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ketoprofen (Diractin / ketoprofen, IDEA / Diractin)

✓ Approved

IDEA AG · PTGS1 · 小分子

什么是 ketoprofen？

ketoprofen 是一种小分子，由IDEA AG研发。该药已获批，用于治疗相关适应症，给药途径：Topical、Transdermal。

药物档案

商品名Diractin, ketoprofen, IDEA, Diractin
公司IDEA AG
药物类别小分子
分子靶点PTGS1, PTGS2
给药途径Topical, Transdermal
状态Approved
来源： ClinicalTrials.gov, IDEA AG

作用机制

分子靶点

ketoprofen 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

ketoprofen 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Musculoskeletal and connective tissue disordersMusculoskeletal pain✓ Approved

相关研究文献

PubMedAntibiotics (Basel, Switzerland)2026-07-27

Suppression of Quorum Sensing and Virulence Factors by Meloxicam and Celecoxib in Methicillin-Resistant Staphylococcus aureus Clinical Isolates.

Ali Reham R, El-Domany Ramadan A RA, Shaaban Mona I MI

Background:Staphylococcus aureus is a major cause of life-threatening infections, and increasing antimicrobial resistance necessitates alternative therapeutic strategies. This study evaluated the antiquorum sensing and antivirulence activities of selected nonsteroidal anti-inflammatory drugs (NSAIDs) against S. aureus clinical isolates by targeting the accessory gene regulator (agr). Methods: Antimicrobial susceptibility and virulence factor production were evaluated in 56 S. aureus clinical isolates. The MICs of six NSAIDs (Diclofenac, ketoprofen, ketorolac, meloxicam, indomethacin and celecoxib) were determined by broth microdilution, and the effects of sub-MICs (½ and ¼ MIC) on virulence factors were assessed. The expression of agrA, hlb, and hld was analyzed by qRT-PCR, and molecular docking was performed to evaluate interactions with AgrA receptor. Results: Among the isolates, high resistance rates were accompanied with cefoxitin, ceftazidime, and cefepime. Hemolysin, protease, and lipase production were detected in 42.86%, 89.28%, and 94.64% of isolates, respectively. Meloxicam and celecoxib at sub-MIC levels significantly reduced hemolysin, protease, and lipase activities. Additionally, both drugs markedly downregulated agrA expression by 88.9-95.3% and significantly reduced hlb and hld expression by 90.5-99.9% without affecting bacterial growth. Molecular docking demonstrated favorable binding interactions with AgrA. Conclusions: Meloxicam and celecoxib could be promising adjunctive therapies against S. aureus through suppression of the Agr-regulated virulence traits.

PMID 42505670
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PubMedPharmaceutical research2026-07-18

Mechanistic Insights into Membrane- and Release-Controlled Drug Permeation from Ketoprofen-Lidocaine Eutectic Fluids.

Sugino Masahiro M, Igarashi Yui Y, Shiina Suzuka S, Nakadate Shou S et al.

Eutectic fluids (EFs) are liquid pharmaceutical systems formed through intermolecular interactions between their components. This study aims to clarify the mechanistic basis of membrane- and release-controlled drug permeation from the ketoprofen-lidocaine (KP-LD) EFs by characterizing their physicochemical properties and molecular interactions. Two types of liquid EFs were prepared by mixing and heating KP with LD. The prepared EFs were characterized using thermodynamic, rheological, and NMR-based analyses to obtain parameters related to phase behavior, viscosity, molecular dynamics, and molecular diffusion. Silicone membrane permeation behavior was evaluated to elucidate how these physicochemical properties influence membrane‑controlled and release‑controlled drug permeation. Differential scanning calorimetry indicated the absence of detectable crystallinity, and the mixtures appeared to form a homogeneous liquid phase. Rheological analysis revealed a Newtonian flow behavior, and the viscosity of EFA (KP:LD = 1:1) was markedly lower than that of EFB (KP:LD = 2:1). Permeation studies showed KP permeation was membrane-controlled, whereas LD permeation was release-controlled within the EFs, allowing for the calculation of its diffusion coefficient. Analyses of 1H-1H NOESY and DOSY suggested close spatial proximity and weak intermolecular interactions, indicating cooperative molecular dynamics between KP and LD. EFs examined in this study can accommodate a high drug content and function as reservoirs of active pharmaceutical ingredients. In particular, EFA exhibited unique physicochemical and permeation properties that are not observed in aqueous solutions or conventional formulations, suggesting its potential as a novel EF system for transdermal drug delivery.

PMID 42469514
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PubMedThe journal of physical chemistry. B2026-07-18

Breaking Permeation Barriers of Charged Molecules with Excess Permeation Enhancers.

Bernaldez Mabel M, Kang Christopher C, Stamatis Stephen D SD, Rose John P JP et al.

Permeation enhancers (PEs) are a class of amphiphilic molecules that promote the passive permeation of drug molecules through cellular membranes. There is currently a lack of understanding of the mechanism of action for permeation enhancers. Two PEs are studied in this manuscript, sodium caprate (C10) and salcaprozate sodium (SNAC), which are commonly used in coformulations and clinical trials. All-atom molecular dynamics simulations are carried out to probe their interactions with a membrane made of POPC. The permeation of water and three charged small molecule drugs (ketoprofen, propranolol, and salicylic acid) through a PE-embedded POPC membrane is studied. The results show that 1) the lipid bilayers can be saturated with PEs up to 250 mol % without losing structural integrity, 2) PEs embedded in the membrane facilitate the insertion of water into the tail groups in the center of the membrane, and 3) charged molecules, which are known to have a prohibitively high free energy barrier of permeation, have a significantly decreased free energy barrier of permeation in the presence of high concentration of PEs. Hydrogen bond contacts made between PEs and water molecules with the charged molecules when they are in the center of the membrane are primarily responsible for the decrease in the free energy barrier. This study provides insight about the permeation of larger molecules, which may have multiple charged states, namely peptides.

