Page last updated: 2024-11-12

rolapitant

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID10311306
CHEMBL ID3707331
CHEBI ID90908
SCHEMBL ID354305
MeSH IDM0582062

Synonyms (50)

Synonym
varubi (tn)
sch 619734
varubi
8-((1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro(4,5)decan-2-one
552292-08-7
rolapitant ,
sch-619734
unii-nle429izuc
nle429izuc ,
rolapitant [usan:inn]
(5s,8s)-8-(((1r)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro(4.5)decan-2-one
(5s,8s)-8-(((r)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro[4.5]decan-2-one
S5476
gtpl5749
(5s,8s)-8-[[(1r)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-1,9-diazaspiro[4.5]decan-2-one
varuby
rolapitant [mi]
1,7-diazaspiro(4.5)decan-2-one, 8-(((1r)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-, (5s,8s)-
(5s,8s)-8-{[(1r)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl}-8-phenyl-1,7-diazaspiro[4.5]decan-2-one
rolapitant [inn]
rolapitant [usan]
rolapitant [who-dd]
SCHEMBL354305
(5s,8s)-8-({(1r)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}methyl)-8-phenyl-1,7-diazaspiro[4.5]decan-2-one
CHEBI:90908 ,
CHEMBL3707331
rolapitant (usan/inn)
D10742
AC-30924
bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-1,9-diazaspiro[4.5]decan-2-one
DTXSID90203740 ,
DB09291
EX-A1288
rolapitant(sch619734)
AKOS030234023
rolapitant free base
mfcd23105917
HY-14751
CS-6387
5552292-08-7 (free base)
BCP09609
CCG-269691
MS-29288
brand name: varubi
sch619734 sch-619734
EN300-18166845
fivsjygqaiemoc-zgnkegeesa-n
dtxcid20126231
a04ad14
rolapitantum

Research Excerpts

Overview

Rolapitant is a highly selective neurokinin-1 receptor antagonist. orally administered for a single dose of 180 mg before chemotherapy with granisetron D1, dexamethasone 8 mg BID on day 2-4.

