| Drug ID: | Drug10 |
|---|---|
| Drug Name: | Azathioprine |
| CID: | 2265 |
| DrugBank ID: | DB00993 |
| Modality: | Small Molecule |
| Groups: | approved |
| US Approved: | YES |
| Other Approved: | YES |
| Identifier: | NCT03370601, , NCT02413047, , NCT06213857, , NCT02281799, , NCT03101800, , NCT04882683, , NCT03151525, , NCT00984568, , NCT02579733, , NCT01817972 |
| Molecular Formula: | C9H7N7O2S |
| Molecular Weight: | 277.27 g/mol |
| Isomeric SMILES: | CN1C=NC(=C1SC2=NC=NC3=C2NC=N3)[N+](=O)[O-] |
| Synonyms: | azathioprine; 446-86-6; Azothioprine; Azathioprin; Azamun; Azanin; Azatioprin; Azasan; Ccucol; Imurek |
| Phase 0: | 3 |
| Phase 1: | 7 |
| Phase 2: | 38 |
| Phase 3: | 59 |
| Phase 4: | 44 |
| Description: | An immunosuppressive antimetabolite pro-drug. It is an imidazolyl derivative of 6-mercaptopurine and many of its biological effects are similar to those of the parent compound. Azathioprine is converted into 6-mercaptopurine in the body where it blocks purine metabolism and DNA synthesis. |
Molecular Structure
Knowledge Graph
| dtID | CID | Compound Name | Gene ID | Gene Name | Species | PubMed IDs | Action |
|---|---|---|---|---|---|---|---|
| dt80 | 2265 | Azathioprine | 5243 | ABCB1 | Homo sapiens (human) | 17262810 | ABCB1 gene polymorphism affects the susceptibility to azathioprine |
| dt81 | 2265 | Azathioprine | 8647 | ABCB11 | Rattus norvegicus (Norway rat) | 27765674 | Azathioprine results in decreased expression of ABCB11 mRNA |
| dt82 | 2265 | Azathioprine | 5244 | ABCB4 | Rattus norvegicus (Norway rat) | 27765674 | Azathioprine results in increased expression of ABCB4 mRNA |
| dt83 | 2265 | Azathioprine | 1244 | ABCC2 | Homo sapiens (human) | 22623647 | Azathioprine results in increased expression of ABCC2 mRNA |
| dt84 | 2265 | Azathioprine | 1244 | ABCC2 | Rattus norvegicus (Norway rat) | 27765674 | Azathioprine results in increased expression of ABCC2 mRNA |
| dt85 | 2265 | Azathioprine | 8714 | ABCC3 | Rattus norvegicus (Norway rat) | 27765674 | Azathioprine results in increased expression of ABCC3 mRNA |
| dt86 | 2265 | Azathioprine | 10257 | ABCC4 | Rattus norvegicus (Norway rat) | 27765674 | Azathioprine results in increased expression of ABCC4 mRNA |
| dt87 | 2265 | Azathioprine | 9429 | ABCG2 | Rattus norvegicus (Norway rat) | 27765674 | Azathioprine results in decreased expression of ABCG2 mRNA |
| dt88 | 2265 | Azathioprine | 64240 | ABCG5 | Rattus norvegicus (Norway rat) | 27765674 | Azathioprine results in decreased expression of ABCG5 mRNA |
| dt89 | 2265 | Azathioprine | 63874 | ABHD4 | Homo sapiens (human) | 22623647 | Azathioprine results in increased expression of ABHD4 mRNA |
- No data available
Phase Distribution
Phase Description
- Phase 0: Exploratory trials to assess drug behavior in humans
- Phase 1: Safety trials to determine safe dosage range
- Phase 2: Efficacy trials to evaluate therapeutic effects
- Phase 3: Large-scale trials to confirm efficacy and safety
- Phase 4: Post-marketing surveillance for long-term safety and efficacy
| Trial ID | Title | Phase | Status | Sponsor | Indications | Interventions | |
|---|---|---|---|---|---|---|---|
| NCT04882683 | Clinical Study of Cord Blood Mononuclear Cells on Treatment of Hormone-resistant or Hormone-dependent Ulcerative Colitis | None | UNKNOWN | Shandong Qilu Stem Cells Engineering Co., Ltd. | Ulcerative Colitis | DRUG: Prednisone|DRUG: Azathioprine|DRUG: Adalimu… | Details |
| NCT03151525 | Two Therapeutic Strategies for the Maintenance of Remission in Patients With Ulcerative Colitis | PHASE4 | UNKNOWN | Istituto Clinico Humanitas | Colitis, Ulcerative | DRUG: Azathioprine|DRUG: Infliximab | Details |
| NCT00984568 | Conventional Step-Up Versus Infliximab Monotherapy in Patients With Ulcerative Colitis (P05553) | PHASE3 | TERMINATED | Merck Sharp & Dohme LLC | Colitis, Ulcerative | BIOLOGICAL: Infliximab|DRUG: Prednisolone|DRUG: 5… | Details |
| NCT00537316 | Efficacy & Safety of Infliximab Monotherapy Vs Combination Therapy Vs AZA Monotherapy in Ulcerative Colitis (Part 1) Maintenance Vs Intermittent Therapy for Maintaining Remission (Part 2)(Study P04807) | PHASE3 | TERMINATED | Merck Sharp & Dohme LLC | Ulcerative Colitis | BIOLOGICAL: Infliximab (IFX)|DRUG: Azathioprine (… | Details |
| NCT02579733 | Azathioprine Based on Endoscopy After Clinical Remission in Moderate to Severe Ulcerative Colitis | PHASE4 | TERMINATED | Kyungpook National University Hospital | Ulcerative Colitis | DRUG: Azathioprine|DRUG: Placebo | Details |
