"Casopitant"

Randomized phase II trial of the neurokinin-1 receptor antagonist (NK-1 RA) casopitant mesylate with ondansetron (ond)/dexamethasone (dex) for chemotherapy-induced nausea/vomiting (CINV) in patients (pts) receiving highly emetogenic chemotherapy (HEC).

Phase III study of single-dose casopitant in combination with ondansetron and dexamethasone for the prevention of oxaliplatin-induced nausea and vomiting.

A pharmacokinetic, pharmacodynamic, and safety study of intravenous cyclophosphamide with an oral casopitant antiemetic regimen in cancer patients. Casopitant is a potent and selective neurokinin-1 receptor antagonist formerly under development for a number of indications, including the treatment of chemotherapy-induced nausea and vomiting. This study was an open-label, randomized, multi-center , two-period crossover casopitant-cyclophosphamide interaction study. Subjects were cancer patients receiving cyclophosphamide based chemotherapy. The objectives of the study were to assess the effect of 3-day, repeat-dose, 150 mg oral casopitant on the pharmacokinetics (PK), safety, tolerability, and pharmacodynamics (white blood cell count) of single-dose IV cyclophosphamide. PK data from 14

* or antimetic* or "anti-metic*" or antinausea* or "anti-nausea*" or C-4 antivomit* or "anti-vomit*" or Aprepitant or azasetron or batanopride or belidral or bendectin or benzquinamide or bromopride or buclizine or casopitant or chlorcyclizine or chlorphenethazine or Chlorpromazine or cinnarizine or cisapride or clebopride or Cyclizine or dazopride or debendox or Dexamethasone or Diazepam or difenidol

Single-dose intravenous casopitant in combination with ondansetron and dexamethasone for the prevention of oxaliplatin-induced nausea and vomiting: a multicenter, randomized, double-blind, active-controlled, two arm, parallel group study. The primary objective was to determine if a single dose of casopitant 90 mg added to ondansetron and dexamethasone would improve the control of chemotherapy -induced nausea and vomiting (CINV) over 0-120 h following initiation of oxaliplatin-based moderately emetic chemotherapy (MEC) compared to ondansetron and dexamethasone alone. Patients with colorectal cancer received either casopitant or placebo intravenously (IV) added to ondansetron 8 mg bid oral on study days 1 to 3 and one dose of dexamethasone 8 mg IV given prior to starting the oxaliplatin on day

Casopitant and ondansetron for postoperative nausea and vomiting prevention in women at high risk for emesis: a phase 3 study Postoperative nausea and vomiting (PONV) are associated with a variety of complications. Neurokinin subtype 1 receptor antagonists have antiemetic activity in the postoperative setting, and the neurokinin subtype 1 receptor antagonist casopitant mesylate (GW679769 ) was well tolerated and effective at reducing the incidence of PONV in phase 1 and phase 2 trials. A multicenter, randomized, double-blind, parallel-group, phase 3 analysis was designed to evaluate the safety and efficacy of casopitant in combination with a single intravenous dose of the serotonin subtype 3 receptor antagonist ondansetron hydrochloride for the prevention of PONV in the perioperative

and 3 is recom-mended [MASCC level of confidence: moderate; MASCC levelof consensus: moderate; ESMO level of evidence II; ESMOgrade of recommendation: B].oxaliplatinThefirst double-blind trial to evaluate the role of an NK1RA foroxaliplatin was carried out in 710 colorectal cancer patients re-ceiving casopitant or placebo [33]. Casopitant 90 mg i.v. on day1 or placebo were administered in combination with ondanse-tron 8 mg bid oral on days 1–3 and dexamethasone 8 mg i.v. onday 1. The incidence of vomiting on days 1–5 was low in botharms (11% and 10% in the placebo and casopitant arms, respect-ively) with the vast majority of emesis occurring in the delayedphase. Both groups received ondansetron on days 2–3 whichmay have increased the control of delayed emesis.A different conclusion about the value

. ..

