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ketoprofen (Menamin SR / ketoprofen, Biovail / Oruvail)

✓ Approved

Roche · PTGS1 · 小分子

什么是 ketoprofen？

ketoprofen 是一种小分子，由Roche研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Menamin SR, ketoprofen, Biovail, Oruvail
公司Roche
药物类别小分子
分子靶点PTGS1, PTGS2
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Roche

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 2 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Gastrointestinal disordersAbdominal pain✓ Approved
Hepatobiliary disordersHepatitis✓ Approved

相关研究文献

PubMedInternational ophthalmology2026-09-06

Neuroprotective effects of ketamine, lamotrigine, and ketoprofen combinations after pars plana vitrectomy and silicone oil injection.

Paques Mila W MW, Bellanda Victor V, Guizzo Renato R, Siqueira Rubens C RC et al.

This experimental study aims to assess the protective impact of combined treatment with ketamine (KTM), lamotrigine (LMT), and ketoprofen (KTP), agents that have demonstrated neuroprotective properties in other experimental contexts, on rabbit retinas in an experimental model of pars plana vitrectomy (PPV) and silicone oil injection (SOI). Thirty-six rabbits were divided into six treatment groups: saline, KTP, KTM+LMT, KTM+KTP, LMT+KTP, and KTM+LMT+KTP. All rabbits underwent PPV and SOI in the right eye. The left eyes served as negative controls. Histological assessments were conducted to evaluate cell densities and structural changes in the ganglion cell layer (GCL), the inner nuclear layer (INL), and the outer nuclear layer (ONL). Apoptosis was evaluated using the TUNEL method. The KTP group exhibited reduced apoptosis and partial protection in all retinal layers. The KTM+LMT combination significantly protected the GCL. The KTM+KTP group showed notable protection in the INL. The LMT+KTP combination was effective for both the INL and GCL. The KTM+LMT+KTP combination provided the most comprehensive protection across the ONL and INL. The cell densities in the ONL, INL, and GCL were significantly greater in the treatment groups than in the positive control group. The combination of KTM, LMT, and KTP exhibited significant neuroprotective effects on rabbit retinas following PPV and SOI. These findings suggest the potential of this combination treatment as a therapeutic strategy for retinal pathologies.

PMID 42700282
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PubMedJournal of translational medicine2026-09-04

Adipose tissue plays a crucial role in obesity-induced postoperative neurocognitive disorders.

Tropis Clémence C, Labaste François F, Sallese Marie M, Dortignac Alizée A et al.

Postoperative neurocognitive disorder (PND) is characterized by cognitive deficits that emerge after surgery. Although often reversible within weeks or months, PND can persist and lead to significant central dysfunction and an increased risk of dementia. Given that obesity is a chronic low-grade inflammatory condition previously associated with structural and functional brain alterations, we hypothesized and demonstrated that it could be a significant risk factor for PND. We assessed the incidence of PND and cognitive performance in obese individuals undergoing cardiac or orthopedic surgeries. In parallel, we developed a preclinical model combining diet-induced obesity in mice with surgically induced tibial fracture. Pharmacological (ketoprofen), surgical (adipose tissue ablation), and behavioral (calorie restriction) interventions were used to target obesity-associated inflammation. Compared with nonobese individuals, obese patients presented a greater incidence of early postoperative cognitive changes and lower cognitive performance (p < 0.009). In mice, the combination of obesity and surgery results in exacerbated signs of PND. Importantly, obesity-related PND in mice was prevented by interventions that reduced central and systemic inflammation. These findings identify obesity-driven fat mass and inflammation as strong risk factors for PND for the first time. Targeting obesity-associated inflammatory mechanisms may represent an effective strategy to reduce the incidence of this debilitating postoperative condition.

PMID 42693469
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PubMedAnimal reproduction science2026-09-03

Combined hCG and ketoprofen treatment improves dairy cow pregnancy rates through proposed complementary mechanisms: Luteal metabolic reprogramming and endometrial PGF2α suppression.

Kolachi Hubdar Ali HA, Zhang Xiaomeng X, Shahzad Muhammad M, Ayantoye Jesse Oluwaseun JO et al.

We investigated whether combining human chorionic gonadotropin (hCG) with ketoprofen after timed artificial insemination (TAI) improves pregnancy rates and explored the underlying mechanisms through serum metabolomics and in vitro endometrial cell analysis. Dairy cows (n = 710) were allocated to three groups: hCG + ketoprofen (1500 IU hCG on day 7 and ketoprofen at 3 mg/kg on days 15-16 of TAI; n = 249), hCG only (1500 IU hCG on day 7 of TAI; n = 246), or control (n = 215). After adjusting for parity, days in milk, body condition score, and milk yield using multivariable logistic regression, the overall treatment effect was significant (χ² = 7.24, df = 2, P = 0.027). The hCG + ketoprofen group had a higher pregnancy rate than the control (adjusted OR = 1.63; 95% CI: 1.12-2.37; P = 0.028, Tukey-adjusted). However, the hCG-only group did not differ significantly from the control group (adjusted OR = 1.15; 95% CI: 0.79-1.68; P = 0.756, Tukey-adjusted). Serum metabolomic profiling by liquid chromatography-mass spectrometry (LC-MS) identified 17 significantly differential metabolites between hCG + ketoprofen and hCG only groups, with KEGG pathway enrichment revealing unsaturated fatty acid biosynthesis as the most prominently altered pathway. In lipopolysaccharide (LPS) challenged bovine endometrial epithelial cells (BEECs), ketoprofen significantly enhanced cell viability (0.5998 ± 0.0043 vs. 0.4498 ± 0.0037; p < 0.0001), reduced reactive oxygen species (ROS) accumulation, and suppressed PGF2α secretion by 36% (29.2 ± 2.77 vs. 45.6 ± 5.36 pg/mL; p < 0.0001). Additionally, ketoprofen downregulated the expression of key prostaglandin synthesis and steroidogenesis genes, including PTGS2, PLA2G4A, PTGFR, VEGFA, STAR, and CYP11A1. These findings suggest that hCG + ketoprofen treatment may enhance pregnancy rates through potentially complementary mechanisms, though these proposed mechanisms remain hypothetical and require in vivo confirmation.

