aprepitant 40 mg - 30 mg Oxycodone Intranasal15.092
Aprepitant 40 mg- 20 mg Oxycodone Oral13.281
Aprepitant 40 mg - 40 mg Oxycodone Oral17.244
Aprepitant 200 mg - 15 mg Oxycodone Intranasal17.195
Aprepitant 200 mg - 30 mg Oxycodone Intranasal28.211
Aprepitant 200 mg- 20 Oxycodone Oral8.196
Aprepitant 200 mg- 40 Oxycodone Oral26.322

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Efficacy of the Aprepitant/Ramosetron/Dexamethasone Regimen in Terms of the Proportion of Patients With a Complete Response (CR) During the 120 Hour Following Initiation of Chemotherapy.

Complete Response is defined as No vomiting with no rescue therapy. These response criteria will be applied to the following time periods: Overall: from 0 (chemotherapy initiation) to the morning of day 6, Acute: 0 to 24 hours following the initiation of chemotherapy, Delayed: 25 hours to the morning of day 6(D6). (NCT01012336)
Timeframe: 120 hours

InterventionPercentage of Participants (Number)
Aprepitant89.4

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Participants With Specific Side Effects, Including Pain Sensation/Soreness at the Infusion Site, Headache, and Dizziness

Participants who self report pain/soreness at drug infusion site, headache, or dizziness at any of the study time points (2, 12, or 24 hours after receiving fosaprepitant) are measured in this outcome. (NCT01031953)
Timeframe: up to 24 hours after study drug administered.

Interventionparticipants (Number)
Participants That Received Fosaprepitant5

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Improvement in Nausea Score From 2 Hours to 24 Hours

"The outcome measure is the number of participants that self report improvement in a nausea score from 2 hours after receiving fosaprepitant to 24 hours post dose. This includes only participants who report breakthrough nausea or vomiting after chemotherapy and after receiving prophylactic anti-emetics. The outcome is measured using the visual analogue scale, a self report scale from No Nausea to Nausea as bad as it can be; a value can be indicated anywhere on this scale using a free hand mark by the participant and gauged with ruler by study staff. Any participant reporting a lower value on the scale at the 12 or 24 hour time point would be considered in this outcome measure." (NCT01031953)
Timeframe: 2 hours to 24 hours after study drug administered.

Interventionparticipants (Number)
Change in Nausea Score From 2 Hours to 12 and 24 Hours7

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Improvement in Nausea Score From Baseline to 2 Hours as Assessed by the Numerical Visual Analogue Scale

"The outcome measure is the number of participants that self report improvement in a nausea score from baseline, prior to fosaprepitant, to 2 hours post dose. This includes only participants who report breakthrough nausea or vomiting after chemotherapy and after receiving prophylactic anti-emetics. The primary outcome is measured using the visual analogue scale, a self report scale from No Nausea to Nausea as bad as it can be; a value can be indicated anywhere on this scale using a free hand mark by the participant and gauged with ruler by study staff. Any participant that reported a lower value on the scale 2 hours from baseline would be considered in this outcome measure." (NCT01031953)
Timeframe: Baseline to 2 hours after study drug administered.

Interventionparticipants (Number)
Participants Receiving Fosaprepitant10

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Number of Participants Who Experienced Vomiting Episodes From Baseline to 24 Hours

Participants were asked to report any episodes of vomiting before (baseline) and up to 24 hours after receiving Fosaprepitant. The outcome considers the number of participants reporting any episodes of emesis after receiving Fosaprepitant. (NCT01031953)
Timeframe: Baseline to 24 hours after study drug administered.

Interventionparticipants (Number)
Participants Who Recieved Fosaprepitant2

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Participants Achieving a Complete Response (no Emesis, no Additional Rescue Medication Required)

The recommended dose Fosaprepitant (MK-0517) is 115 mg administered intravenously 30 minutes before chemotherapy treatment. In this study, a 150 mg dose will be given to study patients as rescue therapy after chemotherapy only in the event of breakthrough nausea or vomiting. Those participants who did not report episodes of emesis or did not require additional rescue medications are measured in this outcome (NCT01031953)
Timeframe: up to 24 hours after receiving fosaprepitant

Interventionparticipants (Number)
Participants That Received Fosaprepitant1

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Improvement in Nausea Score From Baseline to 12 Hours

"The outcome measure is the number of participants that self report improvement in a nausea score from baseline, prior to fosaprepitant, to 12 hours post dose. This includes only participants who report breakthrough nausea or vomiting after chemotherapy and after receiving prophylactic anti-emetics. The primary outcome is measured using the visual analogue scale, a self report scale from No Nausea to Nausea as bad as it can be; a value can be indicated anywhere on this scale using a free hand mark by the participant and gauged with ruler by study staff. Any participant that reported a lower value on the scale 12 hours from baseline would be considered in this outcome measure." (NCT01031953)
Timeframe: Baseline to 12 hours after study drug administered.

Interventionparticipants (Number)
Participants Receiving Fosaprepitant11

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Participants Who Required the Use of Second Rescue Drug (Time to Treatment Failure)

Participants with persistent nausea/vomiting after 2 hours and who desired further treatment, received standard rescue therapy at the discretion of provider with prochlorperazine, metoclopramide or haloperidol with or without additional lorazepam until relief (NCT01031953)
Timeframe: 2 hours after administration of Fosaprepitant 150 mg IV

Interventionparticipants (Number)
Participants That Received Fosaprepitant9

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Participants With Increased Fatigue or Sedation Within 24 Hours After Receiving Fosaprepitant

Participants meeting this outcome self report experiencing drowsiness at any of the study time points (2, 12 or 24 hours after receiving fosaprepitant). (NCT01031953)
Timeframe: up to 24 hours after study drug administered.

Interventionparticipants (Number)
Participants That Received Fosaprepitant7

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Investigator Global Assessment of Participants' Response to Therapy With EMEND (Aprepitant) for the Prevention of Acute and Delayed Nausea Following Chemotherapy

The investigators assessed a participant's response to therapy with EMEND to prevent acute and delayed nausea and vomiting associated with initial and repeat courses of chemotherapy when used concomitantly with other antiemetics. The response categories were: excellent (best possible anticipated response, considering the severity and stage of disease), good (good response, but less than the best possible anticipated response), fair (definite response, but could be better), poor (minimal response, unacceptable), or none (no response, absence of drug effect). (NCT01074255)
Timeframe: Up to 14 days following the cessation of treatment

Interventionparticipants (Number)
ExcellentGoodFairPoorNone
Participants Treated With EMEND4382056446523

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Brain NK1-receptor Occupancy at 120 Hours Post Dose

(NCT01111851)
Timeframe: 120 hours post dose

InterventionPercent of occupancy (Geometric Mean)
Fosaprepitant 150 mg59.93
Aprepitant 165 mg54.32

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Brain NK1-receptor Occupancy at 48 Hours Post Dose

(NCT01111851)
Timeframe: 48 hours post dose

InterventionPercent of occupancy (Geometric Mean)
Fosaprepitant 150 mg98.62
Aprepitant 165 mg98.79

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Brain NK1-receptor Occupancy at 24 Hours Post Dose

(NCT01111851)
Timeframe: 24 hours post dose

InterventionPercent of occupancy (Geometric Mean)
Fosaprepitant 150 mg100.40
Aprepitant 165 mg100.20

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Brain NK1-receptor Occupancy at the Time of the Maximum Concentration (Tmax)

(NCT01111851)
Timeframe: 30 minutes after the end of the 20-minute infusion of fosaprepitant or at 4 hours after oral dosing of aprepitant

InterventionPercent of occupancy (Geometric Mean)
Fosaprepitant 150 mg100.25
Aprepitant 165 mg99.99

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PAGI-SYM Severity Index: Heartburn During the Day Severity

The PAGI-SYM Severity index: Heartburn during the day severity is the participant's assessment of heartburn (burning pain rising in your chest or throat) during the day over the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Heartburn During the Day severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.2
Aprepitant-placebo-0.6

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PAGI-SYM Severity Index: Heartburn When Lying Down Severity

The PAGI-SYM Severity index: Heartburn when lying down severity is the participant's assessment of heartburn (burning pain rising in your chest or throat) when lying down over the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Heartburn When Lying Down severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.2
Aprepitant-placebo-0.7

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PAGI-SYM Severity Index: Loss of Appetite Severity

PAGI-SYM Severity index: Loss of appetite severity is the participant's assessment of loss of appetite during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Loss of appetite severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.9
Aprepitant-placebo-0.9

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PAGI-SYM Severity Index: Lower Abdominal Discomfort Severity

The PAGI-SYM Severity index: Lower Abdominal Discomfort severity is the participant's assessment of lower abdominal discomfort (below the navel) during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Lower Abdominal Discomfort severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.1
Aprepitant-placebo-0.6

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PAGI-SYM Severity Index: Lower Abdominal Pain Severity

The PAGI-SYM Severity index: Lower Abdominal Pain severity is the participant's assessment of lower abdominal pain (below the navel) during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Lower Abdominal Pain severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.8
Aprepitant-placebo-0.6

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PAGI-SYM Severity Index: Nausea Severity

The PAGI-SYM Severity index: Nausea severity is the participant's assessment of nausea (feeling sick to your stomach as if you were going to vomit or throw up) during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Nausea Severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.8
Aprepitant-placebo-1.0

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PAGI-SYM Severity Index: Nausea/Vomiting Severity Subscore

The PAGI-SYM Severity index: Nausea/vomiting severity subscore is the average of 3 items: nausea, retching, and vomiting. Each item is the participant's assessment of severity of the symptom during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Nausea/vomiting severity subscore, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.7
Aprepitant-placebo-0.7

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PAGI-SYM Severity Index: Regurgitation During the Day Severity

The PAGI-SYM Severity index: Regurgitation during the day severity is the participant's assessment of regurgitation or reflux (fluid or liquid from your stomach coming up into throat) during the day over the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Regurgitation During the Day severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.2
Aprepitant-placebo-0.5

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PAGI-SYM Severity Index: Regurgitation When Lying Down Severity

The PAGI-SYM Severity index: Regurgitation when lying down severity is the participant's assessment of regurgitation or reflux (fluid or liquid from your stomach coming up into throat) when lying down over the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Regurgitation When Lying Down severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.3
Aprepitant-placebo-0.5

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PAGI-SYM Severity Index: Retching Severity

The PAGI-SYM Severity index: Retching Severity is the participant's assessment of retching (heaving as if to vomit, but nothing comes up) during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Retching Severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.7
Aprepitant-placebo-0.8

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PAGI-SYM Severity Index: Stomach Distention Severity

The PAGI-SYM Severity index: Stomach distention severity is the participant's assessment of stomach distention (stomach or belly visibly larger) during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Stomach Distention severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.1
Aprepitant-placebo-0.7

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PAGI-SYM Severity Index: Stomach Fullness Severity

PAGI-SYM Severity index: Stomach Fullness severity is the participant's assessment of stomach fullness during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Stomach Fullness severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.1
Aprepitant-placebo-0.5

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PAGI-SYM Severity Index: Unable to Finish Meal Severity

PAGI-SYM Severity index: Unable to Finish Meal severity is the participant's assessment of being unable to finish a normal size meal during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Unable to Finish Meal severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.8
Aprepitant-placebo-0.6

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PAGI-SYM Severity Index: Upper Abdominal Discomfort Severity

The PAGI-SYM Severity index: Upper Abdominal Discomfort severity is the participant's assessment of upper abdominal discomfort (above the navel) during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Upper Abdominal Discomfort severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.2
Aprepitant-placebo-0.7

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PAGI-SYM Severity Index: Upper Abdominal Pain Severity

The PAGI-SYM Severity index: Upper Abdominal Pain severity is the participant's assessment of upper abdominal pain (above the navel) during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Upper Abdominal Pain severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.0
Aprepitant-placebo-0.5

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PAGI-SYM Severity Index: Upper Abdominal Pain Subscore

The PAGI-SYM Severity index: Upper Abdominal Pain subscore is the average of 2 items (upper abdominal pain, upper abdominal discomfort). Each item is the participant's assessment of severity of the symptom during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Upper Abdominal Pain Subscore, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.1
Aprepitant-placebo-0.6

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PAGI-SYM Severity Index: Vomiting Severity

The PAGI-SYM Severity index: Vomiting Severity is the participant's assessment of vomiting during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Vomiting Severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.6
Aprepitant-placebo-0.5

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PAGI-SYM Severity: Bitter Taste Severity

The PAGI-SYM Severity index: Bitter Taste severity is the participant's assessment of bitter, acid, or sour taste in mouth during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Bitter Taste Severity score, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.8
Aprepitant-placebo-0.5

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Platelet Count

Change from baseline in platelet count (NCT01149369)
Timeframe: 4 weeks

Interventionx10^3 cells/microliter (Mean)
Aprepitant-7.3
Aprepitant-placebo4.8

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Potassium

Change from baseline in potassium (mEq/L) (NCT01149369)
Timeframe: 4 weeks

InterventionmEq/L (Mean)
Aprepitant0.1
Aprepitant-placebo0.0

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Red Blood Cell Count (RBC)

Change from baseline in red blood cell count (RBC) (NCT01149369)
Timeframe: 4 weeks

Interventionx10^6 cells/microliter (Mean)
Aprepitant-0.1
Aprepitant-placebo-0.1

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Satiety Test, Volume Consumed

The Satiety Test measures the total volume of liquid (Ensure) that the participant is able to consume. The participant drinks 150 mL of Ensure every 5 minutes until he/she is completely full. The outcome measure is the change from baseline in volume of liquid (Ensure) consumed (mL), where positive values indicate a positive outcome (improvement). (NCT01149369)
Timeframe: 4 weeks

InterventionmL (Median)
Aprepitant-13.0
Aprepitant-placebo9.2

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Sodium

Change from baseline in sodium (mEq/L) (NCT01149369)
Timeframe: 4 weeks

InterventionmEq/L (Mean)
Aprepitant-0.3
Aprepitant-placebo-0.7

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State-Trait Anxiety Inventory (STAI): State Anxiety Score

The State-Trait Anxiety Inventory (STAI): State anxiety score is the sum of scores from 20 questions relating to state anxiety, which is a temporary state varying in intensity. The possible range of scores is from 20 to 80, with increasing scores considered a worse outcome. The outcome measure, change from baseline in STAI State Anxiety score, has a possible range from -60 to +60, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-3.1
Aprepitant-placebo-1.7

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State-Trait Anxiety Inventory (STAI): Trait Anxiety Score

The State-Trait Anxiety Inventory (STAI): Trait anxiety score is the sum of scores from 20 questions pertaining to trait anxiety, which is a general propensity to be anxious. The possible range of scores is from 20 to 80, with increasing scores considered a worse outcome. The outcome measure, change from baseline in STAI Trait Anxiety score, has a possible range from -60 to +60, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.8
Aprepitant-placebo-0.7

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White Blood Cell Count (WBC)

Change from baseline in white blood cell count (WBC) (NCT01149369)
Timeframe: 4 weeks

Interventionx10^9 cells/L (Mean)
Aprepitant-0.3
Aprepitant-placebo-0.3

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Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Upper Abdominal Pain Severity

Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Upper Abdominal Pain Severity is the participant's assessment of upper abdominal pain (above the navel) during the past 24 hours, where 0=none, 1=mild, 2=moderate, 3=severe, and 4=very severe. The range of scores is 0 to 4, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Upper Abdominal Pain Severity, has a possible range from -4 to +4, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.7
Aprepitant-placebo-0.3

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Beck Depression Inventory (BDI) Score

The Beck Depression Inventory (BDI) survey is comprised of 21 multiple choice questions that relate to depression, cognition, and physical well-being and is used to quantify depression. The BDI total score is the sum of the 21 items, where each item ranges from 0 to 3 (lower scores are less severe, higher scores are more severe). The range for the BDI total score is 0 to 63, where lower scores indicate less depression and higher scores indicate more severe depression. The outcome measure, change from baseline in BDI score, has a possible range from -63 to +63, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-4.6
Aprepitant-placebo-2.4

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Blood Urea Nitrogen (BUN)

Change from baseline in blood urea nitrogen (BUN) (mg/dL) (NCT01149369)
Timeframe: 4 weeks

Interventionmg/dL (Mean)
Aprepitant-0.9
Aprepitant-placebo-0.3

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Brief Pain Inventory: Interference Score

The Brief Pain Inventory: Interference Score is the average of seven questions in which the participant rates the degree to which his or her pain interferes with daily functions and mood: general activity, mood, walking ability, normal work, relationships, sleep, enjoyment of life. The range of possible scores is 0 to 10, with higher scores indicating more interference caused by pain. The outcome measure, change from baseline in Brief Pain Inventory Interference Score, has a possible range from -10 to +10, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.1
Aprepitant-placebo-1.0

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Brief Pain Inventory: Severity Score

The Brief Pain Inventory: Severity Score is the average of four questions in which the participant rates his or her pain: the worse pain in the past 24 hours, the least pain in the past 24 hours, average pain, and pain right now. The range of possible scores is 0 to 10, with higher scores indicating more severe pain. The outcome measure, change from baseline in Brief Pain Inventory Severity Score, has a possible range from -10 to +10, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.0
Aprepitant-placebo-0.7

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Calcium

Change from baseline in calcium (mg/dL) (NCT01149369)
Timeframe: 4 weeks

Interventionmg/dL (Mean)
Aprepitant-0.1
Aprepitant-placebo-0.1

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Carbon Dioxide

Change from baseline in carbon dioxide (mEg/L) (NCT01149369)
Timeframe: 4 weeks

InterventionmEq/L (Mean)
Aprepitant-0.4
Aprepitant-placebo0.4

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Chloride

Change from baseline in chloride (mEq/L) (NCT01149369)
Timeframe: 4 weeks

InterventionmEq/L (Mean)
Aprepitant0.6
Aprepitant-placebo-0.2

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Clinical Global Patient Impression Score (Patient-rated)

The Clinical Global Patient Impression Score quantifies the overall relief of the patient's symptom, by asking the participant to consider how they felt over the past week in regard to stomach symptoms and overall well-being, and rate relief of symptoms in comparison to how they felt before entering the study. Possible scores are: -3=very considerably worse, -2=considerably worse, -1=somewhat worse, 0=unchanged, 1=somewhat better, 2=considerably better, 3=completely better. The range of scores is -3 to 3, where higher scores are considered a better outcome. The outcome measure, change from baseline in Clinical Global Patient Impression Score, has a possible range of -6 to +6, with positive values indicating a better outcome (improvement) and negative values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant1.3
Aprepitant-placebo1.0

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Creatinine

Change from baseline in creatinine (mg/dL) (NCT01149369)
Timeframe: 4 weeks

Interventionmg/dL (Mean)
Aprepitant-0.1
Aprepitant-placebo0.0

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Electrogastrography (EGG): Bradygastria (1-<2.5 Cpm) at 4 Weeks, 0-30 Post-satiety Measurement

Electrogastrography (EGG) is a test which records the electrical pacemaking signals that travel through the stomach muscles and control the muscles' contractions. The 0-30 post-satiety measurement of the test is that taken 30 minutes after the participant consumes Ensure until feeling completely full. Normal pacing is considered 2.5-3.7 cycles per minute (cpm). Bradygastria is when the rate of electrical activity in the stomach is <2.5 cycles per minute for at least 1 minute. Average power in frequency region is the % of time that the dominant EGG frequencies are in a given frequency: bradygastria, normal, tachygastria, or duodenal. The outcome measure is the change from baseline (baseline refers to test performed during screening, not baseline value of the EGG test) in % of time with frequencies in the ranges. Negative values for bradygastria indicate improvement (less time in a dysrhythmic state). (NCT01149369)
Timeframe: 4 weeks

Interventionaverage power in frequency region, % (Mean)
Aprepitant2.1
Aprepitant-placebo0.5

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Electrogastrography (EGG): Bradygastria (1-<2.5 Cpm) at 4 Weeks, Baseline Measurement

Electrogastrography (EGG) is a test which records the electrical pacemaking signals that travel through the stomach muscles and control the muscles' contractions. Normal pacing is considered 2.5-3.7 cycles per minute (cpm). Bradygastria is when the rate of electrical activity in the stomach is <2.5 cycles per minute for at least 1 minute (a decrease in electrical activity in the stomach). The average power in frequency region is the percentage of time that the dominant EGG frequencies are in a given frequency: bradygastria, normal, tachygastria, or duodenal. The outcome measure is the change from baseline (here, baseline refers to the test performed during screening, not the baseline value of the EGG test) in percent of time with frequencies in the ranges, where negative values for bradygastria indicate improvement (less time in a dysrhythmic state). (NCT01149369)
Timeframe: 4 weeks

Interventionaverage power in frequency region, % (Mean)
Aprepitant-4.6
Aprepitant-placebo2.8

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Electrogastrography (EGG): Duodenal (>10-15 Cpm) at 4 Weeks, 0-30 Post-satiety Measurement

Electrogastrography (EGG) is a test which records the electrical pacemaking signals that travel through the stomach muscles and control the muscles' contractions. The 0-30 post-satiety measurement that taken 30 minutes after the participant consumes Ensure until feeling completely full. Normal pacing is considered 2.5-3.7 cycles per minute (cpm). Duodenal is when the rate of electrical activity in the stomach is >10-15 cycles per minute for at least 1 minute. The average power in frequency region is the percentage of time that the dominant EGG frequencies are in a given frequency: bradygastria, normal, tachygastria, or duodenal. The outcome measure is the change from baseline (here, baseline refers to the test performed during screening, not the baseline value of the EGG test) in percent of time with frequencies in the ranges, where negative values for duodenal indicate improvement (less time in a dysrhythmic state). (NCT01149369)
Timeframe: 4 weeks

Interventionaverage power in frequency region, % (Mean)
Aprepitant-0.8
Aprepitant-placebo-0.5

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Electrogastrography (EGG): Duodenal (>10-15 Cpm) at 4 Weeks, Baseline Measurement

Electrogastrography (EGG) is a test which records the electrical pacemaking signals that travel through the stomach muscles and control the muscles' contractions. Normal pacing is considered 2.5-3.7 cycles per minute (cpm). Duodenal is when the rate of electrical activity in the stomach is >10-15 cycles per minute for at least 1 minute. The average power in frequency region is the percentage of time that the dominant EGG frequencies are in a given frequency: bradygastria, normal, tachygastria, or duodenal. The outcome measure is the change from baseline (here, baseline refers to the test performed during screening, not the baseline value of the EGG test) in percent of time with frequencies in the ranges, where negative values for duodenal indicate improvement (less time in a dysrhythmic state). (NCT01149369)
Timeframe: 4 weeks

Interventionaverage power in frequency region, % (Mean)
Aprepitant2.1
Aprepitant-placebo-0.2

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Electrogastrography (EGG): Normogastria (2.5-<3.8 Cpm) at 4 Weeks, 0-30 Post-satiety Measurement

