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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

PubMedThe Journal of oral implantology2026-06-05

Preemptive Analgesia With Steroidal and Nonsteroidal Anti-Inflammatory Drugs in Dental Implant Surgeries: A Systematic Review.

Gomes da Frota Eduardo E, Bergamaschi Cristiane de Cássia CC, Lopes Luciane Cruz LC, de Deus Lages Lívio Portela LP et al.

This systematic review aimed to evaluate the efficacy and safety of preemptive analgesia using oral steroidal and nonsteroidal anti-inflammatory drugs (NSAIDs) in adults undergoing dental implant surgery. A comprehensive search was conducted in the Cochrane Central Register of Controlled Trials (CENTRAL), MEDLINE (via PubMed), Excerpta Medica Database (EMBASE), Virtual Health Library (VHL), Web of Science, and other databases with no restrictions on language or publication date. Randomized clinical trials (RCTs) comparing oral steroidal drugs or NSAIDs with placebo or other anti-inflammatory drugs were included. The primary outcomes were postoperative pain, edema, trismus, discomfort, and use of rescue medication. Pairs of reviewers independently extracted data and assessed the risk of bias. Owing to clinical heterogeneity among the included studies, a narrative synthesis was conducted. Seven RCTs (n = 589 patients) evaluated aceclofenac 100 mg (in combination with acetaminophen), dexamethasone 4 mg, dexketoprofen 25 mg, etoricoxib 90 mg, ibuprofen 600 mg, ketorolac 10 mg, meloxicam 15 mg, nimesulide 100 mg, piroxicam 40 mg, and tenoxicam 20 mg. Favorable results have been reported with etoricoxib 90 mg, ibuprofen 600 mg, and nimesulide 100 mg for controlling postoperative pain and discomfort in single-implant procedures. Meloxicam and tenoxicam have demonstrated efficacy in invasive surgeries involving multiple implants and advanced techniques. Some studies have extended anti-inflammatory use to the postoperative period beyond rescue medication, potentially biasing the interpretation of preemptive efficacy. To date, no adverse drug reactions have been reported. Owing to the heterogeneity in protocols, drug regimens, and outcome measures, definitive conclusions regarding the most effective and safest preemptive agents could not be drawn. Future trials should emphasize methodological standardization and focus on widely used drugs to support evidence-based decisions in implant dentistry.

PMID 42242696
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PubMedJournal of orthopaedic surgery and research2026-06-03

Intra-articular platelet-rich plasma demonstrates superior clinical and serum biomarker outcomes compared with corticosteroids and NSAIDs in late-stage knee osteoarthritis: a randomised controlled trial.

Lacko Marek M, Awad Omar O, Matúška Martin M, Strážik Michal M et al.

To assess the efficacy of two autologous platelet-rich plasma injections (PRP) in treating late-stage knee osteoarthritis and their effects on joint pain, stiffness and function as well as serum biomarkers reflecting inflammation, and cartilage turnover. Ninety patients (aged 40-80 years) with symptomatic KL 3-4 KOA on arthroplasty waiting lists were randomized to PRP (two injections one week apart) and CS (a single injection of betamethasone), or NSAID (aceclofenac tablets) as the control groups. Primary outcomes included VAS pain scores, WOMAC scores, opioid use, and serum biomarkers (COMP, MMP-3, CGRP, CCL2, VEGF, IL-6, IL-18, TNF-α, CX3CL1, sTREM2, sRAGE, TGF-β1, BDNF) were measured at baseline, 3 months, and 6 months. Eighty-two patients completed the 6-month follow-up. Baseline characteristics (VAS, WOMAC) were comparable among the groups. PRP treatment resulted in significant and sustained reductions in VAS pain scores at 3 and 6 months compared with those at baseline (p < 0.001) and in both control groups (3 months: p < 0.001 vs. CS and NSAID; 6 months: p = 0.004 vs. CS; p = 0.002 vs. NSAID). WOMAC total and subscale scores (pain, stiffness, function) improved significantly only in the PRP group at both follow-up points (all p ≤ 0.03), with significant intergroup differences favoring PRP. Opioid consumption was significantly lower in the PRP group than in the CS and NSAID groups at 3 months (p = 0.002 and p = 0.025, respectively) and than in the CS group at 6 months (p = 0.006). At 3 months, PRP significantly reduced levels of proinflammatory and cartilage degradation biomarkers (COMP, MMP-3, IL-6, IL-18, TNF-α) and CGRP compared with controls, while increasing levels of anti-inflammatory markers (sTREM2, sRAGE, TGF-β1). Several effects were maintained at 6 months, including continued reductions in COMP, IL-6, and IL-18 levels compared with the CS group and in IL-6 and TNF-α levels compared with the NSAIDs group. No significant changes were observed in MCP-1, VEGF, CX3CL1, BDNF, or β-NGF. Adverse events were mild and transient in the PRP group. Two PRP injections demonstrated greater 6-month clinical and biomarker improvements compared to CS and NSAIDs in late-stage KOA, supporting PRP as a safe bridge therapy prior to arthroplasty.