ExcerptReferenceRelevance
"Rolapitant is a functionally competitive antagonist, as measured by calcium efflux, with a calculated Kb of 0.17 nM."( Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets.
Duffy, RA; Higgins, GA; Lachowicz, JE; Morgan, C; Naylor, R; Parker, EM; Varty, GB, 2012
)
2.54
"Rolapitant is a highly selective neurokinin-1 receptor antagonist, orally administered for a single dose of 180 mg before chemotherapy with granisetron D1, dexamethasone 8 mg BID on day 2-4. "( Differential clinical pharmacology of rolapitant in delayed chemotherapy-induced nausea and vomiting (CINV).
Abdel-Rahman, O; Rashad, N, 2017
)
2.17
"Rolapitant is a highly selective neurokinin-1 (NK-1) receptor antagonist with very good oral activity, central nervous system penetration and a long (180-hour) plasma half-life."( Rolapitant: An NK-1 Receptor Antagonist for the Prevention of Chemotherapy- Induced Nausea and Vomiting.
Rapoport, BL, 2017
)
2.62
"Rolapitant is a selective and long-acting neurokinin-1 receptor antagonist approved in an oral formulation in combination with other antiemetic agents for the prevention of delayed chemotherapy-induced nausea and vomiting in adults. "( Effects of Rolapitant Administered Intravenously or Orally on the Pharmacokinetics of Digoxin (P-glycoprotein Substrate) and Sulfasalazine (Breast Cancer Resistance Protein Substrate) in Healthy Volunteers.
Arora, S; Christensen, J; Hughes, L; Kansra, V; Lu, S; Powers, D; Wang, J; Wang, X; Zhang, ZY, 2018
)
2.31
"Rolapitant is a novel selective neurokinin-1 receptor antagonist (NK-1 RA), which was clinically approved for prevention of CINV."( Meta-analysis of safety and efficacy of rolapitant, NK-1 receptor antagonist for prevention of chemotherapy-induced nausea and vomiting.
Abdel-Daim, MM; Abushouk, AI; Ahmed, H; Hammad, AM; Negida, A; Salem, M; Zidan, M,
)
1.12
"Rolapitant is a selective and long-acting neurokinin-1 receptor antagonist approved in an oral formulation in combination with other antiemetic agents for the prevention of delayed chemotherapy-induced nausea and vomiting in adults. "( Pharmacokinetics of Rolapitant in Patients With Mild to Moderate Hepatic Impairment.
Arora, S; Kansra, V; Lu, S; Wang, J; Wang, X; Zhang, ZY, 2018
)
2.25
"Rolapitant is a selective and long-acting neurokinin-1 receptor antagonist approved in an oral formulation in combination with dexamethasone and a 5-hydroxytryptamine type 3 receptor antagonist for the prevention of delayed chemotherapy-induced nausea and vomiting in adults. "( Pharmacokinetics, Safety, and Tolerability of Rolapitant Administered Intravenously Following Single Ascending and Multiple Ascending Doses in Healthy Subjects.
Arora, S; Kansra, V; Lu, S; Powers, D; Wang, J; Wang, X; Zhang, ZY, 2019
)
2.21
"Rolapitant is a neurokinin-1 receptor antagonist that is approved in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting (CINV) associated with initial and repeat courses of emetogenic cancer chemotherapy, including but not limited to highly emetogenic chemotherapy. "( Absorption, metabolism, and excretion of the antiemetic rolapitant, a selective neurokinin-1 receptor antagonist, in healthy male subjects.
Kansra, V; Wang, J; Wang, X; Zhang, ZY, 2019
)
2.2
"Rolapitant is a neurokinin-1 receptor antagonist indicated in combination with other antiemetic agents in adults for the prevention of delayed chemotherapy-induced nausea and vomiting. "( Effects of rolapitant administered orally on the pharmacokinetics of dextromethorphan (CYP2D6), tolbutamide (CYP2C9), omeprazole (CYP2C19), efavirenz (CYP2B6), and repaglinide (CYP2C8) in healthy subjects.
Kansra, V; Lu, S; Powers, D; Wang, J; Wang, X; Zhang, ZY, 2019
)
2.35
"Rolapitant (Varubi) is a neurokinin-1 receptor antagonist approved for the prevention of chemotherapy-induced nausea and vomiting. "( Pharmacokinetic Interactions of Rolapitant With Cytochrome P450 3A Substrates in Healthy Subjects.
Arora, S; Christensen, J; Hughes, L; Lu, S; Wang, J; Wang, X; Zhang, ZY, 2019
)
2.24
"Rolapitant is a novel, long-acting neurokinin-1 (NK-1) receptor antagonist. "( Study of rolapitant, a novel, long-acting, NK-1 receptor antagonist, for the prevention of chemotherapy-induced nausea and vomiting (CINV) due to highly emetogenic chemotherapy (HEC).
Arora, S; Chua, D; Fein, LE; Poma, A; Rapoport, B; Wang, Y, 2015
)
2.28
"Rolapitant (Varubi™) is an orally active neurokinin-1 receptor antagonist developed by TESARO and approved in the USA for use in combination with other antiemetic agents for the prevention of delayed chemotherapy-induced nausea and vomiting (CINV) in adults. "( Rolapitant: first global approval.
Syed, YY, 2015
)
3.3
"Rolapitant is a long-acting NK-1 receptor antagonist with proven efficacy in controlling CINV as part of the prophylaxis regimen."( Rolapitant for the treatment of chemotherapy-induced nausea and vomiting: a review of the clinical evidence.
Chasen, MR; Rapoport, BL, 2016
)
2.6

Toxicity

Rolapitant was safe and well tolerated across all studies. The most frequently reported treatment-related treatment-emergent adverse events were fatigue, constipation, and headache.