Electrogastrography (EGG) is a test which records the electrical pacemaking signals that travel through the stomach muscles and control the muscles' contractions. The 0-30 post-satiety measurement that taken 30 minutes after the participant consumes Ensure until feeling completely full. Normal pacing (normogastria) is considered 2.5-3.7 cycles per minute (cpm). The average power in frequency region is the percentage of time that the dominant EGG frequencies are in a given frequency: bradygastria, normal, tachygastria, or duodenal. The outcome measure is the change from baseline (baseline refers to the test performed during screening, not the baseline value of the EGG test) in percent of time with frequencies in the ranges, where positive values for normal rates indicate an increase in the normal pacing (improvement). (NCT01149369)
Timeframe: 4 weeks

Interventionaverage power in frequency region, % (Mean)
Aprepitant1.0
Aprepitant-placebo0.8

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Electrogastrography (EGG): Normogastria (2.5-<3.8 Cpm) at 4 Weeks, Baseline Measurement

Electrogastrography (EGG) is a test which records the electrical pacemaking signals that travel through the stomach muscles and control the muscles' contractions. Normal pacing (normogastria) is considered 2.5-3.7 cycles per minute (cpm). The average power in frequency region is the percentage of time that the dominant EGG frequencies are in a given frequency: bradygastria, normal, tachygastria, or duodenal. The outcome measure is the change from baseline (here, baseline refers to the test performed during screening, not the baseline value of the EGG test) in percent of time with frequencies in the ranges, where positive values for normal rates indicate an increase in the normal pacing (improvement). (NCT01149369)
Timeframe: 4 weeks

Interventionaverage power in frequency region, % (Mean)
Aprepitant1.0
Aprepitant-placebo-1.0

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Electrogastrography (EGG): Tachygastria (3.8-10 Cpm) at 4 Weeks, 0-30 Post-satiety Measurement

Electrogastrography (EGG) is a test which records the electrical pacemaking signals that travel through the stomach muscles and control the muscles' contractions. The 0-30 post-satiety measurement that taken 30 minutes after the participant consumes Ensure until feeling completely full. Normal pacing is considered 2.5-3.7 cycles per minute (cpm). Tachygastria is when the rate of electrical activity in the stomach is 3.8-10 cycles per minute for at least 1 minute (an increase in electrical activity in the stomach). The average power in frequency region is the percentage of time that the dominant EGG frequencies are in a given frequency: bradygastria, normal, tachygastria, or duodenal. The outcome measure is the change from baseline (here, baseline refers to the test performed during screening, not the baseline value of the EGG test) in percent of time with frequencies in the ranges, where negative values for tachygastria indicate improvement (less time in a dysrhythmic state). (NCT01149369)
Timeframe: 4 weeks

Interventionaverage power in frequency region, % (Mean)
Aprepitant-2.1
Aprepitant-placebo-0.8

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Electrogastrography (EGG): Tachygastria (3.8-10 Cpm) at 4 Weeks, Baseline Measurement

Electrogastrography (EGG) is a test which records the electrical pacemaking signals that travel through the stomach muscles and control the muscles' contractions. Normal pacing is considered 2.5-3.7 cycles per minute (cpm). Tachygastria is when the rate of electrical activity in the stomach is 3.8-10 cycles per minute for at least 1 minute (an increase in electrical activity in the stomach). The average power in frequency region is the percentage of time that the dominant EGG frequencies are in a given frequency: bradygastria, normal, tachygastria, or duodenal. The outcome measure is the change from baseline (here, baseline refers to the test performed during screening, not the baseline value of the EGG test) in percent of time with frequencies in the ranges, where negative values for tachygastria indicate improvement (less time in a dysrhythmic state). (NCT01149369)
Timeframe: 4 weeks

Interventionaverage power in frequency region, % (Mean)
Aprepitant1.5
Aprepitant-placebo-1.6

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Gastrointestinal Symptom Rating Scale (GSRS): Abdominal Pain Score

The Gastrointestinal Symptom Rating Scale (GSRS) is a 15-item questionnaire for participants with gastrointestinal discomfort. The GSRS Abdominal Pain Score is a measure of how bothered the participant has been by pain or discomfort in the upper abdomen or pit of the stomach during the past week. The range of scores is 0 to 7, where 0 indicates no discomfort and 7 indicates very severe discomfort. Higher scores are considered a worse outcome.The outcome measure, change from baseline in GSRS Abdominal Pain Score, has a possible range from -7 to +7, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 week

Interventionunits on a scale (Mean)
Aprepitant-1.3
Aprepitant-placebo-0.7

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Gastrointestinal Symptom Rating Scale (GSRS): Constipation Score

The Gastrointestinal Symptom Rating Scale (GSRS) is a 15-item questionnaire for participants with gastrointestinal discomfort. The GSRS Constipation Score is a measure of how bothered the participant has been by constipation during the past week. The range of scores is 0 to 7, where 0 indicates no discomfort and 7 indicates very severe discomfort. Higher scores are considered a worse outcome.The outcome measure, change from baseline in GSRS Constipation Score, has a possible range from -7 to +7, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.8
Aprepitant-placebo-0.4

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Gastrointestinal Symptom Rating Scale (GSRS): Diarrhea Score

The Gastrointestinal Symptom Rating Scale (GSRS) is a 15-item questionnaire for participants with gastrointestinal discomfort. The GSRS Diarrhea Score is a measure of how bothered the participant has been by diarrhea during the past week. The range of scores is 0 to 7, where 0 indicates no discomfort and 7 indicates very severe discomfort. Higher scores are considered a worse outcome.The outcome measure, change from baseline in GSRS Diarrhea Score, has a possible range from -7 to +7, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.5
Aprepitant-placebo0.1

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Gastrointestinal Symptom Rating Scale (GSRS): Indigestion Score

The Gastrointestinal Symptom Rating Scale (GSRS) is a 15-item questionnaire for participants with gastrointestinal discomfort. The GSRS Indigestion Score is a measure of how bothered the participant has been by indigestion during the past week. The range of scores is 0 to 7, where 0 indicates no discomfort and 7 indicates very severe discomfort. Higher scores are considered a worse outcome.The outcome measure, change from baseline in GSRS Indigestion Score, has a possible range from -7 to +7, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.7
Aprepitant-placebo-0.7

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Gastrointestinal Symptom Rating Scale (GSRS): Reflux Score

The Gastrointestinal Symptom Rating Scale (GSRS) is a 15-item questionnaire for participants with gastrointestinal discomfort. The GSRS Reflux Score is a measure of how bothered the participant has been by acid reflux during the past week. The range of scores is 0 to 7, where 0 indicates no discomfort and 7 indicates very severe discomfort. Higher scores are considered a worse outcome.The outcome measure, change from baseline in GSRS Reflux Score, has a possible range from -7 to +7, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.1
Aprepitant-placebo-0.7

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Gastrointestinal Symptom Rating Scale (GSRS): Total Score

The Gastrointestinal Symptom Rating Scale (GSRS) is a 15-item questionnaire for participants with gastrointestinal discomfort. The GSRS Total Score is the average of the 15 items. Each item is rated on a 0 to 7 scale, where 0 indicates no discomfort and 7 indicates very severe discomfort. The range of scores is 0 to 7, where higher scores are considered a worse outcome.The outcome measure, change from baseline in GSRS Total Score, has a possible range from -7 to +7, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.8
Aprepitant-placebo-0.5

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Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Bloating Severity

Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Bloating Severity is the participant's assessment of bloating (feeling like you need to loosen your clothes) during the past 24 hours, where 0=none, 1=mild, 2=moderate, 3=severe, and 4=very severe. The range of scores is 0 to 4, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Bloating Severity, has a possible range from -4 to +4, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.6
Aprepitant-placebo-0.4

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Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Early Satiety Severity

Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Early Satiety Severity is the participant's assessment of early satiety (not able to finish normal-size meal) during the past 24 hours, where 0=none, 1=mild, 2=moderate, 3=severe, and 4=very severe. The range of scores is 0 to 4, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Early Satiety Severity, has a possible range from -4 to +4, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant0.1
Aprepitant-placebo0.08

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Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Excessive Fullness Severity

Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Excessive Fullness Severity is the participant's assessment of excessive fullness (feeling excessively full after meals) during the past 24 hours, where 0=none, 1=mild, 2=moderate, 3=severe, and 4=very severe. The range of scores is 0 to 4, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Excessive Fullness Severity, has a possible range from -4 to +4, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.6
Aprepitant-placebo-0.4

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Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): GCSI Total Score

The Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): GCSI total score is the average of 3 subscores: Nausea (average of two items: nausea and vomiting), Early Satiety (average of two items: not able to finish normal size meal and feeling excessively full after meals), and Bloating (feeling like you need to loosen your clothes). Each item is the participant's assessment of severity of the symptom during the past 24 hours, where 0=none, 1=mild, 2=moderate, 3=severe, and 4=very severe. The range of scores is 0 to 4, where higher scores are considered a worse outcome. The outcome measure, change from baseline in GCSI total score, has a possible range from -4 to +4, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.5
Aprepitant-placebo-0.4

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Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Nausea (Hours)

Measure Description: Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Nausea is the participant's assessment of the number of hours of nausea experienced in the past 24 hours. The range is 0 to 24 hours. The outcome measure, change from baseline in number of hours of nausea, has a possible range from -24 to +24, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionhours of nausea (Mean)
Aprepitant-2.5
Aprepitant-placebo-1.2

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Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Nausea Severity

Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Nausea severity is the participant's assessment of nausea (feeling sick to your stomach as if you were going to vomit or throw up) during the past 24 hours, where 0=none, 1=mild, 2=moderate, 3=severe, and 4=very severe. The range of scores is 0 to 4, where higher scores are considered a worse outcome. The outcome measure, change from baseline in GCSI score, has a possible range from -4 to +4, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.8
Aprepitant-placebo-0.5

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Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Overall Symptom Severity

Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Overall Symptom Severity is the participant's assessment of overall severity of gastroparesis symptoms during the past 24 hours, where 0=none, 1=mild, 2=moderate, 3=severe, and 4=very severe. The range of scores is 0 to 4, where higher scores are considered a worse outcome. The outcome, change from baseline in Overall Symptom Severity score, has a possible range from -4 to +4, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.7
Aprepitant-placebo-0.4

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Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Retching (No. Episodes)

Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Retching is the participant's assessment of the number of episodes of retching (heaving as if to vomit, but nothing comes up) experienced in the past 24 hours. The outcome is the change from baseline in the number of retching episodes, where negative numbers indicate improvement in retching frequency, and positive numbers indicate worsening in retching frequency. (NCT01149369)
Timeframe: 4 weeks

Interventionnumber of episodes (Mean)
Aprepitant-0.5
Aprepitant-placebo-0.7

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Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Vomiting (No. Episodes)

Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Vomiting is the participant's assessment of the number of episodes of vomiting experienced in the past 24 hours. The outcome is the change from baseleine in number of times vomited, where negative numbers indicate improvement in vomiting frequency, and positive numbers indicate worsening in vomiting frequency. (NCT01149369)
Timeframe: 4 weeks

Interventionnumber of episodes (Mean)
Aprepitant-0.5
Aprepitant-placebo-0.4

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Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Vomiting Severity

Gastroparesis Cardinal Symptom Index Daily Diary (GCSI-DD): Vomiting Severity is the participant's assessment of vomiting during the past 24 hours, where 0=none, 1=mild, 2=moderate, 3=severe, and 4=very severe. The range of scores is 0 to 4, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Vomiting Severity, has a possible range from -4 to +4, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.4
Aprepitant-placebo-0.2

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Glucose

Change from baseline in glucose (mg/dL) (NCT01149369)
Timeframe: 4 weeks

Interventionmg/dL (Mean)
Aprepitant9.6
Aprepitant-placebo7.0

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Hematocrit

Change from baseline in hematocrit (NCT01149369)
Timeframe: 4 weeks

Interventionpercentage RBCs (Mean)
Aprepitant-0.4
Aprepitant-placebo-0.4

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Hemoglobin

Change from baseline in hemoglobin (g/dL) (NCT01149369)
Timeframe: 4 weeks

Interventiong/dL (Mean)
Aprepitant-0.1
Aprepitant-placebo-0.2

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Hemoglobin A1c (HbA1c)

Change from baseline in hemoglobin A1c (HbA1c) (%) (NCT01149369)
Timeframe: 4 weeks

Interventionpercent glycosylated hemoglobin (Mean)
Aprepitant-0.1
Aprepitant-placebo0.1

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Liver Enzymes and Proteins: Alanine Aminotransferase (ALT)

Change from baseline in serum alanine aminotransferase (ALT), U/L (NCT01149369)
Timeframe: 4 weeks

InterventionU/L (Mean)
Aprepitant2.3
Aprepitant-placebo0.8

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Liver Enzymes and Proteins: Albumin

Change from baseline in albumin (g/dL) (NCT01149369)
Timeframe: 4 weeks

Interventiong/dL (Mean)
Aprepitant-0.1
Aprepitant-placebo-0.1

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Liver Enzymes and Proteins: Aspartate Aminotransferase (AST)

Change from baseline in aspartate aminotransferase (AST), U/L (NCT01149369)
Timeframe: 4 weeks

InterventionU/L (Mean)
Aprepitant3.1
Aprepitant-placebo0.9

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Liver Enzymes and Proteins: Total Protein

Change from baseline in total protein (g/dL) (NCT01149369)
Timeframe: 4 weeks

Interventiong/dL (Mean)
Aprepitant0.0
Aprepitant-placebo-0.1

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Magnesium

Change from baseline in magnesium (mg/dL) (NCT01149369)
Timeframe: 4 weeks

Interventionmg/dL (Mean)
Aprepitant0.0
Aprepitant-placebo-0.0

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Number of Participants With Improvement in Nausea

The primary outcome measure is a binary (0,1) variable indicating improvement in nausea or not in the mean of available visual analog scale (VAS) scores over the 28 day treatment period compared to the mean of VAS scores during the 7 day baseline period. The criteria for improvement are either a 25 mm or more reduction in mean VAS or attaining a mean VAS during the treatment period of < 25 mm. (NCT01149369)
Timeframe: 4 weeks

Interventionparticipants (Number)
Aprepitant29
Aprepitant-placebo25

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PAGI-SYM Severity Index: Bloating Severity

The PAGI-SYM Severity index: Bloating Severity is the participant's assessment of bloating (feel like you need to loosen your clothes) during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Bloating Severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.2
Aprepitant-placebo-0.5

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PAGI-SYM Severity Index: Bloating Subscore

The PAGI-SYM Severity index: Bloating Subscore is the average of 2 items: bloating (feeling like you need to loosen your clothes) and stomach visibly larger. Each item is the participant's assessment of severity of the symptom during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The outcome measure, change from baseline in Bloating Subscore, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.2
Aprepitant-placebo-0.6

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PAGI-SYM Severity Index: Chest Discomfort During Sleep Time Severity

The PAGI-SYM Severity index: Chest discomfort during sleep severity is the participant's assessment of feeling of discomfort inside the chest at night (during sleep time) over the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Chest Discomfort During Sleep Time severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.9
Aprepitant-placebo-0.6

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PAGI-SYM Severity Index: Chest Discomfort During the Day Severity

The PAGI-SYM Severity index: Chest discomfort during the day severity is the participant's assessment of feeling of discomfort inside the chest during the day over the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Chest Discomfort During the Day severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.1
Aprepitant-placebo-0.7

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PAGI-SYM Severity Index: Constipation Severity

The PAGI-SYM Severity index: Constipation severity is the participant's assessment of constipation during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Constipation Severity score, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.8
Aprepitant-placebo-0.3

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PAGI-SYM Severity Index: Diarrhea Severity

The PAGI-SYM Severity index: Diarrhea severity is the participant's assessment of constipation during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Diarrhea Severity score, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-0.1
Aprepitant-placebo-0.2

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PAGI-SYM Severity Index: Excessive Fullness Severity

PAGI-SYM Severity index: Excessive fullness severity is the participant's assessment of feeling excessively full after meals during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Excessive Fullness severity, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.1
Aprepitant-placebo-0.6

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PAGI-SYM Severity Index: Fullness/Early Satiety Subscore

The PAGI-SYM Severity index: Fullness/Early Satiety Subscore is the average of 4 items: stomach fullness, not able to finish normal size meal, felling excessively full after meals, and loss of appetite. Each item is the participant's assessment of severity of the symptom during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in Fullness/Early Satiety Subscore, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.0
Aprepitant-placebo-0.7

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PAGI-SYM Severity Index: Gastroparesis Cardinal Symptom Index (GCSI) Score

PAGI-SYM Severity index: Gastroparesis Cardinal Symptom Index (GCSI) score is the average of 3 subscores: Nausea (average of 3 items: nausea, retching, and vomiting), Fullness/Early Satiety (average of 4 items: stomach fullness, not able to finish normal size meal, feeling excessively full after meals, and loss of appetite), and Bloating (average if 2 items: bloating and stomach visibly larger). Each item is the participant's assessment of severity of the symptom during the past 24 hours, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The outcome measure, change from baseline in GCSI score, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.3
Aprepitant-placebo-0.7

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PAGI-SYM Severity Index: GERD Subscore

PAGI-SYM Severity index: Gastroesophageal Reflux (GERD) Subscore is the average of 7 items (heartburn during day, heartburn lying down, chest discomfort day, chest discomfort during sleep, regurgitation during day, regurgitation lying down, bitter taste in mouth). Each item is the participant's assessment of severity of the symptom, where 0=none, 1=very mild, 2=mild, 3=moderate, 4=severe, and 5=very severe. The range of scores is 0 to 5, where higher scores are considered a worse outcome. The outcome measure, change from baseline in GERD Subscore, has a possible range from -5 to +5, with negative values indicating a better outcome (improvement) and positive values indicating a worse outcome. (NCT01149369)
Timeframe: 4 weeks

Interventionunits on a scale (Mean)
Aprepitant-1.1
Aprepitant-placebo-0.6

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Alcohol Craving as Measured by the Visual Analog Scale (VAS) 1

The VAS is a 100 mm line anchored at both ends. Participants mark where on the line their craving falls, with closer to 0 indicating less craving, and closer to 100 indicating more craving. Data are analyzed by using a ruler to determine the actual mm value of the participant mark. (NCT01176591)
Timeframe: Session 1

Interventionunits on a scale (Mean)
Placebo Session 1, Aprepitant Session 226.25
Placebo Session 1, Placebo Session 238.92

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Alcohol Craving as Measured by the Visual Analog Scale (VAS) 2

The VAS is a 100 mm line anchored at both ends. Participants mark where on the line their craving falls, with closer to 0 indicating less craving, and closer to 100 indicating more craving. Data are analyzed by using a ruler to determine the actual mm value of the participant mark. (NCT01176591)
Timeframe: Session 2

Interventionunits on a scale (Mean)
Placebo Session 1, Aprepitant Session 233.22
Placebo Session 1, Placebo Session 20.17

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Cocaine Craving as Measured on the Visual Analog Scale (VAS) 1

The VAS is a 100 mm line anchored at both ends. Participants mark where on the line their craving falls, with closer to 0 indicating less craving, and closer to 100 indicating more craving. Data are analyzed by using a ruler to determine the actual mm value of the participant mark. (NCT01176591)
Timeframe: Session 1

Interventionunits on a scale (Mean)
Placebo Session 1, Aprepitant Session 219
Placebo Session 1, Placebo Session 248

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Cocaine Craving as Measured on the Visual Analog Scale (VAS) 2

The VAS is a 100 mm line anchored at both ends. Participants mark where on the line their craving falls, with closer to 0 indicating less craving, and closer to 100 indicating more craving. Data are analyzed by using a ruler to determine the actual mm value of the participant mark. (NCT01176591)
Timeframe: Session 2

Interventionunits on a scale (Mean)
Placebo Session 1, Aprepitant Session 220
Placebo Session 1, Placebo Session 24

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Multiple Choice Procedure (MCP) 1

The MCP measures the relative reinforcing value of a hypothetical single dose of cocaine, as compared to various monetary values. The lower the monetary value where participants switch from preferring cocaine to preferring money, the less value they place on cocaine. MCP findings of cocaine devaluation typically correlate with cocaine abstinence in clinical trials. (NCT01176591)
Timeframe: Session 1

Interventiondollars (Mean)
Placebo Session 1, Aprepitant Session 28.58
Placebo Session 1, Placebo Session 217.33

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Multiple Choice Procedure (MCP) 2

The MCP measures the relative reinforcing value of a hypothetical single dose of cocaine, as compared to various monetary values. The lower the monetary value where participants switch from preferring cocaine to preferring money, the less value they place on cocaine. MCP findings of cocaine devaluation typically correlate with cocaine abstinence in clinical trials. (NCT01176591)
Timeframe: Session 2

Interventiondollars (Mean)
Placebo Session 1, Aprepitant Session 27.59
Placebo Session 1, Placebo Session 217.33

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Control Rate of Delayed Phase Nausea, Vomiting, and Retching in Patients Undergoing Multiple Fraction Radiotherapy

"Percentage of participants experiencing no nausea, vomiting, and retching was assessed.~Assessments of nausea, vomiting, and antiemetic use will be taken daily within 2-10 following the radiation therapy based on patient self-report nausea/vomiting diaries." (NCT01183481)
Timeframe: Days 2-10 following radiotherapy

Interventionpercentage of participants (Number)
Control rate of delayed phase nauseaControl rate of delayed phase vomiting/retching
Aprepitant and Granisetron8383

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Control Rate of Delayed Phase Nausea, Vomiting, and Retching in Patients Undergoing Single Fraction Radiotherapy

"Percentage of participants in the single fraction arm experiencing no nausea, vomiting, and retching was assessed.~Assessments of nausea, vomiting, and antiemetic use will be taken daily within 2-10 following the radiation therapy based on patient self-report nausea/vomiting diaries." (NCT01183481)
Timeframe: Days 2-10 following radiotherapy

Interventionpercentage of participants (Number)
Control rate of delayed phase nauseaControl rate of delayed phase vomiting/retching
Aprepitant and Granisetron6285

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Control Rate of Acute Phase Nausea, Vomiting, and Retching in Patients Undergoing Single Fraction Radiotherapy

"Percentage of participants experiencing no nausea, vomiting, and retching during the acute phase was assessed.~Assessments of nausea, vomiting, and antiemetic use will be taken daily following the radiation therapy based on patient self-report nausea/vomiting diaries." (NCT01183481)
Timeframe: Day of radiotherapy and 24 hours following

Interventionpercentage of participants (Number)
Control rate of acute phase nauseaControl rate of acute phase vomiting/retching
Aprepitant and Granisetron100100

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Control Rate of Acute Phase Nausea, Vomiting, and Retching in Patients Undergoing Multiple Fraction Radiotherapy

"Percentage of participants in the multiple fraction arm experiencing no nausea, vomiting, and retching was assessed.~Data will be measured by research staff at baseline and patient self-report nausea diaries will be taken on each day within this time frame." (NCT01183481)
Timeframe: During radiotherapy (5 days) and the 24 hours following radiotherapy

Interventionpercentage of participants (Number)
Control rate of acute phase nauseaControl rate of acute phase vomiting/retching
Aprepitant and Granisetron6767

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The Proportion of Patients Experiencing no Vomiting and no Nausea, Without Use of Any Rescue Antiemetic Medication(s), From Days 2-10 Following the Radiation Therapy (Delayed RINV).