PMID 42231445
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PubMedAndrology2026-05-29

Diacerein Disrupts Testicular Homeostasis: The Essential Role of Basal Cytokines in Maintaining Sertoli Cell Integrity and the Immune Microenvironment.

Jesus Elide Loise Freitas de ELF, Silva André Acácio Souza da AASD, Akinsomisoye Olumide Stephen OS, Silva Erick J R EJR et al.

Pro-inflammatory cytokines, TNF and IL-1B, are essential for testicular homeostasis. Diacerein, an anti-inflammatory drug, inhibits these cytokines, impairing M2 macrophages and Leydig cells (LCs). However, its impact on Sertoli cells (SCs) and M1 (CD68) macrophages remains unknown. To investigate the impact of diacerein-induced cytokine downregulation on SC integrity and the testicular immune profile. Male rats were treated with diacerein (100 mg/kg) or saline for 30 days. The seminiferous epithelium was evaluated by light and transmission electron microscopy. The number of spermatocytes and Ki-67+ cells was quantified. SC structural (actin, vimentin, claudin-1, connexin-43) and functional (transferrin, Ldha) proteins, and the interstitial immunolocalization of macrophage inhibitory factor (MIF), CD68, CD45, IL-1B, iNOS, NF-κB, and karyopherin were assessed, alongside immune response genes (Tnfa, Il1b, Nfkb1, Nos2, Tgfb1) and nitrite levels. TUNEL method was also performed. TNF and IL-1B were downregulated; steroidogenesis and IL-1B production by LCs decreased, coupled with reduced MIF levels. SCs exhibited electron-dense cytoplasm, disrupted filaments, and decreased blood-testis barrier proteins. Transferrin and Ldha expression were reduced, underlying reduced spermatocyte counts, arrested proliferation, and germ cell death. TUNEL-positive apoptotic bodies (probably from LCs) were found within macrophages. Despite increased CD45+ and CD68+ macrophages, a noninflammatory phenotype was observed due to NF-κB cytoplasmic sequestration and weak karyopherin expression, corroborating Tgfb1 upregulation and reduced Nos2 expression and nitrite levels. Basal cytokines are essential for SC structure and function. Despite testicular damage, diacerein shifted the immune response toward a homeostatic and immunotolerant profile, avoiding a self-destructive inflammatory process.

PMID 42212543
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PubMedJournal of applied toxicology : JAT2026-05-28

The Effect of Pregabalin and Aceclofenac on Testicular Tissue of Adult Albino Rats: Evaluation of Toxicity and Potential Reversibility of Toxic Effects.

Mostafa Heba El-Sayed HE, Elmahdi Faris Mergheni FM, Fareed Shimaa Antar SA, Allmlah Amani Abdel Wahab AAW et al.

Male reproductive function is highly susceptible to drug-induced toxicity, particularly following prolonged use of nonsteroidal anti-inflammatory drugs (NSAIDs) and antiepileptic agents. Despite the frequent co-prescription of aceclofenac and pregabalin for chronic pain management, their combined effects on testicular function remain poorly understood. This study aimed to evaluate the testicular toxicity induced by aceclofenac and pregabalin, administered individually and concurrently, and to assess the potential reversibility of these effects following drug withdrawal. Thirty-five adult male albino rats were divided into control, aceclofenac-treated, pregabalin-treated, combined-treatment, and corresponding recovery groups evaluated 8 weeks after drug cessation. Serum testosterone levels, oxidative stress markers (SOD, GSH, and MDA), inflammatory markers (TNF-α and ALP), histopathological changes, immunohistochemical expression of PCNA and c-Kit, and sperm ultrastructure using transmission electron microscopy (TEM) were assessed. Both drugs induced significant testicular toxicity, evidenced by reduced testosterone levels, increased oxidative stress, and elevated inflammatory markers. Histopathological examination demonstrated degeneration of seminiferous tubules, with the most severe damage observed in the combined-treatment group. Expression of PCNA and c-Kit was markedly reduced, whereas TEM analysis confirmed extensive ultrastructural abnormalities in sperm flagella. Following drug withdrawal, pregabalin-treated rats showed near-complete recovery, whereas aceclofenac-treated rats demonstrated only partial improvement. The combined-treatment group exhibited the least degree of recovery. In conclusion, aceclofenac and pregabalin significantly impair testicular function, with combined administration exacerbating damage through synergistic oxidative and inflammatory mechanisms. Although pregabalin-induced effects appear largely reversible, aceclofenac causes more persistent structural and ultrastructural damage to testicular tissue and sperm cells.

