Dipentum (olsalazine sodium) / Viatris, UCB - LARVOL DELTA

Evaluating rat and canine microbiota models for predicting human colonic prodrug metabolism. (PubMed, Eur J Pharm Sci) - "Degradation kinetics of sulfasalazine, balsalazide, and olsalazine were first assessed. When benchmarked against published human in vitro data, rat degradation rates were closely aligned with human values, particularly for sulfasalazine (rat: K = 0.025 min⁻¹; human: K = 0.021 min⁻¹) and balsalazide (rat: K = 0.015 min⁻¹; human: K = 0.009 min⁻¹). These findings highlight rat faecal material as a practical and translationally relevant model for microbiota-sensitive prodrug metabolism, offering a low-impact alternative to invasive sampling and larger animal studies."

Journal • Preclinical

A clinically inspired olsalazine-based metal-organic framework enables a universal nanodrugs platform for diverse disease. (PubMed, J Colloid Interface Sci) - "A spherical Olsa-based Cu/Fe metal-organic framework (MOF) was developed for colorectal cancer (CRC) therapy to encapsulate doxorubicin (DOX) and address the intrinsic hydrogen peroxide (H2O2) deficiency in tumor microenvironments through a self-catalytic H2O2 regeneration mechanism. This spatiotemporally controlled release profile resulted in significant downregulation of pro-inflammatory cytokines and complete restoration of tight junction protein expression. This study pioneers a transformative nanocarrier that revolutionizes therapeutic nanocarrier design through three innovations: (i) the synergistic integration of therapeutic and nanocarrier functionalities using intrinsically bioactive molecules, (ii) universal disease adaptability for precision intervention across multiple pathological conditions through modular coordination switching, and (iii) clinically validated, Food and Drug Administration (FDA)-approved molecules with proven biocompatibility."

IO biomarker • Journal • Colorectal Cancer • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Oncology • Solid Tumor • Ulcerative Colitis

Cannabidiol Enhances the Therapeutic Efficacy of Olsalazine and Cyclosporine in a Murine Model of Colitis. (PubMed, Int J Mol Sci) - "Combination therapies significantly ameliorated colitis, reducing DAI, MPO activity, and inflammatory cytokines, while restoring colon length and GLP-1 levels-without inducing liver or kidney toxicity. These findings demonstrate that combining a low dose of CBD with standard IBD drugs enhances therapeutic efficacy while minimizing side effects, supporting its integration into future combination strategies for more effective and safer IBD management."

Journal • Preclinical • Gastroenterology • Gastrointestinal Disorder • Hematological Disorders • Immunology • Inflammation • Inflammatory Bowel Disease • MPO

A Colon-Targeted Oral Nanosystem Disrupts the Inflammatory Loop in Enteric Glia to Alleviate Ulcerative Colitis. (PubMed, ACS Nano) - "Herein, we develop a S100B inhibitor pentamidine (PTM)-loaded olsalazine-based nanoneedle, Zn2(Olsa)/PTM, to break this vicious cycle and alleviate ulcerative colitis...The oral administration of ZOP@Eud considerably ameliorates disease severity and restores mucosal barrier integrity and immune homeostasis in a murine ulcerative colitis model, which is evidenced by heightened expression of tight junction proteins and reduced levels of colonic proinflammatory S100B and cytokines. These findings suggest that nanosystems targeting EGCs offer a promising approach for mitigating gut inflammation."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Ulcerative Colitis • S100B • S100B

An Olsalazine-Loaded Hollow Mesoporous Prussian Blue/Polydopamine Nanozyme Alleviates Anxiety/Depression-like Behavior and Enhances Brain Neural Activity in Colitis Mice. (PubMed, ACS Appl Mater Interfaces) - "As the observed modulation of the dysfunction of neuroinflammation and neuronal activation of CA1 hippocampus, Olsa@HMPB/PDA NPs treatment alleviated anxiety/depression-like behavior in DSS mice. Overall, this nanozyme established a paradigm in combined IBD therapy with psychological comorbidities."

Journal • Preclinical • CNS Disorders • Depression • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Mental Retardation • Metabolic Disorders • Mood Disorders • Psychiatry

Oral olsalazine/ellagic acid/ZnCl2-modified in situ-forming hydrogels alleviates anxiety/depression-like symptoms and brain neural activity in colitis mice. (PubMed, Mater Today Bio) - "We demonstrated that the oral administration of drug-loaded in situ-forming hydrogel with excellent antioxidant, anti-inflammatory activities, cytocompatibility, intestinal retention capacity of the drug, significantly enhanced the IBD therapeutic outcomes, and relieve accompanying depression-like symptoms in colitis mice. Overall, this designed in situ-forming hydrogel oral delivery system will open up new pathway in combined gastrointestinal therapy and psychological comorbidities for IBD patients, especially those with dysphagia."

Journal • Preclinical • CNS Disorders • Depression • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Mood Disorders • Psychiatry

Persistence and Adherence Among Patients with Chronic Spontaneous Urticaria Initiating Advanced Therapies: A Real-World, Claims Database Study (AAD 2025) - " Using IQVIA PharMetrics claims data, patients (12–64 years) who newly initiated AT (systemic immunosuppressant [SI] [cyclosporine, tacrolimus, mycophenolate mofetil, methotrexate, azathioprine], systemic anti-inflammatories [SAI] [colchicine, dapsone, hydroxychloroquine, olsalazine, sulfasalazine] or omalizumab; first dispensation=index date) within 14 days of a diagnosis code for CSU between January 2021 and December 2022 were identified. Persistence and adherence to AT in CSU were suboptimal, highlighting the need for additional treatment options."

Adherence • Claims database • Clinical • Metastases • Real-world • Real-world evidence • Chronic Spontaneous Urticaria • Dermatology • Immunology • Urticaria

A Rapid and Reliable Absorbance Assay to Identify Drug-Drug Interactions with Thiopurine Drugs. (PubMed, Metabolites) - "With purified TPMT on hand and the absorbance activity assay, we confirmed several compounds that inhibit TPMT, and the results were comparable to a mass spectral assay that measured 6-MP methylation. Understanding the impact of co-administered drugs on TPMT activity will improve the safety and efficacy of thiopurine-based treatment regimens."

Journal • Immunology • Oncology

TESTING MACHINE LEARNING WITH FINNISH REGISTER DATA TO PREDICT NON-RESPONSE TO CONVENTIONAL TREATMENT IN PATIENTS WITH INFLAMMATORY BOWEL DISEASE (UEGW 2024) - "CT failure outcomes (within one year from CT initiation) for CD, UC, and combined cohorts.CT failure outcomesCD, nCD, %UC, nUC, %Total, nTotal, %Prescription for biologics17185.6%8282.7%1,5463,6%IBD-related surgery8036.3%7282.4%1,5313.6%90-day gap in CT medication (5-ASA2, IM3)2,33918.2%5,32517.6%7,66417.8%≥2 corticosteroid4 prescriptions6,34749.5%14,30247.4%20,64948.0%IBD-related inpatient stay1,33910.4%2,1607.2%3,4998.1%IBD-related ED visit1931.5%3981.3%5911.4%Any of the above8,22364.2%18,45361.1%26,67662.0%1adalimumab, vedolizumab, infliximab, golimumab, ustekinumab, and tofacitinib; 2mesalazine, olsalazine, and sulfasalazine; 3methotrexate, mercaptopurine, azathioprine, cyclosporine, and metronidazole; 4prednisolone, hydrocortisone, budesonide, methylprednisolone, prednisone, and dexamethasone. Data quality is critical to build high-performance models. Even though Finnish registries provide access to comprehensive longitudinal data allowing the generation of..."

Clinical • Machine learning • CNS Disorders • Crohn's disease • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Psychiatry • Rheumatology • Schizophrenia • Ulcerative Colitis

Association of Intestinal Anti-Inflammatory Drug Target Genes with Psychiatric Disorders: A Mendelian Randomization Study (WCPG 2024) - ": We uncovered a causal link between TPMT (a target of olsalazine) expression in the amygdala and bipolar disorder (BD) risk (odds ratio [OR] = 1.08; P = 4.29 × 10−4). This association was observed even when the sigmoid colon and whole blood eQTL were considered as exposures. Colocalization analysis revealed a shared genetic variant (rs11751561) between TPMT expression and BD, with a posterior probability of 61.6%."

Bipolar Disorder • CNS Disorders • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Mental Retardation • Mood Disorders • Obsessive-Compulsive Disorder • Psychiatry • ACAT1

INTERVENTIONS FOR THE MANAGEMENT OF COMPLICATIONS IN PATIENTS WITH INFLAMMATORY BOWEL DISEASE AND PERMANENT ILEOSTOMY FOR THE ENDOTRIAL CONSORTIUM: A SYSTEMATIC REVIEW (UEGW 2024) - "This study highlights that the evidence base to inform care for patients with IBD and PI is almost non-existent. There is an urgent need for focused research in this area to inform evidence-based treatment decisions. The items identified in this review as well as knowledge gaps will inform consensus steps for development of future care pathways and expert guidelines.Table 1."

Clinical • Review • Crohn's disease • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Oncology • Ulcerative Colitis

CANNABIDIOL, WHEN COMBINED WITH OLSALAZINE, OFFERS A NOVEL TREATMENT APPROACH FOR ULCERATIVE COLITIS (UEGW 2024) - "While using CBD alone for treating colitis is ineffective, and high doses of olsalazine used in the clinics often come with adverse effects and lose effectiveness over time, our data show that combining low doses of CBD and olsalazine significantly reduces colitis without adverse effects. Therefore, the low-dose combination of CBD and olsalazine offers a promising novel treatment for ulcerative colitis."

Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Metabolic Disorders • Pain • Ulcerative Colitis • MPO

5-AMINOSALICYLATES FOR PATIENTS WITH ACTIVE OR QUIESCENT CROHN’S DISEASE: AN UMBRELLA REVIEW OF SYSTEMATIC REVIEWS (UEGW 2024) - "One study compared 6-MP to 5-ASA, one study compared AZA to sulfasalazine- the two studies were pooled together in meta-analysisAdultsMaintenance6-MP: 1 mg kg/ d Methotrexate: 10 mg/wk; 76 weeks AZA: 1- 2.5 mg/kg/ d5-ASA: 3g/d; 76 wkOnly two RCTs; no statistically significant difference in the proportion of patients who maintained remission between AZA (1.0 to 2.5 mg/kg/day) or 6-MP (1.0 mg/day) and mesalamine (3 g/day) or sulfasalazine (0.5 g/15 kg/day) therapy.NMAMoja, 2015Oct 2014MEDLINE, EMBASE, the Cochrane library and clinicaltrials.gov25 RCTs (induction =11, maintenance n=14)Budesonide or mesalamine vs placebo or against each other in active or quiescent CDAdultsBothMesalamine: 1 - 4 g/d; 6 wk for induction, 6 mo for maintenanceBudesonide: 3 -18 mg/d; 6 wk for induction, 6 mo for maintenancePlacebo or mesalamine or budesonide in different dosesBudesonide 9mg/d or higher for induction of remission in active mild-to-moderate CD and 6mg/d for maintenance of remission..."

Clinical • Review • Crohn's disease • Gastroenterology • Immunology • Inflammatory Bowel Disease • Pediatrics

An Innovative Inhibitor with a New Chemical Moiety Aimed at Biliverdin IXβ Reductase for Thrombocytopenia and Resilient against Cellular Degradation. (PubMed, Pharmaceutics) - "During the pursuit of inhibitors targeting BLVRB, olsalazine (OSA) became apparent as one of the most potent candidates...Furthermore, we have found that both OSK and OSA inhibit BLVRB, regardless of the presence of nicotinamide adenine dinucleotide phosphate, unlike other known inhibitors. This discovery opens new avenues for investigating the roles of BLVRB in blood disorders, including thrombocytopenia."

Journal • Hematological Disorders • Thrombocytopenia

Thermodynamic modeling of cooperative CO2 adsorption on porous materials (ACS-Fall 2024) - "For example, such behavior is observed during CO2 adsorption on diamine-appended olsalazine MOFs which show potential for direct air capture applications...The model unambiguously reveals atomistic details such as the number of diamine molecules per cooperative network, the energy of cooperation, and the translational degrees of freedom of the bound adsorbate. CO2 adsorption isotherms for the material ee-2–Mg2(olz) at several temperatures fitted to a temperature-dependent global model and the corresponding global model equations."

Refractory Crohn's Disease Responsive to Dietary Therapy: A Case Report. (PubMed, Cureus) - "This report describes a case of treatment-resistant Crohn's disease in a patient who was given all categories of pharmaceutical therapies including prednisone, budesonide, sulfasalazine, olsalazine, 6-mercaptopurine, methotrexate, mesalamine, and adalimumab. In conclusion, for patients whose disease is refractory to different treatments, or who develop antibodies to the medication, AIDs may offer a solution to reduce disease symptoms and progression. Education of healthcare professionals and patients alike is vital in order for Crohn's patients to gain the benefits from dietary therapy."

Journal • Allergy • Crohn's disease • Gastroenterology • Gastrointestinal Disorder • Immunology • Infectious Disease • Inflammation • Inflammatory Bowel Disease

Discovery of putative inhibitors of human Pkd1 enzyme: Molecular docking, dynamics and simulation, QSAR, and MM/GBSA. (PubMed, Environ Res) - "High biological activity and binding free energies of two complexes calculated using 3D QSAR and Schrodinger module, respectively further validated our results. Therefore, the molecular docking and dynamics simulation-based in-silico approach used in this study revealed olsalazine and diosmetin as potential drug candidates to combat polycystic kidney disease by targeting Pkd1 enzyme."

Journal • Genetic Disorders • Nephrology • Polycystic Kidney Disease • Renal Disease • PKD1 • PRKD1

Olsalazine pretreatment augments chemosensitivity of gemcitabine in hepatocellular carcinoma. (PubMed, J Biochem Mol Toxicol) - "Histopathology and IHC showed improved liver morphology with potentiated the induction of P53 upon olsalazine pretreatment in combination with gemcitabine. In conclusion, sequential combination of olsalazine and gemcitabine improved the treatment outcomes during the progression of HCC."

Journal • Breast Cancer • Gastrointestinal Cancer • Hepatocellular Cancer • Oncology • Solid Tumor • CRP • DNMT1 • IL6 • TNFA • TP53

Association of intestinal anti-inflammatory drug target genes with psychiatric Disorders: A Mendelian randomization study. (PubMed, J Adv Res) - "These findings provide novel targets for the treatment of psychiatric disorders, underscore the potential of repurposing olsalazine, and emphasize the importance of TPMT and ACAT1 in future drug development."

