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flurbiprofen (Yakuban Tape)

✓ Approved

Kaken Pharmaceutical · PTGS1 · 小分子

什么是 flurbiprofen？

flurbiprofen 是一种小分子，由Kaken Pharmaceutical研发。该药已获批，用于治疗相关适应症，给药途径：Transdermal。

药物档案

商品名Yakuban Tape
公司Kaken Pharmaceutical
药物类别小分子
分子靶点PTGS1, PTGS2
给药途径Transdermal
状态Approved
来源： ClinicalTrials.gov, Kaken Pharmaceutical

作用机制

分子靶点

flurbiprofen 作用于 2 个分子靶点：

PTGS1prostaglandin-endoperoxide synthase 1 (COX3, PCOX1)
PTGS2prostaglandin-endoperoxide synthase 2 (GRIPGHS, hCox-2)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

flurbiprofen 针对 5 个适应症，涉及 3 个治疗领域。

治疗领域疾病/病症分期
Gastrointestinal disordersAbdominal pain✓ Approved
Injury, poisoning and procedural complicationsEpicondylitis✓ Approved
Musculoskeletal and connective tissue disordersMusculoskeletal pain✓ Approved
Musculoskeletal and connective tissue disordersOsteoarthritis✓ Approved
Musculoskeletal and connective tissue disordersTendonitis✓ Approved

相关研究文献

PubMedPacing and clinical electrophysiology : PACE2026-10-26

The Effectiveness and Safety of Deep Sedation Protocols for Pulsed Field Ablation of Atrial Fibrillation.

Zhao Yize Y, Li Fadong F, Wang Jue J, Zhou Le L et al.

Deep sedation (DS) is increasingly utilized during pulsed field ablation (PFA) for atrial fibrillation (AF), but the optimal electrophysiologist-led sedation regimen remains unclear. To compare sedative effectiveness and safety of three electrophysiologist-led DS protocols. In this prospective, single-center study, AF patients undergoing focal-form PFA received (1) midazolam + fentanyl (Midazolam group), (2) flurbiprofen axetil + midazolam + fentanyl (Flurbiprofen group), or (3) dexmedetomidine + fentanyl (Dexmedetomidine group). The primary endpoint was the achievement of the target sedation level at ablation initiation (Ramsay Sedation Score ≥3). Secondary endpoints included intraoperative pain, sedation difficulty, operator satisfaction, and sedation-related adverse events. 166 patients (mean age, 62.2 ± 10.8 years; 62.7% male; 48.2% with paroxysmal AF) were enrolled, with 53, 67, and 46 patients included in the Midazolam, Flurbiprofen, and Dexmedetomidine groups, respectively. The primary outcome occurred more frequently in the Flurbiprofen (73.1%) and Dexmedetomidine (82.6%) groups compared to Midazolam (47.2%) (overall p < 0.001); Flurbiprofen and Dexmedetomidine group did not differ significantly. Intraoperative pain scores were lowest with Dexmedetomidine (overall p < 0.001). Both Flurbiprofen and Dexmedetomidine groups showed lower sedation difficulty and higher operator satisfaction than the Midazolam group (both overall p < 0.001). Dexmedetomidine was associated with more intraoperative hypotension (overall p = 0.047). Electrophysiologist-led DS protocols with Flurbiprofen and Dexmedetomidine were associated with higher target sedation attainment than the specific low-dose Midazolam regimen during PFA, but Dexmedetomidine is linked to higher hypotension rates, warranting caution.

PMID 42929317
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PubMedGels (Basel, Switzerland)2026-10-26

Engineering Smart Hydrogels Through Dynamic Polymer Networks for Controlled Drug Delivery.

Choi Chanju C, Seo Dongseong D, Kim Taeho T, Park Jonghyun J et al.