PMID 42468514
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PubMedCrystal growth & design2026-07-13

Norfloxacin-NSAID Pharmaceutical Salts: Structure-Property Relationships for Enhanced Solubility and Stability.

Belmont-Sánchez Jeannette Carolina JC, Alarcón-Payer Carolina C, Frontera Antonio A, Acebedo-Martínez Francisco Javier FJ et al.

The use of antibiotics is usually associated with mucosal damage and antimicrobial resistance due to inefficient dosing. This issue is particularly relevant for norfloxacin (NOR), whose amphoteric nature leads to strongly pH-dependent solubility and low oral bioavailability. To overcome these limitations, this work presents three novel drug-drug pharmaceutical salts of NOR with the anti-inflammatory drugs ketoprofen (KET), dexketoprofen (DKT), and niflumic acid (NIF). Salts were synthesized by mechanochemical and slurry strategies and fully characterized using thermal, spectroscopic, and X-ray diffraction techniques. The crystal structure, along with DFT and QTAIM computational analyses, showed that salts are governed by tetrameric assembly formation. However, while NOR-KET and NOR-DKT are stabilized by robust charge-assisted hydrogen bonds, NOR-NIF packing arrangement is dominated by weaker hydrogen bonds together with π-π and CF3···π interactions. These supramolecular differences were directly reflected in the pharmaceutical performance. The salts suppressed the rapid hydration of NOR under aqueous environments and showed improved stability at physiological pH. Moreover, NOR-KET and NOR-DKT significantly enhanced the solubility of both NOR and the corresponding NSAIDs in PBS at pH 6.8, while all salts provided a more controlled NOR dissolution profile under acidic conditions. These findings demonstrate that salt formation is an effective strategy to overcome the solubility and stability limitations in NOR and NSAIDs, offering a framework for improving the performance not only of NOR but also of other APIs facing similar challenges.

PMID 42441081
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PubMedPreventive veterinary medicine2026-07-12

Use of non-steroidal anti-inflammatory drugs for Finnish sows.

Hokkanen Ann-Helena AH, Swan Kirsi K, Ahlqvist Kristina K, Hedlund Milla M et al.

Farrowing, diseases, and injuries all cause acute nociceptive pain to sows. Pain can strain the body, cause negative emotions and poor welfare, slow healing, and hinder piglet health and growth. Non-steroidal anti-inflammatory drugs (NSAIDs) are efficient and practical in alleviating nociceptive pain in sows, although more research about the efficiency, safety, and use in practice is needed. Thus, this observational, retrospective, cross-sectional, register-based study aimed to describe veterinary instructions for NSAID use in Finnish sow herds and to compare them with recorded use during January-December 2022. We also explored, using logistic regression, whether herd type or size was associated with NSAID use. A total of 70% of the 50 study herds had written veterinary instructions for NSAID use for sows. Although widespread, NSAID use was highly variable. Most herds administered pain alleviation to sows frequently, while five herds reported no NSAID use. Most often, ketoprofen or meloxicam was used to treat sows having anorexia without other symptoms, farrowing-related disorders and diseases, reproduction problems, or musculoskeletal diseases. Caretakers also administered NSAIDs for indications not instructed by the herd health veterinarian and used treatment durations longer than instructed. The median number (interquartile range, IQR) of total NSAID (ketoprofen plus meloxicam) treatment courses per sow was 0.35 (1.52), and the median number of NSAID doses used per 100 sows per day (NSAID_DDD_100) was 0.22 (IQR 0.58) in the study herds. Neither herd type nor herd size was associated with NSAID use.

PMID 42435675
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PubMedJournal of veterinary pharmacology and therapeutics2026-07-11

The Impact of Ketoprofen on the Pharmacokinetics of Marbofloxacin at Variable Intravenous Doses in Sheep.

Uslu Muhittin M, Canbar Rahmi R, Corum Orhan O, Durna Corum Duygu D et al.

The objective of this study was to determine the effect of ketoprofen (3 mg/kg, IV) on the pharmacokinetics of marbofloxacin administered intravenously at 2 and 10 mg/kg in sheep, and to identify possible changes in key pharmacokinetic parameters when combined. Twelve healthy Merino sheep were enrolled in a two-stage crossover pharmacokinetic study. Each animal received intravenous marbofloxacin at 2 and 10 mg/kg, administered either alone or in combination with ketoprofen (3 mg/kg, IV). Blood samples were collected over 48 h, and plasma marbofloxacin levels were measured using HPLC-UV. Pharmacokinetic parameters were calculated by non-compartmental analysis. Compared to the 2 mg/kg dose, the AUC and t1/2ʎz increased and ClT decreased at the 10 mg/kg dose of marbofloxacin (p < 0.05). Combination administration with ketoprofen decreased ClT and Vdss values in both dose groups, and increased AUC and t1/2ʎz values (p < 0.05). Ketoprofen significantly alters marbofloxacin's pharmacokinetic parameters, increasing its systemic exposure. It is thought that the increased AUC, especially with high-dose or combined administration, may enhance antibacterial efficacy by raising the AUC/MIC ratio. Potential drug interactions should be considered in clinical practice.

PMID 42432991
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