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ketoprofen (Menamin SR / ketoprofen, Biovail / Oruvail)

✓ Approved

Roche · PTGS1 · Small Molecule

What is ketoprofen?

ketoprofen is a small molecule developed by Roche. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesMenamin SR, ketoprofen, Biovail, Oruvail
CompanyRoche
Drug ClassSmall Molecule
Molecular TargetPTGS1, PTGS2
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Roche

Mechanism of Action

Molecular Targets

ketoprofen acts on 2 molecular targets:

PTGS1prostaglandin-endoperoxide synthase 1 (COX3, PCOX1)
PTGS2prostaglandin-endoperoxide synthase 2 (GRIPGHS, hCox-2)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

ketoprofen is developed for 2 unique indications across 2 therapeutic areas.

Therapeutic AreaConditionPhase
Gastrointestinal disordersAbdominal pain✓ Approved
Hepatobiliary disordersHepatitis✓ Approved

Related Research Articles

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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PubMedEnvironmental health and preventive medicine2026-07-06

Occurrence of antibacterials, antivirals, and anti-inflammatory pharmaceuticals for COVID-19 treatment as emerging contaminants in the Chinese freshwater environment before, during and after the pandemic: the need for dynamic eco-pharmacovigilance.

Ma Sijia S, Chen Hongxia H, Wang Jun J

Global epidemic diseases such as COVID-19 have driven both the excessive use of pharmaceuticals and shifts in their usage spectrum. Consequently, the profile of pharmaceuticals in the environment (PiE) may undergo dynamic temporal changes, posing a significant challenge to eco-pharmacovigilance (EPV), a specialized branch of pharmacovigilance focused on detecting, evaluating, understanding, and preventing the adverse environmental effects of pharmaceuticals. Based on data extracted from 89 studies published between 2014 and 2025, this review conducts a focused comparison of the occurrence patterns of 43 selected typical anti-COVID-19 drugs (20 antibacterials, 11 antivirals, and 12 anti-inflammatory pharmaceuticals) as contaminants in distinct regions across China's seven major river basins before, during, and after the pandemic. The need of dynamic EPV was then analyzed. Before the COVID-19 outbreak, erythromycin, ampicillin, roxithromycin, and acetaminophen dominated the PiE profile in terms of reported maximum residual concentrations; during the pandemic lockdown, ciprofloxacin, ofloxacin, azithromycin, and ketoprofen were identified as the top-priority anti-COVID-19 PiE; after the pandemic, azithromycin, norfloxacin, ofloxacin, ciprofloxacin, and roxithromycin remained the dominant PiE. Residual levels of individual PiE at the same location varied noticeably across the three periods. Results revealed highly distinct regional and temporal variations in surface freshwater pollution by these COVID-19-associated PiE across the three periods, with no consistent regularity observed, thereby further highlighting the necessity of implementing EPV in a "dynamic" manner. Drawing on the framework of dynamic pharmacovigilance, the implementation of dynamic EPV can be promoted by establishing a dynamic watch-list mechanism, clarifying stakeholder roles, and advancing supportive policies and technological platforms, so as to enable adaptive interventions for the timely management of event-driven pharmaceutical pollution.

PMID 42402418
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PubMedInternational journal of pharmaceutics2026-06-27

Cyclodextrin inclusion as a pharmaceutical reaction field: kinetic, pathway and structural control beyond equilibrium.

Hiroshige Ryosuke R, Goto Satoru S

Cyclodextrins (CDs) are widely used pharmaceutical excipients typically evaluated within equilibrium thermodynamic frameworks. However, many degradation processes, including radical-driven oxidation, photochemical reactions, and tautomerism-coupled instability, proceed under nonequilibrium conditions that cannot be fully explained by binding constants alone. This review presents CDs as molecular-scale reaction fields that modulate kinetic accessibility, pathway competition, and structural population distributions. Using three representative systems, we illustrate distinct modes of control: kinetic suppression of radical encounters in edaravone oxidation, pathway reorganization in ketoprofen photochemistry revealed by singular value decomposition (SVD), and structural equilibrium bias in avobenzone. By integrating kinetic analysis, time-resolved spectroscopy, and multivariate approaches, we present evidence that CDs can regulate reaction behavior beyond equilibrium complexation. This framework provides a basis for understanding formulation-dependent stability and offers design principles for CD-enabled stabilization strategies under nonequilibrium conditions.

PMID 42362000
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PubMedToxicology and applied pharmacology2026-06-24

Membrane-mediated mechanisms of NSAID-induced cardiotoxicity independent of cyclooxygenase selectivity: Evidence from rat and zebrafish models.

Jha Akash Kumar AK, Subramaniyan Vetriselvan V, Gupta Stuti S, Kumari Rishika R et al.

Non-steroidal anti-inflammatory drugs (NSAIDs) are associated with cardiovascular adverse events that are not fully explained by cyclooxygenase (COX) inhibition. Here, we investigated the contribution of membrane-mediated mechanisms to NSAID-induced toxicity using integrated in vivo, developmental, and biophysical approaches. Ketoprofen, indomethacin, and celecoxib were evaluated in rats (serum biomarkers and histopathology) and zebrafish embryos (cardiac function), alongside mechanistic studies in cardiac-mimicking lipid membranes using differential scanning calorimetry, NMR spectroscopy, and molecular dynamics simulations. Ketoprofen significantly increased serum creatine kinase and lactate dehydrogenase levels and induced moderate myocardial damage. Indomethacin produced minimal changes in circulating biomarkers but caused mild-to-moderate histological alterations. Celecoxib showed limited toxicity in adult tissues but significantly reduced zebrafish heart rate, indicating pronounced developmental cardiotoxicity. In membrane systems, ketoprofen increased transition temperature and enthalpy, consistent with bilayer condensation and enhanced lipid order. Celecoxib decreased transition enthalpy and increased vesicle heterogeneity, indicating membrane destabilization. Indomethacin reduced transition cooperativity with modest effects on bilayer structure. NMR and simulation data supported differential drug-insertion and lipid-interaction profiles. These findings demonstrate that NSAIDs exhibit compound-specific toxicity profiles that depend on biological context and are linked to distinct drug-membrane interactions. Membrane perturbation represents a COX-independent mechanism contributing to NSAID-associated cardiotoxicity and provides a framework for integrating molecular and organism-level toxicological responses.

PMID 42336296
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