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diacerein + aceclofenac

✓ Approved

Glenmark Pharmaceuticals Limited · PTGS2 · 小分子

什么是 diacerein + aceclofenac？

diacerein + aceclofenac 是一种小分子，由Glenmark Pharmaceuticals Limited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

公司Glenmark Pharmaceuticals Limited
药物类别小分子
分子靶点PTGS2
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Glenmark Pharmaceuticals Limited

作用机制

分子靶点

diacerein + aceclofenac 作用于 1 个分子靶点：

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

diacerein + aceclofenac 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

PubMedJB & JS open access2026-09-06

A Comparison of Clinical Outcomes Among Undenatured Collagen Type II, Glucosamine Sulfate, and Diacerein on Osteoarthritic Knee Treatment: A Randomized Clinical Trial.

Narkbunnam Rapeepat R, Awirotananon Kit K, Chareancholvanich Keerati K, Achawakulthep Chaiwat C et al.

Knee osteoarthritis (OA) causes significant disability with limited effective treatments. Undenatured collagen type II (UC-II), prescription-grade crystalline glucosamine sulfate (pCGS), and diacerein have been proposed as alternatives to conventional analgesics, but their comparative efficacy remains uncertain. We hypothesized that each supplement would demonstrate superior efficacy over placebo in reducing total Western Ontario and McMaster Universities Arthritis Index (WOMAC) score at Week 24 in patients with mild-to-moderate knee OA. This 4-arm, randomized, double-blind, placebo-controlled trial enrolled 216 Thai adults with symptomatic knee OA (Kellgren-Lawrence grade 2-3). Participants received UC-II (40 mg once daily), pCGS (500 mg 3 times daily), diacerein (50 mg once to twice daily), or placebo for 24 weeks, with follow-up to 36 weeks. The primary outcome was total WOMAC score (22 items; pain, stiffness, and physical function; scored 0-220, higher = worse) at Week 24. Analyses followed intention-to-treat principles using multiple imputation by chained equations (m = 10) and linear mixed-effects models. Of 216 randomized Thai participants, 208 (96.3%) completed follow-up (mean age 61.7 ± 7.1 years; 90.9% female; 73.6% Kellgren-Lawrence grade 2). At Week 24, no supplement demonstrated superiority over placebo. Between-group differences in total WOMAC score were as follows: UC-II -4.7 (95% CI -18.6 to 9.1), pCGS -8.1 (95% CI -21.8 to 5.7), and diacerein -12.3 (95% CI -25.9 to 1.3). All 95% CIs included zero, and all point estimates were at or below, and none clearly exceeded, the minimum clinically important difference threshold. At 36 weeks, results were consistent: UC-II -1.8 (95% CI -15.5 to 12.0), pCGS -4.8 (95% CI -18.4 to 8.7), and diacerein -1.3 (95% CI -14.9 to 12.3). Secondary outcomes including pain scores, joint space width, and functional performance showed no significant between-group differences. Adverse events were mild and comparable across groups; no serious adverse events occurred. Among Thai patients with mild-to-moderate knee OA, UC-II, pCGS, and diacerein did not demonstrate superiority over placebo in reducing pain or improving function at 24 weeks. These findings do not support their routine use as monotherapy for knee OA. Thailand Clinical Trial Registry (TCTR20210901003). Therapeutic Level I. See Instructions for Authors for a complete description of levels of evidence.

PMID 42698930
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PubMedApplied biochemistry and biotechnology2026-08-20

Diacerein Protects Against Obesity-Related Cardiovascular Injury: Evidence from In Silico and In Vivo Studies.

Alatawi Shahad M SM, Aljadrawi Sara F SF, Alanazi Layan S LS, Aljohani Yara A YA et al.

