Delving into the Latest Updates on Casopitant Mesylate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Casopitant, Casopitant mesylate (USAN), Rezonic

+ [4]

Target

NK1R

Mechanism

NK1R antagonists(Neurokinin 1 receptor antagonists)

Therapeutic Areas

Other DiseasesNeoplasmsNervous System Diseases+ [2]

Active Indication-

Inactive Indication

Chemotherapy-induced nausea and vomitingDepressive Disorder, MajorDyspepsia+ [12]

Originator Organization

GSK Plc

Active Organization-

Inactive Organization

GSK Plc

Drug Highest PhaseDiscontinuedNDA/BLA

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC31H39F7N4O5S

InChIKeyYRFKYVWDPCOSTE-REWBLLDVSA-N

CAS Registry414910-30-8

View All Structures (2)

This is a phase III study designed to demonstrate the superiority of single-dose 90 mg intravenous (IV) casopitant over placebo, each in combination with ondansetron and dexamethasone, for the prevention of emesis over the first 0-120 hours (overall phase) following initiation of the cisplatin infusion in the first cycle of highly emetogenic chemotherapy (HEC). Eligibility is limited to subjects who are scheduled to receive their first cycle of chemotherapy which includes at least 60 mg/m2 of cisplatin administered on Day 1 only of a 21 day or 28 day cycle. All subjects will receive IV ondansetron and oral dexamethasone on Day 1 prior to initiation of the cisplatin infusion, followed by oral dexamethasone on Days 2-4. Additionally, subjects will be randomized to receive single-dose 90 mg IV casopitant or matching placebo prior to initiation of a cisplatin-based HEC regimen.

Start Date01 Sep 2009

Sponsor / Collaborator

GSK Plc

NCT00601172

/ CompletedPhase 3

A Study of Single Dose Intravenous Casopitant in Combination With Ondansetron and Dexamethasone for the Prevention of Oxaliplatin Induced Nausea and Vomiting.

This a Phase III trial designed to determine if IV casopitant plus dexamethasone and ondansetron is more effective in the prevention of vomiting and nausea then dexamethasone and ondansetrone alone following the administration of moderately emetogenic oxaliplatin-based chemotherapy.

Start Date10 Mar 2008

Sponsor / Collaborator

GSK Plc

EUCTR2007-005169-36-BE

/ Not yet recruitingNot Applicable

NKV110721, A Study of Single Dose Intravenous Casopitant in Combination with Ondansetron and Dexamethasone for the Prevention of Oxaliplatin-Induced Nausea and Vomiting

Start Date07 Feb 2008

Sponsor / Collaborator

GlaxoSmithKline Research & Development Ltd.

100 Clinical Results associated with Casopitant Mesylate

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100 Translational Medicine associated with Casopitant Mesylate

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100 Patents (Medical) associated with Casopitant Mesylate

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56

Literatures (Medical) associated with Casopitant Mesylate

01 Dec 2024·Journal of PeriAnesthesia Nursing

Pharmacological Strategies for Postdischarge Nausea and Vomiting: Evidence-based Review Update

Review

Author: Kane, Terri D ; Tubog, Tito D

PURPOSEEvaluate the effectiveness of various drugs in preventing postdischarge nausea and vomiting (PDNV).DESIGNSystematic review.METHODSA search for evidence was conducted in PubMed, CINAHL, Cochrane Collaboration, and Google Scholar and gray literature. Only randomized controlled trials examining a pharmacological agent to prevent PDNV were included in the study. The quality appraisal of the literature was conducted using the proposed algorithm described in the Johns Hopkins Nursing Evidence-Based Practice Evidence Level and Quality Guide.FINDINGSA total of 8 randomized controlled trials involving 1,441 patients were analyzed. The efficacy of pharmacological agents, including dexamethasone, olanzapine, ondansetron, palonosetron, ramosetron, promethazine, and casopitant in the prevention of PDNV, varied. Additionally, a combination of two or more drugs is a more effective therapy than using a single drug in mitigating PDNV. The review also underscored the individual patient factors that can play a significant role in identifying appropriate prevention and treatment modalities.CONCLUSIONSThere is limited evidence on the efficacy of pharmacological agents in preventing PDNV. The scarcity of large-scale, clinical trials specifically focusing on PDNV restricts the ability to recommend prophylactic drug therapy for reducing its incidence.

01 Feb 2024·Biotechnology and Applied Biochemistry

Homology modeling, virtual screening, molecular docking, and ADME approaches to identify a potent agent targeting NK2R protein

Article

Author: Soltani, Arash ; Hashemy, Seyed Isaac

AbstractNeurokinin/tachykinin receptors are classified as the G‐protein coupled receptor superfamily. The neurokinin 2 receptor (NK2R) is widely expressed in different tissues. NK2R is associated with a range of biological events, such as inflammation, smooth muscle contraction, intestinal motor functions, and asthma. Despite these diverse activities, no approved drugs targeting NK2R have been developed yet. Our study focuses on finding potential inhibitors for NK2R using virtual screening, molecular docking, and ADME (absorption, distribution, metabolism, and excretion) approaches. We used a homology modeling approach and AlphaFold DB to obtain the three‐dimensional structure of mouse and human NK2R proteins, respectively. The homology model of NK2R was predicted using MODELLER v10.3 and further refined and validated using the 3Drefine tool and RAMPAGE server, respectively. Molecular docking was performed using a library of 910 structurally similar molecules to four NK1R antagonists: aprepitant, casopitant, fosaprepitant, and rolapitant. Molecular docking revealed six small molecules that displayed high Chemscore fitness scores, and binding energies with desirable ligand–NK2R interactions. The evaluation of the in silico ADME profile, solubility, and permeability of the ligand molecules has revealed that the small molecules are potentially nontoxic and have the chance of exhibiting biological activity after oral administration. Further experimental studies (in vitro and in vivo assays) are required to evaluate the effectiveness of these inhibitors as therapeutic targets.