ExcerptReferenceRelevance
"Chemotherapy-induced nausea and vomiting is a common side-effect of many antineoplastic regimens and can occur for several days after treatment."( Safety and efficacy of rolapitant for prevention of chemotherapy-induced nausea and vomiting after administration of moderately emetogenic chemotherapy or anthracycline and cyclophosphamide regimens in patients with cancer: a randomised, active-controlled
Arora, S; Chasen, MR; Gridelli, C; Modiano, MR; Navari, RM; Poma, A; Rapoport, BL; Schnadig, ID; Schwartzberg, LS; Urban, L, 2015
)
0.73
" The incidence of adverse events was similar in the rolapitant and control groups, with the most frequently reported treatment-related treatment-emergent adverse events being fatigue, constipation, and headache."( Safety and efficacy of rolapitant for prevention of chemotherapy-induced nausea and vomiting after administration of moderately emetogenic chemotherapy or anthracycline and cyclophosphamide regimens in patients with cancer: a randomised, active-controlled
Arora, S; Chasen, MR; Gridelli, C; Modiano, MR; Navari, RM; Poma, A; Rapoport, BL; Schnadig, ID; Schwartzberg, LS; Urban, L, 2015
)
0.98
" The incidence of adverse events was similar across treatment groups."( Safety and efficacy of rolapitant for prevention of chemotherapy-induced nausea and vomiting after administration of cisplatin-based highly emetogenic chemotherapy in patients with cancer: two randomised, active-controlled, double-blind, phase 3 trials.
Arora, S; Chasen, MR; Gridelli, C; Kansra, V; Modiano, MR; Navari, RM; Poma, A; Rapoport, BL; Schnadig, ID; Schwartzberg, LS; Urban, L, 2015
)
0.73
" The incidence of treatment-related adverse events during cycles 2-6 was similar in rolapitant (5."( Efficacy and safety of rolapitant for prevention of chemotherapy-induced nausea and vomiting over multiple cycles of moderately or highly emetogenic chemotherapy.
Arora, S; Chasen, M; Navari, R; Powers, D; Rapoport, B; Schnadig, I; Schwartzberg, L, 2016
)
0.97
" To analyze potential drug-drug interactions between rolapitant and concomitant medications, this integrated safety analysis of four double-blind, randomized phase II or III studies of rolapitant examined adverse events (AEs) by use versus non-use of drug substrates of CYP2D6 or BCRP."( Integrated safety analysis of rolapitant with coadministered drugs from phase II/III trials: an assessment of CYP2D6 or BCRP inhibition by rolapitant.
Aapro, M; Arora, S; Barbour, S; Herrstedt, J; Kansra, V; Powers, D; Smit, T; Wang, X, 2017
)
0.99
" Rolapitant was safe and well tolerated across all studies, with no serious or severe rolapitant-related treatment-emergent adverse events."( Pharmacokinetics, Safety, and Tolerability of Rolapitant Administered Intravenously Following Single Ascending and Multiple Ascending Doses in Healthy Subjects.
Arora, S; Kansra, V; Lu, S; Powers, D; Wang, J; Wang, X; Zhang, ZY, 2019
)
1.68

Pharmacokinetics

The pharmacokinetic and safety profiles of intravenous (IV) rolapitant were evaluated in two open-label, phase 1 trials in healthy subjects. This was a single oral dose of 180 mg of ro Lapitant and its major active metabolite, M19, in subjects with mild and moderate hepatic impairment compared with healthy matched controls.

ExcerptReferenceRelevance
" This was a phase 1 open-label, parallel-group pharmacokinetic and safety study of a single oral dose of 180 mg of rolapitant and its major active metabolite, M19, in subjects with mild and moderate hepatic impairment compared with healthy matched controls."( Pharmacokinetics of Rolapitant in Patients With Mild to Moderate Hepatic Impairment.
Arora, S; Kansra, V; Lu, S; Wang, J; Wang, X; Zhang, ZY, 2018
)
1.01
" The pharmacokinetic and safety profiles of intravenous (IV) rolapitant were evaluated in two open-label, phase 1 trials in healthy subjects."( Pharmacokinetics, Safety, and Tolerability of Rolapitant Administered Intravenously Following Single Ascending and Multiple Ascending Doses in Healthy Subjects.
Arora, S; Kansra, V; Lu, S; Powers, D; Wang, J; Wang, X; Zhang, ZY, 2019
)
1.01
" Three phase 1, open-label, drug-drug interaction studies were conducted to examine the pharmacokinetic interactions of orally administered rolapitant with midazolam, rolapitant with ketoconazole, and rolapitant with rifampin."( Pharmacokinetic Interactions of Rolapitant With Cytochrome P450 3A Substrates in Healthy Subjects.
Arora, S; Christensen, J; Hughes, L; Lu, S; Wang, J; Wang, X; Zhang, ZY, 2019
)
1
" Population pharmacokinetic analysis was performed via nonlinear mixed-effects modeling."( Population Pharmacokinetics of Rolapitant in Patients With Chemotherapy-Induced Nausea and Vomiting.
Kansra, V; Wang, J; Wang, X; Zhang, ZY, 2019
)
0.8

