Delving into the Latest Updates on Flurbiprofen with Synapse

The diagnosis of chronic pain currently lacks objective and quantifiable biomarkers. This study aims to observe the EEG characteristics of patients with chronic pain following spinal cord injury and subsequently administer analgesic interventions with remifentanil, esketamine, flurbiprofen, and spinal cord stimulation. The correlation between EEG features and pain intensity will be examined. The research aims to advance the objectification of chronic pain diagnosis and treatment.

Start Date25 Aug 2024

Sponsor / Collaborator-

NCT06566794 / Not yet recruitingNot ApplicableIIT

KF2022#4-tutkimus:Beetasalpaajan ja tulehduskipulääkkeen Vaikutus CYP-entsyymivälitteiseen lääkeainemetaboliaan

Carvedilol is a non-selective beta-blocker in common clinical use, used to treat hypertension, heart failure, and angina pectoris symptoms associated with coronary artery disease. Diclofenac is a non-selective anti-inflammatory drug in general use, which is used to treat rheumatic diseases, osteoarthritis, musculoskeletal pain conditions, menstrual pains and migraines, among others. In our recent experiments involving liver cell enzymes, both carvedilol and diclofenac were found to inhibit several cytochrome P450 (CYP) enzymes central to drug metabolism, potentially leading to adverse drug interactions with other drugs metabolized by the same enzyme. The purpose of this study is to investigate the effects of the use of carvedilol and diclofenac on the activity of key CYP enzymes in drug metabolism in healthy volunteers using a low-dose model drug combination covering seven CYP enzymes.
In an open three-phase, randomized, crossover study with 12 healthy volunteers, the subjects will receive a drug combination of caffeine, bupropion, repaglinide, flurbiprofen, omeprazole, dextromethorphan, midazolam and simvastatin and as a premedication either placebo, carvedilol or diclofenac. Blood samples will be collected and carvedilol, diclofenac, caffeine, bupropion, repaglinide, flurbiprofen, omeprazole, dextromethorphan, midazolam and simvastatin pharmacokinetics will be monitored up to 23 hours post dose.

Start Date20 Aug 2024

Sponsor / Collaborator

Helsinki University Central Hospital

[+1]

CTR20242384 / CompletedNot Applicable

氟比洛芬凝胶贴膏生物等效性试验

[Translation] Bioequivalence study of flurbiprofen gel patch

主要研究目的：按有关生物等效性试验的规定，选择持证商为Mikasa Seiyaku Co.,Ltd的氟比洛芬凝胶贴膏（商品名：泽普思®，规格：40mg）为参比制剂，对江苏万高药业股份有限公司生产并提供的受试制剂氟比洛芬凝胶贴膏（规格：40mg）进行空腹外用条件下人体生物等效性试验，比较受试制剂中药物的吸收速度和吸收程度与参比制剂的差异是否在可接受的范围内，评价两种制剂在外用条件下的生物等效性。次要研究目的： 1、观察中国健康受试者外用受试制剂氟比洛芬凝胶贴膏（规格：40mg）和参比制剂氟比洛芬凝胶贴膏（商品名：泽普思®，规格：40mg）后的安全性。 2、评估健康志愿受试者在试验期间，外用受试制剂氟比洛芬凝胶贴膏（规格：40mg ）或参比制剂氟比洛芬凝胶贴膏（商品名：泽普思®，规格：40mg）的附着力及外用刺激性情况。

[Translation]

Main research purpose: According to the relevant provisions of bioequivalence test, the flurbiprofen gel patch (trade name: Zepusi®, specification: 40mg) with the license holder Mikasa Seiyaku Co., Ltd was selected as the reference preparation, and the test preparation flurbiprofen gel patch (specification: 40mg) produced and provided by Jiangsu Wangao Pharmaceutical Co., Ltd. was subjected to human bioequivalence test under fasting external use conditions, to compare whether the absorption rate and degree of the drug in the test preparation were within the acceptable range with the reference preparation, and to evaluate the bioequivalence of the two preparations under external use conditions. Secondary research objectives: 1. Observe the safety of Chinese healthy subjects after external use of the test preparation flurbiprofen gel patch (specification: 40mg) and the reference preparation flurbiprofen gel patch (trade name: Zepusi®, specification: 40mg). 2. Evaluate the adhesion and external irritation of the test preparation flurbiprofen gel patch (specification: 40mg ) or the reference preparation flurbiprofen gel patch (trade name: Zepus®, specification: 40mg) applied externally to healthy volunteers during the trial.