Assessments of nausea, vomiting, and antiemetic use will be taken daily within 2-10 following the radiation therapy based on patient self-report nausea/vomiting diaries. (NCT01183481)
Timeframe: Days 2-10 following radiotherapy

Interventionparticipants (Number)
Aprepitant and Granisetron19

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Frequency of Adverse Effects as Assessed by the NCI CTCAE v 4.0

Adverse events at least possibly related to treatment (NCT01275664)
Timeframe: Up to day 6

InterventionParticipants (Count of Participants)
ConstipationFatigueDiarrheaHyponatremiaAlanine Aminotransferase IncreasedGGT Increased
Treatment (Granisetron, Dexamethasone, Aprepitant)111111

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Number of Participants With Complete Control Defined as no Vomiting and no Use of Rescue Medications (for Nausea or Emesis)

Number of participants who had complete control defined by no vomiting (NCT01275664)
Timeframe: During the 6 days following chemotherapy

InterventionParticipants (Count of Participants)
Treatment (Granisetron, Dexamethasone, Aprepitant)1

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Number of Participants With Complete Response (CR) in Cycle 2 for Patient Without Complete Response in Cycle 1

To evaluate in cycle 2 the efficacy of aprepitant (days 1, 2 and 3) as secondary prevention in patients without complete response in cycle 1. A vomiting episode is defined as one or more episodes of emesis (expulsion of stomach contents through the mouth) or retches (an attempt to vomit that is not productive of stomach contents). Distinct vomiting episodes are, by definition, separated by the absence of emesis and retching for at least 1 minute. The timing (date and time) of each vomiting episode will be recorded by the patient in each cycle diary at the time of occurrence. Assessments of efficacy will begin at the initiation of chemotherapy infusion (0 hours) until the morning of Day 6 (approximately 120 hours) after chemotherapy during 1-2 cycles. (NCT01298193)
Timeframe: Up to cycle 2, and average of 6 weeks

InterventionParticipants (Count of Participants)
Aprepitant NCR12

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Total Impact of Chemotherapy-Induced Nausea and Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2

"To determine the total incidence of Chemotherapy-Induced Nausea and Vomiting associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of Chemotherapy-Induced Nausea and Vomiting on daily life. There are 18 items, each on a 7-point scale. Results are reported as a total score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of nausea or vomiting (better outcome) (Maximum 126, Minimum 18)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 2 pre-chemotherapy NCR patientsCycle 2 post-chemotherapy NCR patientsCycle 2 pre-chemotherapy CR patientsCycle 2 post-chemotherapy CR patients
Aprepitant NCR37.864.443.2847.7

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Impact of Chemotherapy-Induced Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2

"To determine the incidence of vomiting associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of vomiting on daily life. There are 9 items, each on a 7-point scale. Results are reported as a vomiting score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of vomiting (better outcome) (Maximum 63, Minimum 9)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 2 pre-chemotherapy NCR patientsCycle 2 post-chemotherapy NCR patientsCycle 2 pre-chemotherapy CR patientsCycle 2 post-chemotherapy CR patients
Aprepitant NCR20.0928.1923.7123.43

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Total Impact of Chemotherapy-Induced Nausea and Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1

"To determine the incidence of Chemotherapy-Induced Nausea and Vomiting associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of Chemotherapy-Induced Nausea and Vomiting on daily life. There are 18 items, each on a 7-point scale. Results are reported as a total score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of nausea or vomiting (better outcome) (Maximum 126, Minimum 18)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 1 pre-chemotherapy NCR patientsCycle 1 post-chemotherapy NCR patientsCycle 1 pre-chemotherapy CR patientsCycle 1 post-chemotherapy CR patients
Aprepitant43.759.242.544.22

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Impact of Chemotherapy-Induced Vomiting on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1

"To determine the incidence of vomiting associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of vomiting on daily life. There are 9 vomiting-related items, each on a 7-point scale. Results are reported as a vomiting score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of vomiting (better outcome) (Maximum 63, Minimum 9)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 1 pre-chemotherapy NCR patientsCycle 1 post-chemotherapy NCR patientsCycle 1 pre-chemotherapy CR patientsCycle 1 post-chemotherapy CR patients
Aprepitant23.8627.4623.5324.15

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Impact of Chemotherapy-Induced Nausea on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 2

"To determine the incidence of Nausea associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of Nausea on daily life. There are 9 items, each on a 7-point scale. Results are reported as a nausea score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of nausea (better outcome) (Maximum 63, Minimum 9)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 2 pre-chemotherapy NCR patientsCycle 2 post-chemotherapy NCR patientsCycle 2 pre-chemotherapy CR patientsCycle 2 post-chemotherapy CR patients
Aprepitant NCR17.7136.1619.5724.30

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Impact of Chemotherapy-Induced Nausea on Daily Life by the Functional Living Index-Emesis Questionnaire in Cycle 1

"To determine the incidence of nausea associated with the Docetaxel-Cyclophosphamide regimen in early breast cancer patients, a Functional Living Index-Emesis (FLIE) questionnaire was collected on treatment Day 1 (prior to initiation of chemotherapy) and Day 6, which referenced the entire treatment period since the initiation of chemotherapy for non clinical responders (NCR) against clinical responders (CR).~The FLIE questionnaire is a validated, patient-reported instrument to measure the impact of Chemotherapy-Induced Nausea and vomiting on daily life. There are 9 nausea-related items, each on a 7-point scale. Results are reported as a nausea score. For the purposes of this study, higher scores indicate less impairment on daily life as a result of nausea (better outcome) (Maximum 63, Minimum 9)." (NCT01298193)
Timeframe: Up to day 6

Interventionscore on a scale (Mean)
Cycle 1 pre-chemotherapy NCR patientsCycle 1 post-chemotherapy NCR patientsCycle 1 pre-chemotherapy CR patientsCycle 1 post-chemotherapy CR patients
Aprepitant19.8531.7318.9320.27

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Number of Participants With Complete Response (CR)

Complete response is defined as no vomiting and no use of rescue treatment within the first cycle of Docetaxel-Cyclophosphamide for the treatment of early-stage breast cancer patients. A vomiting episode is defined as one or more episodes of emesis (expulsion of stomach contents through the mouth) or retches (an attempt to vomit that is not productive of stomach contents). Distinct vomiting episodes are, by definition, separated by the absence of emesis and retching for at least 1 minute. The timing (date and time) of each vomiting episode will be recorded by the patient in each cycle diary at the time of occurrence. Assessments of efficacy will begin at the initiation of chemotherapy infusion (0 hours) until the morning of Day 6 (approximately 120 hours) after chemotherapy during 1-2 cycles. (NCT01298193)
Timeframe: Up to 21 days after cycle 1 of chemotherapy treatment

InterventionParticipants (Count of Participants)
Observational Phase (First Cycle):161

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Percentage of Participants With Incidence of Vomiting/Retching From Day 1 Through End of Day 5

Cumulative incidence will be determined by the patient self-assessment form, supplemented by the nursing inpatient records. (NCT01334086)
Timeframe: Day 1 through end of Day 5

Interventionpercentage of particpants (Number)
Aprepitant26.3

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Percentage of Patients' Use of Supplemental Anti-emetics as Determined by the Total Number of Doses Per Day and in Total, From Days 1-8.

(NCT01334086)
Timeframe: Days 1 to 8

Intervention% of pts receiving breakthrough (Number)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7Day 8
Aprepitant1829395865756853

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Daily Number of Vomiting or Retching Incidents From Days 1-8

This will be determined by both self-assessment form which will be filled out by the patient on a daily basis, and review of the nursing inpatient records. (NCT01334086)
Timeframe: Days 1 to 8

Interventionincidents (Number)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7Day 8
Aprepitant711161313241311

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Percentage of Patients Experiencing Nausea From Days 1-8.

(NCT01334086)
Timeframe: Days 1 to 8

Interventionpercentage of particpants (Number)
Aprepitant68.4

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Percentage of Participants Experiencing Vomiting or Retching From Days 1-8.

This will be determined by both self-assessment form which will be filled out by the patient on a daily basis, and review of the nursing inpatient records. (NCT01334086)
Timeframe: Days 1 to 8

Interventionpercentage of particpants (Number)
Aprepitant34.2

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Percentage of Participants With a Complete Response in the Overall Phase of Cycle 1

Overall phase was defined as 0 to 120 hourse after the start of chemotherapy. Complete response was defined as no vomiting or retching and no use of rescue medication in the overall phase of Cycle 1. (NCT01362530)
Timeframe: 0 to 120 hours after initiation of chemotherapy

InterventionPercentage of participants (Number)
Aprepitant Regimen40.1
Control Regimen20.0

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Percentage of Participants With a Complete Response in the Delayed Phase of Cycle 1

Delayed Phase was defined as 25-120 hours after the start of chemotherapy. Complete response was defined as no vomiting or retching and no use of rescue medication in the delayed phase of Cycle 1. (NCT01362530)
Timeframe: 25 to 120 hours after the start of chemotherapy

InterventionPercentage of participants (Number)
Aprepitant Regimen50.7
Control Regimen26.0

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Percentage of Participants With No Vomiting in the Overall Phase of Cycle 1

Overall phase was defined as 0 to 120 hourse after the start of chemotherapy. No vomiting was defined as no emesis or retching or dry heaves in the overall phase of Cycle 1. (NCT01362530)
Timeframe: 0 to 120 hours after initiation of chemotherapy

InterventionPercentage of participants (Number)
Aprepitant Regimen46.7
Control Regimen21.3

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Percentage of Participants With a Complete Response in the Acute Phase of Cycle 1

Acute phase was defined as 0 to 24 hours after the start of chemotherapy. Complete response was defined as no vomiting or retching and no use of rescue medication in the acute phase of Cycle 1. (NCT01362530)
Timeframe: 0 to 24 hours after initiation of chemotherapy

InterventionPercentage of participants (Number)
Aprepitant Regimen66.4
Control Regimen52.0

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Percentage of Patients With Adverse Events

This was a safety study where Adverse Events is the primary outcome (defined by the current ICH Guideline for Good Clinical Practice). Patients were randomized according to a 3:1 ratio (netupitant/palonosetron:aprepitant/palonosetron). No formal comparison was planned, the presence of a control in the same patient population helped interpret any unexpected safety finding in the experimental arm.The number of patients was estimated in order to have more than 100 patients treated with the netupitant/palonosetron comination for up to at least six cycles. Based on 100 patients, if a given AE is not observed, an AE incidence of 3% or greater can be excluded with 95% confidence. (NCT01376297)
Timeframe: Participants will be followed for the duration of the chemotherapy, an expected average duration of up to 24 weeks assuming 6 chemotherapy cycles given every 4 weeks

Interventionpercentage of patients with TEAE (Number)
Netupitant and Palonosetron Plus Dexamethasone86.0
Aprepitant and Palonosetron Plus Dexamethasone91.3

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Percentage of Participants With No Vomiting and No Retching During Cycle 2 of Chemotherapy

A vomiting episode is defined as one or more episodes of emesis (expulsion of stomach contents through the mouth) or retching (an attempt to vomit that is not productive of stomach contents). Distinct vomiting episodes are separated by the absence of emesis and retching for at least one minute. The date and time of each vomiting episode was recorded by participants in diaries at the time of occurrence. The percentage of partcipants with no vomiting and no retching episodes 0-120 hours following chemotherapy in Cycle 2 was calculated. (NCT01405924)
Timeframe: Up to 120 hours following initiation of chemotherapy in Cycle 2

InterventionPercentage of Participants (Number)
Fosaprepitant 150 mg57.43

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Percentage of Participants With No Significant Nausea During Cycle 2 of Chemotherapy

"Participants rated their degree of nausea in response to How much nausea have you had over the last 24 hours? using a 100-mm visual analog scale (VAS, 0=no nausea, 100=nausea as bad as it could be) on Days 2-6 following initiation of chemotherapy. No significant nausea was defined as VAS score <25 mm over the 24-120 hours following initiation of chemotherapy. The percentage of participants who experienced no significant nausea during Cycle 2 of chemotherapy was calculated." (NCT01405924)
Timeframe: From 24 to 120 hours following initiation of chemotherapy in Cycle 2

InterventionPercentage of Participants (Number)
Fosaprepitant 150 mg47.52

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Percentage of Participants With a Complete Response During Cycle 2 of Chemotherapy

A complete response is defined as no vomiting/no retching episodes and no use of rescue medication during the 120 hours following initiation of chemotherapy. The percentage of participants with a complete response during Cycle 2 of chemotherapy was calculated. (NCT01405924)
Timeframe: Up to 120 hours following initiation of chemotherapy in Cycle 2

InterventionPercentage of Participants (Number)
Fosaprepitant 150 mg21.78

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Percentage of Participants Who Used No Rescue Medication During Cycle 2 of Chemotherapy

Participants recorded any use of rescue medication for established nausea/vomiting in their daily diaries from initiation of chemotherapy infusion through the morning of Day 6. The percentage of participants who used no rescue medication during Cycle 2 of chemotherapy was calculated. (NCT01405924)
Timeframe: Up to 120 hours following initiation of chemotherapy in Cycle 2

InterventionPercentage of Participants (Number)
Fosaprepitant 150 mg30.69

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Percentage of Participants With No Vomiting and No Retching During Cycle 2 of Chemotherapy Per Type of Chemotherapy

A vomiting episode is defined as one or more episodes of emesis (expulsion of stomach contents through the mouth) or retching (an attempt to vomit that is not productive of stomach contents). Distinct vomiting episodes are separated by the absence of emesis and retching for at least one minute. The date and time of each vomiting episode was recorded by participants in diaries at the time of occurrence. The percentage of partcipants with no vomiting and no retching episodes 0-120 hours following initiation of chemotherapy in Cycle 2 was calculated based on type of chemotherapy received. (NCT01405924)
Timeframe: Up to 120 hours following initiation of chemotherapy in Cycle 2

InterventionPercentage of Participants (Number)
Fosaprepitant 150 mg: AC-like Chemotherapy62.30
Fosaprepitant 150 mg: CT Chemotherapy50.00

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Functional Living Index - Emesis (FLIE) Total Score During Cycle 2 of Chemotherapy

"The FLIE Total Score is an 18-question quality-of-life questionnaire on the impact of nausea and vomiting (9 questions on nausea and 9 questions on vomiting) on daily life. Each question uses a visual analog scale (VAS) to rate the impact of nausea/vomiting from 1 to 7. FLIE Total Scores are calculated by summing the responses to the 18 questions and can range from 18-126 (18=a great deal of impairment, 126=no impairment), with a higher score indicating less impairment due to nausea and vomiting. No Impact on daily life was defined as a FLIE Total Score >108. Participants completed the FLIE questionnaire on the morning of Day 6 following initiation of chemotherapy in Cycle 2; their responses covered their experiences with nausea and vomiting over the previous 5 days." (NCT01405924)
Timeframe: From Day 1 (prior to initiation of chemotherapy in Cycle 2) to morning of Day 6 (up to ~120 hours following initiation of chemotherapy in Cycle 2)

InterventionScore on a Scale (Mean)
Day 1 (prior to chemotherapy)Day 6
Fosaprepitant 150 mg92.9080.50

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Overall Complete Response Rate

no emetic episodes or rescue therapy following the initiation of chemotherapy (NCT01432015)
Timeframe: 13 months

Interventionpercentage of participants (Number)
Fosaprepitant Including Placebo10
Aprepitant Including Placebo10

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Impact on Daily Living Activities

Proportion of patients reporting no impact on daily living activities following initiation of chemotherapy (NCT01432015)
Timeframe: 13 months

Interventionpercentage of participants (Number)
Fosaprepitant Including Placebo10
Aprepitant Including Placebo10

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Patient's Global Satisfaction With the Antiemetic Regimen

"Patients' global satisfaction with the antiemetic regimen is measured using the Osoba survey, which was administered on days 1-7. This survey asks patients In the past 24 hours, did vomiting or dry heaves a) interfere with your appetite, b) affect your sleep, c) interfere with your physical activities, d) interfere with your social life, and e) interfere with your enjoyment of life? Patients responded on a scale of 1-4 ranging from 'Not at all' to 'Very much.' Global satisfaction was defined as responding 'Not at all' for all questions related to vomiting/retching for each study day. The proportion of patients responding 'Not at all' for all Osoba vomiting/retching questions over the study period is reported." (NCT01450826)
Timeframe: 7 days

Interventionproportion of patients (Number)
Aprepitant+Ondansetron0.87
Ondansetron0.81

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Proportion of Patients Achieving Complete Control (CC)

Complete control (CC): study days 1-7 (acute and delayed CINV) the proportion of patients achieving complete control (CC); defined as no emetic episode, no need for rescue medication during days 1-7; number of emetic episodes daily; time to first emetic episode; as captured by the MAT (MASCC Antiemesis Tool)/Osoba survey (MASCC refers to Multinational Association for Supportive Care in Cancer™). Severity of nausea and other toxicities measured daily by the NCI Common Toxicity Criteria (version 4.0). (NCT01450826)
Timeframe: 7 days

Interventionproportion of patients (Number)
Aprepitant+Ondansetron0.59
Ondansetron0.55

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Time to Treatment Failure

Median time in days to first emetic episode or first need of rescue medication, whichever occurred first as measured by the MAT/Osoba survey, among those patients experiencing an emetic episode or need of rescue medication (NCT01450826)
Timeframe: 7 days

Interventiondays (Median)
Aprepitant+Ondansetron5
Ondansetron4

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Proportion of Patients Achieving an Acute and Delayed Complete Response (CR)

CR is the proportion of patients with no emetic episode and no rescue medication. (1) Assessed from the beginning of study day 1, CR is defined for acute CINV as no emetic episode and no use of rescue anti-nausea medication during the first 24 hours following chemotherapy administration. An emetic episode is defined as one episode of vomiting or a sequence of episodes in very close succession not relieved by a period of relaxation of at least 1 min, any number of unproductive emetic episodes (retches) in any given 5 minute period, or an episode of retching lasting <5 minutes combined with vomiting not relieved by a period of relaxation of at least 1 minute; (2) Complete response (CR) on study days 2-7 (delayed CINV) is defined as the proportion of patients achieving a CR during the delayed time period. The data will be captured by the validated ultinational Association of Supportive Care in Cancer (MASCC) Anti-emesis Tool (MAT)/Osoba survey. (NCT01450826)
Timeframe: 7 days

,
Interventionproportion of patients (Number)
Acute CINV CRDelayed CINV CR
Aprepitant+Ondansetron0.970.59
Ondansetron0.880.58

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Post Operative Nausea and Vomiting (PONV) Scores on a Verbal Response Scale

"To assess the efficacy of triple therapy with Scopolamine, Ondansetron and Dexamethasone for prevention of post operative nausea and vomiting (PONV) in high risk patients during a delayed period after neurological surgery under general anesthesia.~- Assess the severity of nausea and vomiting during the first 24 hours after neurological surgery.~Nausea is evaluated by a standard verbal response scale (VRS) ranging from 0-10, 0 being no nausea and 10 being severe nausea. Vomiting is evaluated by the investigator or nursing staff numerically as either 0, no vomiting;, 1, mild vomiting;, 2, moderate vomiting;, or 3, severe vomiting." (NCT01474915)
Timeframe: 24 hours post-operatively

,
Interventionunits on a scale (Mean)
Nausea episodesVomiting episodes
Aprepitant11.5
Ondansetron11.5

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Proportion of Patients With a Complete Response/Complete Control During the First 24 Hours After Neurological Surgery Under General Anesthesia

"To assess the efficacy of triple therapy with Scopolamine, Ondansetron and Dexamethasone for prevention of post operative nausea and vomiting (PONV) in high risk patients during the first 24 hours after neurological surgery under general anesthesia.~- Proportion of patients with a complete response/complete control during the first 24 hours after neurological surgery under general anesthesia.~Complete Control is defined as no emetic episode, no need for rescue medication and no more than mild nausea overall after neurological surgery and general anesthesia.~Complete Response is defined as no vomiting and no rescue therapy after neurological surgery and general anesthesia." (NCT01474915)
Timeframe: 24 hours post operatively

,
Interventionparticipants (Number)
Complete ControlComplete Response
Aprepitant3830
Ondansetron4130

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Complete Response

Complete response (CR) defined as: No emetic episodes and no rescue medications. This is a cross-over designed study, the outcomes by single dose, two doses and control cycles were evaluated by combining the results from both cycle 1 and cycle 2 according to the treatment received. (NCT01490060)
Timeframe: From Day 1 to Day 5 in two 21-days cycles (Cycle 1 and Cycle 2).