PMID 42691782
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PubMedTranslational sports medicine2026-09-03

Topical Analgesic Therapies for Acute, Sports-Associated Soft Tissue Injuries.

Howard Mitchell S MS, Lee-Smith Wade W, Reinert Justin P JP

Acute musculoskeletal injuries are common among sports participants and are frequently treated with topical analgesics; however, the comparative efficacy and safety of topical formulations remain under investigation. The objective of this study was to evaluate the efficacy and safety of topical nonsteroidal anti-inflammatory drugs (NSAIDs) and alternative topical therapies in the management of acute sports-associated soft tissue injuries, including sprains, strains, contusions, and soreness. A systematic review and meta-analysis were conducted following Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) criteria, including randomized controlled trials that evaluated topical NSAIDs or other topical analgesics in patients with acute sports-related musculoskeletal injuries. Bias was assessed with the RoB-2 tool. The primary efficacy outcome was reduction in pain, measured by the visual analog scale (VAS) or similar validated tools, while the primary safety outcome was the incidence of treatment-emergent adverse effects. Eight randomized controlled trials comprising 1027 patient encounters met inclusion criteria. Across studies, topical diclofenac, ibuprofen, ketoprofen, and etofenamate demonstrated statistically significant reductions in VAS pain scores compared with placebo. Meta-analysis of all included trials revealed no significant reduction in pain intensity in active topical interventions versus placebo (95% CI -0.3768-5.2806; p = 0.09). A direct comparative analysis of diclofenac versus other NSAIDs did not demonstrate a statistically significant difference (effect size -2.07; 95% CI -5.60-1.46; p = 0.25), though heterogeneity of studies may limit these findings. Adverse effects were primarily mild and localized and were no different between groups (RR = 0.79; 95% CI 0.45-1.39; p = 0.41). Topical NSAIDs and alternative topical formulations may provide improved pain outcomes but did not show superiority between NSAID agents.

PMID 42688406
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PubMedDaru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences2026-09-01

Antifungal activities and toxicity studies of water-soluble non-steroidal analgesic salts.

Arrieta Julian Gonzalo JG, Carrizo Natali Ivana NI, Aguilar Franco Augusto FA, Garcia Pitalluga Guillermo Antonio GA et al.

The emergence of antifungal resistance among Candida albicans strains poses a growing clinical challenge, underscoring the urgent need for alternative therapeutic strategies. Drug repositioning of non-steroidal anti-inflammatory drugs (NSAIDs) has attracted attention due to their reported antimicrobial properties and well-established safety profiles. This study aimed to synthesize and characterize water-soluble sodium salts of ibuprofen (IBU-Na), ketoprofen (KET-Na), and indomethacin (IM-Na), and to evaluate their antifungal activity and toxicity profiles, individually and in combination with fluconazole (FLU), against C. albicans strains. NSAID sodium salts were synthesized and characterized, and their antifungal activity, synergistic interactions with FLU, and toxicity profiles were evaluated against FLU-susceptible and -resistant C. albicans strains. IBU-Na and KET-Na exhibited inhibitory and fungicidal activities against both FLU-susceptible and -resistant C. albicans strains, whereas IM-Na was inactive. Combination assays revealed strong synergistic interactions with FLU (FICI = 0.008-0.009), resulting in marked reductions in fungal viability. Neither hemolytic activity nor genotoxic effects were detected at the tested concentrations. Water-soluble NSAID salts, particularly IBU-Na, demonstrate potent synergistic antifungal activity with FLU and favorable safety profiles, supporting their potential as candidates for antifungal drug repurposing. These findings emphasize the importance of reassessing sodium salt derivatives rather than assuming equivalence with their acidic precursors.

PMID 42675329
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PubMedThe journal of pain2026-08-17

Behavioral depression induced by dental pain in mice and its resistance to analgesics.

Filippini Helena F HF, Taylor Kaia K, Negus S Stevens SS

Acute dental pain contributes to ∼10% of opioid analgesic prescriptions in the U.S., highlighting a critical need for safer, non-opioid alternatives. This study supports the NIH HEAL initiative by developing a preclinical model to investigate behavioral depression as one class of behavioral signs that are both caused by dental pain and useful for analgesic discovery. Specifically, we assessed depression of locomotor and oral activity and stimulation of postural hunching and facial grimace as pain-related behaviors produced by a set of dental-pain manipulations. We then evaluated effectiveness of the nonsteroidal anti-inflammatory drug ketoprofen and opioid agonist morphine to alleviate these behavioral effects. Male and female ICR mice received one of four dental-pain manipulations: (1) Control - anesthesia only, (2) Open -pulp exposure, (3) Closed-Sal - pulp exposure with saline-soaked point and sealing, (4) Closed-CFA - pulp exposure with complete Freund's adjuvant-soaked point and sealing. Locomotor activity along with posture and grimace scores were assessed 6 h after surgery. Retrieval and consumption of sunflower seeds were assessed after 24 h to assess oral activity required to crush the hull and extract the kernel. Relative to control treatment, dental-pain manipulations produced significant, graded depression of locomotion and seed retrieval/consumption (Open

PMID 42607824
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