Bioavailability

ExcerptReferenceRelevance
" Two studies in healthy volunteers evaluated 1) absolute bioavailability and 2) NK-1 receptor occupancy of oral rolapitant."( Rolapitant Absolute Bioavailability and PET Imaging Studies in Healthy Adult Volunteers.
Kansra, V; Lu, S; Powers, D; Wang, J; Wang, X; Zhang, ZY, 2017
)
2.11
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
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.
neurokinin-1 receptor antagonistAn antagonist at the neurokinin-1 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 (5)

ClassDescription
etherAn organooxygen compound with formula ROR, where R is not hydrogen.
azaspiro compoundAn azaspiro compound is a spiro compound in which at least one of the cyclic components is a nitrogen heterocyle.
pyrrolidin-2-onesA pyrrolidinone in which the oxo group is at position 2 of the pyrrolidine ring.
piperidines
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
[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 (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency26.21230.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency26.21230.00339.158239.8107AID1347411
[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)
Substance-P receptorHomo sapiens (human)Ki0.00070.00000.79368.7470AID1340842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (68)

Processvia Protein(s)Taxonomy
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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
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)
tachykinin receptor activitySubstance-P receptorHomo sapiens (human)
protein bindingSubstance-P receptorHomo sapiens (human)
substance P receptor activitySubstance-P receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1346346Human NK1 receptor (Tachykinin receptors)2012Pharmacology, biochemistry, and behavior, Jul, Volume: 102, Issue:1
Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (46)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's41 (89.13)24.3611
2020's5 (10.87)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 46.76

