Delving into the Latest Updates on ABP-700 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

CPMM, Cyclopropyl-methoxycarbonyl metomidate

+ [1]

Target

GABAA receptor

Mechanism

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

Therapeutic Areas

Other Diseases

Active Indication

AnesthesiaSedation

Inactive Indication-

Originator Organization

The Medicines Company (Spain) SL

Active Organization

The Medicines Co.

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

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Structure

Molecular FormulaC17H18N2O4

InChIKeyDRAFVCKNYNQOKR-GFCCVEGCSA-N

CAS Registry1446482-29-6

This is a phase II, two-part, multiple-dose, dose-finding, single-blind study in adult participants undergoing elective colonoscopy for screening or diagnostic purposes. This study is designed to test various ABP-700 infusion regimens for rational selection of one or more dosage regimen(s) to be used for future clinical development of ABP-700 in procedural sedation.

Start Date01 May 2016

Sponsor / Collaborator

The Medicines Co.

NTR5832 / SuspendedNot ApplicableIIT

A phase II, randomized, single-blind study to investigate the safety and efficacy of 3 dosing regimens of ABP-700 for procedural sedation in adult patients undergoing colonoscopy.

Start Date25 Apr 2016

Sponsor / Collaborator-

NTR5442 / RecruitingNot Applicable

A Phase 1, Single-Center, Open-Label, Induction Dose Study of ABP-700 in Healthy, Adult Subjects

Start Date09 Nov 2015

Sponsor / Collaborator

The Medicines Co.

100 Clinical Results associated with ABP-700

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100 Translational Medicine associated with ABP-700

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100 Patents (Medical) associated with ABP-700

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8

Literatures (Medical) associated with ABP-700

01 Oct 2021·Clinical PharmacokineticsQ2 · MEDICINE

Etomidate and its Analogs: A Review of Pharmacokinetics and Pharmacodynamics

Q2 · MEDICINE

Review

Author: Struys, Michel M R F ; Valk, Beatrijs I

Etomidate is a hypnotic agent that is used for the induction of anesthesia. It produces its effect by acting as a positive allosteric modulator on the γ-aminobutyric acid type A receptor and thus enhancing the effect of the inhibitory neurotransmitter γ-aminobutyric acid. Etomidate stands out among other anesthetic agents by having a remarkably stable cardiorespiratory profile, producing no cardiovascular or respiratory depression. However, etomidate suppresses the adrenocortical axis by the inhibition of the enzyme 11β-hydroxylase. This makes the drug unsuitable for administration by a prolonged infusion. It also makes the drug unsuitable for administration to critically ill patients. Etomidate has relatively large volumes of distributions and is rapidly metabolized by hepatic esterases into an inactive carboxylic acid through hydrolyzation. Because of the decrease in popularity of etomidate, few modern extensive pharmacokinetic or pharmacodynamic studies exist. Over the last decade, several analogs of etomidate have been developed, with the aim of retaining its stable cardiorespiratory profile, whilst eliminating its suppressive effect on the adrenocortical axis. One of these molecules, ABP-700, was studied in extensive phase I clinical trials. These found that ABP-700 is characterized by small volumes of distribution and rapid clearance. ABP-700 is metabolized similarly to etomidate, by hydrolyzation into an inactive carboxylic acid. Furthermore, ABP-700 showed a rapid onset and offset of clinical effect. One side effect observed with both etomidate and ABP-700 is the occurrence of involuntary muscle movements. The origin of these movements is unclear and warrants further research.

01 Jan 2021·AnesthesiologyQ1 · MEDICINE

Modeling the Effect of Excitation on Depth of Anesthesia Monitoring in γ-Aminobutyric Acid Type A Receptor Agonist ABP-700: Erratum

Q1 · MEDICINE

Article

Author: I den Daas ; A. R. Absalom ; P. Meyer ; J. A. Campagna ; S. Meier ; Michel Struys ; S. P. Sweeney ; D. J. Eleveld ; K. van Amsterdam ; Valk, B., I

01 Jan 2021·AnesthesiologyQ1 · MEDICINE

Modeling the Effect of Excitation on Depth of Anesthesia Monitoring in γ-Aminobutyric Acid Type A Receptor Agonist ABP-700

Q1 · MEDICINE

Article

Author: Campagna, Jason A. ; Meier, Sascha ; Struys, Michel M. R. F. ; van Amsterdam, Kai ; Sweeney, Steven P. ; Meyer, Peter ; den Daas, Izaak ; Valk, Beatrijs I. ; Absalom, Anthony R. ; Eleveld, Douglas J.

Backgroundγ-Aminobutyric acid type A (GABAA) receptor agonists are known to cause involuntary muscle movements. The mechanism of these movements is not known, and its relationship to depth of anesthesia monitoring is unclear. We have explored the effect of involuntary muscle movement on the pharmacokinetic-pharmacodynamic model for the GABAA receptor agonist ABP-700 and its effects on the Bispectral Index (BIS) as well as the Modified Observer’s Assessment of Alertness/Sedation (MOAA/S) scores.MethodsObservations from 350 individuals (220 men, 130 women) were analyzed, comprising 6,312 ABP-700 concentrations, 5,658 ABP-700 metabolite (CPM-acid) concentrations, 25,745 filtered BIS values, and 6,249 MOAA/S scores, and a recirculatory model developed. Various subject covariates and pretreatment with an opioid or a benzodiazepine were explored as covariates. Relationships between BIS and MOAA/S models and involuntary muscle movements were examined.ResultsThe final model shows that the pharmacokinetics of ABP-700 are characterized by small compartmental volumes and rapid clearance. The BIS model incorporates an effect-site for BIS suppression and a secondary excitatory/disinhibitory effect-site associated with a risk of involuntary muscle movements. The secondary effect-site has a threshold that decreases with age. The MOAA/S model did not show excitatory effects.ConclusionsThe GABAA receptor agonist ABP-700 shows the expected suppressive effects for BIS and MOAA/S, but also disinhibitory effects for BIS associated with involuntary muscle movements and reduced by pretreatment. Our model provides information about involuntary muscle movements that may be useful to improve depth of anesthesia monitoring for GABAA receptor agonists.Editor’s PerspectiveWhat We Already Know about This TopicWhat This Article Tells Us That Is New

100 Deals associated with ABP-700

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