Smart hydrogels are increasingly explored as adaptive platforms for controlled drug delivery because their polymer networks can respond dynamically to chemical, biological, and physical cues. Among these systems, dynamic polymer networks formed through reversible covalent and noncovalent interactions provide a unique means of coupling molecular-scale bond exchange with time-dependent changes in hydrogel structure, mechanics, degradation, and therapeutic transport. This review presents an integrated framework linking dynamic crosslink chemistry, exchange kinetics, network properties, and drug-release behavior. Dynamic covalent, supramolecular, metal-ligand, and hybrid network strategies are compared with particular emphasis on how crosslink lifetime, mesh accessibility, swelling, viscoelasticity, stress relaxation, and degradation govern therapeutic cargo loading, retention, diffusion, and release. Representative release mechanisms and kinetic models are discussed together with cargo-specific design considerations for small molecules, proteins and peptides, nucleic acids, and nanoparticle-based therapeutics. Biomedical applications are further considered according to therapeutic requirements and administration routes, including injectable local depots, topical and transdermal delivery, and regenerative systems. Finally, key translational challenges involving physiological complexity, biocompatibility, reproducibility, scale-up, sterilization, and storage stability are critically assessed. By connecting molecular interaction dynamics with network-level behavior and therapeutic performance, this review provides design principles for developing more predictable, programmable, and clinically translatable dynamic hydrogel drug-delivery systems.

PMID 42929917
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PubMedJournal of chromatography. B, Analytical technologies in the biomedical and life sciences2026-10-25

GC-Orbitrap-HRMS coupled with microdialysis: A novel approach for non-targeted analysis of transdermal constituents in topical patch preparation.

Wang Haolu H, Nie Lixing L, Wu Yu Y, Li Lianjia L et al.

Acupoint sticking therapy (AST) is a traditional Chinese transdermal treatment widely used for chronic conditions such as asthma and dyspepsia. Despite its clinical efficacy, the material basis of AST, particularly the penetration dynamics of its active transdermal components, remains unclear, hindering further investigation into its therapeutic mechanisms. This study developed an integrated platform combining in vivo microdialysis with GC-Orbitrap-HRMS to characterize transdermal components and penetration profiles of AST, using the Jianpi Patch (JPT) as a model due to its proven efficacy in pediatric functional dyspepsia. Firstly, 204 volatile compounds in JPT were identified, including terpenoids, hydrocarbons, esters, ketones and alcohols. Furthermore, through real-time microdialysis at the Shenque (CV8) acupoint in rats, 66 compounds were identified as transdermal constituents by GC-Orbitrap-HRMS. Based on their transdermal profiles, these penetrating components were categorized into three distinct patterns: rapid penetration (peak within 1-2 h), delayed peak (gradual increase, maximum at 3-4 h), and sustained release (progressive rise, peak at 5-6 h). This work established a minimally invasive platform for screening the material basis of transdermal herbal formulations and provided new insights into the permeation behavior of AST.

PMID 42927677
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PubMedFrontiers in bioengineering and biotechnology2026-10-25

A melatonin textile transdermal patch based on physicochemical synergistic permeation-enhancement strategy for circadian rhythm regulation.

Zhao Juyang J, Liu Jinzhi J, Lin Jiahan J, Liu Mingtao M et al.

Melatonin, an endogenous circadian rhythm-regulating hormone, has faced challenges in achieving prolonged exogenous regulation due to its low oral bioavailability and short half-life. Existing transdermal strategies are difficult to balance efficacy, safety, and accessibility. To address this, we propose a physicochemical synergistic permeation-enhancement strategy and have developed a melatonin textile transdermal patch based on the synergistic action of electret and permeation enhancer. The patch is designed with a three-layer composite structure, composed of a textile-based electret backing layer, a drug-loading pressure sensitive adhesive layer containing melatonin and permeation enhancer, and a protective layer to prevent drug leakage. Electret and permeation enhancer enhance transdermal efficiency through a physicochemical synergistic permeation-enhancement strategy without disrupting the skin barrier. In vitro studies revealed that among various permeation enhancers (menthol, azone, oleic acid) and electret parameters, the combination of a -1500 V electret with 10% oleic acid exhibited the optimal synergistic effect. In vivo pharmacokinetic studies demonstrated that the patch reached a peak plasma concentration (>30 ng/mL) within 1 h and maintained effective therapeutic levels (>5 ng/mL) for up to 8 h. The patch significantly improved the sleep quality in insomniac rats, with no observed skin irritation or cytotoxicity. This study not only accomplishes an efficient, non-invasive, and parametrically tunable transdermal delivery of melatonin but also validates the feasibility of synergistic enhancement through physical field regulation and chemical permeation, thereby providing a viable strategy for developing safe and long-acting textile-based transdermal drug delivery systems aimed at neuroendocrine small-molecule hormones similar to melatonin.