Start Date09 Jul 2024

Sponsor / Collaborator

Jiangsu Vanguard Pharmaceutical Co.,Ltd.

100 Clinical Results associated with Flurbiprofen

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100 Translational Medicine associated with Flurbiprofen

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100 Patents (Medical) associated with Flurbiprofen

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2,671

Literatures (Medical) associated with Flurbiprofen

31 Dec 2024·Journal of the International Society of Sports Nutrition

The dose-response effects of flurbiprofen, indomethacin, ibuprofen, and naproxen on primary skeletal muscle cells

Article

Author: Roberts, Brandon M ; Matheny, Ronald W ; Geddis, Alyssa V

BACKGROUND:

Non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen, flurbiprofen, naproxen sodium, and indomethacin are commonly employed for their pain-relieving and inflammation-reducing qualities. NSAIDs work by blocking COX-1 and/or COX-2, enzymes which play roles in inflammation, fever, and pain. The main difference among NSAIDs lies in their affinity to these enzymes, which in turn, influences prostaglandin secretion, and skeletal muscle growth and regeneration. The current study investigated the effects of NSAIDs on human skeletal muscle cells, focusing on myoblast proliferation, differentiation, and muscle protein synthesis signaling.

METHODS:

Using human primary muscle cells, we examined the dose-response impact of flurbiprofen (25-200 µM), indomethacin (25-200 µM), ibuprofen (25-200 µM), and naproxen sodium (25-200 µM), on myoblast viability, myotube area, fusion, and prostaglandin production.

RESULTS:

We found that supraphysiological concentrations of indomethacin inhibited myoblast proliferation (-74 ± 2% with 200 µM; -53 ± 3% with 100 µM; both p < 0.05) compared to control cells and impaired protein synthesis signaling pathways in myotubes, but only attenuated myotube fusion at the highest concentrations (-18 ± 2% with 200 µM, p < 0.05) compared to control myotubes. On the other hand, ibuprofen had no such effects. Naproxen sodium only increased cell proliferation at low concentrations (+36 ± 2% with 25 µM, p < 0.05), and flurbiprofen exhibited divergent impacts depending on the concentration whereby low concentrations improved cell proliferation (+17 ± 1% with 25 µM, p < 0.05) but high concentrations inhibited cell proliferation (-32 ± 1% with 200 µM, p < 0.05).

CONCLUSION:

Our findings suggest that indomethacin, at high concentrations, may detrimentally affect myoblast proliferation and differentiation via an AKT-dependent mechanism, and thus provide new understanding of NSAIDs' effects on skeletal muscle cell development.

01 Nov 2024·INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

Flurbiprofen inhibits cAMP transport by MRP4/ABCC4 increasing the potency of gemcitabine treatment in PDAC cell models

Article

Author: Agustín, Gouts ; Natalia, Gómez ; Ana, Sahores ; Betina, González ; Carlos, Davio ; Carina, Shayo ; Agustín, Yaneff ; Héctor, Cerviño Ramiro

Pancreatic ductal adenocarcinoma (PDAC) remains a highly malignant cancer with a grim prognosis due to its early metastasis and resistance to current chemotherapies, such as Gemcitabine (GEM). We have previously demonstrated that cAMP exclusion by MRP4 is critical for PDAC cell proliferation, establishing this transporter as a promising prognostic marker and therapeutic target. In search for novel therapeutic options to improve GEM efficacy, we conducted a drug repositioning screening to identify potential inhibitors of cAMP transport by MRP4. Several non-steroidal anti-inflammatory drugs (NSAIDs) can inhibit the transport of certain MRP4 substrates. In this study, we assessed the efficacy of sixteen NSAIDs in inhibiting cAMP transport mediated by MRP4, identifying seven potent inhibitors based on their IC₅₀ values. The most potent inhibitors were further tested for their effect on cell proliferation and migration. Flurbiprofen emerged as the most potent inhibitor of both MRP4-mediated cAMP transport and cell proliferation. Overexpression of MRP4 in BxPC-3 cells significantly increased GEM resistance, and co-administration of flurbiprofen with GEM markedly enhanced the latter's potency inhibiting PDAC cells proliferation. These findings position flurbiprofen as a potent inhibitor of cAMP transport by MRP4 and a promising adjunctive therapy to enhance GEM effectiveness in PDAC treatment.