Obesity constitutes a significant worldwide health challenge and a primary risk factor for cardiovascular diseases. Diacerein, an anti-inflammatory medication approved for osteoarthritis, is being studied as a potential modulator of inflammatory signaling. However, its role in obesity-associated cardiovascular injury remains incompletely understood. In the present study, computational docking and 300-ns MD simulations supported preferential, stable binding of diacerein to the TLR4 complex through a deep, hydrophobic, solvent-shielded pose, consistent with coordinated protein dynamics. Then, the cardioprotective effects of diacerein were examined in a high-fat diet (HFD)-induced obesity model. Male Sprague-Dawley rats were divided into three groups: normal control, HFD, and HFD combined with diacerein (50 mg/kg/day) for 10 weeks. Metabolic parameters, lipid profile, serum troponin I, and C-reactive protein (CRP) were evaluated. A histopathological examination of the heart and aorta was conducted, and the tissue levels of TLR4, MyD88, IRAK1, TRAF6, NF-κB, and downstream pro-inflammatory cytokines (IL-6 and TNF-α) were assessed. Inflammatory cell infiltration was evaluated using CD45 immunohistochemistry. The HFD led to insulin resistance, dyslipidemia, increased troponin I and CRP levels, and significant histological alterations in cardiac and aortic tissues, accompanied by the activation of the TLR4/NF-κB inflammatory pathway and enhanced inflammatory cell infiltration. Diacerein treatment markedly alleviated metabolic abnormalities, diminished cardiac injury and systemic inflammation, improved histological features, and reduced tissue protein levels of the TLR4/NF-κB pathway and pro-inflammatory cytokines. In conclusion, diacerein provides marked protection against obesity-induced cardiovascular injury, at least partially, by inhibiting the TLR4/NF-κB inflammatory pathway, supporting its potential as a therapeutic strategy for obesity-related cardiovascular complications.

PMID 42622962
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PubMedBiochemical pharmacology2026-08-19

Rhein alleviates lethal renal ischemia-reperfusion injury via inhibition of NLRP3 inflammasomes by targeting PPARγ.

Fu Cheng C, Hu Tianyi T, Zhao Xiangli X, Huang Yahui Y et al.

Rhein, an anthraquinone-derivative monomer isolated from the rhubarb plant, is the active ingredient of the drug Diacerein® (generic name: diacetylrhein), which possesses anti-inflammatory and antioxidant properties. It has been reported that rhein is effective in protecting against cerebral and retinal ischemia-reperfusion injury (IRI), but whether it can protect against renal IRI remains unknown. Here, a lethal renal IRI model was established with a 100 % mortality rate in untreated mice. Treatment with 100 mg/kg of rhein for 5 consecutive days before ischemia resulted in 100 % survival, maximal preservation of renal function, and a significant reduction in pathological damage, apoptosis and inflammation. In addition, rhein pretreatment significantly inhibited the upregulation of NLRP3, caspase-1, IL-1β and NGAL seen in the IRI control group. Through a series of experiments (including Co-Immunoprecipitation (Co-IP), pull-down, molecular dynamics simulation and surface plasmon resonance (SPR)), we confirmed that rhein has a strong binding affinity with PPARγ. By using the specific inhibitor T0070907 to block PPARγ, the protective effect of rhein on renal IRI in vivo and the protective effect on cell damage in the NLRP3 inflammasome activation model induced by (LPS + Nig) in vitro can be largely eliminated. We demonstrate here that rhein can potently protect against lethal renal IRI in mice. This protection is mainly achieved by targeting and enhancing the expression of PPARγ, thereby inhibiting the activation of the NLRP3 inflammasome. Thus, rhein may be therapeutically useful for the clinical prevention and treatment of renal IRI.

PMID 42617753
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PubMedRSC advances2026-08-13

Development and characterization of aceclofenac-LDH/alginate porous microspheres for pH-responsive drug release.

Chen Yanling Y, Wu Xiaowen X

The antipyretic and anti-inflammatory drug aceclofenac (ACF) causes the serious side effect of adverse gastrointestinal reactions. With the aim to provide sustained action and prevent drug release into the stomach, aceclofenac-LDH/alginate porous microspheres were developed via an emulsion method to achieve sustained and pH-responsive drug release. The obtained microspheres were characterized by XRD, SEM, FT-IR, and TG-DSC. The SEM images show a porous morphology of microspheres with diameters of 2 µm. TG-DSC data prove that the thermal stability was greatly increased by the interaction of the LDH and alginate. In vitro drug release was studied in PBS (pH 7.4 and 4.0) at 37 °C. Compared with the physical mixture and ACF-LDH nanohybrids, ACF release from the porous LDH/Alg microspheres was 50% (pH 4.0) within 16 h, whereas 62% of the drug was released at pH 7.4, indicative of a sustained and pH-responsive drug release profile.

