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

+ [8]

Target

NF-κB

Mechanism

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

Therapeutic Areas

Immune System DiseasesNervous System DiseasesSkin and Musculoskeletal Diseases+ [1]

Active Indication

MyalgiaPeriarthritisTendinopathy+ [2]

Inactive Indication

Alzheimer DiseaseLocalized Prostate Carcinoma

Originator Organization

Loma Linda University

Active Organization

Lead Chemical Co., Ltd.

Inactive Organization

Myrexis, Inc.

Drug Highest PhaseApproved

First Approval Date

JP (29 Mar 1988),

Osteoarthritis

Regulation-

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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

[+1]

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

[+1]

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

13 Aug 2024·Cureus

Efficacy of S-Flurbiprofen Plaster for Analgesia Following Total Hip Arthroplasty

Article

Author: Mitani, Shigeru ; Kawamoto, Toyohiro ; Furuichi, Shuro ; Namba, Yoshifumi ; Miyake, Yoshiaki ; Umehara, Norifumi

PURPOSES-flurbiprofen (SFP) plaster, a non-steroidal anti-inflammatory drug preparation that penetrates effectively into deep tissue, is currently used as a conservative treatment for osteoarthritis. We investigated the analgesic and adverse effects of SFP plaster after total hip arthroplasty (THA).METHODSA retrospective comparative study identified 100 patients who underwent primary THA in our department. Group A consisted of 50 patients who received the selective cyclooxygenase-2 inhibitor celecoxib for 14 days after surgery, while Group B consisted of 50 patients who received SFP plaster for 14 days after surgery. We noted the numerical rating pain intensity scale (NRS) score, body temperature, and adverse effects of the analgesics.RESULTSGroups A and B showed no significant difference in NRS scores (p > 0.05). The body temperature was significantly higher in Group B than in Group A on days one, two, three, and five (p < 0.01). In Group A, two patients (4%) showed drug-induced renal dysfunction, and one patient (2%) showed gastrointestinal disturbance. Patients in Group B showed no systemic or local adverse effects.CONCLUSIONSThe application of SFP plaster after THA provided an analgesic effect similar to that obtained with oral celecoxib without causing obvious side effects. Applying an SFP plaster may be an effective solution for postoperative analgesia.

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.

100 Deals associated with Tarenflurbil

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External Link

KEGG	Wiki	ATC	Drug Bank
D09010	Tarenflurbil	-	DB05289

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Myalgia	JP	Lead Chemical Co., Ltd.	01 Sep 1989
Periarthritis	JP	Lead Chemical Co., Ltd.	01 Sep 1989
Tendinopathy	JP	Lead Chemical Co., Ltd.	01 Sep 1989
Tumescence	JP	Lead Chemical Co., Ltd.	01 Sep 1989
Osteoarthritis	JP	Lead Chemical Co., Ltd.	29 Mar 1988

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	Discovery	US	Myrexis, Inc.	01 Feb 2005
Localized Prostate Carcinoma	Discovery	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 \| J Coll Physicians Surg Pak)	Phase 3	Alzheimer Disease	1,684	Tarenflurbil 800 mg	(yofbkysyoe) = mefranqbbm apnrwrkhgf (irbzetbqbr )	Negative	16 Dec 2009
AAIC2008	Not Applicable	-	-	Tarenflurbil 400 mg	(rceachfyho) = zrrdnwrfru uatpraunjb (rzahpkodoz ) View more	-	01 Jul 2008
				Tarenflurbil 800 mg	(rceachfyho) = xosgcgnbgg uatpraunjb (rzahpkodoz ) View more
AAIC2008	Not Applicable	-	-	Tarenflurbil 800 mg (Fed)	(mvunsmosii) = htoffussxp goojgnjket (ictuynzvlr, 35.7 - 80.0)	-	01 Jul 2008
				Tarenflurbil 800 mg (Fasted)	(mvunsmosii) = ylcecqojoh goojgnjket (ictuynzvlr, 50.9 - 98.6)
AAIC2008	Not Applicable	Liver Injury	6	Tarenflurbil (Control subjects)	(gskybmhgkg) = xgnkfffxzt ragohifupt (ugaqbloftn ) View more	-	01 Jul 2008
				Tarenflurbil (Subjects with mild hepatic impairment)	(gskybmhgkg) = fqiyafgure ragohifupt (ugaqbloftn ) View more