Interventionpercentage of participants (Number)
Control Cycle (Arm A/Arm B)17
Arm A: Single Dose, Day 110
Arm B: Two Doses, Day 1 + Day 450

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Overall Survival

(NCT01504711)
Timeframe: Time of initiation of treatment until death or censor assessed up to 26 months

Interventionmonths (Median)
Treatment (Nausea and Vomiting Prophylaxis)11.5

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Percentage of Participants With Control of Vomiting and Rescue Medication Control

Achieved if a patient has no episodes of vomiting and requires no rescue medication during the first 120 hours after fosaprepitant dimeglumine administration. (NCT01504711)
Timeframe: From 0-120 hours after first course of chemotherapy

Interventionpercentage of participants (Number)
Treatment (Nausea and Vomiting Prophylaxis)26.9

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Percentage of Participants With Control of Both Acute and Delayed Vomiting

Achieved if a patient has no episodes of vomiting at both 24 and 120 hours after fosaprepitant dimeglumine administration. (NCT01504711)
Timeframe: in approximately 28 months

Interventionpercentage of participants (Number)
Treatment (Nausea and Vomiting Prophylaxis)65.4

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Percentage of Participants With Control of Both Acute and Delayed Nausea

Achieved if a patient has no episodes of nausea at both 24 and 120 hours after fosaprepitant dimeglumine administration. (NCT01504711)
Timeframe: in approximately 28 months

Interventionpercentage of participants (Number)
Treatment (Nausea and Vomiting Prophylaxis)28.0

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Number of Patients With Gastrointestinal Toxicities (Grade 3 and 4 Nausea and Vomiting) Associated With Delivering Fluorouracil/Gemcitabine Hydrochloride-based Chemotherapy With Upper Abdominal Radiation

Toxicity will be determined using the revised National Cancer Institute (NCI) Common Toxicity Criteria (CTC) version 3.0 for Toxicity and Adverse Event Reporting. Descriptive statistics (means, standard deviations, frequencies, etc.) will be presented for pretreatment patient characteristics. The rate of grade 3 and 4 nausea will be compared to the cut points during interim and final analyses. (NCT01534637)
Timeframe: Over 10 weeks

Interventionparticipants (Number)
Treatment (Antiemetic, Chemotherapy, and Radiation Therapy)3

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Impact of Aprepitant/5HT-3 Antagonist Therapy on the Patient Quality of Life as Measured by the Number of Patients Taking Anti Nausea Drugs

(NCT01534637)
Timeframe: Week 5

Interventionparticipants (Number)
Treatment (Antiemetic, Chemotherapy, and Radiation Therapy)5

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Impact of Aprepitant/5HT-3 Antagonist Therapy on the Patient Quality of Life as Measured by the Number of Patients Using Anti Nausea Drugs

(NCT01534637)
Timeframe: Week 1

Interventionparticipants (Number)
Treatment (Antiemetic, Chemotherapy, and Radiation Therapy)6

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Intensity of Breathlessness

"Time-weighted averages of intensity of breathlessness.~Subject rating of intensity of breathlessness was obtained at 1 minute intervals during RLB on a 100 mm Visual Analog Scale anchored at the bottom by No Intensity and at the top by Greatest Intensity." (NCT01580423)
Timeframe: At 1 minute intervals during Resistive Load Breathing at Period 1 (Day 3 or 4) and Period 2 (Day 5, 6 or 7)

Interventionunits on a scale (Mean)
Aprepitant80.8
Inert Powder77.9

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Intensity of Pain

"Time-weighted averages for intensity of pain.~Subject rating of intensity of pain on a 100 mm Visual Analog Scale anchored at the bottom by No Intensity and at the top by Greatest Intensity was obtained during immersion of the subject's non-dominant hand in cold water." (NCT01580423)
Timeframe: Every 15 seconds during immersion of hand in cold water for up to 5 minutes at Period 1 (Day 3 or 4) and Period 2 (Day 5, 6 or 7)

Interventionunits on a scale (Mean)
Aprepitant85.8
Inert Powder81.9

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Unpleasantness of Breathlessness

"Time-weighted averages of unpleasantness of breathlessness.~Subject rating of unpleasantness of breathlessness was obtained at 1 minute intervals during RLB on a 100 mm Visual Analog Scale anchored at the bottom by No Unpleasantness and at the top by Greatest Unpleasantness." (NCT01580423)
Timeframe: At 1 minute intervals during Resistive Load Breathing at Period 1 (Day 3 or 4) and Period 2 (Day 5, 6 or 7)

Interventionunits on a scale (Mean)
Aprepitant76.2
Inert Powder72.2

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Percentage of Participants With Severe Infusion-site Reactions

The percentages of participants with severe infusion-site reactions, including severe site pain, or severe site redness (erythema) or severe site hardness (induration) are presented. (NCT01594749)
Timeframe: Day 1 through Day 17, inclusive

InterventionPercentage of Participants (Number)
Fosaprepitant Regimen0.0
Control Regimen0.0

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Percentage of Participants With Complete Response From 0 to 120 Hours After Initiation of MEC

A Complete Response was defined as no vomiting and no use of rescue medication. (NCT01594749)
Timeframe: 0 to 120 hours after initiation of MEC

InterventionPercentage of Participants (Number)
Fosaprepitant Regimen77.1
Control Regimen66.9

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Percentage of Participants With No Vomiting From 0 to 120 Hours After Initiation of MEC

No Vomiting was defined as no emetic (vomiting) episodes, including no vomiting and no retching or dry heaves (attempts to vomit that are not productive of stomach contents), regardless of use of rescue medication. (NCT01594749)
Timeframe: 0 to 120 hours after initiation of MEC

InterventionPercentage of participants (Number)
Fosaprepitant Regimen82.7
Control Regimen72.9

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Percentage of Participants With Infusion-site Thrombophlebitis

The percentages of participants with infusion-site thrombophlebitis are presented. Thrombophlebitis was defined as a condition affecting a superficial vein used for an IV infusion, associated with red color, hardness upon palpation, and the presence of a tender cord and possible fever. (NCT01594749)
Timeframe: Day 1 through Day 17, inclusive

InterventionPercentage of Participants (Number)
Fosaprepitant Regimen0.6
Control Regimen0.0

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Percentage of Participants With Complete Response From 0 to 24 Hours After Initiation of MEC

A Complete Response was defined as no vomiting and no use of rescue medication. (NCT01594749)
Timeframe: 0 to 24 hours after initiation of MEC

InterventionPercentage of Participants (Number)
Fosaprepitant Regimen93.2
Control Regimen91.0

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Percentage of Participants With Complete Response From 25 to 120 Hours After Initiation of Moderately Emetogenic Chemotherapy (MEC)

A Complete Response was defined as no vomiting and no use of rescue medication. (NCT01594749)
Timeframe: 25 to 120 hours after initiation of MEC

InterventionPercentage of Participants (Number)
Fosaprepitant Regimen78.9
Control Regimen68.5

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Change From Week 0 in Cannabis Use Using Urinary CN-THCCOOH Levels at Week 8

Urinary THC/Cr ratio, also known as CN-THCCOOH (creatinine normalized tetrahydrocannabinol carboxylic acid), is a highly sensitive and specific quantitative analytic procedure to determine current marijuana metabolite levels in the urine as well as new marijuana use or abstinence. Gas chromatography mass spectrometric levels of 11-nor-9-carboxy-9-THC (THC-COOH), the primary marijuana metabolite, are normalized to the urine creatinine (CN) concentration to reduce the variability of drug measurement attributable to urine dilution. Negative values indicate decreased use. Change = (Week 8 value - Week 0 value). (NCT01611948)
Timeframe: Week 0 and Week 8

Interventionng/mg (Mean)
Aprepitant: 125mg/Day-334.21
Matched Placebo-359.95

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Quality of Life

"The secondary endpoint is the quality of life as measured on the Dermatology Quality of Life Index (DLQI).~For a series of 10 questions the responses are scored: Very much, scored 3; A lot, scored 2; A little, scored 1; Not at all, scored 0; Not relevant, scored 0; and Question unanswered, scored 0. The scores are summed and the larger the score the greater the effect of the dermatological disease impact on quality of life.~Maximum response for all ten questions 30, minimum 0." (NCT01625455)
Timeframe: one week

Interventionscores on a scale (Mean)
Aprepitant14.2
Placebo14.8

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Severity of Pruritus

The primary endpoint is the severity of pruritus as measured on the visual analogue scale. A score of 100 indicated the worst pruritus imaginable, while 0 indicated no pruritus. (NCT01625455)
Timeframe: one week

Interventionunits on a scale (Mean)
Aprepitant58.20
Placebo47.47

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Number of Participants With No Use of a Rescue Therapy - Overall, Acute, and Delayed Stages

The percentage of participants who used no rescue therapy after initiation of MEC is presented for the Overall, Acute and Delayed Stages. Overall Stage=0 to 120 hours after initiation of MEC. Acute Stage=0 to 24 hours after initiation of MEC. Delayed Stage=25 to 120 hours after initiation of MEC. (NCT01636947)
Timeframe: Day 1 to Day 5

,
InterventionPercentage of Participants (Number)
Overall StageAcute StageDelayed Stage
Aprepitant Regimen84.898.784.8
Control Regimen87.799.288.5

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Percentage of Participants With a Complete Response - Overall, Acute, and Delayed Stages

A Complete Response was defined as no vomiting or dry heaves and no use of a rescue therapy. Overall Stage=0 to 120 hours after initiation of MEC. Acute Stage=0 to 24 hours after initiation of MEC. Delayed Stage=25 to 120 hours after initiation of MEC. (NCT01636947)
Timeframe: Hour 0 on Day 1 to Day 5 (approximately 120 hours)

,
InterventionPercentage of Participants (Number)
Overall StageAcute StageDelayed Stage
Aprepitant Regimen73.495.874.3
Control Regimen70.497.971.2

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Percentage of Participants With No Vomiting - Acute and Delayed Stages

A vomiting episode was defined as one or more episodes of emesis (expulsion of stomach contents through the mouth) or retches (an attempt to vomit that is not productive of stomach contents). Acute Stage=0 to 24 hours after initiation of MEC. Delayed Stage=25 to 120 hours after initiation of MEC. (NCT01636947)
Timeframe: Day 1, Day 2 to Day 5

,
InterventionPercentage of Participants (Number)
Acute StageDelayed Stage
Aprepitant Regimen95.878.5
Control Regimen98.872.4

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Number of Emetic Events - Overall Stage

The number of emetic events that occurred during the Overall Stage (0 to 120 hours after initiation of MEC) are presented. (NCT01636947)
Timeframe: Hour 0 on Day 1 to Day 5 (approximately 120 hours)

InterventionNumber of Emetic Events (Number)
Aprepitant Regimen54
Control Regimen68

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Percentage of Participants With No Impact on Daily Life - Overall Stage

"The Functional Living Index-Emesis questionnaire (FLIE) is a validated, participant-reported instrument to measure the impact of chemotherapy-induced nausea and vomiting on daily life. There are 9 nausea-related items and 9 vomiting-related items, each on a 7-point scale. For the purposes of this study, No Impact on daily life was defined as an average item score of >6 on the 7-point scale; a total score >108 indicates no impact on daily life. Overall Stage=0 to 120 hours after initiation of MEC." (NCT01636947)
Timeframe: Day 6

InterventionPercentage of Participants (Number)
Aprepitant Regimen76.8
Control Regimen73.8

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Percentage of Participants With No Vomiting and No Significant Nausea - Overall Stage

"Nausea was to be assessed using a 100-mm horizontal visual analogue scale (VAS) located in the participant diary labeled: How much nausea have you had over the last 24 hours? The left end of the scale (0 mm) was labeled no nausea, and the right end of the scale (100 mm) is labeled nausea as bad as it could be. In this study, No Significant Nausea was defined as a VAS nausea rating <25 mm." (NCT01636947)
Timeframe: Days 1 to Day 5

InterventionPercentage of Participants (Number)
Aprepitant Regimen76.4
Control Regimen72.4

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Percentage of Participants With One or More Clinical Adverse Event

An adverse event was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the study drug, whether or not considered related to the use of the study drug. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition, which is temporally associated with the use of the study drug, is also an adverse event. Nausea and vomiting experienced during Days 1-6 were not counted as adverse events unless they were reported as a serious adverse event. (NCT01636947)
Timeframe: Day 1 through Day 29 (Up to 28 days after first dose of study drug)

InterventionPercentage of Participants (Number)
Aprepitant Regimen56.2
Control Regimen53.2

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The Percentage of Participants With No Vomiting - Overall Stage

A vomiting episode was defined as one or more episodes of emesis (expulsion of stomach contents through the mouth) or retches (an attempt to vomit that is not productive of stomach contents). No vomiting during the Overall Stage was defined as no episodes of emesis during the 120 hours (Days 1-5) after initiation of moderately emetogenic chemotherapy (MEC). (NCT01636947)
Timeframe: Hour 0 on Day 1 to Day 5 (approximately 120 hours)

InterventionPercentage of Participants (Number)
Aprepitant Regimen77.2
Control Regimen72.0

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Delayed CR (Complete Response)

After the First Course of HEC, Defined as no Emesis and no Use of Rescue Medication From Time 24to 120 Hours. (NCT01640340)
Timeframe: 24-120 hours after chemotherapy

Interventionpercentage of participants (Number)
Arm A (Palonosetron 0.25 mg IV on Day 1)65
Arm B (Ondansetron 24 mg Oral on Day 1)45

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Use of Rescue Medication for Each Treatment Arm

(NCT01640340)
Timeframe: From time 0 to 120 hours

Interventionpercentage of participants (Number)
Arm A (Palonosetron 0.25 mg IV on Day 1)35
Arm B (Ondansetron 24 mg Oral on Day 1)55

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Acute CR (Complete Response)

After the First Course of HEC, Defined as no Emesis and no Use of Rescue Medication from time 0 to 24 hours. (NCT01640340)
Timeframe: 0-24 hours after chemotherapy

Interventionpercentage of particpants (Number)
Arm A (Palonosetron 0.25 mg IV on Day 1)75
Arm B (Ondansetron 24 mg Oral on Day 1)55

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Overall CR(Complete Response)After the First Course of HEC, Defined as no Emesis and no Use of Rescue Medication

We will use exact binomial methods to estimate proportions and their associated 95% confidence intervals. (NCT01640340)
Timeframe: Up to 120 hours after completion of chemotherapy

Interventionpercentage of patients (Number)
Arm A (Palonosetron 0.25 mg IV on Day 1)65
Arm B (Ondansetron 24 mg Oral on Day 1)40

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Percentage of Patients Who Experienced Grade 1, 2 or 3 Nausea From Time 0 to 120 Hours

The percentage of patients who experienced grade 1, 2 or 3 nausea from time 0 to 120 hours. Nausea graded using the National Cancer Institute (NCI) CTCAE (Common Toxicity Criteria for Adverse Effects)version 4.0 Nausea Grading Scale. Grade 1=Loss of appetite without alteration in eating habits, Grade 2= Oral intake decreased without significant weight loss, dehydration or malnutrition, Grade 3= Inadequate oral caloric or fluid intake; tube feeding, TPN, or hospitalization indicated. (NCT01640340)
Timeframe: Time 0 to 120 hours

Interventionpercentage of participants (Number)
Arm A (Palonosetron 0.25 mg IV on Day 1)55
Arm B (Ondansetron 24 mg Oral on Day 1)65

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Percentage of Patients Who Experienced Grade 1, 2 or 3 Vomiting From Time 0 to 120 Hours

The percentage of patients who experienced grade 1, 2 or 3 vomiting from time 0 to 120 hours. Nausea graded using the National Cancer Institute (NCI) CTCAE v 4.0 vomiting Grading Scale. Grade 1=Loss of appetite without alteration in eating habits, Grade 2= Oral intake decreased without significant weight loss, dehydration or malnutrition, Grade 3= Inadequate oral caloric or fluid intake; tube feeding, TPN, or hospitalization indicated. (NCT01640340)
Timeframe: From time 0 to 120 hours

Interventionpercentage of participants (Number)
Arm A (Palonosetron 0.25 mg IV on Day 1)5
Arm B (Ondansetron 24 mg Oral on Day 1)15

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Area Under the Concentration-time Curve of Aprepitant From Time 0 to Infinity (AUC 0-∞) in Participants 0 to <2 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The AUC 0-∞ for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhr•ng/mL (Mean)
Fosaprepitant 5 mg/kg: 0 to <2 Years-Cycle 137200

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Area Under the Concentration-time Curve of Aprepitant From Time 0 to 24 Hours (AUC 0-24hr) in Participants 0 to <2 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The AUC 0-24hr for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhr•ng/mL (Mean)
Fosaprepitant 5 mg/kg: 0 to <2 Years-Cycle 136800

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Apparent Total Body Clearance (CL/F) of Aprepitant in Participants 0 to <2 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The CL/F for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

InterventionmL/min (Mean)
Fosaprepitant 5 mg/kg: 0 to <2 Years-Cycle 124.2

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Apparent Terminal Half-life (t1/2) of Aprepitant in Participants 0 to <2 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The t1/2 for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhours (Mean)
Fosaprepitant 5 mg/kg: 0 to <2 Years-Cycle 17.94

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C24hr of Aprepitant in Participants 6 to <12 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The C24hr for aprepitant was determined by measuring aprepitant levels in the time frame of 23 to 25 hours post-infusion. (NCT01697579)
Timeframe: Approximately 24 hours (from 23 to 25 hours) post-infusion

Interventionng/mL (Mean)
Fosaprepitant 5 mg/kg: 6 to <12 Years-Cycle 11210
Fosaprepitant 3 mg/kg: 6 to <12 Years-Cycle 1589
Fosaprepitant 1.2 mg/kg: 6 to <12 Years-Cycle 1219
Fosaprepitant 0.4 mg/kg: 6 to <12 Years-Cycle 170.4

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AUC 0-24hr of Aprepitant in Participants 6 to <12 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The AUC 0-24hr for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhr•ng/mL (Mean)
Fosaprepitant 5 mg/kg: 6 to <12 Years-Cycle 147400
Fosaprepitant 3 mg/kg: 6 to <12 Years-Cycle 129200
Fosaprepitant 1.2 mg/kg: 6 to <12 Years-Cycle 112000
Fosaprepitant 0.4 mg/kg: 6 to <12 Years-Cycle 14260

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C24hr of Aprepitant in Participants 12 to 17 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The C24hr for aprepitant was determined by measuring aprepitant levels in the time frame of 23 to 25 hours post-infusion. (NCT01697579)
Timeframe: Approximately 24 hours (from 23 to 25 hours) post-infusion

Interventionng/mL (Mean)
Fosaprepitant 3 mg/kg: 12 to 17 Years-Cycle 1735
Fosaprepitant 1.2 mg/kg: 12 to 17 Years-Cycle 1142
Fosaprepitant 0.4 mg/kg: 12 to 17 Years-Cycle 1101

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Cmax of Aprepitant in Participants 2 to <6 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The Cmax for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionng/mL (Mean)
Fosaprepitant 5 mg/kg: 2 to <6 Years-Cycle 14270
Fosaprepitant 3 mg/kg: 2 to <6 Years-Cycle 12320
Fosaprepitant 1.2 mg/kg: 2 to <6 Years-Cycle 12030
Fosaprepitant 0.4 mg/kg: 2 to <6 Years-Cycle 1323

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C48hr of Aprepitant in Participants 2 to <6 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The C48hr for aprepitant was determined by measuring aprepitant levels in the time frame of 46 to 50 hours post-infusion. The C48hr was only planned to be measured in the 5 mg/mL dose for each age group. (NCT01697579)
Timeframe: Approximately 48 hours (from 46 to 50 hours) post-infusion

Interventionng/mL (Mean)
Fosaprepitant 5 mg/kg: 2 to <6 Years-Cycle 1232

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Cmax of Aprepitant in Participants 6 to <12 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The Cmax for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionng/mL (Mean)
Fosaprepitant 5 mg/kg: 6 to <12 Years-Cycle 14400
Fosaprepitant 3 mg/kg: 6 to <12 Years-Cycle 13550
Fosaprepitant 1.2 mg/kg: 6 to <12 Years-Cycle 11360
Fosaprepitant 0.4 mg/kg: 6 to <12 Years-Cycle 1507

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Concentration of Aprepitant After 24 Hours (C24hr) in Participants 0 to <2 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The C24hr for aprepitant was determined by measuring aprepitant levels in the time frame of 23 to 25 hours post-infusion. (NCT01697579)
Timeframe: Approximately 24 hours (from 23 to 25 hours) post-infusion

Interventionng/mL (Mean)
Fosaprepitant 5 mg/kg: 0 to <2 Years-Cycle 1691

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Concentration of Aprepitant After 48 Hours (C48hr) in Participants 0 to <2 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The C48hr for aprepitant was determined by measuring aprepitant levels in the time frame of 46 to 50 hours post-infusion. The C48hr was only planned to be measured in the 5 mg/mL dose for each age group. (NCT01697579)
Timeframe: Approximately 48 hours (from 46 to 50 hours) post-infusion

Interventionng/mL (Mean)
Fosaprepitant 5 mg/kg: 0 to <2 Years-Cycle 1352

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CL/F of Aprepitant in Participants 12 to 17 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The CL/F for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

InterventionmL/min (Mean)
Fosaprepitant 3 mg/kg: 12 to 17 Years-Cycle 176.2
Fosaprepitant 1.2 mg/kg: 12 to 17 Years-Cycle 191.7
Fosaprepitant 0.4 mg/kg: 12 to 17 Years-Cycle 1105

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Maximum Concentration (Cmax) of Aprepitant in Participants 0 to <2 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The Cmax for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionng/mL (Mean)
Fosaprepitant 5 mg/kg: 0 to <2 Years-Cycle 13550

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Percentage of Participants Who Experienced at Least One Adverse Event (AE) in Cycle 1

AE was defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which did not necessarily have to have a causal relationship with this treatment. An AE could therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product/protocol specified procedure, whether or not considered related to the medicinal product/protocol specified procedure. Any worsening of a preexisting condition temporally associated with the use of the product was also an AE. (NCT01697579)
Timeframe: Up to 14 days postdose in Cycle 1

InterventionPercentage of participants (Number)
Fosaprepitant 5 mg/Kg-Cycle 187.8
Fosaprepitant 3 mg/Kg-Cycle 183.3
Fosaprepitant 1.2 mg/Kg-Cycle 190.7
Fosaprepitant 0.4 mg/Kg-Cycle 180.0
Placebo Control-Cycle 177.1

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Percentage of Participants Who Experienced at Least One Adverse Event (AE) in Cycles 2-6

AE was defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which did not necessarily have to have a causal relationship with this treatment. An AE could therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product/protocol specified procedure, whether or not considered related to the medicinal product/protocol specified procedure. Any worsening of a preexisting condition temporally associated with the use of the product was also an AE. (NCT01697579)
Timeframe: Up to 14 days postdose for each cycle (Cycles 2-6)

InterventionPercentage of participants (Number)
Fosaprepitant 5 mg/Kg-Cycles 2-693.6
Fosaprepitant 3 mg/Kg-Cycles 2-675.5

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t1/2 of Aprepitant in Participants 12 to 17 Years of Age Hours

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The t1/2 for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhours (Mean)
Fosaprepitant 3 mg/kg: 12 to 17 Years-Cycle 110.5
Fosaprepitant 1.2 mg/kg: 12 to 17 Years-Cycle 17.92
Fosaprepitant 0.4 mg/kg: 12 to 17 Years-Cycle 18.27

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t1/2 of Aprepitant in Participants 2 to <6 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The t1/2 for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhours (Mean)
Fosaprepitant 5 mg/kg: 2 to <6 Years-Cycle 19.27
Fosaprepitant 3 mg/kg: 2 to <6 Years-Cycle 16.55
Fosaprepitant 1.2 mg/kg: 2 to <6 Years-Cycle 17.27
Fosaprepitant 0.4 mg/kg: 2 to <6 Years-Cycle 16.18

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C24hr of Aprepitant in Participants 2 to <6 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The C24hr for aprepitant was determined by measuring aprepitant levels in the time frame of 23 to 25 hours post-infusion. (NCT01697579)
Timeframe: Approximately 24 hours (from 23 to 25 hours) post-infusion

Interventionng/mL (Mean)
Fosaprepitant 5 mg/kg: 2 to <6 Years-Cycle 11060
Fosaprepitant 3 mg/kg: 2 to <6 Years-Cycle 1278
Fosaprepitant 1.2 mg/kg: 2 to <6 Years-Cycle 1332
Fosaprepitant 0.4 mg/kg: 2 to <6 Years-Cycle 19.23

