Delving into the Latest Updates on GW-406381 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

COX-2

Mechanism

COX-2 inhibitors(Cyclooxygenase-2 inhibitors)

Therapeutic Areas

Immune System DiseasesNervous System DiseasesMouth and Tooth Diseases+ [2]

Active Indication-

Inactive Indication

HyperalgesiaNeuralgiaOsteoarthritis, Knee+ [4]

Originator Organization

GSK Plc

Active Organization-

Inactive Organization

GSK Plc

Drug Highest PhasePendingPhase 3

First Approval Date-

Regulation-

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Structure

Molecular FormulaC21H19N3O3S

InChIKeyNXMZBNYLCVTRGB-UHFFFAOYSA-N

CAS Registry221148-46-5

This study will assess the pharmacokinetics and tolerability of a single dose of GW406381 in subjects with moderate hepatic impairment in comparison to matched healthy volunteers. The hepatically impaired and healthy groups will be given a single 20 mg oral dose of GW406381. Blood samples for PK analysis will be collected pre-dose and over the 72 hours post dosing. Subjects will be housed from the evening before dosing until 24 hours after dosing. A follow-up visit will be conducted between 7 to 10 days from the last dose of study drug.

Start Date19 Oct 2005

Sponsor / Collaborator

GSK Plc

EUCTR2005-000158-61-AT / Not yet recruitingNot Applicable

A Phase III, 12-Week, Multicentre, Double-Blind, Randomised, Placebo- and Active Comparator-Controlled, Parallel Group Study to Investigate the Efficacy and Safety of GW406381, 5mg, 10mg, 25mg, and 50mg administered orally once daily, in Adults with Rheumatoid Arthritis

Start Date10 Aug 2005

Sponsor / Collaborator

GlaxoSmithKline Research & Development Ltd.

NCT00113308 / CompletedPhase 3

A Phase III, 12-Week, Multicentre, Double-Blind, Randomised, Placebo- and Active Comparator-Controlled, Parallel Group Study to Investigate the Efficacy and Safety of GW406381, 5mg, 10mg, 25mg, and 50mg Administered Orally Once Daily, in Adults With Rheumatoid Arthritis

This study is being conducted to find out if an investigational drug called GW406381 can help people with rheumatoid arthritis.

Start Date01 Jun 2005

Sponsor / Collaborator

GSK Plc

100 Clinical Results associated with GW-406381

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100 Translational Medicine associated with GW-406381

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100 Patents (Medical) associated with GW-406381

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7

Literatures (Medical) associated with GW-406381

01 Sep 2009·The Clinical Journal of PainQ3 · MEDICINE

A Randomized, Controlled, Dose-ranging Study Investigating Single Doses of GW406381, Naproxen Sodium, or Placebo in Patients With Acute Pain After Third Molar Tooth Extraction

Q3 · MEDICINE

Article

Author: Lomax, Mark ; Varner, Julie ; Blum, David ; Quessy, Steve

OBJECTIVESTo evaluate the efficacy and tolerability of 4 doses of GW406381, a cyclooxygenase-2 inhibitor, compared with placebo in a standard model of acute inflammatory pain.METHODSThis randomized, double-blind, placebo-controlled, single-center study compared single doses of GW406381 (10 to 70 mg) or naproxen sodium 550 mg with placebo in patients after extraction of 2 or more partially bony impacted third molar teeth. A total of 300 patients were randomized (50 per group). The primary efficacy variable was the pain relief intensity difference score at each time point, which was calculated as the sum of the pain intensity difference and pain relief categorical scores at each time point. Each treatment was compared with placebo at each time point using an ordered hierarchical approach with closed testing procedures and last observation carried forward imputation methods.RESULTSPain relief intensity differences from placebo were statistically significant beginning at 1.5 hours postdosing for GW406381 70 and 50 mg and at 2-hour postdosing for GW406381 25 and 10 mg. The median time to onset of analgesia was 71 minutes for GW406381 50 mg, 72 minutes for GW406381 70 mg, and 36 minutes for naproxen. The median duration of analgesia was 5.9 hours for GW406381 50 mg, 7.9 hours for GW406391 70 mg, and 11.3 hours for naproxen. All treatments were well tolerated.DISCUSSIONGW406381 50 and 70 mg demonstrated clinically meaningful analgesia in this acute pain setting, although the onset of analgesia was greater than 1 hour.