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index46.76 (24.57)
Research Supply Index4.23 (2.92)
Research Growth Index4.54 (4.65)
Search Engine Demand Index70.64 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (46.76)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials17 (33.33%)5.53%
Reviews14 (27.45%)6.00%
Case Studies1 (1.96%)4.05%
Observational0 (0.00%)0.25%
Other19 (37.25%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (12)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized, Double-Blind, Double-Dummy, Dose-Ranging, Active- and Placebo-Controlled Study of Single-Dose Oral Rolapitant Monotherapy for the Prevention of Postoperative Nausea and Vomiting (PONV) [NCT00539721]Phase 2619 participants (Actual)Interventional2007-10-31Completed
An Open-Label, Randomized, Pivotal, Bioequivalence Study of Oral and Intravenous Rolapitant [NCT02285647]Phase 1138 participants (Actual)Interventional2014-09-30Completed
Phase II Study of Rolapitant Plus Olanzapine, Palonosetron, and Dexamethasone in Patients With Germ Cell Tumors Undergoing 5-day Cisplatin-based Chemotherapy. [NCT03960151]Phase 20 participants (Actual)Interventional2018-05-31Withdrawn(stopped due to Compound was sold by funder and development ceased.)
Study of the Efficacy and Safety of SCH 619734 in Subjects With Chronic Idiopathic Cough [NCT00506545]Phase 235 participants (Actual)Interventional2007-01-31Completed
Phase II Randomized Study to Evaluate Efficacy, Patient Satisfaction, and Compliance of the Oral Combination of Rolapitant (Varubi®) Plus Ondansetron vs. Ondansetron Monotherapy in Malignant Glioma Patients Receiving Radiotherapy (RT) and Concomitant Temo [NCT02991456]Phase 248 participants (Actual)Interventional2017-10-09Completed
A Phase 2, MultiCenter, Randomized, Placebo-Controlled, Double-Blind, Dose Finding Study to Determine the Safety and Efficacy of SCH 619734 for the Treatment of Chemotherapy Induced Nausea and Vomiting (CINV) in Subjects Receiving Highly Emetogenic Chemot [NCT00394966]Phase 2450 participants (Anticipated)Interventional2006-09-30Completed
Phase 3, Multicenter, Randomized, Double Blind, Active-Controlled Study of the Safety & Efficacy of Rolapitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV) in Subjects Receiving Highly Emetogenic Chemotherapy (HEC) [NCT01499849]Phase 3532 participants (Actual)Interventional2012-02-29Completed
A Phase 1, 2-Part, Single Ascending Dose Assessment of the Safety, Tolerability, and Pharmacokinetics of Rolapitant Intravenous in Healthy Volunteers [NCT02382666]Phase 1100 participants (Actual)Interventional2015-01-31Completed
An Open Label, Single Dose, Three Part Study to Assess the Effects of Rolapitant (1.8 mg/mL Rolapitant IV Solution) on the Pharmacokinetics of Digoxin (P-gp); Sulfasalazine (BCRP); and the Cooperstown Cocktail (Midazolam [CYP3A4], Omeprazole [CYP2C19], Wa [NCT02434861]Phase 1102 participants (Actual)Interventional2015-05-31Completed
A Phase 3, Multicenter, Randomized, Double Blind, Active-Controlled Study of the Safety and Efficacy of Rolapitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV) in Subjects Receiving Highly Emetogenic Chemotherapy [NCT01500213]Phase 3555 participants (Actual)Interventional2012-02-29Completed
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)
Phase 3, Multicenter, Randomized, Double Blind, Active-Controlled Study of the Safety and Efficacy of Rolapitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV) in Subjects Receiving Moderately Emetogenic Chemotherapy [NCT01500226]Phase 31,369 participants (Actual)Interventional2012-02-29Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01499849 (3) [back to overview]Acute Phase Response
NCT01499849 (3) [back to overview]No Emetic Episodes and No Rescue Medication
NCT01499849 (3) [back to overview]Overall Response Rate
NCT01500213 (3) [back to overview]Acute Phase Response
NCT01500213 (3) [back to overview]No Emetic Episodes and No Rescue Medication
NCT01500213 (3) [back to overview]Overall Response Rate
NCT01500226 (3) [back to overview]Acute Phase Response
NCT01500226 (3) [back to overview]No Emetic Episodes and No Rescue Medication
NCT01500226 (3) [back to overview]Overall Response Rate
NCT02732015 (1) [back to overview]Number of Participants With Complete Response (CR) of Rolapitant Hydrochloride Administered as a Single-dose
NCT02991456 (17) [back to overview]Chemoradiation-induced Nausea (cRIN) Rate Over All Six Weeks
NCT02991456 (17) [back to overview]Chemoradiation-induced Nausea (cRIN) Rate Over First Two Weeks
NCT02991456 (17) [back to overview]Chemoradiation-induced Nausea (cRIN) Rate Over First Two Weeks and Supplemented by Nurses Notes
NCT02991456 (17) [back to overview]Chemoradiation-induced Vomiting (cRIV) Rate Over All Six Weeks
NCT02991456 (17) [back to overview]Chemoradiation-induced Vomiting (cRIV) Rate Over First Two Weeks
NCT02991456 (17) [back to overview]Chemoradiation-induced Vomiting (cRIV) Rate Over First Two Weeks With Supplemental Nurses Notes
NCT02991456 (17) [back to overview]Complete Response (CR) Rate as Measured by Antiemesis Tool (MAT)
NCT02991456 (17) [back to overview]Complete Response (CR) Rate as Measured by MAT With Supplemental Nurses Notes
NCT02991456 (17) [back to overview]Ondansetron Medication Compliance Weeks 1-3
NCT02991456 (17) [back to overview]Ondansetron Medication Compliance Weeks 4-6
NCT02991456 (17) [back to overview]Proportion of Participants With Grade 3, 4 or 5 Treatment-related Adverse Events
NCT02991456 (17) [back to overview]Week 3 Patient Satisfaction: Convenience
NCT02991456 (17) [back to overview]Week 3 Patient Satisfaction: Effectiveness
NCT02991456 (17) [back to overview]Week 3 Patient Satisfaction: Overall Satisfaction
NCT02991456 (17) [back to overview]Week 6 Patient Satisfaction: Convenience
NCT02991456 (17) [back to overview]Week 6 Patient Satisfaction: Effectiveness
NCT02991456 (17) [back to overview]Week 6 Patient Satisfaction: Overall Satisfaction

