Delving into the Latest Updates on Fospropofol Disodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Fospropofol, Fospropofol disodium (USAN), 磷丙泊酚

+ [9]

Target

GABAA receptor

Action

agonists

Mechanism

GABAA receptor agonists(Gamma-aminobutyric acid A receptor agonists)

Therapeutic Areas

Other Diseases

Active Indication

AnesthesiaSedation

Inactive Indication

AnalgesiaAnxiety DisordersCarpal Tunnel Syndrome+ [3]

Originator Organization

Eisai Co., Ltd.

Active Organization

Yichang Humanwell Pharmaceuticals Co., Ltd.

Inactive Organization

West China Hospital

Eisai, Inc.

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (08 Dec 2008),

Anesthesia

RegulationSpecial Review Project (China)

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Structure/Sequence

Molecular FormulaC13H21O5P

InChIKeyQVNNONOFASOXQV-UHFFFAOYSA-N

CAS Registry258516-89-1

View All Structures (2)

This is a study on the efficacy and safety of fospropofol disodium for injection in painless endoscopic diagnosis and treatment, project No.2024-YCRF-M1021, which will take more than 2 years to complete.
This is a multicenter, randomized, double-blind, controlled clinical study. Using a computer-generated randomized number table, the patients were divided into two groups: the group L (fospropofol disodium group) and the group B (propofol group). After determining the group of enrolled patients, the drug was administered by two fixed anesthesiologists By participating in this study, it is possible to make your anesthesia induction stable, stable intraoperative circulation, awake and safe and comfortable, to reduce the incidence of intraoperative hypoxemia, intraoperative awareness, cardiovascular and cerebrovascular malignant events (malignant arrhythmia, cardiac arrest), which is conducive to your rapid postoperative recovery and reduce hospitalization costs.

Start Date01 Mar 2025

Sponsor / Collaborator

Affiliated Hospital of Nantong University

100 Clinical Results associated with Fospropofol Disodium

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100 Translational Medicine associated with Fospropofol Disodium

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100 Patents (Medical) associated with Fospropofol Disodium

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142

Literatures (Medical) associated with Fospropofol Disodium

01 Nov 2024·Journal of Computational Biophysics and Chemistry

Molecular Docking, Quantum Mechanics and Molecular Dynamics Simulation of Anti-CAD Drugs Against High-Risk Xanthine Dehydrogenase Variants Associated with Oxidative Stress Pathways

Author: Ahmed, Shiek S. S. J. ; Ahmad, Sheikh F. ; Emran, Talha Bin ; Janakiraman, V. ; Attia, Sabry M. ; Sudhan, M.

Xanthine dehydrogenase (XDH) contributes significantly to generating reactive oxygen species in coronary artery disease (CAD). XDH has been proposed as a therapeutic target, but its genetic variants could affect protein structure and drug response. We aimed to assess protein structure modification occur due to genetic variants and to screen 215 CAD drugs for their utility in personalized CAD treatment against the XDH variants. A series of computational methods were implemented to identify pathogenic variants that cause XDH structure instability localized at the con served regions contributing to functional significance. Then, the XDH structures with the pathogenic variants were modeled using two different approaches to select the best models for docking with the CAD drugs. Finally, the stability of the docked complexes and their ability to transfer electrons were evaluated using molecular dynamics (MD) simulations and quantum mechanics/molecular mechanics (QM/MM) calculation. Among 751 variants examined; R149C and Q919R showed high pathogenicity, localized in conserved regions could alter protein structure and function. Further, docking of CAD drugs against XDH (native, R149C and Q919R) showed vericiguat with higher affinity, ranging from −7.95 kcal/mol to −10.41 kcal/mol, than the well-known XDH inhibitor (febuxostat, −5.73 kcal/mol to −8.35 kcal/mol). This indicates that vericiguat will be effective in CAD treatment, regardless of the XDH variants. Additionally, MD simulation and QM/MM confirmed vericiguat stability and electron transfer ability to form hydrogen bonds with the XDH protein. In conclusion, vericiguat will be beneficial for the personalized treatment of CAD by inhibiting XDH variants. Additional clinical studies are necessary to confirm our findings.

01 Aug 2024·Journal of Clinical Anesthesia

Fospropofol disodium versus propofol for long-term sedation during invasive mechanical ventilation: A pilot randomized clinical trial

Article

Author: Qi, Hong ; Fang, Xiangzhi ; Gao, Xuehui ; Shang, You ; Tang, Yun ; Shu, Huaqing ; Yuan, Yin ; Yang, Xiaobo ; Li, Ruiting ; Zou, Xiaojing

STUDY OBJECTIVEFospropofol disodium is a propofol prodrug that is water-soluble and has a reduced risk of bacterial contamination and hypertriglyceridemia compared with propofol. Prior to implementing a large randomized trial, we investigated the feasibility, initial efficacy, and safety of fospropofol disodium compared with propofol in long-term mild-to-moderate sedation in intensive care units (ICUs).DESIGNSingle-centered, prospective, unblind, randomized, parallel-group clinical trial.SETTINGThe general ICU of university-affiliated teaching hospital.PATIENTSAdult patients (n = 60) expected to have mechanical ventilation for >24 h were enrolled and randomly assigned to the fospropofol or propofol group.INTERVENTIONSThe fospropofol group received continuous fospropofol disodium infusions and the propofol group received continuous propofol infusions. The sedation goal was a score of -3 to 0 on the Richmond Agitation and Sedation Scale (RASS).MEASUREMENTSThe primary outcome was the percentage of time spent in the target sedation range without rescue sedation. Safety outcomes were based on adverse events. Blood samples were collected to measure formate concentration in plasma.MAIN RESULTSThe median dose was 4.33 (IQR, 3.08-4.94) mg/kg/h in the fospropofol group and 1.96 (IQR, 1.44-2.94) mg/kg/h in the propofol group. The median percentage of time spent in the target RASS range without rescue sedation was identical in both groups, with 83.33% (IQR, 74.43%-100.00%) in the fospropofol group and 83.33% (IQR, 77.45%-100.00%) in the propofol group (p = 0.887). At least one adverse event was identifed in 23 (76.7%) fospropofol patients and 27 (90.0%) propofol patients. The most common adverse events were tachycardia and hypotension. No paresthesia, catheter-related bloodstream infection or propofol infusion syndrome in both groups was reported. Three patients in the fospropofol group had mild hypertriglyceridemia, and nine patients in propofol group had hypertriglyceridemia (mild in eight patients and moderate in one patient) (10% versus 30%, p = 0.104). The formate concentration in plasma was very low, and no significant difference was identified at any time point between the two groups.CONCLUSIONSFospropofol disodium appears to be a feasible, effective and safe sedative for patients receiving invasive mechanical ventilation with long-term sedation.

