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diacerein + aceclofenac

✓ Approved

Glenmark Pharmaceuticals Limited · PTGS2 · Small Molecule

What is diacerein + aceclofenac?

diacerein + aceclofenac is a small molecule developed by Glenmark Pharmaceuticals Limited. It is approved for therapeutic indications via oral (po).

Drug Profile

CompanyGlenmark Pharmaceuticals Limited
Drug ClassSmall Molecule
Molecular TargetPTGS2
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Glenmark Pharmaceuticals Limited

Mechanism of Action

Molecular Targets

diacerein + aceclofenac acts on 1 molecular target:

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

Therapeutic Indications

diacerein + aceclofenac is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Musculoskeletal and connective tissue disordersMusculoskeletal pain✓ Approved

Related Research Articles

PubMedCardiovascular toxicology2026-10-12

Targeting NF-κB/TLR4/ERK/MYD88 and Caspase-1/IL-1β Pathways by Diacerein in Alleviation of 5-Fluorouracil-Induced Myocardial, Corneal, and Retinal Injury.

Refaie Marwa Monier Mahmoud MMM, Ibrahim Randa Ahmed RA, Hasan Asmaa A AA, Muhammed Asmaa A AA et al.

Chemotherapeutic agents, including 5-fluorouracil (5-FU), are widely used to treat various types of malignant disorders, but cardiac injury limits their clinical benefit. Thus, we aimed to evaluate the usefulness of diacerein (DIA) in alleviating 5-FU myocardial and ocular injury. 50 male Wistar rats were included in the current model, and 5-FU was administered as a single intraperitoneal dose (150 mg/kg) on the first day of the study to induce myocardial and ocular injury, followed by co-administration of DIA (25, 50 mg/kg/day) by oral gavage for 7 days. 5-FU-induced myocardial and ocular injury was detected as structural changes in cardiac, corneal, and retinal tissues, with significant increases in the cardiac injury biomarkers, toll-like receptor 4 (TLR4), extracellular signal-regulated kinase (ERK), total oxidant status (TOS), oxidative stress index (OSI), nuclear factor kappa b (NF-κB), interleukin 1β (IL-1β), caspase-3, and caspase-1 expressions. Conversely, there were marked decreases in the serum total antioxidant capacity (TAC) and toxic features in the histopathological evaluation. However, co-administration of DIA ameliorated 5-FU-induced toxic effects and improved biochemical and structural changes. This beneficial effect of DIA is attributed to its ability to modulate the NF-κB/TLR4/ERK/caspase-1/IL-1β pathway, suppressing apoptosis and oxidative stress. DIA may be a future adjuvant medical therapy to reduce 5-FU side effects.

PMID 42860469
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PubMedCurrent rheumatology reviews2026-09-15

A Randomized Controlled Trial: Efficacy of Wangbi Capsule Plus Conventional Therapy for Knee Osteoarthritis and Its Modulation of the Ferroptosis Pathway.

Wang Xiaoqing X, Wang Mei M, Zhao Zhenyi Z, Wen Zhong Z et al.

Knee osteoarthritis (KOA) is a prevalent degenerative disease lacking structural disease-modifying agents. According to TCM theory, its progression involves internal liver-kidney deficiency and external qi/blood stasis with meridian obstruction. We evaluated Wangbi Capsule (WBC) plus diacerein/glucosamine vs. controls (n=180) over 12 weeks. Primary: WOMAC change; secondary: VAS, Lequesne, PhGA, HAQ. In an exploratory subgroup (n=75), PBMC mRNA for GPX4, SLC7A11, ACSL4, plus ESR, hs-CRP, and β-CTX were measured. WBC yielded superior WOMAC reduction (17.77 vs. 22.81, P=0.025), higher excellent response rates, and better all secondary outcomes (P<0.05). hs-CRP fell more with WBC. KOA patients had lower GPX4 and higher ACSL4 vs. healthy controls. Post-treatment, WBC restored both GPX4 and ACSL4 to healthy levels, while controls only reduced ACSL4. In the WBC group, ΔGPX4 and ΔSLC7A11 inversely correlated with ΔESR, Δhs-CRP, and Δβ-CTX (all P<0.01). Safety was comparable. These exploratory PBMC mRNA findings suggest WBC may restore systemic redox homeostasis and lipid metabolism via the GPX4/ACSL4 axis, potentially improving the joint's "metabolic-inflammatory" microenvironment. However, these are correlational, not causal, and are limited to mRNA data without protein or functional ferroptosis markers (e.g., MDA, glutathione), absence of joint tissue validation, an open-label design, and a small subgroup size. Furthermore, the lack of P53 changes hints at possible pathways independent of classical P53-mediated ferroptosis, but this remains speculative. Thus, all mechanistic inferences are hypothesis-generating. WBC plus conventional therapy improved symptoms safely over 12 weeks; its ferroptosis-related effects await verification in dedicated mechanistic studies.

PMID 42736683
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PubMedJournal of diabetes and metabolic disorders2026-09-13

The effects of 2-year SYSADOA treatment on glycemic level in patients with comorbid primary knee osteoarthritis and type 2 diabetes mellitus.

Tawansareewattana Yanonut Y, Amornwacharapong Panparamee P, Khongjaew Itthiphat I, Jirawatthanasakda Kasidit K et al.

To evaluate the effects of long-term use of symptomatic slow-acting drugs for osteoarthritis (SYSADOA), including glucosamine and diacerein, on glycemic control in patients with knee osteoarthritis (KOA) and type 2 diabetes mellitus (T2DM). We conducted a retrospective cohort study of patients aged ≥ 40 years with KOA and T2DM. Participants were categorized into glucosamine, diacerein, and non-SYSADOA groups. Glycemic outcomes, including glycated hemoglobin (HbA1c) and fasting blood glucose (FBG), were assessed every three months over 24 months. Baseline covariables were collected to control for potential confounding factors, including sex, age, body mass index, baseline glycemic control (poor glycemic control defined as HbA1c > 7% or FBG > 130 mg/dL), number of antidiabetic drug classes, and the use of NSAIDs, opioid analgesics, lipid-lowering agents, and antihypertensive medications. Longitudinal changes were analyzed using multivariable multilevel Gaussian regression time-by-group interaction. A total of 409 patients were included in the FBG analysis and 304 in the HbA1c analysis. Baseline characteristics were generally comparable across treatment groups. Over the 24-month follow-up period, neither glucosamine nor diacerein was associated with significant changes in glycemic outcomes compared with non-SYSADOA use. Adjusted baseline differences in HbA1c were 0.06% (95% CI -0.15 to 0.28) for glucosamine and - 0.05% (95% CI -0.32 to 0.21) for diacerein. Corresponding adjusted differences in FBG were - 2.35 mg/dL (95% CI -8.35 to 3.66) and - 3.32 mg/dL (95% CI -11.20 to 4.55). SYSADOA use was not associated with clinically meaningful changes in glycemic control over 24 months in patients with KOA and T2DM. The online version contains supplementary material available at https://doi.org/10.1007/s40200-026-02069-1.

PMID 42732213
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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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