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AUC 0-24hr of Aprepitant in Participants 12 to 17 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The AUC 0-24hr for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhr•ng/mL (Mean)
Fosaprepitant 3 mg/kg: 12 to 17 Years-Cycle 130400
Fosaprepitant 1.2 mg/kg: 12 to 17 Years-Cycle 19700
Fosaprepitant 0.4 mg/kg: 12 to 17 Years-Cycle 14820

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AUC 0-∞ of Aprepitant in Participants 6 to <12 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The AUC 0-∞ for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhr•ng/mL (Mean)
Fosaprepitant 5 mg/kg: 6 to <12 Years-Cycle 155300
Fosaprepitant 3 mg/kg: 6 to <12 Years-Cycle 134300
Fosaprepitant 1.2 mg/kg: 6 to <12 Years-Cycle 110700
Fosaprepitant 0.4 mg/kg: 6 to <12 Years-Cycle 12860

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AUC 0-∞ of Aprepitant in Participants 2 to <6 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The AUC 0-∞ for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhr•ng/mL (Mean)
Fosaprepitant 5 mg/kg: 2 to <6 Years-Cycle 146400
Fosaprepitant 3 mg/kg: 2 to <6 Years-Cycle 115300
Fosaprepitant 1.2 mg/kg: 2 to <6 Years-Cycle 116000
Fosaprepitant 0.4 mg/kg: 2 to <6 Years-Cycle 12070

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t1/2 of Aprepitant in Participants 6 to <12 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The t1/2 for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhours (Mean)
Fosaprepitant 5 mg/kg: 6 to <12 Years-Cycle 19.77
Fosaprepitant 3 mg/kg: 6 to <12 Years-Cycle 17.69
Fosaprepitant 1.2 mg/kg: 6 to <12 Years-Cycle 18.23
Fosaprepitant 0.4 mg/kg: 6 to <12 Years-Cycle 16.58

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Time to Maximum Concentration (Tmax) of Aprepitant in Participants 0 to <2 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The Tmax for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhours (Mean)
Fosaprepitant 5 mg/kg: 0 to <2 Years-Cycle 12.01

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Tmax of Aprepitant in Participants 12 to 17 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The Tmax for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhours (Mean)
Fosaprepitant 3 mg/kg: 12 to 17 Years-Cycle 10.546
Fosaprepitant 1.2 mg/kg: 12 to 17 Years-Cycle 10.722
Fosaprepitant 0.4 mg/kg: 12 to 17 Years-Cycle 10.736

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C48hr of Aprepitant in Participants 6 to <12 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The C48hr for aprepitant was determined by measuring aprepitant levels in the time frame of 46 to 50 hours post-infusion. The C48hr was only planned to be measured in the 5 mg/mL dose for each age group. (NCT01697579)
Timeframe: Approximately 48 hours (from 46 to 50 hours) post-infusion

Interventionng/mL (Mean)
Fosaprepitant 5 mg/kg: 6 to <12 Years-Cycle 1164

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Tmax of Aprepitant in Participants 6 to <12 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The Tmax for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhours (Mean)
Fosaprepitant 5 mg/kg: 6 to <12 Years-Cycle 12.92
Fosaprepitant 3 mg/kg: 6 to <12 Years-Cycle 11.99
Fosaprepitant 1.2 mg/kg: 6 to <12 Years-Cycle 12.14
Fosaprepitant 0.4 mg/kg: 6 to <12 Years-Cycle 11.68

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AUC 0-∞ of Aprepitant in Participants 12 to 17 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The AUC 0-∞ for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhr•ng/mL (Mean)
Fosaprepitant 3 mg/kg: 12 to 17 Years-Cycle 133800
Fosaprepitant 1.2 mg/kg: 12 to 17 Years-Cycle 112300
Fosaprepitant 0.4 mg/kg: 12 to 17 Years-Cycle 13500

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AUC 0-24hr of Aprepitant in Participants 2 to <6 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The AUC 0-24hr for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhr•ng/mL (Mean)
Fosaprepitant 5 mg/kg: 2 to <6 Years-Cycle 145000
Fosaprepitant 3 mg/kg: 2 to <6 Years-Cycle 121800
Fosaprepitant 1.2 mg/kg: 2 to <6 Years-Cycle 119700
Fosaprepitant 0.4 mg/kg: 2 to <6 Years-Cycle 11840

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CL/F of Aprepitant in Participants 2 to <6 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The CL/F for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

InterventionmL/min (Mean)
Fosaprepitant 5 mg/kg: 2 to <6 Years-Cycle 131.8
Fosaprepitant 3 mg/kg: 2 to <6 Years-Cycle 166.2
Fosaprepitant 1.2 mg/kg: 2 to <6 Years-Cycle 129.6
Fosaprepitant 0.4 mg/kg: 2 to <6 Years-Cycle 148.5

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CL/F of Aprepitant in Participants 6 to <12 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The CL/F for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

InterventionmL/min (Mean)
Fosaprepitant 5 mg/kg: 6 to <12 Years-Cycle 142.1
Fosaprepitant 3 mg/kg: 6 to <12 Years-Cycle 169.2
Fosaprepitant 1.2 mg/kg: 6 to <12 Years-Cycle 178.8
Fosaprepitant 0.4 mg/kg: 6 to <12 Years-Cycle 189.6

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Cmax of Aprepitant in Participants 12 to 17 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The Cmax for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionng/mL (Mean)
Fosaprepitant 3 mg/kg: 12 to 17 Years-Cycle 13500
Fosaprepitant 1.2 mg/kg: 12 to 17 Years-Cycle 11180
Fosaprepitant 0.4 mg/kg: 12 to 17 Years-Cycle 1582

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Tmax of Aprepitant in Participants 2 to <6 Years of Age

Fosaprepitant is a pro-drug that is rapidly converted to aprepitant. Because of this rapid conversion to aprepitant, fosaprepitant cannot be assessed directly. The pharmacokinetics for each fosaprepitant dose were determined by analyzing aprepitant in plasma. The Tmax for aprepitant was determined by measuring aprepitant levels at pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion. (NCT01697579)
Timeframe: Pre-infusion, immediately after infusion, and 2-4, 5-7, 8-10, 23-25, and 46-50 hours post-infusion

Interventionhours (Mean)
Fosaprepitant 5 mg/kg: 2 to <6 Years-Cycle 11.90
Fosaprepitant 3 mg/kg: 2 to <6 Years-Cycle 12.29
Fosaprepitant 1.2 mg/kg: 2 to <6 Years-Cycle 11.36
Fosaprepitant 0.4 mg/kg: 2 to <6 Years-Cycle 11.34

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Cmax of Aprepitant Following Administration of 125 mg Dose Equivalent in Birth to <2 Year Age Group

Cmax was analyzed independently for participants in the 125 mg dose equivalent arm aged birth to <2 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Cmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative plasma Cmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionng/mL (Geometric Mean)
Aprepitant Dose 1: Equivalent to 125 mg in Adults; Birth to <21280

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Cmax of Aprepitant Following Administration of 40 mg Dose Equivalent in 2 to <6 Year Age Group

Cmax was analyzed independently for participants in the 40 mg dose equivalent arm aged 2 to <6 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Cmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Cmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionng/mL (Geometric Mean)
Aprepitant Dose 2: Equivalent to 40 mg in Adults; 2 to <61290

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Cmax of Aprepitant Following Administration of 40 mg Dose Equivalent in 6 to <12 Year Age Group

Cmax was analyzed independently for participants in the 40 mg dose equivalent arm aged 6 to <12 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Cmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Cmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionng/mL (Geometric Mean)
Aprepitant Dose 2: Equivalent to 40 mg in Adults; 6 to <12930

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Cmax of Aprepitant Following Administration of 40 mg Dose Equivalent in Birth to <2 Year Age Group

Cmax was analyzed independently for participants in the 40 mg dose equivalent arm aged birth to <2 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Cmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Cmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionng/mL (Geometric Mean)
Aprepitant Dose 2: Equivalent to 40 mg in Adults; Birth to <21570

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Maximum Concentration (Cmax) of Aprepitant Following Administration of 125 mg Dose Equivalent in 12 to 17 Year Age Group

Cmax was analyzed independently for participants in the 125 mg dose equivalent arm aged 12 to 17 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Cmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Cmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionng/mL (Geometric Mean)
Aprepitant Dose 1: Equivalent to 125 mg in Adults; 12 to 171340

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Percentage of Participants Discontinuing Study Due to an AE

An AE was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR's product, whether or not considered related to the use of the product. Any worsening of a pre-existing condition which is temporally associated with the use of the SPONSOR's product, was also an AE. Changes resulting from normal growth and development which did not vary significantly in frequency or severity from expected levels were not to be considered adverse events. Vomiting and retching were not defined as AEs during the period of data collection (24 hours following the end of surgery) unless they met the definition of an SAE. The percentage of participants discontinuing study due to an AE was reported by dose group. (NCT01732458)
Timeframe: From pre-operative phase up to Follow-up (Day 1 to Day 15)

Interventionpercentage of participants (Number)
Aprepitant Dose 1: Equivalent to 125 mg in Adults0
Aprepitant Dose 2: Equivalent to 40 mg in Adults0
Aprepitant Dose 3: Equivalent to 10 mg in Adults0
Ondansetron0

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Time to Maximum Concentration (Tmax) of Aprepitant Following Administration of 125 mg Dose Equivalent in 12 to 17 Year Age Group

Tmax was analyzed independently for participants in the 125 mg dose equivalent arm aged 12 to 17 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Tmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Tmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhour (hr) (Geometric Mean)
Aprepitant Dose 1: Equivalent to 125 mg in Adults; 12 to 174.86

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Tmax Following Administration of 40 mg Dose Equivalent in 12 to 17 Year Age Group

Tmax was analyzed independently for participants in the 40 mg dose equivalent arm aged 12 to 17 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Tmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Tmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr (Geometric Mean)
Aprepitant Dose 2: Equivalent to 40 mg in Adults; 12 to 174.17

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Tmax of Aprepitant Following Administration of 10 mg Dose Equivalent in 12 to 17 Year Age Group

Tmax was analyzed independently for participants in the 10 mg dose equivalent arm aged 12 to 17 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Tmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Tmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr (Geometric Mean)
Aprepitant Dose 3: Equivalent to 10 mg in Adults; 12 to 173.53

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Tmax of Aprepitant Following Administration of 10 mg Dose Equivalent in 2 to <6 Year Age Group

Tmax was analyzed independently for participants in the 10 mg dose equivalent arm aged 2 to <6 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Tmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Tmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr (Geometric Mean)
Aprepitant Dose 3: Equivalent to 10 mg in Adults; 2 to <63.36

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Tmax of Aprepitant Following Administration of 10 mg Dose Equivalent in 6 to <12 Year Age Group

Tmax was analyzed independently for participants in the 10 mg dose equivalent arm aged 6 to <12 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Tmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Tmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr (Geometric Mean)
Aprepitant Dose 3: Equivalent to 10 mg in Adults; 6 to <123.75

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Tmax of Aprepitant Following Administration of 125 mg Dose Equivalent in 2 to <6 Year Age Group

Tmax was analyzed independently for participants in the 125 mg dose equivalent arm aged 2 to <6 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Tmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Tmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr (Geometric Mean)
Aprepitant Dose 1: Equivalent to 125 mg in Adults; 2 to <64.91

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Tmax of Aprepitant Following Administration of 125 mg Dose Equivalent in 6 to <12 Year Age Group

Tmax was analyzed independently for participants in the 125 mg dose equivalent arm aged 6 to <12 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Tmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Tmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr (Geometric Mean)
Aprepitant Dose 1: Equivalent to 125 mg in Adults; 6 to <126.82

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Tmax of Aprepitant Following Administration of 125 mg Dose Equivalent in Birth to <2 Year Age Group

Tmax was analyzed independently for participants in the 125 mg dose equivalent arm aged birth to <2 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Tmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Tmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr (Geometric Mean)
Aprepitant Dose 1: Equivalent to 125 mg in Adults; Birth to <24.71

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Tmax of Aprepitant Following Administration of 40 mg Dose Equivalent in 2 to <6 Year Age Group

Tmax was analyzed independently for participants in the 40 mg dose equivalent arm aged 2 to <6 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Tmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Tmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr (Geometric Mean)
Aprepitant Dose 2: Equivalent to 40 mg in Adults; 2 to <63.35

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Tmax of Aprepitant Following Administration of 40 mg Dose Equivalent in 6 to <12 Year Age Group

Tmax was analyzed independently for participants in the 40 mg dose equivalent arm aged 6 to <12 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Tmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Tmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr (Geometric Mean)
Aprepitant Dose 2: Equivalent to 40 mg in Adults; 6 to <124.22

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Tmax of Aprepitant Following Administration of 40 mg Dose Equivalent in Birth to <2 Year Age Group

Tmax was analyzed independently for participants in the 40 mg dose equivalent arm aged birth to <2 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Tmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Tmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr (Geometric Mean)
Aprepitant Dose 2: Equivalent to 40 mg in Adults; Birth to <24.94

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Percentage of Participants Experiencing at Least One Adverse Event (AE)

An AE was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the SPONSOR's product, whether or not considered related to the use of the product. Any worsening of a pre-existing condition which is temporally associated with the use of the SPONSOR's product, was also an AE. Changes resulting from normal growth and development which did not vary significantly in frequency or severity from expected levels were not to be considered adverse events. Vomiting and retching were not defined as AEs during the period of data collection (24 hours following the end of surgery) unless they met the definition of an SAE. The percentage of participants experiencing ≥1 AE was reported by dose group. (NCT01732458)
Timeframe: From pre-operative phase up to Follow-up (Day 1 to Day 15)

Interventionpercentage of participants (Number)
Aprepitant Dose 1: Equivalent to 125 mg in Adults31.6
Aprepitant Dose 2: Equivalent to 40 mg in Adults43.6
Aprepitant Dose 3: Equivalent to 10 mg in Adults35.7
Ondansetron48.1

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Tmax of Aprepitant Following Administration of 10 mg Dose Equivalent in Birth to <2 Year Age Group

Tmax was analyzed independently for participants in the 10 mg dose equivalent arm aged from birth to <2 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Tmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Tmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr (Geometric Mean)
Aprepitant Dose 3: Equivalent to 10 mg in Adults; Birth to <24.11

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Area Under the Concentration-time Curve of Aprepitant From Time 0 to the Last Measurable Concentration (AUC0-last) Following Administration of 125 mg Dose Equivalent in 12 to 17 Year Age Group

AUC0-last was analyzed independently for participants in the 125 mg dose equivalent arm aged 12 to 17 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant AUC0-last assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma AUC0-last was evaluated using a noncompartmental analysis (NCA). The limit of quantitation (LOQ) value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr*ng/mL (Geometric Mean)
Aprepitant Dose 1: Equivalent to 125 mg in Adults; 12 to 177120

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AUC0-last Following Administration of 10 mg Dose Equivalent in 12 to 17 Year Age Group

AUC0-last was analyzed independently for participants in the 10 mg dose equivalent arm aged 12 to 17 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant AUC0-last assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma AUC0-last was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr*ng/mL (Geometric Mean)
Aprepitant Dose 3: Equivalent to 10 mg in Adults; 12 to 17806

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AUC0-last Following Administration of 40 mg Dose Equivalent in 12 to 17 Year Age Group

AUC0-last was analyzed independently for participants in the 40 mg dose equivalent arm aged 12 to 17 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant AUC0-last assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma AUC0-last was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr*ng/mL (Geometric Mean)
Aprepitant Dose 2: Equivalent to 40 mg in Adults; 12 to 172570

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AUC0-last of Aprepitant Following Administration of 10 mg Dose Equivalent in 2 to <6 Year Age Group

AUC0-last was analyzed independently for participants in the 10 mg dose equivalent arm aged 2 to <6 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant AUC0-last assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma AUC0-last was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr*ng/mL (Geometric Mean)
Aprepitant Dose 3: Equivalent to 10 mg in Adults; 2 to <61580

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AUC0-last of Aprepitant Following Administration of 10 mg Dose Equivalent in 6 to <12 Year Age Group

AUC0-last was analyzed independently for participants in the 10 mg dose equivalent arm aged 6 to <12 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant AUC0-last assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma AUC0-last was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr*ng/mL (Geometric Mean)
Aprepitant Dose 3: Equivalent to 10 mg in Adults; 6 to <121390

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AUC0-last of Aprepitant Following Administration of 10 mg Dose Equivalent in Birth to <2 Year Age Group

AUC0-last was analyzed independently for participants in the 10 mg dose equivalent arm aged from birth to <2 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant AUC0-last assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma AUC0-last was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr*ng/mL (Geometric Mean)
Aprepitant Dose 3: Equivalent to 10 mg in Adults; Birth to <21800

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AUC0-last of Aprepitant Following Administration of 125 mg Dose Equivalent in 2 to <6 Year Age Group

AUC0-last was analyzed independently for participants in the 125 mg dose equivalent arm aged 2 to <6 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant AUC0-last assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma AUC0-last was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr*ng/mL (Geometric Mean)
Aprepitant Dose 1: Equivalent to 125 mg in Adults; 2 to <612000

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AUC0-last of Aprepitant Following Administration of 125 mg Dose Equivalent in 6 to <12 Year Age Group

AUC0-last was analyzed independently for participants in the 125 mg dose equivalent arm aged 6 to <12 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant AUC0-last assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma AUC0-last was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr*ng/mL (Geometric Mean)
Aprepitant Dose 1: Equivalent to 125 mg in Adults; 6 to <1210300

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AUC0-last of Aprepitant Following Administration of 125 mg Dose Equivalent in Birth to <2 Year Age Group

AUC0-last was analyzed independently for participants in the 125 mg dose equivalent arm aged birth to <2 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant AUC0-last assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma AUC0-last was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr*ng/mL (Geometric Mean)
Aprepitant Dose 1: Equivalent to 125 mg in Adults; Birth to <26410

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AUC0-last of Aprepitant Following Administration of 40 mg Dose Equivalent in 2 to <6 Year Age Group

AUC0-last was analyzed independently for participants in the 40 mg dose equivalent arm aged 2 to <6 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant AUC0-last assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma AUC0-last was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr*ng/mL (Geometric Mean)
Aprepitant Dose 2: Equivalent to 40 mg in Adults; 2 to <66320

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AUC0-last of Aprepitant Following Administration of 40 mg Dose Equivalent in 6 to <12 Year Age Group

AUC0-last was analyzed independently for participants in the 40 mg dose equivalent arm aged 6 to <12 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant AUC0-last assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma AUC0-last was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr*ng/mL (Geometric Mean)
Aprepitant Dose 2: Equivalent to 40 mg in Adults; 6 to <124730

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AUC0-last of Aprepitant Following Administration of 40 mg Dose Equivalent in Birth to <2 Year Age Group

AUC0-last was analyzed independently for participants in the 40 mg dose equivalent arm aged birth to <2 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant AUC0-last assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma AUC0-last was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionhr*ng/mL (Geometric Mean)
Aprepitant Dose 2: Equivalent to 40 mg in Adults; Birth to <27910

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Cmax Following Administration of 40 mg Dose Equivalent in 12 to 17 Year Age Group

Cmax was analyzed independently for participants in the 40 mg dose equivalent arm aged 12 to 17 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Cmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Cmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionng/mL (Geometric Mean)
Aprepitant Dose 2: Equivalent to 40 mg in Adults; 12 to 17513

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Cmax of Aprepitant Following Administration of 10 mg Dose Equivalent in 12 to 17 Year Age Group

Cmax was analyzed independently for participants in the 10 mg dose equivalent arm aged 12 to 17 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Cmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Cmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionng/mL (Geometric Mean)
Aprepitant Dose 3: Equivalent to 10 mg in Adults; 12 to 17131

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Cmax of Aprepitant Following Administration of 10 mg Dose Equivalent in 2 to <6 Year Age Group

Cmax was analyzed independently for participants in the 10 mg dose equivalent arm aged 2 to <6 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Cmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Cmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionng/mL (Geometric Mean)
Aprepitant Dose 3: Equivalent to 10 mg in Adults; 2 to <6300

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Cmax of Aprepitant Following Administration of 10 mg Dose Equivalent in 6 to <12 Year Age Group

Cmax was analyzed independently for participants in the 10 mg dose equivalent arm aged 6 to <12 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Cmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Cmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionng/mL (Geometric Mean)
Aprepitant Dose 3: Equivalent to 10 mg in Adults; 6 to <12289

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Cmax of Aprepitant Following Administration of 10 mg Dose Equivalent in Birth to <2 Year Age Group

Cmax was analyzed independently for participants in the 10 mg dose equivalent arm aged from birth to <2 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Cmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Cmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionng/mL (Geometric Mean)
Aprepitant Dose 3: Equivalent to 10 mg in Adults; Birth to <2336

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Cmax of Aprepitant Following Administration of 125 mg Dose Equivalent in 2 to <6 Year Age Group

Cmax was analyzed independently for participants in the 125 mg dose equivalent arm aged 2 to <6 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Cmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Cmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionng/mL (Geometric Mean)
Aprepitant Dose 1: Equivalent to 125 mg in Adults; 2 to <62260

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Cmax of Aprepitant Following Administration of 125 mg Dose Equivalent in 6 to <12 Year Age Group

Cmax was analyzed independently for participants in the 125 mg dose equivalent arm aged 6 to <12 years old due to age- and dose-dependent differences in aprepitant absorption and clearance. Because the opportunity to collect specimens for PK analyses in children is limited, a flexible sparse sampling scheme using ranges of collection times was to be utilized which would limit the burden to participants. Plasma for aprepitant Cmax assessment was obtained at 30-60 minutes prior to aprepitant administration, 2-4 hours post aprepitant administration, 5-7 hours post aprepitant administration, and 8-10 hours post aprepitant administration. Post-operative aprepitant plasma Cmax was evaluated using an NCA. The LOQ value for this analysis was 10 ng/mL. (NCT01732458)
Timeframe: 30-60 minutes pre-administration, 2-4 hours post administration, 5-7 hours post administration, 8-10 hours post administration

Interventionng/mL (Geometric Mean)
Aprepitant Dose 1: Equivalent to 125 mg in Adults; 6 to <121870

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Self-Reported Assessment of Nausea

"the patient's self-reported assessment of nausea Days 1-8 using a 0-100mm visual analog scale (VAS) median.~The Visual Analouge (VAS) 100mm Scale Score for Chemotherapy Induced Nausea and Vomiting (CINV). Participants were asked to mark a linear scale 100mm in length representing their level of nausea with 0mm indicating no nausea and 100mm indicating severe nausea. Median VAS scores (in mm) are reported, per day." (NCT01736917)
Timeframe: Days 1-8 of chemotherapy regimen

Interventionmillimeters (Median)
median VAS score - day 1median VAS score - day 2median VAS score - day 3median VAS score - day 4median VAS score - day 5median VAS score - day 6median VAS score - day 7median VAS score - day 8
Fosaprepitant + 5HT3 Receptor Antagonists + Dexamethasone004.518.523.512.573

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Percentage of Participants With Complete Response of Acute and Delayed Chemotherapy Induced Nausea and Vomiting

complete response (CR) of both acute (days 1 through 5) and delayed (days 6 through 8) CINV, defined by no emetic episodes or use of rescue medications (NCT01736917)
Timeframe: Days 1-8 of chemotherapy regimen

Interventionpercentage of participants (Number)
acute phase(days 1 through 5)delayed phase (days 6 through 8)overall
Fosaprepitant + 5HT3 Receptor Antagonists + Dexamethasone29.646.324.1

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Use of Rescue Medications.

