Delving into the Latest Updates on Tarenflurbil with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(2R)-2-(2-fluorobiphenyl-4-yl)propanoic acid, (R)-2-fluoro-α-methyl(1,1'-biphenyl)-4-acetic acid, (R)-flurbiprofen

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Target

NF-κB

Mechanism

NF-κB inhibitors(Nuclear factor NF-kappa-B complex inhibitors)

Therapeutic Areas

Nervous System DiseasesNeoplasmsUrogenital Diseases

Active Indication-

Inactive Indication

Alzheimer DiseaseLocalized Prostate Carcinoma

Originator Organization

Loma Linda University

Active Organization-

Inactive Organization

Myrexis, Inc.

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

Regulation-

Structure

Molecular FormulaC15H13FO2

InChIKeySYTBZMRGLBWNTM-SNVBAGLBSA-N

CAS Registry51543-40-9

The purpose of this study is to assess the impact of TMP001 in the treatment of patients with relapsing-remitting multiple sclerosis (RRMS). Therefore the average total number of contrast enhancing lesions (CELs) on brain MRI scans at weeks 12, 16, 20, and 24 during treatment with TMP001 is compared to the average total number of CELs on brain MRI scans at week -4 and baseline in these patients .
Based on promising preclinical results, the investigators assume a comparable effect of TMP001 on reduction of contrast-enhancing lesions as shown for other immunomodulatory substances in recent clinical studies.

Start Date01 Aug 2015

Sponsor / Collaborator

Fraunhofer Institute For Molecular Biology & Applied Ecology

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EUCTR2014-004483-38-DE / Not yet recruitingPhase 2

TMP001 in relapsing-remitting multiple sclerosis: a multicentre open, baseline-controlled phase IIa clinical trial

Start Date16 Jul 2015

Sponsor / Collaborator-

NCT02206854 / CompletedPhase 1IIT

Bioavailability, Pharmacokinetics and Tissue Distribution of R-flurbiprofen Capsules in Healthy Subjects

For previous clinical trials, R-flurbiprofen has been prepared in tablet form. In this study R-flurbiprofen, will be available as gelatine capsules.
This study aims to show the bioavailability of R-flurbiprofen when administered in gelatine capsules. The serum availability will be determined by analysis of pharmakokinetic (pK)-blood samples at different time points. To assess the safety of the administered capsules adverse events will be documented.
Analysis of lipid signaling molecules in plasma will be done to assess the role of this molecules as variable for therapeutic effects.

Start Date01 Jun 2014

Sponsor / Collaborator

Johann Wolfgang Goethe-Universität Frankfurt am Main

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100 Clinical Results associated with Tarenflurbil

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100 Translational Medicine associated with Tarenflurbil

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100 Patents (Medical) associated with Tarenflurbil

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182

Literatures (Medical) associated with Tarenflurbil

25 Apr 2024·The Journal of Physical Chemistry B

Variation of Activation Volume as an Indicator of the Difference in Clusterization Phenomenon Induced by H-Bonding and F−Π Stacking Interactions in Enantiomers and a Racemate of Flurbiprofen

Article

Author: Hachuła, Barbara ; Jesionek, Paulina ; Hreczka, Marek ; Włodarczyk, Patryk ; Kamiński, Kamil ; Jurkiewicz, Karolina ; Kamińska, Ewa

In this paper, X-ray diffraction (XRD), differential scanning calorimetry (DSC), broadband dielectric (BDS), and Fourier transform infrared (FTIR) spectroscopy supported by molecular dynamics (MD) simulations and quantum chemical computations were applied to investigate the structural and thermal properties, molecular dynamics, and H-bonding pattern of R-, S-, and RS-flurbiprofen (FLP). Experimental data indicated various spatial molecular arrangements in crystalline forms of examined systems, which seemed to disappear in the liquid state. Surprisingly, deeper analysis of high-pressure dielectric data revealed unexpected variation in the activation volume of pure enantiomers and a racemate. MD simulations showed that it is an effect of the clusterization phenomenon and a higher population of small associates in the former samples. Moreover, theoretical consideration exposed the particular role of unspecific F-Π interactions as a driving force underlying local molecular arrangements of molecules in the liquid and the crystal lattice of R-, S-, and RS-FLP.

