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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

PubMedColloids and surfaces. B, Biointerfaces2026-10-23

Carboxymethylcellulose-engineered κ-carrageenan/agar beads for gastric-phase drug retention and controlled oral delivery of aceclofenac.

Farias Ana Beatriz Vitorino de ABV, Munhoz Gustavo Fernandes GF, Vieira Melissa Gurgel Adeodato MGA

Natural polysaccharide-based multiparticulate systems are promising alternatives to synthetic polymers for oral modified-release applications due to their biocompatibility, low toxicity, and tunable network properties, particularly for drugs associated with gastrointestinal irritation, such as aceclofenac. Here, κ-carrageenan/agar beads were prepared by ionotropic gelation and modified with proanthocyanidin (PA) and tannic acid (TA) as physical crosslinking agents, or carboxymethylcellulose (CMC) as a release-modifying agent. Their effects on drug entrapment efficiency, gastro-resistance, and in vitro aceclofenac release were evaluated. All formulations showed entrapment efficiencies ranging from 78.8 to 92.9%, although lower values were observed for TA-containing beads, likely due to pH-dependent effects. In simulated gastric fluid, PA-modified beads exceeded the predefined 10% release threshold adopted from the USP criterion for delayed-release dosage forms, whereas CMC improved gastric-phase drug retention, with CMC2 limiting aceclofenac release to 8.4%. Selected CMC-modified beads exhibited concentration-dependent swelling and sustained release in simulated intestinal fluid, with a significantly slower release profile than the commercial reference formulation. Kinetic modeling suggested release governed by diffusion coupled with polymer relaxation and/or surface erosion. Physicochemical characterization indicated that CMC promoted structural changes consistent with a more restrictive polymer network, resulting in reduced aceclofenac release under simulated gastric conditions and prolonged release at intestinal pH. Overall, CMC effectively modulated the structural and release properties of κ-carrageenan/agar beads, supporting their potential as a natural polymer-based platform for gastric-phase drug retention and controlled oral delivery of aceclofenac.

PMID 42914837
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PubMedJournal of translational medicine2026-10-23

Mitoxyperilysis-based molecular subtyping identifies SPP1+ macrophages and IL1B as critical mediators of tumor progression and immunotherapy resistance in intrahepatic cholangiocarcinoma.

Wang Yafei Y, Ding Kai K, Niu Jiale J, Li Zhi Z et al.

Intrahepatic cholangiocarcinoma (ICC) is an aggressive malignancy characterized by poor clinical outcomes. Although mitoxyperilysis has recently emerged as a novel form of regulated cell death, the clinical relevance of mitoxyperilysis-related molecular subtypes in ICC remains largely unexplored. This study aimed to elucidate the clinical significance, immune microenvironment features, and potential therapeutic targets of mitoxyperilysis-related molecular subtypes in ICC. Based on the expression profiles of 45 mitoxyperilysis-related genes, ICC patients were classified into two subtypes using consensus clustering, and the robustness of the classification was validated in the independent GSE89749 cohort. Survival analysis, immune microenvironment characterization, single-cell transcriptomic profiling, in vitro/in vivo experiments, and nomogram construction were subsequently performed to investigate the underlying biological mechanisms and therapeutic implications. Two robust mitoxyperilysis-related molecular subtypes were identified. Patients in the high-mitoxyperilysis subtype exhibited significantly poorer overall survival (OS), and subtype classification remained an independent predictor of adverse prognosis. The high-mitoxyperilysis subtype was closely associated with lymph node metastasis, elevated CA19-9 levels, and KRAS mutation. Furthermore, this subtype demonstrated pronounced inflammatory activation, an immunosuppressive tumor microenvironment (TME), increased infiltration of neutrophils and M2 macrophages, and elevated expression of immune checkpoint molecules. Single-cell transcriptomic analysis revealed a marked enrichment of SPP1+ macrophages in the high-mitoxyperilysis subtype, with IL1B and CXCL3 identified as key regulatory molecules. IL1B promoted ICC cell invasion and metastasis. Notably, treatment with diacerein, an IL1B inhibitor, synergized with anti-PD-1 immunotherapy to suppress tumor progression and overcome immunotherapy resistance. Mitoxyperilysis-related molecular classification provides a clinically relevant framework for prognostic stratification and prediction of immunotherapeutic responsiveness in ICC. SPP1+ macrophages and IL1B represent potential therapeutic targets, providing a promising strategy for precise diagnosis and treatment of ICC.

PMID 42919277
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PubMedInflammopharmacology2026-10-21

In silico guided design and in vivo evaluation of Diacerein loaded SLNs embedded in situ gels for sustained intra-articular osteoarthritis therapy.

Ayesha Badarqa Tul BT, Erum Alia A, Shahid Nariman N, Tulain Ume Ruqia UR

Osteoarthritis (OA) is a multifactorial joint disorder characterized by inflammation, oxidative stress, and progressive cartilage degeneration, for which conventional therapeutic agents remain limited by low bioavailability and systemic side effects. This study aims to integrate in silico guided and experimental nanoparticle-based drug formulations and in vivo analysis targeting the inflammatory genes, proteins, and oxidative markers in OA therapy. In silico screening was conducted on ligands based on SwissSimilarity and led to the identification of TNF-α inhibitors. High binding affinity and stability of the complex were verified by Docking studies (AutoDock Vina) and molecular dynamics simulations (Desmond), 100 ns. THA was produced. SLNs with Diacerein (DC-SLNs) were prepared and entrapped into thermosensitive in situ gels (ISG) that were made of THA, poloxamer 407 and poloxamer 188. The formulations were assessed physically and in vitro release dynamics. The efficacy of in vivo drug formulation was determined by osteoarthritis rat model with knee diameter, oxidative and inflammatory markers. Swiss-similarity screening with Rhein as a reference ligand identified eight structurally similar compounds in the DrugBank database, including Diacerein, Rheinanthrone, Salsalate, and others, with high similarity scores (> 0.7); DC showed the strongest TNF-α binding (- 10.7 kJ/mol). The complex stability was proved by MD simulations (RMSD 2.6 A). In both gels, gelation was appropriate, injectability was excellent, and non-Fickian release occurred. Thermal studies, PXRD, and SEM showed lower crystallinity and a porous structure. Both formulations yielded significant reductions in joint swelling, pro-inflammatory cytokines (TNF-α, IL-6, NF-κB), improved antioxidant activity, and reduced inflammatory and oxidative mediators associated with cartilage degradation, while the DC-SLN@THA-ISG has better therapeutic efficacy than DC@THA-ISG. In silico in vivo studies prove the efficacy of DC-SLN@THA-ISG as a biocompatible and sustained intra-articular formulation in managing osteoarthritis.

PMID 42902054
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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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