Total number of patients who received rescue medications. (NCT01736917)
Timeframe: Days 1-8 of chemotherapy regimen

Interventionparticipants (Number)
Fosaprepitant + 5HT3 Receptor Antagonists + Dexamethasone37

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Total Number of Emetic Episodes

total number of emetic episodes (NCT01736917)
Timeframe: Days 1-8 of chemotherapy regimen

Interventionepisodes (Number)
Fosaprepitant + 5HT3 Receptor Antagonists + Dexamethasone29

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Intensity of Breathlessness

Intensity of Breathlessness was recorded on a visual analog scale. The scale range is 0-10 where 0 = minimum and 10 = maximal intensity. At each visit, participants were asked to report unpleasantness at 1 minute intervals. The measures were collected up to 20 minutes per visit and combined for a final score. Total minimum score = 0, total maximum score 200. Data is collected during Resistive Load Breathing at Period 1 (Day 3 or 4) and Period 2 (Day 5, 6 or 7) during which either Placebo or Aprepitant was administered. (NCT01854177)
Timeframe: Visit 2 (Approximately Day 3 where either Placebo or Aprepitant was administered).and Visit 3 (approximately Day 6 where either Placebo or Aprepitant was administered)

Interventionunits on a scale (Mean)
Aprepitant83.0
Placebo85.1

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Unpleasantness of Breathlessness

Unpleasantness of breathlessness was reported each minute by the patient on a visual analog scale. The scale range is 0-10 where 0 = No breathlessness and 10 = Severe breathlessness. The measures were collected up to 20 minutes per visit and combined for a final score. Total minimum score = 0, total maximum score 200. Data is collected during Resistive Load Breathing at Period 1 (Day 3 or 4) and Period 2 (Day 5, 6 or 7) during which either Placebo or Aprepitant was administered. A high unpleasantness indicates that breathing difficulty feels very bad or terrifying regardless of whether the intensity is high or low (NCT01854177)
Timeframe: Visit 2 (Approximately Day 3 where either Placebo or Aprepitant was administered).and Visit 3 (approximately Day 6 where either Placebo or Aprepitant was administered)

Interventionunits on a scale (Mean)
Aprepitant69.0
Placebo71.1

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Number of Participants With CR in the Overall Phase.

CR defined as no emesis and no use of rescue medication, in the overall phase (0 to 120 hours after the initiation of chemotherapy) (NCT01857232)
Timeframe: 0 to 120 hours after the initiation of chemotherapy

InterventionParticipants (Count of Participants)
Control33
Placebo11
APD403 10MG21
APD403 20MG17
ADP403 40MG17

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Number of Participants With Delayed Phase Complete Response(CR)

"Delayed phase complete response (CR), defined as an absence of emetic episodes and no rescue medication use in the period from 24 to 120 hours after the initiation of chemotherapy.~The primary endpoint was analysed separately in the strata of chemotherapy regimen and gender, and in the strata of country." (NCT01857232)
Timeframe: 24-120 hours

InterventionParticipants (Count of Participants)
Control37
PLACEBO13
APD403 10MG27
ADP421 20MG21
APD421 40MG20

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Number of Patients With Complete Response During Inpatient Admission

No vomiting from the initiation of through 48 hours following the final dose of HD IL-2 (NCT01874119)
Timeframe: From the initiation of through 48 hours following the final dose of Interleukin-2

InterventionParticipants (Count of Participants)
Fosaprepitant1
Placebo0

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Clinical Score Assessment of Infiltration

"The (sub)investigator will assess the clinical picture at each treated area at baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42 using the following score:~Criteria:~Infiltration~Evaluation:~0 = not existing~= mild~= moderate~= severe~The score will be an integer on the scale 0-3." (NCT01963793)
Timeframe: At baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42

,
Interventionunits on a scale (Mean)
Day 1 (Visit 2)Day 14 (Visit 3)Day 28 (Visit 4)Day 42 (Visit 5)
Aprepitant 10 mg/g Gel1.51.31.11.3
Aprepitant Gel Vehicle1.51.41.31.5

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Lesional Erythema by Mexameter

"The skin colour of the participants was evaluated by use of a Mexameter spectrophotometer. The instrument computed an erythema index (with a range between 0 and 999, where higher values indicate more erythema or redness) which may be used as an indication of skin properties.~Mexameter measurements were performed at baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42 to assess stimulation of microcirculation, irritating effects, and occurring erythema." (NCT01963793)
Timeframe: At baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42

,
Interventionunits on a scale (Mean)
Day 1 (Visit 2)Day 14 (Visit 3)Day 28 (Visit 4)Day 42 (Visit 5)
Aprepitant 10 mg/g Gel438527464457
Aprepitant Gel Vehicle453463491461

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Daily Assessments of Duration of Pruritus (Preceding 12 Hours)

"During the trial participants completed a diary twice daily, in the morning and in the evening, each covering the preceding 12 hours, which collected the number of hours with pruritus within the last 12 hours on both areas by use of a 7-point scale (<0.5 hours, 0.5-1 hours, 1-2 hours, 3-4 hours, 5-6 hours, 7-8 hours, 9-12 hours).~Duration of pruritus was categorized as follows: 1 if <0.5 hours, 2 if 0.5-1 hours, 3 if 1-2 hours, 4 if 3-4 hours, 5 if 5-6 hours, 6 if 7-8 hours and 7 if 9-12 hours.~The evening baseline measure was taken on the evening of Day -1 and the morning baseline measure was taken on the morning of Day 1 before cream was applied." (NCT01963793)
Timeframe: From baseline to Day 31

,,,
Interventionunits on a scale (Mean)
Day -1Day 1Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9Day 10Day 11Day 12Day 13Day 14Day 15Day 16Day 17Day 18Day 19Day 20Day 21Day 22Day 23Day 24Day 25Day 26Day 27Day 28Day 29Day 30Day 31
Evening: Aprepitant 10 mg/g Gel3.73.53.02.92.72.12.52.62.42.42.42.22.12.42.12.42.22.22.12.12.02.01.92.31.92.32.22.01.81.01.0NA
Evening: Aprepitant Gel Vehicle4.03.73.33.33.12.72.92.92.72.82.62.82.52.72.42.52.42.52.32.42.32.22.32.42.12.52.22.12.32.02.0NA
Morning: Aprepitant 10 mg/g GelNA3.03.22.92.82.22.32.52.32.42.42.02.22.22.12.12.12.12.21.92.01.92.02.02.01.92.42.12.01.51.01.0
Morning: Aprepitant Gel VehicleNA3.43.33.13.12.82.62.72.62.82.52.42.72.52.42.52.62.62.62.32.22.12.22.32.12.12.32.22.11.71.52.0

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Pruritus by VAS (Visual Analogue Scale)

"At baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42, participants assessed the intensity of present pruritus of each treated area on a visual analogue scale (VAS) with a score of 0 (no itch at all) to 10 (worst imaginable itch) at the two extremes on a 100 mm line." (NCT01963793)
Timeframe: At baseline (Day 1), Day 14, end of treatment (Day 28), and Day 42

,
Interventionmm (Mean)
Day 1 (Visit 2)Day 14 (Visit 3)Day 28 (Visit 4)Day 42 (Visit 5)
Aprepitant 10 mg/g Gel50.827.119.023.9
Aprepitant Gel Vehicle58.128.721.924.0

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Non-lesional Melanin by Mexameter

"The skin colour of the participants was evaluated by use of a Mexameter spectrophotometer. The instrument computed a melanin index (with a range between 0 and 999, where higher values indicate more melanin) which may be used as an indication of skin properties.~Mexameter measurements were performed at baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42 to assess stimulation of microcirculation, irritating effects, and occurring erythema." (NCT01963793)
Timeframe: At baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42

,
Interventionunits on a scale (Mean)
Day 1 (Visit 2)Day 14 (Visit 3)Day 28 (Visit 4)Day 42 (Visit 5)
Aprepitant 10 mg/g Gel127165149129
Aprepitant Gel Vehicle129215166179

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Daily Assessments of Maximum Intensity of Pruritus by Use of a VAS

"During the trial participants completed a diary twice daily, in the morning and in the evening, each covering the preceding 12 hours, which collected the maximum intensity of pruritus since last evaluation by use of a VAS (ranging from 0 to 100). The participants assessed the intensity of present pruritus of each treated area on a visual analogue scale (VAS) with a score of 0 (no itch at all) to 10 (worst imaginable itch) at the two extremes on a 100 mm line.~The evening baseline measure was taken on the evening of Day -1 and the morning baseline measure was taken on the morning of Day 1 before cream was applied." (NCT01963793)
Timeframe: From baseline to Day 31

,,,
Interventionmm (Mean)
Day -1Day 1Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9Day 10Day 11Day 12Day 13Day 14Day 15Day 16Day 17Day 18Day 19Day 20Day 21Day 22Day 23Day 24Day 25Day 26Day 27Day 28Day 29Day 30Day 31
Evening: Aprepitant 10 mg/g Gel61.149.943.241.637.733.434.135.231.432.029.430.727.131.027.129.428.228.225.624.125.121.320.822.221.122.723.220.912.63.52.0NA
Evening: Aprepitant Gel Vehicle62.754.746.742.742.839.738.439.237.435.034.537.331.834.231.232.132.829.327.727.427.123.021.524.222.023.824.023.118.97.54.0NA
Morning: Aprepitant 10 mg/g GelNA56.048.839.539.532.334.335.332.232.840.028.731.629.130.726.329.125.529.227.723.222.620.123.220.821.824.119.624.75.74.53.0
Morning: Aprepitant Gel VehicleNA62.446.743.647.741.739.138.940.735.941.136.838.631.331.930.732.929.830.433.123.525.722.721.121.120.823.121.324.75.95.54.0

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Clinical Score Assessment of Crusting

"The (sub)investigator assessed the clinical picture at each treated area at baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42 using the following score:~Criteria:~Crusts~Evaluation:~0 = not existing~= mild~= moderate~= severe~The score will be an integer on the scale 0-3." (NCT01963793)
Timeframe: At baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42

,
Interventionunits on a scale (Mean)
Day 1 (Visit 2)Day 14 (Visit 3)Day 28 (Visit 4)Day 42 (Visit 5)
Aprepitant 10 mg/g Gel1.30.90.70.8
Aprepitant Gel Vehicle1.41.11.00.9

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Melanin by Mexameter

"The skin colour of the participants was evaluated by use of a Mexameter spectrophotometer. The instrument computed a melanin index (with a range between 0 and 999, where higher values indicate more melanin) which may be used as an indication of skin properties.~Mexameter measurements were performed at baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42 to assess stimulation of microcirculation, irritating effects, and occurring erythema." (NCT01963793)
Timeframe: At baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42

,
Interventionunits on a scale (Mean)
Day 1 (Visit 2)Day 14 (Visit 3)Day 28 (Visit 4)Day 42 (Visit 5)
Aprepitant 10 mg/g Gel131121152132
Aprepitant Gel Vehicle115134139144

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Non-lesional Erythema by Mexameter

"The skin colour of the participants was evaluated by use of a Mexameter spectrophotometer. The instrument computed an erythema index (with a range between 0 and 999, where higher values indicate more erythema or redness) which may be used as an indication of skin properties.~Mexameter measurements were performed at baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42 to assess stimulation of microcirculation, irritating effects, and occurring erythema." (NCT01963793)
Timeframe: At baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42

,
Interventionunits on a scale (Mean)
Day 1 (Visit 2)Day 14 (Visit 3)Day 28 (Visit 4)Day 42 (Visit 5)
Lateral Side of Aprepitant 10 mg/g Gel304287262284
Lateral Side of Aprepitant Gel Vehicle300312271284

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Percent Change From Baseline in Pruritis Assessed by VAS at End of Treatment

"On the last day of treatment, participants assessed the change of pruritus compared to baseline in percentage by use of a VAS (ranging from 0 to 100). The participants assessed the intensity of present pruritus of each treated area on a visual analogue scale (VAS) with a score of 0 (no itch at all) to 10 (worst imaginable itch) at the two extremes on a 100 mm line." (NCT01963793)
Timeframe: Day 28

Interventionpercent change (Mean)
Aprepitant 10 mg/g Gel50.8
Aprepitant Gel Vehicle41.7

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Pruritus by VAS (Visual Analogue Scale)

"At end of treatment (Day 28) participants assessed the intensity of present pruritus of each treated area on a visual analogue scale (VAS) with a score of 0 (no itch at all) to 10 (worst imaginable itch) at the two extremes on a 100 mm line." (NCT01963793)
Timeframe: At end of treatment (Day 28)

Interventionmm (Least Squares Mean)
Aprepitant 10 mg/g Gel19.7
Aprepitant Gel Vehicle21.2

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Change From Baseline in Participants' Global Assessment on Treatment Areas

At baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42, participants assessed their prurigo on each treated area using the following score: 0 = no symptoms, 1 = mild, 2 = moderate, 3 = severe. The change was calculated as the value at the later time point minus the value at baseline. The change at Day 1 was therefore 0 and negative values represent a decrease in score. (NCT01963793)
Timeframe: At baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42

,
Interventionunits on a scale (Mean)
Day 1 (Visit 2)Day 14 (Visit 3)Day 28 (Visit 4)Day 42 (Visit 5)
Aprepitant 10 mg/g Gel0.0-0.5-0.6-0.3
Aprepitant Gel Vehicle0.0-0.7-0.7-0.4

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Transepidermal Water Loss (TEWL)

"The (sub)investigator will made the following clinical assessment:~Transepidermal water loss was defined as amount of released water from skin surface in g/cm^2 per hour. The TEWL is increased in case of damage of skin barrier." (NCT01963793)
Timeframe: At baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42

,
Interventiong/cm² per hour (Mean)
Day 1 (Visit 2)Day 14 (Visit 3)Day 28 (Visit 4)Day 42 (Visit 5)
Aprepitant 10 mg/g Gel20.622.720.019.4
Aprepitant Gel Vehicle25.224.019.919.9

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Clinical Score Assessment of Erythema

"The (sub)investigator will assess the clinical picture at each treated area at baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42 using the following score:~Criteria:~Erythema~Evaluation:~0 = not existing~= mild~= moderate~= severe~The score will be an integer on the scale 0-3." (NCT01963793)
Timeframe: At baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42

,
Interventionunits on a scale (Mean)
Day 1 (Visit 2)Day 14 (Visit 3)Day 28 (Visit 4)Day 42 (Visit 5)
Aprepitant 10 mg/g Gel2.01.81.51.5
Aprepitant Gel Vehicle2.11.81.71.6

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Clinical Score Assessment of Scratch Artefacts

"The (sub)investigator will assess the clinical picture at each treated area at baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42 using the following score:~Criteria:~Scratch artefacts: Superficial damage to the skin caused by severe scratching.~Evaluation:~0 = not existing~= mild~= moderate~= severe~The score will be an integer on the scale 0-3." (NCT01963793)
Timeframe: At baseline (Day 1), Day 14, end of treatment (Day 28) and Day 42

,
Interventionunits on a scale (Mean)
Day 1 (Visit 2)Day 14 (Visit 3)Day 28 (Visit 4)Day 42 (Visit 5)
Aprepitant 10 mg/g Gel1.71.31.11.4
Aprepitant Gel Vehicle1.81.31.41.4

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Daily Assessments of Average Pruritus by Use of a VAS

"During the trial participants completed a diary twice daily, in the morning and in the evening, each covering the preceding 12 hours, which collected the average intensity of pruritus since last evaluation by use of a VAS (ranging from 0 to 100). The participants assessed the intensity of present pruritus of each treated area on a visual analogue scale (VAS) with a score of 0 (no itch at all) to 10 (worst imaginable itch) at the two extremes on a 100 mm line.~The evening baseline measure was taken on the evening of Day -1 and the morning baseline measure was taken on the morning of Day 1, before cream was applied." (NCT01963793)
Timeframe: From baseline to Day 31

,,,
Interventionmm (Mean)
Day -1Day 1Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9Day 10Day 11Day 12Day 13Day 14Day 15Day 16Day 17Day 18Day 19Day 20Day 21Day 22Day 23Day 24Day 25Day 26Day 27Day 28Day 29Day 30Day 31
Evening: Aprepitant 10 mg/g Gel49.145.035.133.731.827.426.430.423.324.522.023.319.921.820.924.220.820.218.515.616.014.514.315.615.718.215.114.27.83.03.0NA
Evening: Aprepitant Gel Vehicle51.344.738.935.837.531.031.533.228.827.628.228.423.726.423.125.224.321.721.119.919.717.015.917.216.716.816.614.111.65.53.0NA
Morning: Aprepitant 10 mg/g GelNA46.938.333.634.524.226.828.326.526.830.622.323.020.221.919.322.718.821.620.717.816.115.315.816.515.819.813.616.44.73.52.0
Morning: Aprepitant Gel VehicleNA49.339.233.737.233.730.331.930.127.430.229.327.823.424.722.125.422.822.822.418.617.116.614.615.516.516.314.614.94.93.52.0

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Number of Participants With Adverse Events.

Olanzapine will be considered tolerable if less than 10% of patients experience a grade III or IV adverse event attributable to olanzapine. (NCT02097823)
Timeframe: Ongoing, throughout the study. Will be fully evaluated in approximately 1 year, at the conclusion of data collection. Each patient will be followed during 2 cycles of chemotherapy, an expected average of 6 weeks.

Interventionparticipants (Number)
Aprepitant0
Olanzapine0

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Feasibility of Recruitment and Data Collection.

Primary objective of this study is to determine the feasibility of recruitment and data collection for conducting a larger trial. Recruitment and data collection will be feasible if at least 20 subjects can be recruited in 1 year and there is a 90% form completion rate. (NCT02097823)
Timeframe: Approximately 1 year after study opens, at the conclusion of data collection. Participants will be followed during 2 cycles of chemotherapy, an expected average of 6 weeks. Data will be collected over 5 days during each cycle.

Interventionpercentage of completed forms (Number)
All Participants70.4

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Complete Response in Overall Phase

This will measure what percentage of patients have a complete response (no emesis or use of breakthrough medications) in the overall phase (0-120 hours). (NCT02097823)
Timeframe: Participants will be followed during 2 cycles of chemotherapy, an expected average of 6 weeks. Data will be collected over 5 days during each cycle.

Interventionpercentage of participants with CR (Number)
Aprepitant23.1
Olanzapine28.6

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Complete Response in Delayed Phase

This will measure what percentage of patients have a complete response (no emesis or use of breakthrough medications) in the delayed phase (25-120 hours). (NCT02097823)
Timeframe: Participants will be followed during 2 cycles of chemotherapy, an expected average of 6 weeks. Data will be collected over 5 days during each cycle.

Interventionpercentage of participants with CR (Number)
Aprepitant23.1
Olanzapine28.6

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Good Control of Nausea

"Good control of nausea will be ratings <25 on visual analog scale by parents and <2 on baxter retching faces scale by patients. Will look at the proportions of patients with good control of nausea.~The visual analog scale ranged from 0-100, with 0 being no nausea and 100 being very very severe nausea. The Baxter retching faces scale ranged from 0-10 using only even numbers (0,2,4,6,8,10) and each number has a corresponding face depicting someone experiencing varying levels of nausea, with 0 being no nausea and 10 being a picture of face vomiting." (NCT02097823)
Timeframe: Participants will be followed during 2 cycles of chemotherapy, an expected average of 6 weeks. Data will be collected over 5 days during each cycle.

,
Interventionpercentage of participant w/good control (Number)
Visual Analog Scale/ParentsBARF scale/Patients
Aprepitant54.554.5
Olanzapine5050

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Complete Response in Acute Phase

This will measure what percentage of patients have a complete response (no emesis or use of breakthrough medications) in the acute phase (0-24 hours). (NCT02097823)
Timeframe: Participants will be followed during 2 cycles of chemotherapy, an expected average of 6 weeks. Data will be collected over 5 days during each cycle.