08 May 2024·Science Translational Medicine

MRGPRX4 mediates phospho-drug–associated pruritus in a humanized mouse model

Article

Author: Peng, Qi ; Chien, Daphne Chun-Che ; Limjunyawong, Nathachit ; Dong, Xinzhong ; Meixiong, James ; Fay, Jonathan F ; Ho, Cheng-Ying ; Roth, Bryan L ; Cao, Can

The phosphate modification of drugs is a common chemical strategy to increase solubility and allow for parenteral administration. Unfortunately, phosphate modifications often elicit treatment- or dose-limiting pruritus through an unknown mechanism. Using unbiased high-throughput drug screens, we identified the Mas-related G protein–coupled receptor X4 (MRGPRX4), a primate-specific, sensory neuron receptor previously implicated in itch, as a potential target for phosphate-modified compounds. Using both G q -mediated calcium mobilization and G protein–independent GPCR assays, we found that phosphate-modified compounds potently activate MRGPRX4. Furthermore, a humanized mouse model expressing MRGPRX4 in sensory neurons exhibited robust phosphomonoester prodrug–evoked itch. To characterize and confirm this interaction, we further determined the structure of MRGPRX4 in complex with a phosphate-modified drug through single-particle cryo–electron microscopy (cryo-EM) and identified critical amino acid residues responsible for the binding of the phosphate group. Together, these findings explain how phosphorylated drugs can elicit treatment-limiting itch and identify MRGPRX4 as a potential therapeutic target to suppress itch and to guide future drug design.

100 Deals associated with Fospropofol Disodium

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External Link

KEGG	Wiki	ATC	Drug Bank
D04257	Fospropofol Disodium	N01AX10	DB06716

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Anesthesia	China	Yichang Humanwell Pharmaceuticals Co., Ltd.	19 May 2021

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Carpal Tunnel Syndrome	Phase 1	-	Eisai, Inc.	01 Oct 2004
Analgesia	Phase 1	-	Eisai, Inc.	01 Sep 2004
Anxiety Disorders	Phase 1	-	Eisai, Inc.	01 Sep 2004
Sedation	Phase 1	-	Eisai, Inc.	01 Sep 2004
Anesthesia	Preclinical	United States	Eisai, Inc.	08 Dec 2008
Consciousness	Preclinical	United States	Eisai, Inc.	01 Mar 2006
Colonic Polyps	Preclinical	-	Eisai, Inc.	01 Sep 2004
Sedation	Preclinical	-	Eisai, Inc.	01 Sep 2004
Coronary Artery Disease	Preclinical	-	Eisai, Inc.	01 Feb 2004

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01260142 (CTgov)	Phase 4	Anesthesia	36	Fospropofol (Fospropofol 6.5 mg/kg)	fcbssfgjcl(qstzygmeoi) = bgxzlwrstn ytgjraoniy (mqllyqjdki, bfczafydpc - wqinnqophx) View more	-	27 Jan 2017
				Fospropofol (Fospropofol 10 mg/kg)	fcbssfgjcl(qstzygmeoi) = xybrogxegp ytgjraoniy (mqllyqjdki, fetrdaxxde - eusjlurqdw) View more
NCT01401049 (CTgov)	Phase 4	Pain \| Complication of injection	116	Fospropofol (Fospropofol)	kffgvjjaxo(rayhqzrsvu) = lmupxnjqwc ubwvbmezpm (pthorvyfwy, idtbhxwcbi - ozlizonacr) View more	-	26 Jan 2015
				Propofol+Lidocaine (Propofol/Lidocaine)	kffgvjjaxo(rayhqzrsvu) = wbpnylkeus ubwvbmezpm (pthorvyfwy, qualfryrnb - iwbieefxly) View more
NCT01195103 (CTgov)	Phase 4	Sedation \| Anesthesia	13	Fentanyl+Fospropofol disodium (10 mg/kg Lusedra)	pzyadtxdmp(pybwcixymf) = zlldeafsxu cymnrbqgwa (onygrkauzr, encabsjaqi - qwfyuuwwir) View more	-	29 Mar 2012
				Fentanyl+Fospropofol disodium (6.5 mg/kg Lusedra)	pzyadtxdmp(pybwcixymf) = szawtrwndl cymnrbqgwa (onygrkauzr, cljmazselj - wpnagoqqic) View more
NCT00306722 (Pubmed \| Chest)	Phase 3	Sedation	252	Fospropofol 2 mg/kg	kgxpwtactc(kzdebrranc) = huxcorbhsc miauecvrck (panrplraiq ) View more	-	01 Jan 2009
				Fospropofol 6.5 mg/kg	kgxpwtactc(kzdebrranc) = epaxvwviem miauecvrck (panrplraiq ) View more