Carogra (carotegrast methyl) / Kissei, Eisai - LARVOL DELTA

Efficacy and Safety of Carotegrast Methyl in Ulcerative Colitis: A Systematic Review and Meta-Analysis (ACG 2026) - "Five studies, including 279 patients with UC treated with CGM, were analyzed. The pooled clinical remission rate was 38.9% (95% CI, 25.4-53.2%), while endoscopic remission was 25.5% (95% CI, 12.4-43.3%) (Figure 1). Clinical response was observed in 62.4% (95% CI, 49.1-74.0%) and endoscopic improvement in 50.3% (95% CI, 37.8-62.7%)."

Retrospective data • Review • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis • CRP

Real-World and Trial Evidence on Carotegrast Methyl (AJM300) in Conventional Therapy-Resistant Ulcerative Colitis: A Single-Arm Systematic Review and Meta-Analysis (ACG 2026) - "Five studies (2015-2026) involving 273 AJM300-treated patients were included. Four reported Week 8 clinical remission (n=256), pooled at 38.3% (95% CI, 29.3%-47.8%) with moderate heterogeneity (I²=57.6%); individual rates ranged 23.5%-45.2%. Two studies reported Week 8 endoscopic remission (Mayo Endoscopic Subscore [MES] 0; n=64), pooled at 37.0% (95% CI, 7.0-72.0%; Q p=0.02) with substantial heterogeneity (I²=82.7%), likely reflecting varied study designs, populations, and baseline severity ."

Real-world • Real-world evidence • Retrospective data • Review • CNS Disorders • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Rare Diseases • Ulcerative Colitis

CAROTEGRAST METHYL IN ACTIVE ULCERATIVE COLITIS: REAL-WORLD EFFECTIVENESS, ADHERENCE, AND PREDICTORS OF RESPONSE (UEGW 2026) - No abstract available

Adherence • CAR T-Cell Therapy • Clinical • Real-world • Real-world effectiveness • Real-world evidence • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

Effectiveness, Safety, and Post-Discontinuation Outcomes of Carotegrast Methyl in Ulcerative Colitis: A Real-World Multicenter Retrospective Cohort Study (AOCC-IMKASID 2026) - "Carotegrast methyl is an effective and well-tolerated induction therapy for mild-to-moderate UC. However, the high relapse rate after discontinuation highlights the need for optimized maintenance strategies. Keywords: Ulcerative Colitis, Carotegrast Methyl, A4-integrin Antagonist, Real-world Data"

Real-world • Real-world evidence • Retrospective data • CNS Disorders • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Rare Diseases • Ulcerative Colitis

Clinical Outcomes and Mucosal Healing of Carotegrast Methyl in an IBD Clinic (AOCC-IMKASID 2026) - "CGM treatment resulted in favorable clinical and endoscopic remission. It demonstrates both efficacy and safety as a treatment prescribed in IBD clinics. Keywords: Carotegrast Metyl, Ulcertive Colitis, Post-marketing Clinical Practice, Mucosal Healing"

Clinical • Clinical data • CNS Disorders • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Rare Diseases • Ulcerative Colitis • ITGA4

Use of Carotegrast Methyl in 15 Patients with Ulcerative Colitis: A Single-Center Experience (AOCC-IMKASID 2026) - "For maintenance therapy after remission, six patients (86%) were managed with 5-aminosalicylic acid (5-ASA) monotherapy, and one patient (14%) received vedolizumab monotherapy. According to the 2024 Japanese treatment guidelines for UC, CAR is recommended for patients with mild to moderate disease who are refractory or inadequately responsive to 5-ASA. Our findings suggest that CAR may be a useful therapeutic option, particularly in patients with moderate UC in whom the indication for systemic corticosteroids is uncertain. A relatively favorable remission rate was observed in patients with left-sided colitis."

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

Small Molecules as Advanced Therapy for the Treatment of Inflammatory Bowel Disease, Particularly Regarding Ulcerative Colitis. (PubMed, Intern Med) - "Currently, three Janus kinase (JAK) inhibitors (tofacitinib, filgotinib, and upadacitinib), two Sphingosine-1-phosphate receptor (S1PR) modulators (ozanimod and etrasimod), and one alpha4-integrin antagonist (carotegrast methyl) are available in Japan. S1PR modulators have similar mechanisms of action, except for the titration at the beginning and the recovery time of the lymphocyte count after discontinuation. Overall, small-molecule drugs are effective and convenient options for IBD, with safety profiles that require individual patient assessment."

Journal • Cardiovascular • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Arthritis • Inflammatory Bowel Disease • Rheumatoid Arthritis • Rheumatology • Ulcerative Colitis • ITGA4

Impact of Corticosteroid Therapy on Long-term Treatment Outcomes in Ulcerative Colitis: A Retrospective Cohort Study (ECCO-IBD 2026) - "Recent availability of carotegrast methyl and oral budesonide has expanded treatment options before AT initiation, necessitating re-evaluation of CS use strategies...AT breakdown: infliximab/adalimumab/golimumab/vedolizumab/ustekinumab/upadacitinib/tofacitinib/filgotinib = 37/20/15/15/7/2/1/1...Cumulative CS dose ≥3,000 mg increases the risk of refractory disease 4.35-fold. These findings suggest that early transition to AT should be considered in elderly-onset patients, and cumulative CS dose of 3,000 mg may serve as a useful threshold for treatment strategy modification, potentially contributing to individualised UC management."