Acute Phase Response

To determine the effect of rolapitant on complete response rates in the acute (0 to 24 hours)phase of CINV (NCT01499849)
Timeframe: 0 to 24 hours

Interventionpercentage of participants (Number)
Rolapitant + Granisetron + Dexamethasone83.7
Placebo + Granisetron + Dexamethasone73.7

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No Emetic Episodes and No Rescue Medication

The primary objective of this study is to determine whether administration of rolapitant with granisetron and dexamethasone improves CINV in the delayed phase (>24 to 120 hours) of CINV compared with administration of placebo with granisetron and dexamethasone in subjects receiving HEC. The primary outcome will be based on complete response (defined as no emetic episodes and no rescue medication) in the delayed phase (>24 to 120 hours). (NCT01499849)
Timeframe: >24 to 120 hours post chemotherapy

Interventionpercentage of participants (Number)
Rolapitant + Granisetron + Dexamethasone72.7
Placebo + Granisetron + Dexamethasone58.4

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Overall Response Rate

To determine the effect of rolapitant on complete response rates in the overall (0 to 120 hours) phase of CINV. (NCT01499849)
Timeframe: 0 to 120 hours

Interventionpercentage of participants (Number)
Rolapitant + Granisetron + Dexamethasone70.1
Placebo + Granisetron + Dexamethasone56.5

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Acute Phase Response

To determine the effect of rolapitant on complete response rates in the acute (0 to 24 hours) phase of CINV. (NCT01500213)
Timeframe: 0 to 24 hours

Interventionpercentage of participants (Number)
Rolapitant + Granisetron + Dexamethasone83.4
Placebo + Granisetron + Dexamethasone79.5

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No Emetic Episodes and No Rescue Medication

The primary objective of this study is to determine whether administration of rolapitant with granisetron and dexamethasone improves CINV in the delayed phase (>24 to 120 hours) of CINV compared with administration of placebo with granisetron and dexamethasone in subjects receiving HEC. The primary outcome will be based on complete response (defined as no emesis and no rescue medication) in the delayed phase (>24 to 120 hours). (NCT01500213)
Timeframe: >24 to 120 hours post chemotherapy

Interventionpercentage of participants (Number)
Rolapitant + Granisetron + Dexamethasone70.1
Placebo + Granisetron + Dexamethasone61.9

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Overall Response Rate

To determine the effect of rolapitant on complete response rate in the overall (0 to 120 hours) phase of CINV. (NCT01500213)
Timeframe: 0 to 120 hours

Interventionpercentage of participants (Number)
Rolapitant + Granisetron + Dexamethasone67.5
Placebo + Granisetron + Dexamethasone60.4

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Acute Phase Response

To determine the effect of rolapitant on complete response rates in the acute (0 to 24 hours) phase of CINV. (NCT01500226)
Timeframe: 0 to 24 hours

Interventionpercentage of participants (Number)
Rolapitant + Granisetron + Dexamethasone83.5
Placebo + Granisetron + Dexamethasone80.3

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No Emetic Episodes and No Rescue Medication

The primary objective of this study is to determine whether administration of rolapitant with granisetron and dexamethasone improves CINV in the delayed phase (>24 to 120 hours) of CINV compared with administration of placebo with granisetron and dexamethasone in subjects receiving MEC. The primary outcome will be based on complete response (defined as no emesis and no rescue medication) in the delayed phase (>24 to 120 hours). (NCT01500226)
Timeframe: >24 to 120 hours post chemotherapy