PMID 42592196
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PubMedBioorganic chemistry2026-08-07

Discovery of a novel twin drug from Phillygenin and glucosamine for osteoarthritis treatment.

Zhang Jiajing J, Lv Xinxin X, Sun Yicong Y, Lu Jie J et al.

The search for novel anti-OA agents that combine high efficacy with long-term safety remains a great challenge. Herein, we wish to disclose the distinct combined effect of TCM-derived lipophilic phillygenin and naturally-occurred hydrophilic glucosamine (GlcN) in OA treatment, which enables the subsequent design and syntheis of a series of twin drugs from these two OA therapeutic agents via the formation of glycosidic bond and further derivatization of amine group. Among them, twin drug 6 with an unsubstituted amine group and β-configuration exhibited the nost significant and dose-dependent in vivo anti-OA activity while no apparent toxicity was observed. In particular, it displayed comparable therapeutic efficacy and more favorable safety profiles compared to the clinically-used diacerein (DIA) and functions via multiple cellular mechanisms ranging from osteoclast differentiation inhibition and anti-inflammation/anti-oxidation to cartilage protection. Overall, our findings highlight 6 as a promising candidate for anti-OA drug discovery.

PMID 42561561
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PubMedPhytomedicine : international journal of phytotherapy and phytopharmacology2026-07-21

Innovative rhein and hydroxy fatty acid ester prodrugs for the treatment of chronic inflammation.

Han Lu L, Zang Tao T, Li Zhi-Peng ZP, Deng Yao Y et al.

Chronic inflammation is related to heart disease, diabetes, cancer, arthritis, and bowel diseases. The rhubarb-derived natural product rhein is highly effective at treating chronic inflammation. However, the gastrointestinal side effects and liver disorders of rhein have limited the long-term clinical application. Herein, we developed a series of rhein-hydroxy fatty acid prodrugs to alleviate the side effects of rhein while enhancing its therapeutic activity. We developed a novel method to overcome the side effects of rhein and enhance its pharmacological activity. The aim was to synthesize rhein hydroxy fatty acid ester prodrugs that retain anti‑inflammatory activity and alleviate gastrointestinal side effects. A series of rhein hydroxy fatty acid ester prodrugs were synthesized by linking rhein with hydroxy fatty acid. The chemical structure of these prodrugs was characterized by Fourier transform infrared spectroscopy (FTIR), hydrogen proton nuclear magnetic resonance (1H NMR), and high-resolution mass spectrum (HRMS). The cytotoxicity of rhein-hydroxy fatty acid ester prodrugs was evaluated using RAW 264.7 and Caco-2 cells. Additionally, in vitro anti-inflammatory, antioxidant, and anti-apoptotic effects were assessed. The targeted rhein-hydroxy fatty acid ester prodrug was verified using the DSS-induced mouse colitis model. In vitro studies demonstrate that the target compound R-15HA is markedly superior to both the free drug and diacerein in mitigating inflammation, oxidative damage, and apoptosis, while showing almost no cytotoxicity at final concentrations below 160 μmol·L⁻¹. Furthermore, Western blot analysis revealed that R-15HA inhibited the TLR4/NF-κB/MAPK more effectively than free rhein and 15-hydroxypentadecanoic acid. Molecular dynamics simulations demonstrated that the R-15HA compound exhibits a good binding capability with the TLR4 protein. Rhein can partially prevent weight loss, liver and spleen indices colon shortening, expression of proinflammatory cytokines, and epithelial damage, while rhein-hydroxy fatty acid prodrugs R-15HA have a more pronounced effect than rhein in dextran sulfate sodium (DSS)-induced colitis. Overall, our novel rhein-hydroxy fatty acid ester prodrugs are promising candidates for chronic inflammation in clinical therapy. This study might reveal an avenue to develop rhein hydroxy fatty acid ester prodrugs with satisfactory pharmacological activity to resolve various inflammatory diseases.

PMID 42475871
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