Delving into the Latest Updates on Faxeladol with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Faxeladol (USAN/INN)

+ [6]

Target

NET x Opioid receptors x SERT

Action

inhibitors, agonists

Mechanism

NET inhibitors(Norepinephrine transporter inhibitors), Opioid receptors agonists(Opioid receptors agonists), Serotonin reuptake inhibitors

Therapeutic Areas

Immune System DiseasesNervous System DiseasesSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Chronic PainFibromyalgiaNeuralgia+ [1]

Originator Organization

Grunenthal SA

Active Organization-

Inactive Organization

Grünenthal GmbHGrunenthal SA

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC15H23NO

InChIKeyJIRYWFYYBBRJAN-ZFWWWQNUSA-N

CAS Registry433265-65-7

The safety and tolerability of multiple oral administrations of GRT9906 at different doses was investigated in this clinical study. The prolonged-release tablets slowly release the active compound in the intestine. In addition, absorption into the body, distribution, metabolization and excretion of GRT9906 was characterized. Pharmacological effects of GRT9906 in healthy participants was assessed using pupillometry (diameter and reactions of the pupil) and a Cold Pressor Test where pain is measured while hands are placed in icy water for two minutes.

Start Date15 Sep 2004

Sponsor / Collaborator

Grünenthal GmbH

100 Clinical Results associated with Faxeladol

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100 Translational Medicine associated with Faxeladol

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100 Patents (Medical) associated with Faxeladol

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1

Literatures (Medical) associated with Faxeladol

01 Jul 2012·European Journal of PainQ2 · MEDICINE

Randomized controlled trial of the combined monoaminergic and opioid investigational compoundGRT9906in painful polyneuropathy

Q2 · MEDICINE

Article

Author: Meier, T. ; Ashworth, J. ; Jensen, T.S. ; Lehmann, R. ; Sindrup, S.H. ; Winkel, M. ; Baron, R. ; Konder, R.

AbstractGRT9906 is an investigational novel compound with μ‐opioid receptor agonism and inhibition of noradrenalin/serotonin re‐uptake. In this randomized, double‐blind, placebo‐controlled, three‐way cross‐over trial in painful polyneuropathy, the efficacy and safety ofGRT9906 was assessed and compared with tramadol. During 4‐week treatment periods, daily oral doses of eitherGRT9906 120–240 mg, or placebo, or tramadol 200–400 mg were given. These were separated by 1‐week washout periods. The primary endpoint was the average pain intensity (average of daily current pain intensity over the last 3 days of each treatment period rated on a 0 to 10‐point numeric rating scale). One hundred seventeen patients were enrolled and 64 were randomized to one of six treatment sequences. Forty‐seven patients qualified for the per protocol analysis.GRT9906 reduced average pain intensity by 2.1 points compared with a reduction of 0.6 points on placebo (p < 0.0001) and 2.4 points on tramadol.GRT9906 also improved scores on the sleep problem scale and the neuropathic pain symptom inventory and scored better than placebo on the patient global impression of change. Numbers needed to treat to obtain one patient with more than 50% pain relief was 3.9 (95%CI2.4–11.5) for bothGRT9906 and tramadol. The most frequently reported adverse events were nausea, fatigue, constipation and sleep disorder forGRT9906 and tramadol. Four patients dropped out due to adverse events during bothGRT9906 and tramadol treatment and two dropped out during placebo treatment. In conclusion, in painful polyneuropathy,GRT9906 demonstrated analgesic efficacy with a magnitude of effect comparable with tramadol and was well tolerated.

100 Deals associated with Faxeladol

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External Link

KEGG	Wiki	ATC	Drug Bank
D10007	Faxeladol	-	-

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Fibromyalgia	Phase 2	United States	Grünenthal GmbH	19 Sep 2005
Chronic Pain	Phase 2	Germany	Grünenthal GmbH	22 Oct 2003
Chronic Pain	Phase 2	Germany	Grunenthal SA	22 Oct 2003
Visceral Pain	Phase 2	Germany	Grünenthal GmbH	22 Oct 2003
Visceral Pain	Phase 2	Germany	Grunenthal SA	22 Oct 2003
Neuralgia	Phase 2	United Kingdom	Grünenthal GmbH	-
Neuralgia	Phase 2	Germany	Grünenthal GmbH	-
Neuralgia	Phase 2	Denmark	Grünenthal GmbH	-