Interventionpercentage of particpants (Number)
Rolapitant + Granisetron + Dexamethasone71.3
Placebo + Granisetron + Dexamethasone61.6

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Overall Response Rate

To determine the effect of rolapitant on complete response rate in the overall (0 to 120 hours) phase of CINV. (NCT01500226)
Timeframe: 0 to 120 hours

Interventionpercentage of participants (Number)
Rolapitant + Granisetron + Dexamethasone68.6
Placebo + Granisetron + Dexamethasone57.8

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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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Chemoradiation-induced Nausea (cRIN) Rate Over All Six Weeks

The cRIN-CR rate is defined as the proportion of participants who did not use rescue medication for nausea. The cRIN-CR rates were assessed via the modified Multinational Association of Supportive Care in Cancer (MASCC) Antiemesis Tool (MAT). (NCT02991456)
Timeframe: Weeks 1-6

Interventionproportion of participants (Number)
Sequence A0.4737
Sequence B0.4737

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Chemoradiation-induced Nausea (cRIN) Rate Over First Two Weeks

The cRIN-CR rate is defined as the proportion of participants who did not use rescue medication for nausea. The cRIN-CR rates were assessed via the modified Multinational Association of Supportive Care in Cancer (MASCC) Antiemesis Tool (MAT). (NCT02991456)
Timeframe: Weeks 1 and 2

Interventionproportion of participants (Number)
Sequence A0.6160
Sequence B0.6842

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Chemoradiation-induced Nausea (cRIN) Rate Over First Two Weeks and Supplemented by Nurses Notes

The cRIN-CR rate is defined as the proportion of participants who did not use rescue medication for nausea. The cRIN-CR rates were assessed via the modified Multinational Association of Supportive Care in Cancer (MASCC) Antiemesis Tool (MAT) and nurses notes if MATs were missing. (NCT02991456)
Timeframe: Weeks 1 and 2

Interventionproportion of participants (Number)
Sequence A0.6000
Sequence B0.6087

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Chemoradiation-induced Vomiting (cRIV) Rate Over All Six Weeks

The cRIV-CR rate is defined as the proportion of participants without use of rescue medication for vomiting. The cRIV-CR rates were assessed via the modified Multinational Association of Supportive Care in Cancer (MASCC) Antiemesis Tool (MAT). (NCT02991456)
Timeframe: Weeks 1-6

Interventionproportion of participants (Number)
Sequence A0.7368
Sequence B0.8947

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Chemoradiation-induced Vomiting (cRIV) Rate Over First Two Weeks

The cRIV-CR rate is defined as the proportion of participants without use of rescue medication for vomiting. The cRIV-CR rates were assessed via the modified Multinational Association of Supportive Care in Cancer (MASCC) Antiemesis Tool (MAT). (NCT02991456)
Timeframe: Weeks 1 and 2

Interventionproportion of participants (Number)
Sequence A0.8095
Sequence B1.0000

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Chemoradiation-induced Vomiting (cRIV) Rate Over First Two Weeks With Supplemental Nurses Notes

The cRIV-CR rate is defined as the proportion of participants without use of rescue medication for vomiting. The cRIV-CR rates were assessed via the modified Multinational Association of Supportive Care in Cancer (MASCC) Antiemesis Tool (MAT) and nurse notes if MATS are missing. (NCT02991456)
Timeframe: Weeks 1 and 2

Interventionproportion of participants (Number)
Sequence A0.8000
Sequence B0.9565

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Complete Response (CR) Rate as Measured by Antiemesis Tool (MAT)

The Complete Response rate is defined as the proportion of participants with no emetic episode or the use of rescue medication during the first two weeks of radiation therapy and concomitant Temozolomide. The Complete Response rate will be assessed via the modified Multinational Association of Supportive Care in Cancer (MASCC) Antiemesis Tool (MAT). (NCT02991456)
Timeframe: Weeks 1 and 2

Interventionproportion of participants (Number)
Sequence A0.5717
Sequence B0.7368

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Complete Response (CR) Rate as Measured by MAT With Supplemental Nurses Notes