PMID 42204899
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PubMedMolecular biology reports2026-05-22

Diacerein mitigates cisplatin-induced testicular toxicity in rats; Role of Nrf2/ HO-1, NF-κB/caspase-3 and NLRP3/ASC/Caspase-1 signaling pathways.

Kamel Gellan Alaa Mohamed GAM, Hussein Shaimaa S

Cisplatin (CIS) is an effective chemotherapeutic agent; however, its clinical use is limited by serious adverse effects, including testicular toxicity, which is primarily mediated by oxidative stress, inflammation, and cell death pathways. Diacerein (DIA), a slow-acting anti-inflammatory drug, has recently gained attention for its antioxidant and cytoprotective properties. Twenty-four adult male albino rats were randomly allocated into experimental groups and treated with DIA (50 mg/kg, orally) for 14 consecutive days, along with a single intraperitoneal injection of CIS (7 mg/kg) on day 8. At the end of the experimental period, rats were humanely euthanized. Testicular tissues and serum samples were collected for histopathological and biochemical analyses. DIA markedly attenuated CIS-induced testicular damage, as evidenced by improved histological architecture, increased testicular weight, and restored serum testosterone levels. It alleviated oxidative stress by reducing malondialdehyde (MDA) levels and enhancing antioxidant defenses, including superoxide dismutase (SOD), glutathione (GSH), Nrf2, and HO-1 expression. Furthermore, DIA suppressed inflammation via downregulation of NF-κB and pro-inflammatory cytokines (TNF-α and IL-1β). In addition, DIA inhibited CIS-induced pyroptosis by reducing the expression of NLRP3, ASC, and pro-caspase-1. DIA exerts a protective effect against CIS-induced testicular toxicity through its antioxidant, anti-inflammatory, and anti-pyroptotic activities, highlighting its potential as a therapeutic candidate targeting the Nrf2/HO-1, NF-κB, and NLRP3/ASC/caspase-1 signaling pathways.

PMID 42171830
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PubMedEuropean journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V2026-05-18

Mechanistic enhancement of oral bioavailability through a coamorphous apremilast-aceclofenac systems: integrated LC-MS/MS Bioanalysis, in vivo pharmacokinetics, and PBPK modeling.

Khemchandani Rahul R, Pardhi Ekta E, Jadhav Aditya A, Shaikh Nadeem N et al.

Poor aqueous solubility and dissolution-limited absorption remain major challenges in the oral delivery of apremilast (APR) and aceclofenac (ACF). In this study, coamorphous systems (CAMS) of APR-ACF were systematically evaluated to enhance biopharmaceutical and pharmacokinetic performance using an integrated experimental-computational approach. Three CAMS with different stoichiometric ratios (AA11, AA12, and AA21) were prepared and assessed. Solid-state analysis confirmed the formation of single-phase homogeneous CAMS stabilized by intermolecular interactions. CAMS showed significant improvements in solubility and dissolution compared to crystalline and physical mixtures, with AA12 exhibiting the greatest enhancement. A fully validated LC-MS/MS method was developed for simultaneous quantification of APR and ACF in rat plasma. In vivo pharmacokinetic studies revealed formulation-dependent increases in systemic exposure. AA12 enhanced APR's AUC (∼2.6-fold) and Cmax (∼1.5-fold) compared to crystalline drug, while ACF showed more moderate improvements (∼1.5-fold AUC, ∼1.3-fold Cmax). Tmax remained unchanged across formulations, indicating improved absorption extent. Physiologically based pharmacokinetic (PBPK) modeling incorporating the Advanced Compartmental Absorption and Transit (ACAT) framework, along with formulation-specific dissolution inputs, accurately predicted plasma concentration-time profiles and regional gastrointestinal absorption, confirming dissolution-driven absorption enhancement. This integrated in vitro-in vivo-in silico investigation establishes coamorphization as a validated strategy to overcome dissolution-limited absorption, identifying AA12 as the optimized CAMS for combined APR-ACF delivery.

PMID 42144121
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