Interventionpercentage of participants with CR (Number)
Aprepitant76.9
Olanzapine78.6

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Delayed Complete Control (CC) Rate

To determine the effect of APF530 on complete control rates defined as no more than mild nausea, no emetic episodes [vomiting or retching], and no use of rescue medications in the delayed phase (24 to 120 hours) of CINV. (NCT02106494)
Timeframe: 24 - 120 Hours

Interventionpercentage of participants (Number)
APF530 + Fosaprepitant + Dexamethasone60.7
Ondansetron + Fosaprepitant + Dexamethasone53.1

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Delayed Phase Complete Response (CR) Rate

Percentage of Participants with no emesis and no rescue medication in patients receiving HEC in the delayed phase (24 to 120 hours) of CINV. (NCT02106494)
Timeframe: 24 - 120 Hours

Interventionpercentage of participants (Number)
APF530 + Fosaprepitant + Dexamethasone64.7
Ondansetron + Fosaprepitant + Dexamethasone56.6

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Overall Complete Control Rate

To determine the effect of APF530 on complete control rates defined as no more than mild nausea, no emetic episodes [vomiting or retching], and no use of rescue medications in the overall phase (0 to 120 hours) of CINV. (NCT02106494)
Timeframe: 0 - 120 Hours

Interventionpercentage of participants (Number)
APF530 + Fosaprepitant + Dexamethasone54.7
Ondansetron + Fosaprepitant + Dexamethasone49.6

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Rate of No Emetic Episodes

To determine the effect of APF530 on the rate of no emetic episodes (vomiting or retching) in the overall phase (0 to 120 hours) of CINV. (NCT02106494)
Timeframe: 0 - 120 Hours

Interventionpercentage of participants (Number)
APF530 + Fosaprepitant + Dexamethasone82.2
Ondansetron + Fosaprepitant + Dexamethasone79.2

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Overall Complete Response Rate

To determine the effect of APF530 on complete response rates in the overall phase (0 to 120 hours) of CINV. (NCT02106494)
Timeframe: 0 - 120 Hours

Interventionpercentage of participants (Number)
APF530 + Fosaprepitant + Dexamethasone58.4
Ondansetron + Fosaprepitant + Dexamethasone52.9

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Frequency of Rescue Medication

Patients were asked to record daily number of extra nausea/vomiting pills taken because they developed nausea/vomiting in the following categories: None, One, Two, More than two in Nausea and Vomiting Daily Diary Questionnaire. (NCT02116530)
Timeframe: Day 2 to Day 6 after chemotherapy

InterventionParticipants (Count of Participants)
Day 272213840Day 272213839Day 372213839Day 372213840Day 472213839Day 472213840Day 572213840Day 572213839Day 672213839Day 672213840
More than twiceTwiceNoneOnce
Olanzapine156
Placebo117
Olanzapine21
Placebo35
Placebo19
Olanzapine2
Olanzapine158
Placebo124
Olanzapine11
Placebo24
Olanzapine7
Placebo20
Olanzapine4
Placebo10
Olanzapine141
Olanzapine16
Olanzapine10
Placebo17
Olanzapine3
Placebo11
Olanzapine145
Placebo131
Olanzapine19
Placebo23
Olanzapine5
Placebo7
Olanzapine143
Placebo130
Olanzapine12
Placebo16
Placebo14

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Proportion of Patients With Complete Response

Complete response was defined as no emetic episodes and no use of rescue medication during the acute (0-24 hours), delayed (25-120 hours) and overall (0-120 hours) periods as measured by the Nausea and Vomiting Daily Diary/Questionnaire. (NCT02116530)
Timeframe: 0 to 120 hours after chemotherapy

,
Interventionpercentage of participants (Number)
0-24 hours after chemotherapy25-120 hours after chemotherapy0-120 hours after chemotherapy
Olanzapine85.766.963.6
Placebo64.652.440.6

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Proportion of Patients With no Nausea

No nausea was defined as a response of 0 in the nausea item of Nausea and Vomiting Daily Diary/Questionnaire in the acute (0-24 hours), delayed (25-120 hours) and overall (0-120 hours) periods after chemotherapy. (NCT02116530)
Timeframe: 0 to 120 hours after chemotherapy

,
Interventionpercentage of participants (Number)
0-24 hours after chemotherapy25-120 hours after chemotherapy0-120 hours after chemotherapy
Olanzapine73.842.437.3
Placebo45.325.421.9

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Median Nausea Scores

Nausea scores was measured using a visual-analogue scale ranging from 0 (none) to 10 (as bad as it can be). (NCT02116530)
Timeframe: Baseline and Day 2 to Day 6 after chemotherapy

,
Interventionunits on a scale (Median)
BaselineDay 2Day 3Day 4Day 5Day 6
Olanzapine000000
Placebo011111

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Norepinephrine (NE) Concentrations

The primary analyses will focus on blood pressure, heart rate, and norepinephrine (NE) concentrations during ramipril versus ramipril+sitagliptin, and during ramipril+sitagliptin versus ramipril+sitagliptin+aprepitant. We will make similar comparisons within the valsartan- and placebo-treated groups. In addition, we will compare blood pressure and heart rate parameters among the ramipril-treated, valsartan-treated, and placebo-treated groups during comparable concurrent treatment. (NCT02130687)
Timeframe: 4.5 hours on the 7th day of each intervention (placebo, sitagliptin, or sitagliptin+aprepitant)

Interventionpg/mL (Mean)
Amlodipine Plus Placebo/Placebo741.65
Amlodipine Plus Sitagliptin/Placebo730.88
Amlodipine Plus Sitagliptin/Aprepitant610.65
Ramipril Plus Placebo/Placebo470.69
Ramipril Plus Sitagliptin/Placebo627.55
Ramipril Plus Sitagliptin/Aprepitant649.39
Valsartan Plus Placebo/Placebo874.22
Valsartan Plus Sitagliptin/Placebo986.31
Valsartan Plus Sitagliptin/Aprepitant1013.54

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Neuropeptide Y

Measurement of Neuropeptide Y (NPY) concentrations (NCT02130687)
Timeframe: Neuropeptide Y concentration prior to ingestion of the mixed meal.

InterventionpM (Mean)
Amlodipine Plus Placebo/Placebo0.35
Amlodipine Plus Sitagliptin/Placebo0.52
Amlodipine Plus Sitagliptin/Aprepitant0.51
Ramipril Plus Placebo/Placebo0.32
Ramipril Plus Sitagliptin/Placebo0.54
Ramipril Plus Sitagliptin/Aprepitant0.52
Valsartan Plus Placebo/Placebo0.27
Valsartan Plus Sitagliptin/Placebo0.50
Valsartan Plus Sitagliptin/Aprepitant0.47

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Mean Arterial Blood Pressure

The primary analyses will focus on mean arterial blood pressure, heart rate, and norepinephrine (NE) concentrations during ramipril versus ramipril+sitagliptin, and during ramipril+sitagliptin versus ramipril+sitagliptin+aprepitant. We will make similar comparisons within the valsartan- and placebo-treated groups. In addition, we will compare blood pressure and heart rate parameters among the ramipril-treated, valsartan-treated, and placebo-treated groups during comparable concurrent treatment. (NCT02130687)
Timeframe: 4.5 hours on the 7th day of each intervention (placebo, sitagliptin, or sitagliptin+aprepitant)

InterventionmmHg (Mean)
Amlodipine Plus Placebo/Placebo94.42
Amlodipine Plus Sitagliptin/Placebo93.41
Amlodipine Plus Sitagliptin/Aprepitant91.54
Ramipril Plus Placebo/Placebo90.21
Ramipril Plus Sitagliptin/Placebo89.88
Ramipril Plus Sitagliptin/Aprepitant86.95
Valsartan Plus Placebo/Placebo94.54
Valsartan Plus Sitagliptin/Placebo93.71
Valsartan Plus Sitagliptin/Aprepitant93.98

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Dipeptidyl Peptidase IV (DPP4) Activity

Measure of DPP4 inhibitor administration. (NCT02130687)
Timeframe: for 4.5 hours on the 7th day of each intervention (placebo, sitagliptin, sitagliptin+aprepitant)

Interventionnmol/mL/min (Mean)
Amlodipine Plus Placebo/Placebo20.27
Amlodipine Plus Sitagliptin/Placebo7.34
Amlodipine Plus Sitagliptin/Aprepitant6.96
Ramipril Plus Placebo/Placebo20.61
Ramipril Plus Sitagliptin/Placebo8.78
Ramipril Plus Sitagliptin/Aprepitant7.71
Valsartan Plus Placebo/Placebo19.4
Valsartan Plus Sitagliptin/Placebo7.83
Valsartan Plus Sitagliptin/Aprepitant6.70

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Glucose

measure of effectiveness of DPP4 inhibitor (NCT02130687)
Timeframe: fasting at 3 hours on the 7th day of each intervention (placebo, sitagliptin, sitagliptin+aprepitant)

Interventionmg/dL (Mean)
Amlodipine Plus Placebo/Placebo123.78
Amlodipine Plus Sitagliptin/Placebo112.51
Amlodipine Plus Sitagliptin/Aprepitant109.08
Ramipril Plus Placebo/Placebo118.04
Ramipril Plus Sitagliptin/Placebo107.55
Ramipril Plus Sitagliptin/Aprepitant107.66
Valsartan Plus Placebo/Placebo112.01
Valsartan Plus Sitagliptin/Placebo103.69
Valsartan Plus Sitagliptin/Aprepitant99.75

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Heart Rate

The average of measurements made every five minutes prior to (time 0) and for four four hours after ingestion of a mixed meal (NCT02130687)
Timeframe: Value provided is the average of measurements made every five minutes prior to (time 0) and for four four hours after ingestion of a mixed meal.

Interventionbpm (Mean)
Amlodipine Plus Placebo/Placebo71.8
Amlodipine Plus Sitagliptin/Placebo70.3
Amlodipine Plus Sitagliptin/Aprepitant71.7
Ramipril Plus Placebo/Placebo69.9
Ramipril Plus Sitagliptin/Placebo73.3
Ramipril Plus Sitagliptin/Aprepitant72.0
Valsartan Plus Placebo/Placebo70.3
Valsartan Plus Sitagliptin/Placebo71.9
Valsartan Plus Sitagliptin/Aprepitant71.9

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Heart Rate

The primary analyses will focus on blood pressure, heart rate, and norepinephrine (NE) concentrations during ramipril versus ramipril+sitagliptin, and during ramipril+sitagliptin versus ramipril+sitagliptin+aprepitant. We will make similar comparisons within the valsartan- and placebo-treated groups. In addition, we will compare blood pressure and heart rate parameters among the ramipril-treated, valsartan-treated, and placebo-treated groups during comparable concurrent treatment. (NCT02130687)
Timeframe: 4.5 hours on the 7th day of each intervention (placebo, sitagliptin, or sitagliptin+aprepitant)

Interventionbeats per minute (Mean)
Amlodipine Plus Placebo/Placebo69.59
Amlodipine Plus Sitagliptin/Placebo70.43
Amlodipine Plus Sitagliptin/Aprepitant69.41
Ramipril Plus Placebo/Placebo66.58
Ramipril Plus Sitagliptin/Placebo66.30
Ramipril Plus Sitagliptin/Aprepitant66.15
Valsartan Plus Placebo/Placebo66.19
Valsartan Plus Sitagliptin/Placebo65.86
Valsartan Plus Sitagliptin/Aprepitant65.10

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Low Frequency Variability of Blood Pressure Activity

Low frequency variability of systolic blood pressure will be measured using spectral analysis. (NCT02130687)
Timeframe: for 5 minutes on the 7th day of each intervention (placebo, sitagliptin, sitagliptin+aprepitant)

InterventionmmHg2 (Mean)
Amlodipine Plus Placebo/Placebo5.14
Amlodipine Plus Sitagliptin/Placebo7.32
Amlodipine Plus Sitagliptin/Aprepitant7.07
Ramipril Plus Placebo/Placebo8.78
Ramipril Plus Sitagliptin/Placebo7.27
Ramipril Plus Sitagliptin/Aprepitant12.18
Valsartan Plus Placebo/Placebo8.51
Valsartan Plus Sitagliptin/Placebo7.81
Valsartan Plus Sitagliptin/Aprepitant8.58

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24hr Urinary Testing for Sodium

Subjects will collect 24hr urine sample and bring with to the study day for analysis (NCT02130687)
Timeframe: Urine was collected for sodium for 24 hrs prior to each of the study days listed below. Study days occurred after each 7-day treatment arm (placebo/placebo, sitagliptin/placebo, or sitagliptin/aprepitant) within 3 anti-hypertensive groups.

InterventionmEq (Mean)
Amlodipine Plus Placebo/Placebo147.66
Amlodipine Plus Sitagliptin/Placebo146.90
Amlodipine Plus Sitagliptin/Aprepitant154.42
Ramipril Plus Placebo/Placebo177.70
Ramipril Plus Sitagliptin/Placebo162.05
Ramipril Plus Sitagliptin/Aprepitant142.95
Valsartan Plus Placebo/Placebo158.77
Valsartan Plus Sitagliptin/Placebo138.65
Valsartan Plus Sitagliptin/Aprepitant160.92

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Mean Arterial Blood Pressure

Average of measurements made every five minutes beginning just prior to (time 0) and for four hours after the ingestion of a mixed meal (NCT02130687)
Timeframe: Value provided is the AVERAGE of measurements made every five minutes prior to (time 0) and for four four hours after ingestion of a mixed meal.

InterventionmmHg (Mean)
Amlodipine Plus Placebo/Placebo96.0
Amlodipine Plus Sitagliptin/Placebo93.6
Amlodipine Plus Sitagliptin/Aprepitant92.9
Ramipril Plus Placebo/Placebo94.2
Ramipril Plus Sitagliptin/Placebo92.6
Ramipril Plus Sitagliptin/Aprepitant91.0
Valsartan Plus Placebo/Placebo94.2
Valsartan Plus Sitagliptin/Placebo96.1
Valsartan Plus Sitagliptin/Aprepitant94.5

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Insulin

Measure of insulin resistance. (NCT02130687)
Timeframe: fasting insulin measured at 3 hours on the 7th day of each intervention (placebo, sitagliptin, sitatliptin+aprepitant)

InterventionmicroU/mL (Mean)
Amlodipine Plus Placebo/Placebo20.7
Amlodipine Plus Sitagliptin/Placebo20.72
Amlodipine Plus Sitagliptin/Aprepitant20.22
Ramipril Plus Placebo/Placebo26.15
Ramipril Plus Sitagliptin/Placebo22.59
Ramipril Plus Sitagliptin/Aprepitant26.02
Valsartan Plus Placebo/Placebo21.39
Valsartan Plus Sitagliptin/Placebo19.92
Valsartan Plus Sitagliptin/Aprepitant16.83

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Angiotensin Converting Enzyme (ACE) Activity

This is a measure of activity of the angiotensin-converting enzyme (ACE). The assay is a kinetic assay (Labcore) that measures the rate of cleavage of an added ACE substrate over time and the results are reported in Units, which represent the rate of increase in fluorescent metabolite over 30 minutes under standard conditions at 37C. (NCT02130687)
Timeframe: for 4.5 hours on the 7th day of each intervention (placebo, sitagliptin, sitagliptin+aprepitant)

InterventionUnits (Mean)
Amlodipine Plus Placebo/Placebo37.00
Amlodipine Plus Sitagliptin/Placebo40.15
Amlodipine Plus Sitagliptin/Aprepitant35.78
Ramipril Plus Placebo/Placebo15.44
Ramipril Plus Sitagliptin/Placebo14.69
Ramipril Plus Sitagliptin/Aprepitant13.46
Valsartan Plus Placebo/Placebo37.21
Valsartan Plus Sitagliptin/Placebo36.68
Valsartan Plus Sitagliptin/Aprepitant36.89

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Change From Week 0 in Drinking Quantity and Frequency Using Drinks Per Week at Week 8

Standard drinks are equivalent to 14 grams of pure alcohol and number of drinks are assessed with Timeline Follow-Back (TLFB) methods. Change = (Week 8 - Week 0). More negative values indicate less use of alcohol. (NCT02210195)
Timeframe: Week 0 and Week 8

Interventiondrinks/week (Mean)
Aprepitant: 125mg/Day-21.0
Matched Placebo-10.7

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Change From Week 0 in Cannabis Use Using Urinary CN-THCCOOH Levels at Week 8

Urinary THC/Cr ratio, also known as CN-THCCOOH (creatinine normalized tetrahydrocannabinol carboxylic acid), is a highly sensitive and specific quantitative analytic procedure to determine current marijuana metabolite levels in the urine as well as new marijuana use or abstinence. Gas chromatography mass spectrometric levels of 11-nor-9-carboxy-9-THC (THC-COOH), the primary marijuana metabolite, are normalized to the urine creatinine (CN) concentration to reduce the variability of drug measurement attributable to urine dilution. Negative values indicate decreased use. Change = (Week 8 value - Week 0 value). (NCT02210195)
Timeframe: Week 0 and Week 8

Interventionng/mg (Mean)
Aprepitant: 125mg/Day198.3
Matched Placebo55.9

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Proportion of Participants Receiving MEC With No Vomiting in the Overall Phase

"Overall Phase was defined as 0 to 120 hours following initiation of chemotherapy.~No vomiting was defined as no vomiting or retching or dry heaves (included participants who received rescue therapy)." (NCT02484911)
Timeframe: 0-120 hours

InterventionParticipants (Count of Participants)
Olanzapine Regimen30
Control Regimen30

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Proportion of Participants Receiving HEC With Complete Response in Overall Phase

"Overall phase was defined as 0 to 120 hours following initiation of chemotherapy.~Complete response was defined as no vomiting with no rescue therapy." (NCT02484911)
Timeframe: 0 to 120 hours

InterventionParticipants (Count of Participants)
Olanzapine Regimen20
Control Regimen15

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Proportion of Participants Receiving HEC With Complete Response in the Acute Phase

Acute phase was defined as 0 to 24 hours following initiation of chemotherapy. Complete response was defined as no vomiting with no rescue therapy. (NCT02484911)
Timeframe: 0 to 24 hours

InterventionParticipants (Count of Participants)
Olanzapine Regimen20
Control Regimen17

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Proportion of Participants Receiving HEC With Complete Response in the Delayed Phase

"Delayed phase was defined as 24 to 120 hours following initiation of chemotherapy.~Complete response was defined as no vomiting with no rescue therapy." (NCT02484911)
Timeframe: 24 to 120 hours

InterventionParticipants (Count of Participants)
Olanzapine Regimen20
Aprepitant Regimen15

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Proportion of Participants Receiving HEC With No Vomiting in the Acute Phase

"Overall Phase was defined as 0 to 120 hours following initiation of chemotherapy.~No vomiting was defined as no vomiting or retching or dry heaves (included participants who received rescue )" (NCT02484911)
Timeframe: 0 to 24 hours

InterventionParticipants (Count of Participants)
Olanzapine Regimen18
Control Regimen15

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Proportion of Participants Receiving HEC With No Vomiting in the Delayed Phase

"Overall Phase was defined as 24 to 120 hours following initiation of chemotherapy.~No vomiting was defined as no vomiting or retching or dry heaves (included participants who received rescue therapy)." (NCT02484911)
Timeframe: 24 to 120 hours

InterventionParticipants (Count of Participants)
Olanzapine Regimen17
Control Regimen7

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Proportion of Participants Receiving HEC With No Vomiting in the Overall Phase

"Overall phase was defined as 0 to 120 hours following initiation of chemotherapy.~No vomiting was defined as no vomiting or retching or dry heaves (included participants who received rescue therapy)." (NCT02484911)
Timeframe: 0 to 120 hours

InterventionParticipants (Count of Participants)
Olanzapine Regimen17
Control Regimen6

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Proportion of Participants Receiving MEC With Complete Response in Overall Phase

"Overall phase was defined as 0 to 120 hours following initiation of chemotherapy.~Complete response was defined as no vomiting with no rescue therapy." (NCT02484911)
Timeframe: 0 to 120 hours

InterventionParticipants (Count of Participants)
Olanzapine Regimen36
Control Regimen40

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Proportion of Participants Receiving MEC With Complete Response in the Acute Phase

Acute phase was defined as 0 to 24 hours following initiation of chemotherapy. Complete response was defined as no vomiting with no rescue therapy. (NCT02484911)
Timeframe: 0 to 24 hours

InterventionParticipants (Count of Participants)
Olanzapine Regimen36
Control Regimen41

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Proportion of Participants Receiving MEC With Complete Response in the Delayed Phase

"Delayed phase was defined as 24 to 120 hours following initiation of chemotherapy.~Complete response was defined as no vomiting with no rescue therapy." (NCT02484911)
Timeframe: 24 to 120 hours

InterventionParticipants (Count of Participants)
Olanzapine Regimen36
Control Regimen40

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Proportion of Participants Receiving MEC With No Vomiting in the Acute Phase

"Overall Phase was defined as 0 to 24 hours following initiation of chemotherapy.~No vomiting was defined as no vomiting or retching or dry heaves (included participants who received rescue therapy)." (NCT02484911)
Timeframe: 0 to 24 hours

InterventionParticipants (Count of Participants)
Olanzapine Regimen35
Control Regimen40

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Proportion of Participants Receiving MEC With No Vomiting in the Delayed Phase

"Overall Phase was defined as 24 to 120 hours following initiation of chemotherapy.~No vomiting was defined as no vomiting or retching or dry heaves (included participants who received rescue therapy)." (NCT02484911)
Timeframe: 24 to 120 hours

InterventionParticipants (Count of Participants)
Olanzapine Regimen30
Control Regimen31

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Percentage of Participants Who Experienced a Complete Response During the Acute Phase (0 to 24 Hours Post Initiation of Chemotherapy) in Cycle 1

Complete Response was defined as no vomiting, no retching, and no use of rescue medication following the initiation of emetogenic chemotherapy in Cycle 1. A vomiting episode was specified as one or more episodes of emesis (expulsion of stomach contents through the mouth) or retching/dry heaves (an attempt to vomit that is not productive of stomach contents). Distinct vomiting episodes were separated by the absence of emesis and retching for at least one minute. The date and time of each vomiting episode was recorded by participants in diaries at the time of occurrence. The percentage of participants with no vomiting and no retching episodes in the acute phase, defined as the time period of 0 to 24 hours post initiation of chemotherapy in Cycle 1, was calculated. (NCT02519842)
Timeframe: 0 to 24 hours post initiation of chemotherapy (up to 1 day after the dose of study drug)

InterventionPercentage of Participants (Number)
Fosaprepitant Regimen Cycle 170.3
Control Regimen Cycle 158.8

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Percentage of Participants Who Discontinued Study Drug Due to an Adverse Event

An AE is defined as any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a study drug, whether or not it is considered related to the study drug. A statistical analysis was performed to compare the percentage of participants who discontinued in Cycle 1 due to an AE and received fosaprepitant regimen compared with the percentage of participants who received control regimen. (NCT02519842)
Timeframe: Up to 6 months (up to last dose of study drug)

InterventionPercentage of Participants (Number)
Fosaprepitant Regimen Cycle 15.4
Control Regimen Cycle 10.0
Fosaprepitant Regimen Cycles 2-60.0

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Percentage of Participants Who Experienced a Complete Response During the Delayed Phase (>24 to 120 Hours Post Initiation of Chemotherapy) in Cycle 1

Complete Response was defined as no vomiting, no retching, and no use of rescue medication following the initiation of emetogenic chemotherapy in Cycle 1. A vomiting episode was specified as one or more episodes of emesis (expulsion of stomach contents through the mouth) or retching/dry heaves (an attempt to vomit that is not productive of stomach contents). Distinct vomiting episodes were separated by the absence of emesis and retching for at least one minute. The date and time of each vomiting episode was recorded by participants in diaries at the time of occurrence. The percentage of participants with no vomiting and no retching episodes in the delayed phase, defined as the time period of >24 to120 hours post initiation of chemotherapy in Cycle 1, was calculated. (NCT02519842)
Timeframe: >24 to 120 hours post initiation of chemotherapy (1 to 15 days after the dose of study drug)

InterventionPercentage of Participants (Number)
Fosaprepitant Regimen Cycle 148.6
Control Regimen Cycle 141.2

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Percentage of Participants Who Experienced a Complete Response During the Overall Phase (0 to 120 Hours Post Initiation of Chemotherapy) in Cycle 1

Complete Response was defined as no vomiting, no retching, and no use of rescue medication following the initiation of emetogenic chemotherapy in Cycle 1. A vomiting episode was specified as one or more episodes of emesis (expulsion of stomach contents through the mouth) or retching/dry heaves (an attempt to vomit that is not productive of stomach contents). Distinct vomiting episodes were separated by the absence of emesis and retching for at least one minute. The date and time of each vomiting episode was recorded by participants in diaries at the time of occurrence. The percentage of participants with no vomiting and no retching episodes in the overall phase, defined as the time period of 0 to 120 hours post initiation of chemotherapy in Cycle 1, was calculated. (NCT02519842)
Timeframe: 0 to 120 hours post initiation of chemotherapy (up to 15 days after the dose of study drug)