The Complete Response rate is defined as the proportion of participants with no emetic episode or the use of rescue medication during the first two weeks of radiation therapy and concomitant Temozolomide. The Complete Response rate will be assessed via the modified Multinational Association of Supportive Care in Cancer (MASCC) MAT and nurse notes if MATs are missing. (NCT02991456)
Timeframe: Weeks 1 and 2

Interventionproportion of participants (Number)
Sequence A0.6000
Sequence B0.6522

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Ondansetron Medication Compliance Weeks 1-3

Percentage of participants who adhered to ondansetron treatment for more than 21 days during weeks 1-3. (NCT02991456)
Timeframe: Weeks 1-3

Interventionpercentage of participants (Number)
Sequence A91.30
Sequence B100

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Ondansetron Medication Compliance Weeks 4-6

Percentage of participants who adhered to ondansetron treatment for more than 21 days during weeks 4-6. (NCT02991456)
Timeframe: Weeks 4-6

Interventionpercentage of participants (Number)
Sequence A95
Sequence B95.24

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Week 3 Patient Satisfaction: Convenience

Mean convenience scores at week 3 using the 9-item Treatment Satisfaction Questionnaire for Medication (TSQM-9) patient satisfaction survey. The convenience subscale score was computed from the 3 items corresponding to convenience. The resulting convenience score is measured from 0-100 with higher scores corresponding to higher convenience. (NCT02991456)
Timeframe: Weeks 1-3

Interventionscore on a scale (Mean)
Sequence A85.71
Sequence B94.15

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Week 3 Patient Satisfaction: Effectiveness

Mean effectiveness scores at week 3 using the 9-item Treatment Satisfaction Questionnaire for Medication (TSQM-9) patient satisfaction survey. The effectiveness subscale score was computed from the 3 items corresponding to effectiveness. The resulting effectiveness score is measured from 0-100 with higher scores corresponding to higher effectiveness. (NCT02991456)
Timeframe: Weeks 1-3

Interventionscore on a scale (Mean)
Sequence A83.60
Sequence B94.44

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Week 3 Patient Satisfaction: Overall Satisfaction

Mean overall satisfaction scores at week 3 using the 9-item Treatment Satisfaction Questionnaire for Medication (TSQM-9) patient satisfaction survey. The overall satisfaction subscale score was computed from the 3 items corresponding to overall satisfaction. The resulting overall satisfaction score is measured from 0-100 with higher scores corresponding to higher overall satisfaction. (NCT02991456)
Timeframe: Weeks 1-3

Interventionscore on a scale (Mean)
Sequence A81.88
Sequence B90.94

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Week 6 Patient Satisfaction: Convenience

Mean convenience scores at week 6 using the 9-item Treatment Satisfaction Questionnaire for Medication (TSQM-9) patient satisfaction survey. The convenience subscale score was computed from the 3 items corresponding to convenience. The resulting convenience score is measured from 0-100 with higher scores corresponding to higher convenience. (NCT02991456)
Timeframe: Weeks 4-6

Interventionscore on a scale (Mean)
Sequence A86.11
Sequence B91.98

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Week 6 Patient Satisfaction: Effectiveness

Mean effectiveness scores at week 6 using the 9-item Treatment Satisfaction Questionnaire for Medication (TSQM-9) patient satisfaction survey. The effectiveness subscale score was computed by summing the 3 items corresponding to effectiveness. The resulting effectiveness score is measured from 0-100 with higher scores corresponding to higher effectiveness. (NCT02991456)
Timeframe: Weeks 4-6

Interventionscore on a scale (Mean)
Sequence A83.89
Sequence B88.27

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Week 6 Patient Satisfaction: Overall Satisfaction

Mean overall satisfaction scores at week 6 using the 9-item Treatment Satisfaction Questionnaire for Medication (TSQM-9) patient satisfaction survey. The overall satisfaction subscale score was computed from the 3 items corresponding to overall satisfaction. The resulting overall satisfaction score is measured from 0-100 with higher scores corresponding to higher overall satisfaction. (NCT02991456)
Timeframe: Weeks 4-6

Interventionscore on a scale (Mean)
Sequence A81.39
Sequence B88.58

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