Delving into the Latest Updates on AZD-5122 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

CXCR2

Action

antagonists

Mechanism

CXCR2 antagonists(C-X-C motif chemokine receptor 2 antagonists)

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization

AstraZeneca PLC

Active Organization-

Inactive Organization

AstraZeneca PLC

License Organization-

Drug Highest PhasePendingPhase 1

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC18H23F2N5O4S2

InChIKeyQVKPEMXUBULFBM-RISCZKNCSA-N

CAS Registry1204707-71-0

The purpose of the study is to determine how quickly AZD5122 is absorbed into and cleared by the body when given to healthy, non smoking males at different dose levels. This is a 2 part study, in Part B a single group of subjects will be given both an oral dose and intravenous microdose of AZD5122 at a specialist unit. For part B there is no placebo treatment given.

Start Date01 Sep 2009

Sponsor / Collaborator

AstraZeneca PLC

100 Clinical Results associated with AZD-5122

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100 Translational Medicine associated with AZD-5122

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100 Patents (Medical) associated with AZD-5122

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1

Literatures (Medical) associated with AZD-5122

30 May 2016·Journal of Labelled Compounds and RadiopharmaceuticalsQ4 · MEDICINE

The synthesis of [¹⁴C]AZD5122. Incorporation of an IV ¹⁴C‐microtracer dose into a first in human study to determine the absolute oral bioavailability of AZD5122

Q4 · MEDICINE

Article

Author: Kingston, Lee P. ; Allen, Paul H. ; Hickey, Michael J. ; Wilkinson, David J.

AZD5122, N‐(2‐(2,3‐difluorobenzylthio)‐6‐((2R,3R)‐3,4‐dihydroxybutan‐2‐ylamino)pyrimidin‐4‐yl)azetidine‐1‐sulfonamide was under investigation as a potential chemokine receptor CXCR2 antagonist for the treatment for inflammatory diseases. To gain a better understanding of the human pharmacokinetic profile, an exploratory phase I IV microtracer study was conducted using carbon‐14 radiolabelled AZD5122. [14C]AZD5122 was carbon‐14 labelled in the pyrimidine ring in five steps in an overall radiochemical yield of 19% from [14C]thiourea. The absolute oral bioavailability of AZD5122 was assessed in healthy subjects by an oral administration of AZD5122, followed by a concomitant intravenous [14C]AZD5122 microdose.

100 Deals associated with AZD-5122

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