01 Nov 2024·EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Effect of protein binding on the pharmacokinetics of the six substrates in the Basel phenotyping cocktail in healthy subjects and patients with liver cirrhosis

Article

Author: Chapuisat, Fabio ; Krähenbühl, Stephan ; Hanimann, Robin ; Duthaler, Urs

Phenotyping serves to estimate enzyme activities in healthy persons and patients in vivo. Low doses of enzyme-specific substrates are administered, and activities estimated using metabolic ratios (MR, calculated as AUC_metabolite/AUC_parent). We administered the Basel phenotyping cocktail containing caffeine (CYP1A2 substrate), efavirenz (CYP2B6), flurbiprofen (CYP2C9), omeprazole (CYP2C19), metoprolol (CYP2D6) and midazolam (CYP3A) to 36 patients with liver cirrhosis and 12 control subjects and determined free and total plasma concentrations over 24 h. Aims were to assess whether MRs reflect CYP activities in patients with liver cirrhosis and whether MRs calculated with free plasma concentrations (MR_free) provide better estimates than with total concentrations (MR_total). The correlation of MR_total with MR_free was excellent (R² >0.910) for substrates with low (<30 %, caffeine and metoprolol) and intermediate protein binding (≥30 and <99 %, midazolam and omeprazole) but weak (R² <0.30) for substrates with high protein binding (≥99 %, efavirenz and flurbiprofen). The correlations between MR_total and MR_free with CYP activities were good (R² >0.820) for CYP1A2, CYP2C19 and CYP2D6. CYP3A4 activity was reflected better by midazolam elimination than by midazolam MR_total or MR_free. The correlation between MR_total and MR_free with CYP activity was not significant or weak for CYP2B6 and CYP2C9. In conclusion, MRs of substrates with an extensive protein binding (>99 %) show high inter-patient variabilities and do not accurately reflect CYP activity in patients with liver cirrhosis. Protein binding of the probe drugs has a high impact on the precision of CYP activity estimates and probe drugs with low or intermediate protein binding should be preferred.