doses of 1st 5HT3 RA, given from the second day onwards; and palonosetron. For neurokinin-1 receptor antagonist (NK1 RA), including aprepitant, fosaprepitant, casopitant, rolapitant, netupitant, and fosnetupitant, we treated all as equivalent. We included all randomized controlled trials (RCTs) that compared the intervention of interest, mandatorily including at least DEX and a 5HT RA. Different

but not limited too Antihistamineo Antidepressants Neurokinins (NK1, NK2 and NK3) receptor inhibitors, e.g., aprepitant, rolapitant, casopitant, etc. Serotonin selective reuptake inhibitors (SSRIs) Serotonin-nonepinephrine receptor inhibitors (SNRIs) Any othersII. Non-pharmacological interventionsIncluding but not limited to –• Cognitive behavioural therapy (CBT)• Mindfulness• Complementary and alternative , including but not limited too Antihistamineo Antidepressants Neurokinins (NK1, NK2 and NK3) receptor inhibitors, e.g., aprepitant, rolapitant, casopitant, etc. Serotonin selective reuptake inhibitors (SSRIs) Serotonin-norepinephrine receptor inhibitors (SNRIs) Any othersii. Non-pharmacological interventionsIncluding but not limited to –• Cognitive behavioural therapy (CBT)• Mindfulness• Complementary

” or “Haloperidol” or “Perphenazine” or “Scopolamine” or “Aprepitant” or “Olanzapine” or “Chlorpromazine” or “Cyclizine” or “Prochloperazine” or “Trimeprazine” or “Betamethasone” or “Prednisolone” or “Dexamethasone” or “Methylprednisolone” or “Sulpiride” or “Alizapride” or “Bromopride” or “Transdermal Scopolamine” or “Trimethobenzamide” or “Fosaprepitant” or “Netupitant” or “Vestipitant” or “Casopitant ” or “Chlorpromazine” or “Cyclizine” or “Prochloperazine” or “Trimeprazine” or “Betamethasone” or “Prednisolone” or “Dexamethasone” or “Methylprednisolone” or “Sulpiride” or “Alizapride” or “Bromopride” or “Transdermal Scopolamine” or “Trimethobenzamide” or “Fosaprepitant” or “Netupitant” or “Vestipitant” or “Casopitant” or “Rolapitant" or “Dolasetron” or “ramosetron” or “Tiapride” or “Meclozine”）Main outcome(s

neurokinin 1 (NK1) receptor antagonists were taken into human and both were tested as antidepressants and for insomnia. Vestipitant and Casopitant both have high affinity for the human NK1 receptor (pKi = 9.4 and 10.2, respectively). In human, at the chosen clinical doses, receptor occupancy was measured in the frontal cortex, at 24 hours post administration, as ∼90% for vestipitant (15 mg) and ∼100 % for casopitant (30 mg). In patients with moderate to severe major depression, vestipitant given at 15 mg for 8 weeks showed no statistical significant benefit as measured by change in baseline in HAM-D total score; whereas casopitant at 80 mg achieved statistically significant improvement versus placebo at week 8 (LOCF HAMD17 = -2.7, p = 0.023). A lower dose of 30 mg showed a clear but not significant

following different doses of casopitant, a selective NK(1) antagonist. Two PET scans were carried out in each of eight human subjects, with the PET radioligand [(11)C]GR205171, a high-affinity and selective NK(1) receptor antagonist. The first scan was under baseline conditions and the second 24 h after a single oral dose of casopitant (2-120 mg). Arterial blood was collected throughout the scans for determination of plasma and whole blood input functions. Venous blood samples were taken prior to and following oral dosing up to 24 h for a pharmacokinetic study of casopitant concentration in plasma. It was first necessary to establish a suitable kinetic model for the estimation of [(11)C]GR205171 NK(1) receptor binding parameters in human brain tissue. A three-tissue compartment model with simultaneous

Phase II study to evaluate the safety and efficacy of the oral neurokinin-1 receptor antagonist casopitant (GW679769) administered with ondansetron for the prevention of postoperative and postdischarge nausea and vomiting in high-risk patients In recent years, there has been an increased interest in using a multimodal approach with combined agents to treat postoperative nausea and vomiting . This study evaluated whether the addition of an oral dose of the neurokinin-1 receptor antagonist casopitant improved the antiemetic efficacy of an intravenous dose of ondansetron hydrochloride. The authors enrolled 702 premenopausal or perimenopausal, nonsmoking, female patients aged 18-55 yr with a history of postoperative nausea and vomiting and/or motion sickness undergoing a laparoscopic