ID Source | ID |
---|---|
PubMed CID | 10311306 |
CHEMBL ID | 3707331 |
CHEBI ID | 90908 |
SCHEMBL ID | 354305 |
MeSH ID | M0582062 |
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 |
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.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
Rolapitant was safe and well tolerated across all studies. The most frequently reported treatment-related treatment-emergent adverse events were fatigue, constipation, and headache.
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.
Excerpt | Reference | Relevance |
---|---|---|
" 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 |
Excerpt | Reference | Relevance |
---|---|---|
" 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 |
Role | Description |
---|---|
antiemetic | A 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 antagonist | An 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] |
Class | Description |
---|---|
ether | An organooxygen compound with formula ROR, where R is not hydrogen. |
azaspiro compound | An azaspiro compound is a spiro compound in which at least one of the cyclic components is a nitrogen heterocyle. |
pyrrolidin-2-ones | A pyrrolidinone in which the oxo group is at position 2 of the pyrrolidine ring. |
piperidines | |
organofluorine compound | An 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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
PPM1D protein | Homo sapiens (human) | Potency | 26.2123 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
Interferon beta | Homo sapiens (human) | Potency | 26.2123 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Substance-P receptor | Homo sapiens (human) | Ki | 0.0007 | 0.0000 | 0.7936 | 8.7470 | AID1340842 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
cytokine activity | Interferon beta | Homo sapiens (human) |
cytokine receptor binding | Interferon beta | Homo sapiens (human) |
type I interferon receptor binding | Interferon beta | Homo sapiens (human) |
protein binding | Interferon beta | Homo sapiens (human) |
chloramphenicol O-acetyltransferase activity | Interferon beta | Homo sapiens (human) |
tachykinin receptor activity | Substance-P receptor | Homo sapiens (human) |
protein binding | Substance-P receptor | Homo sapiens (human) |
substance P receptor activity | Substance-P receptor | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Process | via Protein(s) | Taxonomy |
---|---|---|
extracellular space | Interferon beta | Homo sapiens (human) |
extracellular region | Interferon beta | Homo sapiens (human) |
plasma membrane | Substance-P receptor | Homo sapiens (human) |
cell surface | Substance-P receptor | Homo sapiens (human) |
dendrite | Substance-P receptor | Homo sapiens (human) |
sperm flagellum | Substance-P receptor | Homo sapiens (human) |
cell body | Substance-P receptor | Homo sapiens (human) |
sperm head | Substance-P receptor | Homo sapiens (human) |
sperm midpiece | Substance-P receptor | Homo sapiens (human) |
plasma membrane | Substance-P receptor | Homo sapiens (human) |
sperm midpiece | Substance-P receptor | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1346346 | Human NK1 receptor (Tachykinin receptors) | 2012 | Pharmacology, 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. |
AID1347411 | qHTS 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) Libary | 2020 | ACS 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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 41 (89.13) | 24.3611 |
2020's | 5 (10.87) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (46.76) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 17 (33.33%) | 5.53% |
Reviews | 14 (27.45%) | 6.00% |
Case Studies | 1 (1.96%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 19 (37.25%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
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 2 | 619 participants (Actual) | Interventional | 2007-10-31 | Completed | ||
An Open-Label, Randomized, Pivotal, Bioequivalence Study of Oral and Intravenous Rolapitant [NCT02285647] | Phase 1 | 138 participants (Actual) | Interventional | 2014-09-30 | Completed | ||
Phase II Study of Rolapitant Plus Olanzapine, Palonosetron, and Dexamethasone in Patients With Germ Cell Tumors Undergoing 5-day Cisplatin-based Chemotherapy. [NCT03960151] | Phase 2 | 0 participants (Actual) | Interventional | 2018-05-31 | Withdrawn(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 2 | 35 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
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 2 | 48 participants (Actual) | Interventional | 2017-10-09 | Completed | ||
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 2 | 450 participants (Anticipated) | Interventional | 2006-09-30 | Completed | ||
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 3 | 532 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
A Phase 1, 2-Part, Single Ascending Dose Assessment of the Safety, Tolerability, and Pharmacokinetics of Rolapitant Intravenous in Healthy Volunteers [NCT02382666] | Phase 1 | 100 participants (Actual) | Interventional | 2015-01-31 | Completed | ||
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 1 | 102 participants (Actual) | Interventional | 2015-05-31 | Completed | ||
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 3 | 555 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
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 2 | 37 participants (Actual) | Interventional | 2016-10-12 | Terminated(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 3 | 1,369 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |