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mesalazine (NKP5191 / SHP429 / Quintasa)

✓ Approved

Nisshin Pharma · PTGS1 · 小分子

什么是 mesalazine？

mesalazine 是一种小分子，由Nisshin Pharma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NKP5191, SHP429, Quintasa
公司Nisshin Pharma
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, Nisshin Pharma

作用机制

分子靶点

mesalazine 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

mesalazine 针对 2 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Gastrointestinal disordersColitis ulcerative✓ Approved
Gastrointestinal disordersCrohn's disease✓ Approved

相关研究文献

PubMedMiddle East journal of digestive diseases2026-10-22

Anti-Tumor Necrosis Factor-Alpha Associated Kaposi Sarcoma in a Patient with Ulcerative Colitis: A Case Report and Literature Review.

Fatemi Reza R, Mahabadi Zeinab Z, Fatemi Seyed Aram SA, Alizadeh Sania S et al.

Kaposi sarcoma (KS) is a rare vascular malignancy associated with human herpesvirus-8 (HHV-8). Tumor necrosis factor-alpha inhibitors (anti-TNF-α agents) are widely used in inflammatory bowel diseases such as ulcerative colitis (UC). While these biologics are effective, they carry a risk of opportunistic infections and, rarely, malignancies. We report a rare case of KS developing in a patient with UC following infliximab treatment. A 67-year-old man with a 3-year history of moderate to severe UC, maintained on azathioprine and mesalazine, initiated induction therapy with infliximab (four 100 mg vials per dose). One week after the first infusion, he developed lower limb edema. Four months later, he presented with multiple violaceous cutaneous plaques. A skin biopsy confirmed KS, and HHV-8 serology was positive. Infliximab was immediately discontinued. The patient subsequently received systemic chemotherapy (liposomal doxorubicin) with complete resolution of the cutaneous lesions. This case highlights KS as a severe, albeit rare, adverse event of anti-TNF-α therapy, emphasizing the need for vigilance, prompt diagnosis, and intervention.

PMID 42903387
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PubMedBMC pediatrics2026-10-22

Very early onset inflammatory bowel disease in Jordan: a single-center case series of clinical, genetic, and therapeutic features.

Altamimi Eyad E, Almomani Hala H, Alsmadi Ayah A, Issi Nicole N et al.

Very early onset inflammatory bowel disease (VEOIBD), defined as onset before six years of age, is increasingly recognized as a distinct entity often linked to monogenic etiologies. Data from the Middle East remain limited. We conducted a retrospective case series of ten pediatric patients diagnosed with VEOIBD at King Abdullah University Hospital, Jordan, between July 2017 and July 2024. Clinical, endoscopic, histopathologic, genetic, treatment, and outcome data were extracted and analyzed descriptively. The cohort comprised ten patients (six males, four females). Median age at symptom onset was 12 months (range 3-60), with median diagnosis at 34 months (range 10-72). Diarrhea (100%), failure to thrive (60%), and recurrent infections (40%) were predominant presenting features. Endoscopy revealed mucosal ulceration in seven patients (70%), with non-caseating granulomas in three (30%) and focal active colitis in three (30%). Genetic testing (n = 8) identified pathogenic or likely pathogenic variants in six patients and variants of uncertain significance (VUS) in two; the genes implicated were MEFV (n = 3), CYBB (n = 2; both VUS), G6PC3, GUCY2C, NPC1, NOD2, RIPK1, and LRBA. Three patients carried variants in two genes. In one pair - a homozygous pathogenic NPC1 frameshift variant with a heterozygous NOD2 VUS - a composite digenic mechanism has been proposed as a candidate contributor to the unusually severe VEOIBD phenotype [21]. Therapies included infliximab (n = 4), mesalazine, azathioprine, budesonide, intravenous immunoglobulin, elemental diet, and colchicine. Three patients were referred for hematopoietic stem cell transplantation (HSCT); one died of infection-related multi-organ failure. The patient with a homozygous LRBA VUS lacked access to targeted therapy with abatacept or sirolimus. VEOIBD in Jordan is characterized by early presentation, genetic heterogeneity including co-occurring variants of uncertain significance, and poor response to conventional therapy. Limited access to targeted agents and HSCT significantly impacts outcomes. Early genomic testing, multidisciplinary management, and improved therapeutic access are essential for better prognosis.

PMID 42907806
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PubMedDrugs - real world outcomes2026-10-12

Real-World Epidemiology of Inflammatory Bowel Disease in Italy: Treatment Patterns, Adherence, and Costs in Patients with Ulcerative Colitis Treated with Mesalazine.

Degli Esposti Luca L, Veronesi Chiara C, Calabria Silvia S, Giannessi Lisa L et al.

Ulcerative colitis (UC) and Crohn's disease (CD) are chronic immune-mediated conditions associated with a substantial clinical and economic burden. Italian epidemiological evidence is limited. Mesalazine remains a cornerstone of UC management. This study aimed to provide updated epidemiological estimates of inflammatory bowel disease (IBD) in Italy, and to evaluate real-world treatment patterns, adherence to oral mesalazine, and healthcare costs among patients with UC initiating mesalazine therapy. A retrospective observational analysis was conducted using Italian administrative databases covering ~4 million beneficiaries. Patients with UC and CD were identified (January 2010-May 2023) using the International Classification of Diseases, Ninth Revision, Clinical Modification (ICD-9-CM) or exemption codes. Patients with UC who were new users of mesalazine were characterized at baseline. Mesalazine treatment patterns, adherence, and direct healthcare costs were described at follow-up. At the end of 2023, UC and CD prevalence rates were 272 (95% confidence interval [CI] 267-278) and 166/100,000 (95% CI 162-170) inhabitants, respectively. Incidence rates in 2023 of UC and CD were 18.9 (95% CI 18-20) and 10.8/100,000 (95% CI 10-12), respectively. Among 2552 patients with UC who were new mesalazine users, 69.6% of time-dependent mesalazine users were adherent (versus 56.1% pH-dependent users). Mean annual cost per patients with UC who were new mesalazine users in 2023 was €4516, mainly driven by hospitalizations. This real-world analysis provides recent epidemiological estimates of UC and CD, and describes a substantial economic burden, highlighting the need for improving adherence and therapeutic pathways.

PMID 42862468
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PubMedRespiratory medicine case reports2026-10-11

Organizing pneumonia in Crohn's disease: a case report and literature review.

Debiche Soumaya S, Cherif Hela H, Ben Rjeb Sarra S, Yangui Ferdaous F et al.

Organizing pneumonia (OP) is a rare pulmonary manifestation in patients with inflammatory bowel disease (IBD). Distinguishing between a primary extra-intestinal manifestation of Crohn's disease (CD) and mesalazine-induced lung injury remains a major clinical challenge, as both conditions are steroid-responsive. We report the case of a 31-year-old woman with CD who developed progressive dyspnea and migratory pulmonary infiltrates one month after initiating mesalazine. Laboratory findings revealed marked peripheral eosinophilia (1276/mm3) and a mixed eosinophilic bronchoalveolar lavage profile (30.8%). Histopathology confirmed OP with Masson bodies. Due to the diagnostic overlap, mesalazine was replaced by azathioprine, and systemic corticosteroid therapy (0.75 mg/kg) was initiated. Complete radiological resolution was achieved at 8 months. This case illustrates the diagnostic complexity of eosinophilic-rich OP in CD and emphasizes that while pathology confirms the pattern, the etiology often remains a dual hypothesis between systemic disease and drug toxicity.

PMID 42859623
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PubMedProbiotics and antimicrobial proteins2026-10-06

Pediococcus acidilactici ZQ-19 Ameliorates Ulcerative Colitis via Remodeling Gut Microbiota and Glutathione Redox Homeostasis.