01 Jun 2009·The Journal of PainQ2 · MEDICINE

A Randomized, Double-Blind, Placebo-Controlled Trial of a Selective COX-2 Inhibitor, GW406381, in Patients With Postherpetic Neuralgia

Q2 · MEDICINE

Article

Author: Steve Quessy ; Richard Rauck ; Rachel Hodge ; David Blum ; Richard Philipson ; Steve Shackelford

In this randomized, double-blind, placebo-controlled study, we evaluated the efficacy and safety of GW406381, an investigational selective cyclooxygenase (COX)-2 inhibitor with both peripheral and central actions, in 209 patients with postherpetic neuralgia (PHN). Patients were randomly assigned to GW406381 25 mg or 50 mg or placebo treatments for 3 weeks. The primary efficacy outcome measure was the change in average daily pain intensity score from baseline to the last week of treatment. Both doses of GW406381 produced greater reduction in pain score than placebo, but the treatment difference did not reach statistical significance. It was possible that the 3-week duration was too short, as there was a tendency for increasing separation from placebo over time that did not appear to reach maximum effect by the end of the study for either GW406381 treatment group. Overall, GW406381 was well tolerated in this elderly population.PERSPECTIVETo our knowledge, this is the first report of a randomized, controlled clinical trial of a selective or nonselective COX inhibitor in neuropathic pain. The results of this study were inconclusive regarding the clinical relevance of the role of COX-2 in modulation of the symptoms of PHN.

01 Apr 2008·European Journal of NeurologyQ2 · MEDICINE

A double‐blind, randomized, placebo‐controlled, single‐dose study of the cyclooxygenase‐2 inhibitor, GW406381, as a treatment for acute migraine

Q2 · MEDICINE

Article

Author: T. B. Jimenez ; S. K. Aurora ; M. Gold ; R. M. Dixon ; A. L. Wentz

The objective of the present study was to explore the clinical efficacy and tolerability of GW406381, a cyclooxygenase‐2 (COX‐2) inhibitor with relatively high CNS penetration, in acute migraine. This was a double‐blind, single‐dose study of GW406381 compared with placebo and naproxen sodium compared with placebo (protocol number CXA20008). Three hundred and thirty‐seven subjects were randomized 1:1:1 to GW406381 (70 mg), naproxen sodium (825 mg), or placebo for the treatment of one migraine headache of moderate or severe intensity in a potential 8‐week period. The primary end‐point was the proportion of subjects with headache relief [reduction in headache severity score from pre‐dose 2 (moderate) or 3 (severe) to 0 (no pain) or 1 (mild)] at 2 h post‐dose for GW406381 compared with placebo. Significantly higher proportions of subjects treated with GW406381 (50%, P = 0.032) or naproxen sodium (56%, P = 0.005) than with placebo (35%) reported headache relief at 2 h post‐dose. Additional significant benefits were observed on many secondary outcomes, including proportions of subjects pain‐free, for both GW406381 and naproxen sodium treatment compared with placebo. Both active treatments were well tolerated. Single‐dose GW406381 (70 mg) and naproxen sodium (825 mg) were effective and well tolerated in the treatment of acute migraine.

100 Deals associated with GW-406381

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External Link

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Osteoarthritis, Knee	Phase 3	NO	GSK Plc	01 May 2005
Osteoarthritis, Knee	Phase 3	DK	GSK Plc	01 May 2005
Osteoarthritis, Knee	Phase 3	KR	GSK Plc	01 May 2005
Osteoarthritis, Knee	Phase 3	SE	GSK Plc	01 May 2005
Toothache	Phase 3	US	GSK Plc	01 Dec 2004
Rheumatoid Arthritis	Phase 2	GR	GSK Plc	01 Jun 2005
Rheumatoid Arthritis	Phase 2	IN	GSK Plc	01 Jun 2005
Osteoarthritis, Knee	Phase 2	ES	GSK Plc	01 May 2005
Osteoarthritis, Knee	Phase 2	NL	GSK Plc	01 May 2005
Rheumatoid Arthritis	Phase 1	LV	GSK Plc	01 Jun 2005