02 Sep 2023·Cureus

Effectiveness and Adherence Rate of S-flurbiprofen Plaster for the Pain Management of Patients With Moderate and End-Stage Knee Osteoarthritis

Article

Author: Takeshita, Katsushi ; Takahashi, Tsuneari ; Iguchi, Masaki

BACKGROUNDS-flurbiprofen plaster (SFPP) is highly skin permeable and represents a new conservative treatment for knee osteoarthritis (KOA) that can attain considerably higher concentrations in the synovium than topical flurbiprofen. To date, no study has investigated the efficacy and adherence rate of SFPP in patients with end-stage KOA. This study aimed to compare the effectiveness and adherence rate of SFPP for pain management in patients with moderate and end-stage KOA.METHODSThis retrospective study included a total of 118 patients with KOA (Kellgren-Lawrence classification grades II (n = 29), III (n = 32), and IV (n = 57)). The difference in SFPP use rate, adverse drug reactions rate, whether 50% pain relief occurred, and the percentage of patients who underwent surgical treatment were calculated.RESULTSThe overall SFPP use rate at one year was 61.0% (88.1% at less than one month, 79.7% at three months, and 61.0% at six months), with no significant differences among Kellgren-Lawrence grade II, III, and IV groups (p = 0.538). Adverse drug reactions such as skin rash (n = 23), skin irritation (n = 8), and gastrointestinal disorders (n = 2) were observed. The one-year SFPP use rate was significantly lower in patients in whom these side effects occurred but did not decrease in patients in whom only a skin rash occurred. Overall, 19 patients underwent surgery after discontinuation of SFPP use. Surgery was statistically selected more by the "over 71 years of age" group (p = 0.038) and the "ineffective" group (p = 0.007).CONCLUSIONSFPP exerts a comparable therapeutic effect even in end-stage KOA and may be an effective treatment option. Even if patients have end-stage KOA, there are cases in which the patient's background does not allow for surgery positively, such as high perioperative risk or desire for conservative treatment. In such cases, SFPP may be an effective treatment option worth trying.

31 Oct 2022·Drug Discoveries & Therapeutics

Comparison of efficacy and safety in the combination therapies of duloxetine and S-flurbiprofen plaster, and of duloxetine and conventional NSAIDs for chronic pain in patients with osteoarthritis (OASIS DUAL study)

Article

Author: Koyama, Kenzo

The purpose of this study is to compare the efficacy and safety of pharmacotherapies for chronic pain due to osteoarthritis (OA) between a group with duloxetine (DLX) and S-flurbiprofen plaster (SFPP) (the SFPP group) and a group with DLX and conventional non-steroidal anti-inflammatory drugs (NSAIDs) (the control group). The subjects were 49 patients (17 men and 32 women). The evaluation of factors associated with treatment termination due to symptoms improvement showed that significantly more women terminated treatment than did men, and significantly more members of the SFPP group terminated treatment than did members of the control group. The visual analogue scale (VAS) score in the SFPP group was significantly improved from 6.6 ± 1.7 before treatment to 3.6 ± 2.1 one month later and showed significant difference until nine months later. The VAS score in the control group was significantly improved from 6.7 ± 1.9 to 4.1 ± 2.8 one month later. The VAS score improvement rate was significantly higher in the SFPP group than in the control group, suggesting that the DLX-SFPP combination had higher efficacy than the DLX-conventional NSAIDs combination. The incidence of adverse drug reactions was 55% in the SFPP group, which is not significantly different from 50% incidence in the control group. The treatment discontinuation rate due to adverse drug reactions, however, was 60% in the control group and 19% in the SFPP group. It was suggested that the efficacy and safety of the DLX-SFPP combination for chronic pain due to OA are equal to or higher than that of the DLX-conventional NSAIDs combination.

100 Deals associated with Tarenflurbil

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External Link

KEGG	Wiki	ATC	Drug Bank
D09010	Tarenflurbil	-	DB05289

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	Phase 3	US	Myrexis, Inc.	01 Feb 2005
Localized Prostate Carcinoma	Phase 3	US	Myrexis, Inc.	01 Feb 2002

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00105547 (Pubmed \| JAMA)	Phase 3	Alzheimer Disease	1,684	Tarenflurbil 800 mg	(vtlvlftcfl) = jiamonboer welqwklqtf (zfixyeddex )	Negative	16 Dec 2009
AAIC2008	Not Applicable	Liver Injury	6	Tarenflurbil (Control subjects)	(nfhxngtyhy) = pqttvqfiki kxtgqohrnq (comolnswvi ) View more	-	01 Jul 2008
				Tarenflurbil (Subjects with mild hepatic impairment)	(nfhxngtyhy) = ropshdsgyo kxtgqohrnq (comolnswvi ) View more
AAIC2008	Not Applicable	-	-	Tarenflurbil 800 mg (Fed)	(xtlgygjokx) = tgrfnbtjcj oofgifwiir (rjobgfgkrr, 35.7 - 80.0)	-	01 Jul 2008
				Tarenflurbil 800 mg (Fasted)	(xtlgygjokx) = fulksgmbkm oofgifwiir (rjobgfgkrr, 50.9 - 98.6)
AAIC2008	Not Applicable	-	-	Tarenflurbil 400 mg	(uzlguybhxj) = nkdzdjjevm qhoyfuwjzb (duhbxxypsw ) View more	-	01 Jul 2008
				Tarenflurbil 800 mg	(uzlguybhxj) = izjulkgkdy qhoyfuwjzb (duhbxxypsw ) View more