Lu Yimeng Y, Liu Qi Q, Chen Hu H, Ding Cunhui C et al.

Ulcerative colitis (UC) is closely linked to intestinal oxidative stress, gut dysbiosis and selenium metabolism disorders. In this study, 449 lactic acid bacteria strains were isolated from yak yogurt on the Qinghai-Tibet Plateau. After H2O2 tolerance screening, 11 highly antioxidant strains were obtained, among which Pediococcus acidilactici ZQ-19 exhibited the highest intracellular GPx activity, outstanding free radical scavenging capacity and excellent probiotic characteristics. In DSS-induced UC mice, ZQ-19 significantly alleviated weight loss, colon shortening and mucosal damage, restored tight junction protein expression, and protected liver and kidney functions. 16 S rRNA sequencing revealed that ZQ-19 was associated with reshaped gut microbiota, enriched butyrate-producing taxa and reduced pro-inflammatory pathogens; such microbial shifts were positively correlated with elevated intestinal GPx activity. Mechanistically, ZQ-19 intervention coincided with enhanced intestinal ROS clearance, altered expression of GR/GST/Trx-1, and a shifted selenoprotein profile favouring GPx isoforms by upregulating colonic SELENOP and GPx1-4 while downregulating DIO1/2. It synergistically activated Nrf2/p53 protective pathways and inhibited the MyD88/COX-2/NOX1/2 pro-oxidative inflammatory axis, with superior local regulation to mesalazine. In conclusion, ZQ-19 ameliorates UC in association with the microbiota-GPx axis and dual pathways, offering a novel probiotic intervention strategy.

PMID 42836931
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PubMedJournal of natural medicines2026-10-05

Extracts of okra mucilage protect intestinal homeostasis through gut microbiota and immune responses.

Qing Mengli M, Sun Benyue B, Li Yuehan Y, Meng Zhiyi Z et al.

Okra pods (Abelmoschus esculentus (L.) Moench) are known as a vegetable, the mucilage of which possesses many bioactivities. Okra mucilage (OM) is a carbohydrate-rich natural extract containing polysaccharides and other bioactive components. However, its efficacy under different types of intestinal stress and its comparison with standard therapeutic agents remain unclear. Chemical characterization demonstrated that OM contains abundant carbohydrates and diverse chemical constituents. In this study, we evaluated the protective effects of OM in dextran sulfate sodium (DSS)-induced colitis and fasting-induced intestinal injury models in mice. Mesalazine and GA were used as a positive control in DSS and fasting-induced injury models, respectively. Generally, OM treatment significantly alleviated intestinal pathological damage, restored intestinal barrier integrity, promoted epithelial regeneration, and modulated gut microbial composition in these two models. In DSS-induced colitis, OM increased the abundance of short-chain fatty acid (SCFA)-producing bacterial families Muribaculaceae and Lachnospiraceae, while reducing pro-inflammation-associated Bacteroidaceae, and suppressed key inflammatory genes and factors, including Cxcl1, Cxcl2, Cxcl5, TNF, NF-κB. Notably, the regulatory effects of OM were comparable to mesalazine. In fasting-induced intestinal injury, OM restored microbial balance by regulating taxa such as Enterobacteriaceae and Erysipelotrichaceae, and downregulated gluconeogenesis-related genes including Klf15, Pck1, and Hmgcs2. OM upregulated genes involved in epithelial barrier function and immune homeostasis such as Btnl7, Btnl8, regulating pathways HIF-1, PI3K-Akt, MAPK and glycolysis/gluconeogenesis pathways. These findings demonstrate that OM alleviates intestinal injury by modulating gut microbiota, suppressing inflammation, and restoring intestinal immune and metabolic homeostasis, highlighting its potential as a natural mucilage-derived ingredient for maintaining intestinal homeostasis.

PMID 42830374
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