1

News (Medical) associated with Flurbiprofen

17 Apr 2023

·www.drugs.com

Get Pain Relief With the Most Common Arthritis Medications

MONDAY, April 17, 2023 -- Arthritis is a common disease that causes pain and inflammation in different body joints, making it difficult to enjoy everyday tasks and physical activity. Fortunately, there are many different medications for arthritis. Depending on what type of arthritis you have and its severity, an arthritis medication may help you manage pain and other symptoms. Here is a breakdown of the most common arthritis medications, how they work and their potential side effects. The Arthritis Foundation lists the following as the medications used to treat arthritis: Analgesics including acetaminophen (Tylenol) and opioids Nonsteroidal anti-inflammatory drugs (NSAIDs) Corticosteroids Disease-modifying antirheumatic drugs (DMARDs) including biologics and targeted DMARDs Analgesics The Arthritis Foundation reports that analgesics may help with mild to moderate pain, but they will not help with the inflammation associated with arthritis. Analgesics work in the nervous system and alter how your brain perceives pain. They can be used to treat the pain associated with any type of arthritis, although more effective options are available. Analgesics can be opioid, non-opioid or a combination. Common analgesics are: Acetaminophen (Tylenol) Codeine Oxycodone Fentanyl Hydrocodone Potential side effects: Kidney damage Liver damage Addiction Constipation Gastrointestinal bleeding Use caution when taking these medications; take only as prescribed. NSAIDs NSAIDs work by blocking prostaglandin. According to the Cleveland Clinic , one role prostaglandins play is forming clots and causing inflammation at the site of an injury. NSAIDs are used to treat the pain and inflammation associated with rheumatoid arthritis and osteoarthritis . Common over-the-counter (OTC) NSAIDs are: Aspirin (Bayer, St. Joseph, Anacin, Excedrin and more) Ibuprofen (Motrin, Advil) Naproxen sodium (Aleve) Prescription NSAIDs are: Celecoxib (Celebrex) Diclofenac (Voltaren, available by brand name in topical form) Fenoprofen (Nalfon) Indomethacin (Indocin, available by brand name in liquid form) Ketorolac tromethamine (Toradol) Meclofenamate sodium (Meclomen) Diflunisal (Dolobid) Tolmetin (Tolectin) Ketoprofen (Orudis) Flurbiprofen (Ansaid) Potential side effects of NSAIDs are: Increased risk of stomach and bowel issues like ulcers and bleeding Increased risk of stroke Heart problems Stomach pain Nausea Diarrhea/constipation Corticosteroids According to the Arthritis Foundation , corticosteroids mimic cortisol, a hormone your body produces naturally. They are used to treat inflammatory types of arthritis, including rheumatoid arthritis and psoriatic arthritis. They are great for short-term relief of inflammation but are not recommended for long-term use because of their side effects. Your doctor may prescribe a lower dose if you require them for long-term use. Common corticosteroids: Prednisone (Deltasone, Prednicot, Cotolone) Prednisolone (Orapred, Omnipred) Cortisone (Cortone) Hydrocortisone (Cortef, Hydrocort) Triamcinolone (Aristocort) Dexamethasone (Decadron) Common side effects of corticosteroids: Blood sugar spikes Weight gain Bone loss Risk of cataracts High blood pressure Infections Mood changes DMARDs The Arthritis Foundation says that DMARDs work with the body to “stop or slow the disease process in inflammatory forms of arthritis.” They work by blocking inflammation. There are many different DMARDs on the market, and they all have different ways of working in the body. Conventional DMARDs work by broadly suppressing the immune system. Often they are used in combination with other therapies. Targeted DMARDs block specific pathways inside immune cells. Biologic DMARDs are produced by live cells and work on specific immune proteins called cytokines. Common DMARDs: Apremilast (Otezla) Baricitinib (Olumiant) Cyclophosphamide (Cytoxan) Cyclosporine (Gengraf, Neoral) Hydroxychloroquine (Plaquenil) Leflunomide (Arava) Methotrexate (Otrexup, Rasuvo, RediTrex) Mycophenolate mofetil (CellCept) Sulfasalazine (Azulfidine) Tofacitinib (Xeljanz, Xeljanz XR) According to the Cleveland Clinic , common side effects of traditional DMARDs include: Loss of appetite Nausea Diarrhea Abdominal pain Rash, allergic reaction Liver problem Increased risk of infection Low blood cell counts Common side effects of biologic DMARDs include: Increased risk of common and serious infections Reactivation of tuberculosis, herpes zoster, and hepatitis B and C Increased cholesterol levels, increased liver enzymes and low blood cell counts Increased risk of clotting When prescribed DMARDs, inform your doctor of any other medications, including over-the-counter medicines, you are taking to avoid drug interactions. Some of these medications can cause teratogenicity (defects in a developing fetus.) Writing recently in the Journal of the American Academy of Physician Assistants (JAAPA ), physician assistant Michelle DiBiase and Dr. Samantha Kohn remind people that "The mainstay of pharmacologic therapy is early intervention with use of nonbiologic and biologic DMARDs together with adjunctive medications such as NSAIDs, oral and intra-articular corticosteroids, and analgesic medications, including opioids." Your primary care provider or rheumatologist will work closely with you to determine which medications are best for your treatment. It is vital to keep them apprised of any side effects and let them know if the treatment is ineffective. They can work with you to find a treatment that helps relieve the pain and inflammation caused by arthritis. Posted April 2023

Drug Approval

100 Deals associated with Flurbiprofen

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KEGG	Wiki	ATC	Drug Bank
D00330	Flurbiprofen	M01AE09 M02AA19 R02AX01	DB00712