Journal • Bipolar Disorder • CNS Disorders • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Mental Retardation • Mood Disorders • Obsessive-Compulsive Disorder • Psychiatry • ACAT1

VISUALIZING HETEROGENEOUS TRAJECTORIES OF SUBJECTS WITH SURGICAL RELAPSE IN INFLAMMATORY BOWEL DISEASE FROM UK BIOBANK GENERAL PRACTICE DATA (CCCongress 2024) - "Additionally, data for the 9 most used IBD prescription medications: budesonide, sulfasalazine, methotrexate, hydrocortisone, balsalazide, olsalazine, prednisolone, azathioprine, and mesalamine was analyzed as well...The majority of patients fell within the states labeled “blue” (azathioprine, sulfasalazine, and prednisone) “red” (mesalamine only) or “purple” (azathioprine, balsalazide, and prednisolone)...We identified three distinct trajectories leading up to surgical relapse. These trajectories show distinctive medication prescription patterns (5-ASA vs. Azathioprine with steroid use), as well as significantly different times to surgical relapse."

Clinical • Heterogeneity • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • CRP

An olsalazine nanoneedle-embedded inulin hydrogel reshapes intestinal homeostasis in inflammatory bowel disease. (PubMed, Bioact Mater) - "Furthermore, analysis of gut microbiota revealed that Cu(Olsa)/Gel treatment increased the diversity of intestinal microflora and decreased the relative abundance of pathogenic bacteria such as Proteobacteria. Overall, this study provides a self-delivering nanodrug and dietary fiber hydrogel composite for IBD therapy, offering an efficient approach to restore intestinal homeostasis."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease

ECONOMIC BURDEN OF SUBOPTIMAL TREATMENT WITH CORTICOSTEROID OVERUSE FOR ULCERATIVE COLITIS (UEGW 2023) - "Pt characteristics and treatment use Pts with CS overuse(N=1820)Pts without CS overuse(N=2184)Age, mean ± standard deviation, years47.7 ± 13.146.4 ± 12.5Female, n (%)1040 (57.1)1171 (53.6)Conventional therapies received in 1L, n (%)Mesalamine511 (28.1)1239 (56.7)CS780 (42.9)393 (18.0)CS + mesalamine359 (19.7)244 (11.2)IM10 (0.5)36 (1.6)IM + mesalamine4 (0.2)22 (1.0)Other regimensa156 (8.6)250 (11.4)​aBalsalazide monotherapy, olsalazine monotherapy, and combinations of CS, IM, and 5-ASA... Approximately half of pts with UC had overused CS while being treated with conventional therapies. In these pts, all-cause HCRU during follow-up, and costs at baseline (except for drug costs) and during follow-up were significantly higher compared with those without CS overuse, suggesting a need for other more effective therapies to be considered for the treatment of these pts. Pts with UC currently treated with prolonged CS courses may benefit from early use of advanced..."

HEOR • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

Rapidly degradable konjac glucomannan hydrogels cross-linked with olsalazine for colonic drug release. (PubMed, Biomed Mater Eng) - "The drug was released more rapidly in a simulated colon environment than in a normal buffer. Furthermore, the drug release was controlled by the degradation of the hydrogel. The KGM hydrogel containing azo crosslinker has great potential for colon drug release."

Journal

The effect of olsalazine of chinese generic drugs on ulcerative colitis induced by dextran sulfate sodium salt in BALB/c mice. (PubMed, Acta Cir Bras) - "It was suggested that olsalazine has a therapeutic effect on ulcerative colitis induced by DSS in mice, and the mechanism may be related to the increase of IL-2, IL-10, IL-22, TGF, and EGF and the decrease of the expression of IL-7, IL-17, TNF-α, IL-1β, and IFN-γ."

Journal • Preclinical • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Oncology • Ulcerative Colitis • EGF • IFNG • IL10 • IL17A • IL1B • IL2 • IL22 • IL7 • TGFB1 • TNFA

Cooperative Carbon Dioxide Capture in Diamine-Appended Magnesium-Olsalazine Frameworks. (PubMed, J Am Chem Soc) - "Spectroscopic characterization and van der Waals-corrected density functional theory calculations indicate that diamine-Mg(olz) materials capture CO via the formation of ammonium carbamate chains. These results point more broadly to the opportunity for fundamentally advancing materials in this class through judicious design."

Journal