Retrospective data • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

Repeated Administration of Carotegrast Methyl Maintained Clinical Remission With Difficult-to-Treat Ulcerative Colitis. (PubMed, Inflamm Bowel Dis) - No abstract available

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

Integrin Inhibitors for Ulcerative Colitis Treatment. (PubMed, Digestion) - "This article describes the mechanism of integrin inhibitors' action, the usefulness and positioning of vedolizumab and carotegrast methyl, which are currently available for clinical use to treat ulcerative colitis, and the status of integrin inhibitor development."

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

A rare case of ulcerative colitis relapse in a diverted colon after rectal cancer surgery: efficacy of carotegrast methyl. (PubMed, Clin J Gastroenterol) - "This case demonstrates that carotegrast methyl may serve as an effective steroid-sparing option for UC relapse in complex postoperative anatomical contexts. It also highlights the potential utility of PET-CT as an adjunctive diagnostic tool for UC-associated cancer."

Journal • Colorectal Cancer • Gastroenterology • Gastrointestinal Disorder • Immunology • Infectious Disease • Inflammatory Bowel Disease • Oncology • Rectal Cancer • Solid Tumor • Ulcerative Colitis • CEACAM5

From Cytokines to Biomarkers: Mapping the Immunopathology of Inflammatory Bowel Disease. (PubMed, Cells) - "New classes of medications with more favorable side effect profiles include anti-integrin antibodies, vedolizumab, etrolizumab, and carotegrast methyl. Additionally, fecal microbiota transplant (FMT) is a newer area of research for treatment of IBD along with TNF-blockers, JAK inhibitors, and S1PR modulators. However, expense and long preparation time have limited the usefulness of FMT."

Biomarker • IO biomarker • Journal • Review • Crohn's disease • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Transplantation • Ulcerative Colitis • ATG16L1 • CARD9 • CTLA4 • MMP9 • MPO

Optimising carotegrast methyl use in ulcerative colitis: patient profiling, predictive biomarkers, and timing of efficacy evaluation (ASPECT study). (PubMed, J Gastroenterol) - "Carotegrast methyl appears most effective in patients with moderately active ulcerative colitis with low disease activity, with week 2 and beyond as an appropriate time point for assessing efficacy. Anti-integrin αvβ6 antibody titre shows promise in predicting response to carotegrast methyl. Faecal calprotectin may serve as a non-invasive surrogate for evaluating endoscopic healing."

Biomarker • Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis • CRP

Real-world effectiveness and safety of carotegrast methyl in patients with ulcerative colitis: a multicenter retrospective cohort study. (PubMed, Intest Res) - "Carotegrast methyl demonstrated good efficacy and safety, potentially benefiting patients with low baseline disease activity. This drug may be a useful treatment option to consider before systemic corticosteroid therapy for ulcerative colitis."

Journal • Real-world evidence • Retrospective data • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

Efficacy and safety of carotegrast methyl in active ulcerative colitis: a real-world prospective cohort study. (PubMed, Intest Res) - "Carotegrast methyl effectively induces both clinical and endoscopic remission in patients with active UC and has a favorable safety profile. Re-administration is safe and effective for patients experiencing relapse."

Journal • Real-world evidence • Gastroenterology • Gastrointestinal Disorder • Hepatology • Immunology • Inflammatory Bowel Disease • Liver Failure • Ulcerative Colitis

NOVEL ORAL INHIBITOR OF Α4Β1 AND Α4Β7 INTEGRINS ABROGATES EXPERIMENTAL COLITIS (DDW 2025) - "While systemic α4 blockade was particularly effective (natalizumab), its use has been limited due to risk of progressive multifocal leukoencephalopathy (PML)...WU-106 has an IC 50 of 0.5 nM in the soluble VCAM assay for inhibition of VLA4, more than 200 times greater potency compared to AJM300 (118.3 nM), and an IC 50 of 5 nM in the α4β7 SPRA assay. WU-106 shows promise as an oral therapeutic agent targeting both α4β7 and α4β1 integrins in colitis models. WU-106 appears particularly effective in gut-specific contexts, with significantly enhanced potency and minimal systemic exposure after oral dosing, warranting further investigation for clinical application."

CNS Disorders • Crohn's disease • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Rare Diseases • Ulcerative Colitis

CAR in UC: Carotegrast Methyl in Ulcerative Colitis (clinicaltrials.gov) - P4 | N=50 | Completed | Sponsor: Takayuki Yamamoto

New P4 trial • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis

Relationship between Total Corticosteroid Dose Prior to Advanced Therapy Induction and Primary Non-Response (ECCO-IBD 2025) - "CS treatment efficacy decreases with repeated use, affecting therapeutic outcomes of GMA and carotegrast...Conclusion As previously reported, elderly-onset UC requires careful management due to potentially poor treatment response. The total CS dose appears to significantly impact primary non-response, suggesting that early transition to Advanced Therapy may be crucial for optimal patient outcomes."