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Myalgia	JP	Mikasa Seiyaku Co. Ltd.	14 Mar 2008
Periarthritis	JP	Mikasa Seiyaku Co. Ltd.	14 Mar 2008
Analgesia	JP	Tokuhon Corp.	14 Mar 2001
Inflammation	JP	Tokuhon Corp.	14 Mar 2001
Musculoskeletal Pain	JP	Taikyo Pharmaceutical Co. Ltd.	10 Mar 1992
Bursitis	JP	Kaken Pharmaceutical Co., Ltd.	01 Sep 1989
Epicondylitis	JP	Kaken Pharmaceutical Co., Ltd.	01 Sep 1989
Tenosynovitis	JP	Kaken Pharmaceutical Co., Ltd.	01 Sep 1989
Tumescence	JP	Kaken Pharmaceutical Co., Ltd.	01 Sep 1989
Low Back Pain	JP	Kaken Pharmaceutical Co., Ltd.	31 Oct 1981
Periodontitis	JP	Kaken Pharmaceutical Co., Ltd.	31 Oct 1981
Pulpitis	JP	Kaken Pharmaceutical Co., Ltd.	31 Oct 1981
Osteoarthritis	JP	Kaken Pharmaceutical Co., Ltd.	19 Apr 1979
Rheumatoid Arthritis	JP	Kaken Pharmaceutical Co., Ltd.	19 Apr 1979

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Osteoarthritis, Knee	Phase 3	CN	Beijing Tide Pharmaceutical Co., Ltd.	31 Mar 2020
Osteoarthritis, Knee	Phase 3	CN	Mikasa Seiyaku Co. Ltd.	31 Mar 2020
Moderate pain	Phase 3	CN	Wuhan Daan Pharmacy Co. Ltd.	08 Nov 2013
Acute pharyngitis	Phase 3	US	Reckitt Benckiser LLC	01 Sep 2013
Cough	Phase 1	AU	Reckitt Benckiser LLC	01 Jul 2023
Respiratory Tract Infections	Phase 1	AU	Reckitt Benckiser LLC	01 Jul 2023

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Clinical Result

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Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01048866 (CTgov)	Phase 3	Pharyngitis	198	acetaminophen 650mg+flurbiprofen (Flurbiprofen 8.75 mg Lozenge)	jonbikpryx(ncciopfftu) = rfqqunfgug awlmmcnrep (mmlblzeivp, uwaksmozhn - tmoxzkxijw) View more	-	21 Sep 2017
				placebo+acetaminophen 650mg (Placebo Lozenge)	jonbikpryx(ncciopfftu) = gyrkmdemtw awlmmcnrep (mmlblzeivp, lpuvdvqkaf - vqqerpurfl) View more
NCT01049334 (CTgov)	Phase 3	Pharyngitis	204	Flurbiprofen (Flurbiprofen 8.75 mg Lozenge)	tdnsztjezj(mqylwuktmk) = wpguvzgszn unngtgfibo (eiooyccclz, gtviuxfvvk - blyqswmhgq) View more	-	21 Sep 2017
				Placebo (Placebo Lozenge)	tdnsztjezj(mqylwuktmk) = ggjrrusdgg unngtgfibo (eiooyccclz, hlmhkjokui - bdtuvdvzed) View more
NCT01986361 (CTgov)	Phase 3	Acute pharyngitis	122	flurbiprofen (Flurbiprofen 8.75 mg Lozenge)	dbatizjsxi(ueimxrreqn) = mgfrvdjzag cudhddqncm (myeniluywq, pzvgvaclsk - idlrefnzkz) View more	-	24 Aug 2017
				placebo (Placebo Lozenge)	dbatizjsxi(ueimxrreqn) = kypsngtojc cudhddqncm (myeniluywq, bpzsnvkybl - kzhynifppn) View more
ARVO2017	Not Applicable	Macular Edema	20	Nepafenac	simrgdikxz(dnmutypigx) = hpoebjgipy orfythrtbq (myrprqwgmv )	-	07 May 2017
				Diclofenac	simrgdikxz(dnmutypigx) = rsztkgskzo orfythrtbq (myrprqwgmv )
NCT01048866 \| NCT01049334 (Pubmed \| Int J Clin Pract)	Phase 3	Streptococcal Infections	402	Flurbiprofen 8.75 mg lozenges	abfbgbcoqm(gjzihrqtza) = A single flurbiprofen lozenge provided significantly greater relief than placebo for all three throat symptoms, lasting 3-4 h for patients with and without Strep A/C doggkpzypl (aewskbemoc ) View more	Positive	01 Jan 2015
Iritis prevention study (ARVO2004)	Not Applicable	Iritis	64	Topical flurbiprofen 300 mcg/ml	rrhvhhzwdg(grkxtaiykk) = 7/30 treated patients and 0/34 control patients had increased stinging aeragaddlv (fcvabmbblz )	Negative	01 May 2004
				Placebo