Delving into the Latest Updates on NXL-105 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

TOP

Action

inhibitors

Mechanism

TOP inhibitors(Topoisomerases inhibitors), Cell wall inhibitors

Therapeutic Areas

Infectious Diseases

Active Indication-

Inactive Indication

Gram-Negative Bacterial InfectionsGram-Positive Bacterial Infections

Originator Organization

Novexel SA

Active Organization-

Inactive Organization

Novexel SA

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC9H13N5O5S

InChIKeyRQBKZSHXCSVMSL-WZTWBHKBSA-N

CAS Registry1070773-80-6

View All Structures (2)

We investigated compounds related to the previously reported antistaphyloccocal agent AVE6971 in an effort to attenuate inhibition of hERG potassium channel current that has been noted for this and related antibacterial drug classes. While most modifications of the original thiophene group compromised antibacterial activity, one selenophene analogue displayed (i) improved activity against the primary target enzyme DNA gyrase, (ii) similar activities against a panel of MRSA clinical isolates, and (iii) reduced hERG channel inhibition.

01 Aug 2007·Journal of Chromatography BQ3 · MEDICINE

Liquid chromatography–tandem mass spectrometric determination of a new antibacterial agent (AVE6971) in human white blood cells

Q3 · MEDICINE

Article

Author: Jean-Yves Gautier ; Henri Merdjan ; Arnaud Salvador ; Olivier Pasquier

An LC-MS/MS assay for the quantitative determination of a new antibacterial agent (AVE6971) has been developed and validated in human white blood cells (WBC). The assay involved a lysing procedure of white blood cells and ultra centrifugation of the extracts. Chromatography was performed on a Supelcosil ABZ+ C(18) (2.1 mm x 50 mm, 5 microm) column using a mobile phase consisting of methanol/acetonitrile/10mM ammonium formate mixture (10:30:60, v/v/v) at a flow rate of 0.2 ml/min. The linearity was within the range of 10-10000 ng/ml of extracts, corresponding to 0.5-500 ng of AVE6971 in WBC pellets tubes. The validated lower limit of quantification was 10 ng/ml. The inter- and intra-run coefficients of variation (CV) for the assay were <12.9% and the accuracy were from -9.0 to -1.2%. AVE6971 was stable in WBC for at least 1 month at -75 degrees C. This assay proved to be suitable for the determination of AVE6971 in WBC from clinical studies.

100 Deals associated with NXL-105

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