Metastases • Crohn's disease • Inflammatory Bowel Disease • Ulcerative Colitis

Real-World Effectiveness and Safety of Carotegrast Methyl in Japanese Patients with Moderately Active Ulcerative Colitis. (PubMed, Inflamm Intest Dis) - "No adverse drug reactions, including progressive multifocal leukoencephalopathy, were reported during the study period. This single-center, retrospective, observational study of 14 Japanese patients with UC showed that CGM was safe and effective as a remission induction treatment for moderately active UC with an inadequate response to 5-aminosalicylates in real-world settings."

Journal • Real-world • Real-world effectiveness • Real-world evidence • CNS Disorders • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Pain • Rare Diseases • Ulcerative Colitis

Old and New Biologics and Small Molecules in Inflammatory Bowel Disease: Anti Integrins (PubMed, Korean J Gastroenterol) - "Etrolizumab (anti-β7) blocks leukocyte trafficking via α4β7 and cell adhesion via αEβ7 integrins. In addition, the introduction of subcutaneous vedolizumab showed similar efficacy and safety with improved patients' convenience. Other investigational anti-integrin therapies include abrilumab (anti-α4β7 IgG2), PN-943 (orally administered and gut-restricted α4β7 antagonist peptide), AJM300 (orally active small molecule inhibitor of α4), and ontamalimab (anti-MAdCAM-1 IgG)."

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

CLINICAL SIGNIFICANCE OF EOSINOPHILS IN CORTICOSTEROID THERAPY FOR ACTIVE ULCERATIVE COLITIS (DDW 2024) - "Currently new immunomodulatory therapies are being developed for the treatment of UC in particular carotegrast methyl a drug showing promise in the treatment of patients with moderate UC refractory to 5-aminosalicylic acid (5-ASA)... Both eosinophil ratios and total count numbers in the blood may be potential biomarkers for steroid responsiveness prior to administration. Histologically changes in eosinophilic infiltration may serve as response indicators for the administration of steroid therapy."

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

The Era of Small Molecules: Good Things Come in Small Packages (IMKASID 2024) - "Following tofacitinib, filgotinib and upadacitinib were also introduced as JAK inhibitors for the treatment of ulcerative colitis...Ozanimod was the first S1PR modulator approved for the treatment o f ulcerative colitis in the United States and Europe, followed by the approval of etrasimod in Europe for the same indication...In Jap an, the oral α4 inhibitor carotegrast methyl is also available for the treatment of ulcerative colitis...They also lack antigenicity, offering the possibility of drug holidays. On the other hand, the development of biomarkers to predict the effectiveness of the numerous molecular targeted therapies, including biologics, for individu al patients is urgently needed."

Cardiovascular • Crohn's disease • Gastroenterology • Gastrointestinal Disorder • Herpes Zoster • Inflammatory Bowel Disease • Macular Edema • Ophthalmology • Ulcerative Colitis • Varicella Zoster • TYK2

Effects of rifampicin on the pharmacokinetics and safety of carotegrast methyl in healthy subjects: A randomized 2 × 2 crossover study. (PubMed, Br J Clin Pharmacol) - "Coadministration of carotegrast methyl with rifampicin significantly increased the exposure of carotegrast compared with carotegrast methyl administration alone. In this single dose study, the incidence of AEs of carotegrast methyl with rifampicin increased compared with carotegrast methyl alone, but the incidence of adverse drug reactions did not increase with combination administration."

Journal • PK/PD data

Evaluation of the potential drug-drug interactions of carotegrast methyl with midazolam, prednisolone, or atorvastatin in healthy adults. (PubMed, Br J Clin Pharmacol) - "Carotegrast methyl was classified as a moderate CYP3A4 inhibitor in humans. Carotegrast methyl might enhance the action of drugs that are metabolized by CYP3A4."

Journal

BIOMARKER OF CORTICOSTEROID THERAPY FOR MODERATELY TO SEVERELY ACTIVE ULCERATIVE COLITIS (UEGW 2023) - "Currently, new immunomodulatory therapies are being developed for the treatment of UC, like carotegrast methyl, a drug showing promise in the treatment of patients with moderate UC refractory to 5-aminosalicylic acid (5-ASA)...The proportion of patients treated with azathioprine was significantly higher in the SNR group (40%) than in the SR group (39%)... Both eosinophil ratios in the blood and rectal mucosa, and neutrophil-lymphocyte ratios in the blood may be potential biomarkers for steroid responsiveness prior to administration."

Biomarker • Gastroenterology • Gastrointestinal Disorder • Hematological Disorders • Immunology • Inflammatory Bowel Disease • Ulcerative Colitis