InterventionPercentage of Participants (Number)
Fosaprepitant Regimen Cycle 140.5
Control Regimen Cycle 132.4

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Percentage of Participants Who Experienced One or More Adverse Events

An adverse event (AE) is defined as any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a study drug, whether or not it is considered related to the study drug. A statistical analysis was performed for Tier 2 AEs in Cycle 1 to compare the percentage of participants who received fosaprepitant regimen and experienced at least 1 Tier 2 AE compared with the percentage of participants in the control regimen. The Tier 2 endpoint included broad clinical and laboratory AE categories consisting of the percentage of participants with any AE, drug-related AE, serious AE, and AEs that are both drug-related and serious. Tier 2 AEs were not pre-specified as events of interest and inclusion in the Tier 2 analysis required that at least 4 participants in any treatment group exhibited the AE. (NCT02519842)
Timeframe: Up to 6.5 months (up to 2 weeks after last dose of study drug)

InterventionPercentage of Participants (Number)
Fosaprepitant Regimen Cycle 189.2
Control Regimen Cycle 179.4
Fosaprepitant Regimen Cycles 2-678.2

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Percentage of Participants Who Experienced No Vomiting, Regardless of Rescue Medication Use, During the Overall Phase (0 to 120 Hours Post Initiation of Chemotherapy) in Cycle 1

Vomiting was assessed, regardless of rescue medicine use, following the initiation of emetogenic chemotherapy in Cycle 1. A vomiting episode was specified as one or more episodes of emesis (expulsion of stomach contents through the mouth) or retching/dry heaves (an attempt to vomit that is not productive of stomach contents). Distinct vomiting episodes were separated by the absence of emesis and retching for at least one minute. The date and time of each vomiting episode was recorded by participants in diaries at the time of occurrence. Rescue medication was permitted to alleviate symptoms of established nausea or vomiting; but not as preventive medication. The percentage of participants with no vomiting and no retching episodes in the overall phase, defined as the time period of 0 to 120 hours post initiation of chemotherapy in Cycle 1, was calculated. (NCT02519842)
Timeframe: 0 to 120 hours post initiation of chemotherapy (up to 15 days after the dose of study drug)

InterventionPercentage of Participants (Number)
Fosaprepitant Regimen Cycle 140.5
Control Regimen Cycle 132.4

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The Incidence of Postoperative Nausea and Vomiting

The incidence of postoperative nausea and vomiting during 24 hours postoperatively (NCT02597907)
Timeframe: 24 hours

InterventionParticipants (Count of Participants)
Aprepitant Plus Palonosetron5
Aprepitant Plus Ramosetron18

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PONV Incidence: Number of Participants With Postoperative Nausea and Vomiting

The occurrence of PONV, as defined by the administration of antiemetics in the PACU between admission to PACU and discharge from PACU. (NCT02625181)
Timeframe: PACU recovery period

InterventionParticipants (Count of Participants)
Baseline Measurement139
CDS Email Recommendations1323
CDS Email + Real TIme Recommenations1343

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Adherence to PONV Guidelines

PONV guideline adherence: percentage of patients who received the exact number of prophylactic interventions for PONV that were recommended by the decision support. (NCT02625181)
Timeframe: A specific time frame on the day of surgery: the start of admission at the holding room to the end of the anesthetic case

InterventionParticipants (Count of Participants)
Baseline Measurement666
CDS Email Recommendations5260
CDS Email + Real TIme Recommenations5863

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Time to Discharge From the Postanesthesia Care Unit (PACU)

This is the number of minutes from admission to the PACU until discharge, assessed up to 2 days (NCT02625181)
Timeframe: A specific time frame on the day of surgery: from the start of admission to the PACU to discharge from the PACU

Interventionminutes (Mean)
Baseline Measurement266
CDS Email Recommendations264
CDS Email + Real TIme Recommenations266

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The Number of Prophylactic Interventions for PONV

the absolute number of prophylactic interventions applied between the admission of the patient in the holding room until admission to the PACU. (NCT02625181)
Timeframe: A specific time frame on the day of surgery: from the start of admission at the holding room to the end of the anesthetic case

Interventionprophylactic antiemetics administered (Mean)
Baseline Measurement2.196
CDS Email Recommendations2.176
CDS Email + Real TIme Recommenations2.129

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Number of Participants With Complete Response (CR) of Rolapitant Hydrochloride Administered as a Single-dose

Complete response (CR) no emetic episodes and no rescue medications. (NCT02732015)
Timeframe: Days 1-10

InterventionParticipants (Count of Participants)
Cohort 10
Cohort 25

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Rate of Minimal Residual Disease (MRD)

Rate of participants who did not have Minimal Residual Disease (MRD) as assessed by flow cytometry. (NCT02780609)
Timeframe: 3 months post HCT

Interventionpercentage of participants (Number)
Phase 1 Level 1: Selinexor Plus HDM HCT33.3
Phase 1 Level 2: Selinexor Plus HDM HCT100
Phase 1 Level 3: Selinexor Plus HDM HCT16.7
Phase 2: Selinexor Plus HDM HCT33.3

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Phase 1 and Phase 2 Percentage of Participants Treated at Dose Level 3/RP2D With Progression Free Survival (PFS)

Progression Free Survival defined as the time from start of treatment to the time of progression or death. (NCT02780609)
Timeframe: at 24 months

Interventionpercent of participants (Number)
Phase 1 Dose Level 3 and Phase 2: Selinexor Plus HDM HCT66.7

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Overall Survival (OS)

Rate of participants' survival at time of evaluation. (NCT02780609)
Timeframe: at 24 months

Interventionpercent (Number)
Phase 1 Dose Level 3 and Phase 2: Selinexor Plus HDM HCT95.2

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Complete Response (CR)

"Complete response (CR) conversion rate. CR: Negative immunofixation of serum and urine, disappearance of any soft tissue plasmacytomas, and ≤ 5% plasma cells in bone marrow.~tissue plasmacytomas, and ≤ 5% plasma cells in bone marrow.~Complete Response conversion rate. CR: Negative immunofixation of serum and urine, disappearance of any soft tissue plasmacytomas, and ≤ 5% plasma cells in bone marrow." (NCT02780609)
Timeframe: 3 months post HCT

Interventionpercentage of participants with CR (Number)
Phase 1 Level 1: Selinexor Plus HDM HCT0
Phase 1 Level 2: Selinexor Plus HDM HCT33.3
Phase 1 Level 3: Selinexor Plus HDM HCT16.6
Phase 2: Selinexor Plus HDM HCT10

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Somatosensory Evoked Potentials (SEPs), Extremity Amplitude (Right Upper Extremity)

"Neuromonitoring modality utilized during surgical procedures potentially affecting sensory component of central and peripheral nervous system.~SEPs are the electrical signals generated by the nervous system in response to somatosensory stimuli - typically through electrical stimulation of the median nerve. SEPs are read on the skull with electroencephalography (EEG). SEPs was recorded using a 4-channel EEG system at baseline (predose) and regularly after study drug administration." (NCT03197064)
Timeframe: Baseline (pre-dose) and 30, 60, and 90 minutes post-dose

InterventionµV (Mean)
Baseline30 minutes60 minutes90 minutes
Fosaprepitant2.382.472.272.47

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Somatosensory Evoked Potentials (SEPs), Extremity Amplitude (Right Lower Extremity)

"Neuromonitoring modality utilized during surgical procedures potentially affecting sensory component of central and peripheral nervous system.~SEPs are the electrical signals generated by the nervous system in response to somatosensory stimuli - typically through electrical stimulation of the median nerve. SEPs are read on the skull with electroencephalography (EEG). SEPs was recorded using a 4-channel EEG system at baseline (predose) and regularly after study drug administration." (NCT03197064)
Timeframe: Baseline (pre-dose) and 30, 60, and 90 minutes post-dose

InterventionµV (Mean)
Baseline30 minutes60 minutes90 minutes
Fosaprepitant1.71.771.811.79

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Somatosensory Evoked Potentials (SEPs), Extremity Amplitude (Left Upper Extremity)

"Neuromonitoring modality utilized during surgical procedures potentially affecting sensory component of central and peripheral nervous system.~SEPs are the electrical signals generated by the nervous system in response to somatosensory stimuli - typically through electrical stimulation of the median nerve. SEPs are read on the skull with electroencephalography (EEG). SEPs was recorded using a 4-channel EEG system at baseline (predose) and regularly after study drug administration." (NCT03197064)
Timeframe: Baseline (pre-dose) and 30, 60, and 90 minutes post-dose

InterventionµV (Mean)
Baseline30 minutes60 minutes90 minutes
Fosaprepitant2.6852.5452.582.292

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Somatosensory Evoked Potentials (SEPs), Extremity Amplitude (Left Lower Extremity)

"Neuromonitoring modality utilized during surgical procedures potentially affecting sensory component of central and peripheral nervous system.~SEPs are the electrical signals generated by the nervous system in response to somatosensory stimuli - typically through electrical stimulation of the median nerve. SEPs are read on the skull with electroencephalography (EEG). SEPs was recorded using a 4-channel EEG system at baseline (predose) and regularly after study drug administration." (NCT03197064)
Timeframe: Baseline (pre-dose) and 30, 60, and 90 minutes post-dose

InterventionµV (Mean)
Baseline30 minutes60 minutes90 minutes
Fosaprepitant1.561.561.471.35

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Motor Evoked Potentials Amplitude (Left Upper Extremity)

"Neuromonitoring modality utilized during surgical procedures affecting motor component of central and peripheral nervous system.~MEPs are generated when stimulation of the brain on the motor cortex (with Transcranial Magnetic Stimulation [TMS]) causes the spinal cord and peripheral muscles to produce neuroelectrical signals. MEPs are typically measured in the hand muscles." (NCT03197064)
Timeframe: Baseline (pre-dose) and 30, 60, and 90 minutes post-dose

InterventionµV (Mean)
Baseline30 minutes60 minutes90 minutes
Fosaprepitant13001573.331634.891544.78

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Complete Control Rate of Chemotherapy-induced Nausea and Vomiting (CINV) Following 2nd Cycle of Chemotherapy

Complete control rate of nausea and vomiting is defined as the percentage of patients without episodes of nausea or emesis, or rescue medication administered, during overall phase of the second chemotherapy cycle. Data was collected by administration of the MASCC Antiemesis Tool. The MASCC Antiemesis Tool is an eight-item questionnaire administered to patients to assess the occurrence of vomiting and nausea both during the first 24 hours after chemotherapy as well as the occurrence of delayed nausea and vomiting from the day after to 120 hours after chemotherapy. (NCT03237611)
Timeframe: 24 hours following the second cycle of chemotherapy

InterventionParticipants (Count of Participants)
VomitingNausea
Low Dose Aprepitant or Fosaprepitant33

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Complete Control Rate of Chemotherapy-induced Nausea and Vomiting (CINV) Following 1st Cycle of Chemotherapy

Complete control rate of nausea and vomiting is defined as the percentage of patients without episodes of nausea or emesis, or rescue medication administered, during the overall phase of the first carboplatin-based chemotherapy cycle. Data was collected by administration of the MASCC Antiemesis Tool. The MASCC Antiemesis Tool is an eight-item questionnaire administered to patients to assess the occurrence of vomiting and nausea both during the first 24 hours after chemotherapy as well as the occurrence of delayed nausea and vomiting from the day after to 120 hours after chemotherapy. (NCT03237611)
Timeframe: From 24 to 120 hours following the first cycle of chemotherapy, approximately 5 days

InterventionParticipants (Count of Participants)
VomitingNausea
Low Dose Aprepitant or Fosaprepitant99

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Complete Control Rate of Chemotherapy-induced Nausea and Vomiting (CINV) Following 1st Cycle of Chemotherapy

Complete control rate of nausea and vomiting is defined as the percentage of patients without episodes of nausea or emesis, or rescue medication administered, during the overall phase of the first carboplatin-based chemotherapy cycle. Data was collected by administration of the MASCC Antiemesis Tool. The MASCC Antiemesis Tool is an eight-item questionnaire administered to patients to assess the occurrence of vomiting and nausea both during the first 24 hours after chemotherapy as well as the occurrence of delayed nausea and vomiting from the day after to 120 hours after chemotherapy. (NCT03237611)
Timeframe: 24 hours following the first cycle of chemotherapy

InterventionParticipants (Count of Participants)
VomitingNausea
Low Dose Aprepitant or Fosaprepitant1110

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Complete Control Rate of Chemotherapy-induced Nausea and Vomiting (CINV) Following 2nd Cycle of Chemotherapy

Complete control rate of nausea and vomiting is defined as the percentage of patients without episodes of nausea or emesis, or rescue medication administered, during overall phase of the second chemotherapy cycle. Data was collected by administration of the MASCC Antiemesis Tool. The MASCC Antiemesis Tool is an eight-item questionnaire administered to patients to assess the occurrence of vomiting and nausea both during the first 24 hours after chemotherapy as well as the occurrence of delayed nausea and vomiting from the day after to 120 hours after chemotherapy. (NCT03237611)
Timeframe: From 24 to 120 hours following the second cycle of chemotherapy, approximately 5 days

InterventionParticipants (Count of Participants)
VomitingNausea
Low Dose Aprepitant or Fosaprepitant33

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Complete Response (CR) (no Emetic Episodes and no Use of Rescue Medication) During the Acute, Delayed and the Overall Periods as Measured by the Nausea and Vomiting Daily Diary/Questionnaire

"The specific measure will be based on the proportion of patients who answered None to both questions concerning Vomiting episode(None, Once, Twice, More than twice) and number of extra nausea/vomiting pills taken (None, One, Two, More than two) in the Nausea and Vomiting Daily Diary/Questionnaire. The CR rate for the overall, the acute, and the delayed period will be summarized by treatment arm and will be compared using a Chi-squared test. The difference in CR rates between arms will be estimated along with a 95% confidence interval." (NCT03578081)
Timeframe: Up to 120 hours

,
InterventionParticipants (Count of Participants)
Complete Response - >> OverallComplete Response - >> AcuteComplete Response ->> Delayed
Arm I (Fosaprepitant Dimeglumine, Olanzapine)179256193
Arm II (Placebo, Olanzapine)151247166

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Potential Toxicities as Ascribed to Olanzapine as Measured by the Nausea and Vomiting Daily Diary/Questionnaire

Potential toxicities includes nausea, undesired sedation, and undesired appetite, measured by three individual items ( nausea, undesired sedation, undesired appetite) of the Nausea and Vomiting Daily Dairy/Questionnaire(scale 0-10, 0 is no symptoms, 10 is worst symptoms). Incidences of toxicities will be summarized by type and by treatment arm. Incidences of toxicities will be compared between arms using a Chi-squared test or the Fisher's exact test as appropriate. In addition, undesired sedation and appetite increase as collected in the Nausea and Vomiting Daily Diary/Questionnaire will be analyzed by repeated measures analyses including descriptive statistics, graphical approaches, and growth curve models to account for the factor of day and time trend. (NCT03578081)
Timeframe: Up to 120 hours

,
InterventionParticipants (Count of Participants)
Overall No Appetite IncreaseOverall Any Appetite IncreaseAcute No Appetite IncreaseAcute Any Appetite IncreaseDelayed No Appetite IncreaseDelayed Any Appetite Increase
Arm I (Fosaprepitant Dimeglumine, Olanzapine)14018623591147179
Arm II (Placebo, Olanzapine)13618423684143177

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Total Frequency of Rescue Medication as Measured by the Nausea and Vomiting Daily Diary/Questionnaire

The specific measure will be based on the single item : number of extra nausea/vomiting pills taken (None, One , Twice, More than twice) of the Nausea and Vomiting Daily Diary/Questionnaire. (NCT03578081)
Timeframe: Over 5 Days per each of the 4 cycles

,
Interventionepisodes (Number)
ZeroOneTwoMore than two
Arm I (Fosaprepitant Dimeglumine, Olanzapine)361435017056
Arm II (Placebo, Olanzapine)354140516274

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Average Nausea Scores (0-10) Repeatedly Measured by the Nausea and Vomiting Daily Diary/Questionnaire

The specific measure will be based on the by the single nausea item (scale 0-10, 0 is no symptoms, 10 is worst symptoms) of the Nausea and Vomiting Daily Diary/Questionnaire. Nausea scores (0-10) repeatedly measured by the Nausea and Vomiting Daily Diary/Questionnaire will be analyzed using the repeated measures analyses and growth curve models as described above for undesired sedation and increase in appetite. (NCT03578081)
Timeframe: Up to 1 year

Interventionscore on a scale (Mean)
Arm I (Fosaprepitant Dimeglumine, Olanzapine)0.8211364
Arm II (Placebo, Olanzapine)0.9177778

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No Nausea Rate Defined as a Response of 0 in the Nausea Item of Nausea and Vomiting Daily Diary/Questionnaire in the Overall (0-120 Hours), Acute (0-24 Hours), and Delayed (24-120 Hours) Periods

The specific measure will be based on the proportion of patients with a value of 0, as measured by the single nausea item (scale 0-10, 0 is no symptoms, 10 is worst symptoms) of the Questionnaire. A modified intent-to-treat principle will be applied for statistical analysis of efficacy in evaluable patients. The proportions of patients with no nausea during the overall, the acute, and the delayed period will be summarized by treatment arm. They will be tested in a sequential manner, using a Simes gatekeeping procedure to maintain the overall significance level at the specified by the Lan-DeMets family of alpha spending function. The difference in no nausea proportions between arms will be estimated along with a one-sided 95% confidence interval. The tests and the confidence intervals will be constructed using normal approximation of the binomial distribution adjusted for the non-inferiority margin. (NCT03578081)
Timeframe: Up to 120 hours

,
InterventionParticipants (Count of Participants)
Overall No NauseaOverall Any NauseaAcute No NauseaAcute Any NauseaDelayed No NauseaDelayed Any Nausea
Arm I (Fosaprepitant Dimeglumine, Olanzapine)123203202124140186
Arm II (Placebo, Olanzapine)97223201119114206

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Mean Area Under the Curve (AUC) of the NRS-R (Windowed Worst Observation Carried Forward) Pain Intensity Scores

"Pain intensity scores are assessed using an 11-point Numeric Rating Scale (NRS) (0-10) where 0 represents no pain and 10 represents worst pain imaginable. NRS scores are measured at rest." (NCT03718039)
Timeframe: 72 hours

Interventionpain intensity score*hr (Mean)
Treatment Group 1: HTX-011251.92
Treatment Group 2: HTX-011 + Aprepitant252.39
Treatment Group 3: HTX-011 + Non-Opioid MMA Regimen113.10

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Mean Total Postoperative Opioid Consumption (in Morphine Equivalents) Through 72 Hours

(NCT03718039)
Timeframe: 72 hours

InterventionMME, morphine milligram equivalents (Mean)
Treatment Group 1: HTX-01111.47
Treatment Group 2: HTX-011 + Aprepitant21.88
Treatment Group 3: HTX-011 + Non-Opioid MMA Regimen1.61

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Percentage of Subjects Receiving no Opioid Rescue

(NCT03718039)
Timeframe: 72 hours

InterventionParticipants (Count of Participants)
Treatment Group 1: HTX-0116
Treatment Group 2: HTX-011 + Aprepitant0
Treatment Group 3: HTX-011 + Non-Opioid MMA Regimen24

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Mean Area Under the Curve (AUC) of the NRS-A (Windowed Worst Observation Carried Forward) Pain Intensity Scores

"Pain intensity scores are assessed using an 11-point Numeric Rating Scale (NRS) (0-10) where 0 represents no pain and 10 represents worst pain imaginable. NRS scores are recorded with activity (NRS-A), sitting with the plantar surface of the ball of the surgically attended foot touching the floor (no weight-bearing)." (NCT03718039)
Timeframe: 72 hours

Interventionpain intensity score*hr (Mean)
Treatment Group 1: HTX-011278.36
Treatment Group 2: HTX-011 + Aprepitant288.23
Treatment Group 3: HTX-011 + Non-Opioid MMA Regimen126.93

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Percentage of Subjects Receiving no Opioid Rescue

Only subjects in Cohort 3 received a scheduled, non-opioid MMA regimen following surgery. (NCT03718039)
Timeframe: Day 7 and Day 28

InterventionParticipants (Count of Participants)
Day 7Day 28
Treatment Group 3: HTX-011 + Non-Opioid MMA Regimen2424

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Percentage of Participants in Cycle 1 Who Discontinued Study Drug Due to an Adverse Event (AE)

An AE is defined as any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a study drug, whether or not it is considered related to the study drug. The percentage of participants in Cycle 1 who discontinue study treatment due to an AE is presented. (NCT04054193)
Timeframe: Up to 3 days

InterventionPercentage of Participants (Number)
Fosaprepitant Treatment2.0

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Percentage of Participants in Cycle 1 Who Experienced One or More Adverse Events (AEs)

An AE is defined as any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a study drug, whether or not it is considered related to the study drug. The percentage of participants in Cycle 1 who experience one or more AE(s) is presented. (NCT04054193)
Timeframe: Up to 17 days

InterventionPercentage of Participants (Number)
Fosaprepitant Treatment80.0

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Time to Discharge From Hospital.

(NCT04470622)
Timeframe: 56 Days.

Interventiondays (Median)
Treatment Group 1: Aprepitant Injectable Emulsion6.0
Treatment Group 2: Placebo8.0

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Incidence of Treatment-emergent Adverse Events.

Number of subjects reporting at least on Treatment-Emergent Adverse Event. Subjects reporting more than one event are counted only once using the highest severity. (NCT04470622)
Timeframe: Through Day 56

InterventionParticipants (Count of Participants)
Treatment Group 1: Aprepitant Injectable Emulsion8
Treatment Group 2: Placebo5

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Time to Death or Respiratory Failure, Defined as Any of the Following: Endotracheal Intubation and Mechanical Ventilation; Oxygen Delivered by High-flow Nasal Cannula; Noninvasive Positive Pressure Ventilation; Extracorporeal Membrane Oxygenation (ECMO).

(NCT04470622)
Timeframe: 56 Days.

Interventiondays (Median)
Treatment Group 1: Aprepitant Injectable EmulsionNA
Treatment Group 2: PlaceboNA

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Proportion of Subjects Alive and Discharged From the Hospital.

ITT Population. (NCT04470622)
Timeframe: 14 Days.

InterventionParticipants (Count of Participants)
Treatment Group 1: Aprepitant Injectable Emulsion11
Treatment Group 2: Placebo10

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Change From Baseline in Interleukin 6 (IL-6).

(NCT04470622)
Timeframe: Days 7, 14, 28, Discharge (from 2 to 43 days; median 6 days (Aprepitant), 8 days (Placebo))

,
Interventionpg/mL (Mean)
BaselineDay 7Day 14Day 28Discharge
Treatment Group 1: Aprepitant Injectable Emulsion18.77-27.98124.00-8.00-17.41
Treatment Group 2: Placebo19.1114.83204.302.90-9.68

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