01 Jul 2022·Pharmacopsychiatry

Novel Antidepressants in the Pipeline (Phase II and III): A Systematic Review of the US Clinical Trials Registry

Review

Author: Tani, Hideaki ; Sakurai, Hitoshi ; Yonezawa, Kengo ; Uchida, Hiroyuki ; Bauer, Michael ; Mimura, Masaru

Abstract Introduction There is an imminent need for faster-acting and more effective antidepressants beyond the monoaminergic hypothesis. Methods We systematically searched the US Clinical Trials registry for antidepressant compounds with completed phase II and III trials. Compounds that demonstrated significant superiority over placebo in the primary outcome measure in the latest phase of phase II and III trials were identified. The collateral information was gathered via a PubMed search and press releases. Results Nine compounds were identified. AXS-05 (a combination of dextromethorphan and bupropion) and ansofaxine hydrochloride showed a positive result over placebo in a phase III study for major depressive disorder or treatment-resistant depression. MIJ821, nitrous oxide, psilocybin, ayahuasca, facial injection of botulinum toxin A, prasterone, and casopitant demonstrated at least one positive result in phase II trials. Ayahuasca showed a greater response rate than placebo at week one, indicating the rapid antidepressant effect. Discussion These new compounds with novel mechanisms of action are expected to provide a greater variety of treatment options for depression if preliminary positive results are confirmed.

100 Deals associated with Casopitant Mesylate

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External Link

KEGG	Wiki	ATC	Drug Bank
D06574	Casopitant Mesylate	-	DB06634

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Vomiting	NDA/BLA	BE	GSK Plc	01 Mar 2006
Vomiting	NDA/BLA	BE	GSK Plc	01 Mar 2006
Vomiting	NDA/BLA	PK	GSK Plc	01 Mar 2006
Vomiting	NDA/BLA	PK	GSK Plc	01 Mar 2006
Chemotherapy-induced nausea and vomiting	NDA/BLA	US	GSK Plc	-
Chemotherapy-induced nausea and vomiting	NDA/BLA	US	GSK Plc	-
Chemotherapy-induced nausea and vomiting	NDA/BLA	EU	GSK Plc	-
Chemotherapy-induced nausea and vomiting	NDA/BLA	EU	GSK Plc	-
Postoperative Nausea and Vomiting	NDA/BLA	EU	GSK Plc	-
Postoperative Nausea and Vomiting	NDA/BLA	EU	GSK Plc	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00601172 (CTgov)	Phase 3	Nausea \| Chemotherapy-induced nausea and vomiting \| Vomiting	710	placebo+casopitant+Ondansetron+dexamethasone (Placebo)	csjkekwzjs(uzdjqczoob) = vbplmrqipp khgkfzpbsa (idkzaynjly, apkwufbkud - suerronorc) View more	-	17 Jan 2018
				Casopitant (Casopitant 90 mg)	csjkekwzjs(uzdjqczoob) = revxffvzai khgkfzpbsa (idkzaynjly, auaypdyzlp - oamdtmbnph) View more
ASCO2011	Phase 3	Drug-induced nausea and vomiting	710	Casopitant 90 mg	(zpdixtsntf) = rhaugkpxec jglqxwqlhd (fhkcvfpzfn )	-	20 May 2011
				Placebo	(zpdixtsntf) = ynhcvtbunq jglqxwqlhd (fhkcvfpzfn )
NCT00326248 (Pubmed)	Phase 3	Postoperative Nausea and Vomiting	484	Casopitant	(mbxufbzpcr) = vvpiemhzli nqnqxgbpjj (zbqwhutqyi ) View more	Positive	01 Feb 2011
				Ondansetron	(mbxufbzpcr) = dnrfwdkzep nqnqxgbpjj (zbqwhutqyi ) View more
NCT00104403 (Pubmed \| Cancer)	Phase 2	Neoplasms	723	Casopitant 50 mg	(izfntdsold) = rdseryswwx rsxeadphbt (qilzetjjdx ) View more	Positive	15 Dec 2009
				Casopitant 100 mg	(izfntdsold) = dqmcqzgtfz rsxeadphbt (qilzetjjdx ) View more
Pubmed \| J Clin Oncol	Phase 3	Chemotherapy-induced nausea and vomiting	-	Control	(rtpqzibwlb) = syogtijdux gixtfazgay (nfdchxncsy )	Positive	10 Nov 2009
				Single-dose oral casopitant	(rtpqzibwlb) = ddwyktwppl gixtfazgay (nfdchxncsy )
ASCO2006	Phase 2	Chemotherapy-induced nausea and vomiting	493	Placebo control	fvhgnpdghj(sfcmfrkafx) = xlkgsottjn obqlsnoydn (cqoyrljzzf ) View more	-	20 Jun 2006
				Casopitant 50mg	fvhgnpdghj(sfcmfrkafx) = skbsymuswj obqlsnoydn (cqoyrljzzf ) View more
ASCO2006	Phase 2	Chemotherapy-induced nausea and vomiting	719	Casopitant mesylate 50mg	(eszmzbpdun) = jjsqdulrym qpqomtqsqm (glpenybpjl )	-	20 Jun 2006
				Casopitant mesylate 100mg	(eszmzbpdun) = mclkwqoofm qpqomtqsqm (glpenybpjl )