PMID 42922935
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PubMedPakistan journal of pharmaceutical sciences2026-10-25

Dose-dependent effects of transdermal fentanyl on hepatic structural integrity, biochemical function and markers of intrinsic mitochondrial apoptosis in rats.

Ozdemir Zeynep Z, Kurt Nurettin N, Keles Omer Faruk OF, Kilic Mehmet M et al.

Transdermal fentanyl is widely used for pain management; however, whether high systemic doses exert direct hepatotoxic effects or trigger intrinsic liver apoptotic pathways independently of systemic hypoxia remains unclear. This study aimed to investigate the dose-dependent effects of transdermal fentanyl on hepatic structural integrity, biochemical function and markers of intrinsic mitochondrial apoptosis (Bcl-2 and caspase-3) in rats. Thirty-two Wistar albino rats were randomly assigned to four groups (n = 8): a control group and three experimental groups treated with transdermal fentanyl at doses of 3.125 µg/kg/h (Group I), 6.25 µg/kg/h (Group II) and 12.5 µg/kg/h (Group III). Patches were applied to the abdominal region and replaced every 72 hours for nine days. At the end of the experiment, liver tissues were collected for biochemical and histopathological and molecular analyses of apoptotic markers. Apoptotic changes were assessed by measuring caspase-3 and Bcl-2 levels. Serum alanine aminotransferase (ALT) and total cholesterol levels were significantly higher in Group II and III than in the control group (p<0.05). Glucose levels were significantly increased in all fentanyl-treated groups (p<0.05). Total protein levels were significantly elevated in Group III compared to the control group (p<0.05). Lactate dehydrogenase (LDH) levels were significantly lower in Groups II and III (p<0.05). The anti-apoptotic marker Bcl-2 was significantly decreased in Group III compared with the other groups (p<0.05), whereas no statistically significant differences were observed in caspase-3 levels among any of the groups. No evident histopathological alterations were detected in liver tissues. High-dose transdermal fentanyl induces significant biochemical alterations and reduces Bcl-2 levels in rat liver tissue, suggesting a potential shift toward apoptotic signaling despite the absence of significant caspase-3 changes. However, short-term administration does not appear to cause evident histopathological damage.

PMID 42924983
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PubMedJCEM case reports2026-10-25

Endometriosis-associated lesions during or after long-term estrogen-only therapy following hysterectomy: 2 cases.

Sugimoto Daisuke D, Ishikawa Hiroshi H, Harada Miyuki M, Kaneda Natsuho N et al.

Estrogen-only menopausal hormone therapy (MHT) is prescribed after hysterectomy; however, occult or residual endometriotic tissue may remain hormonally responsive. We report 2 women in whom endometriotic lesions were identified during or after long-term transdermal estrogen-only MHT after hysterectomy and bilateral salpingo-oophorectomy. The first patient was a 48-year-old woman treated for International Federation of Gynecology and Obstetrics 2009 stage IA, grade 1 endometrioid endometrial carcinoma at 44 years of age. Her estrogen-progestogen MHT for treatment-related premature ovarian insufficiency was changed to transdermal estrogen-only MHT. About 3 years later, she developed a progressively enlarging ileocecal mass, with resection revealing endometriosis. The second patient was a 54-year-old woman who had undergone hysterectomy and bilateral salpingo-oophorectomy for endometriosis at 46 years of age. She received transdermal estrogen-only MHT for approximately 6 years and was diagnosed with atypical endometrial hyperplasia in vaginal cuff endometriosis 1 year after estrogen withdrawal. These observations do not establish a causal relationship between estrogen-only MHT and lesion development. Occult disease, residual disease, or iatrogenic implantation remain plausible explanations. Nevertheless, these cases highlight that new abdominal masses or posthysterectomy vaginal bleeding during or after MHT warrant careful evaluation with histopathologic confirmation. MHT should be individualized according to current clinical guidelines.

PMID 42923654
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