| NCT01817972 | Cimzia Versus Cimzia Plus Azathioprine in the Treatment of Active Crohn's Disease | PHASE3 | UNKNOWN | Gastroenterology Research of America | Crohn's Disease | BIOLOGICAL: Certolizumab pegol|DRUG: Azathioprine | Details |
| CTRI/2023/10/058514 | Evaluation of effectiveness and safety of oral tofacitinib in patients with Parthenium dermatitis: A prospective interventional open label study - NIL | Not Available | Not Recruiting | AIIMS, New Delhi | Health Condition 1: L237- Allergic contact dermat… | Intervention1: Oral Tofacitinib: Tofacitinib is a… | Details |
| ISRCTN95420128 | Subcutaneous CT-P13 monotherapy versus combination with immunomodulation when switching from intravenous infliximab in inflammatory bowel disease A multicentre, randomised withdrawal trial | PHASE4 | Recruiting | Kings Health Partners | Crohn's disease and ulcerative colitis Digestive… | The intervention is the withdrawal of immunomodul… | Details |
| NCT05456776 | Azathioprine Linked With Impaired Intestinal Epithelial Postoperative Regeneration in Crohn's Disease | Not Available | Not recruiting | Centre of Postgraduate Medical Education | None | None | Details |
| NCT04761952 | N-3 Polyunsaturated Fatty Acids Prevent Postoperative Recurrence of Crohn's Disease:a Prospective Randomized Controlled Trial | Not Available | Not recruiting | Sixth Affiliated Hospital, Sun Yat-sen University | Inflammatory Bowel Diseases;Crohn Disease;Polyuns… | Drug: azathioprine;Drug: infliximab;Drug: N-3 Pol… | Details |
| EUCTR2019-002942-19-DK | NORDTREAT_The Nordic IBD treatment strategy trial a randomized controlled trial of access to a protein profile_ | PHASE4 | Not Recruiting | Region ebro l | Crohn's disease and Ulcerative colitis MedDRA ve… | Trade Name: Remicade Infliximab Pharmaceutical Fo… | Details |
| DRKS00013246 | 6-TGN levels (azathioprine drug monitoring) and markers of mucosal healing in patients with inflammatory bowel disease | Not Available | Not Recruiting | MHH OE6810 | K50 K51;Crohn disease [regional enteritis];Ulcer… | Group 1: Patients with IBD and azathioprine monot… | Details |
| EUCTR2016-004112-35-SE | Low-dose azathioprine and allopurinol- versus azathioprine monotherapy in patients with Inflammatory Bowel Disease: An investigator-initiated, open, multicentre, parallel-arm, randomized controlled trial __A SOIBD (The Swedish Organisation for the study of Inflammatory Bowel Diseases) study __ | PHASE4 | Authorised | SOIBD (The Swedish Organisation for the study of Inflammatory Bowel Diseases) | Patients with inflammatory bowel diseae (Ulcerati… | Trade Name: Imurel Product Name: Azathioprine Pro… | Details |
| ChiCTR-OOC-17010617 | Study on the relationship between TPMT and NUDT15 gene polymorphism and azathioprine-induced adverse reactions in patients with inflammatory bowel disease | Not Available | Recruiting | Xiangya Hospital, Central South University | Inflammatory Bowel Disease | Two cohorts:azathioprine treatment; | Details |
| NCT02929706 | Effectiveness of Thiopurine Dose Optimization by NUDT 15 R139C on Reducing Thiopurine-induced Leucopenia in Inflammatory Bowel Disease | Not Available | Not recruiting | Sixth Affiliated Hospital, Sun Yat-sen University | Thiopurine-induced Leukopenia | Genetic: Pre-genotype NUDT15 and optimize azathio… | Details |
| EUCTR2016-000522-18-FR | Risk stratified randomized controlled trial in paediatric Crohn Disease: Methotrexate versus azathioprine or adalimumab for maintaining remission in patients at low or at high risk for aggressive disease course, respectively a treatment strategy - REDUCE-RISKincd-PIBD-TRIAL | PHASE4 | Not Available | PIBDNet | Crohn disease;Therapeutic area: Diseases [C] - Di… | Product Name: humira Pharmaceutical Form: Solutio… | Details |
| ACTRN12613001347752 | A randomized controlled trial of patients with IBD attending specialist clinics comparing de novo combination allopurinol and thiopurine versus thiopurine and placebo (ie standard practice) in terms of objective and clinical outcomes at six months | PHASE3|PHASE4 | Recruiting | Eastern Health | Inflammatory Bowel Disease; Inflammatory Bowel D… | De novo combination therapy with allopurinol 100m… | Details |
| EUCTR2013-001503-37-DK | Effect of low-dose Azathioprine and Allopurinol compared to Azathioprine on clinical outcomes in Inflammatory Bowel Disease | PHASE3 | Not Recruiting | Marianne Kiszka-Kanowitz | Inflammatory Bowel Disease, (Ulcerativ colitis, C… | Trade Name: Imurel Pharmaceutical Form: Tablet IN… | Details |
| ACTRN12611000363987 | The Triple A (Adjunctive Allopurinol and Azathioprine) Study: Use of Ajunctive Allopurinol in Azathioprine/6-Mercaptopurine Non-responders to Optimize 6-Thioguanine Nucleotide Production and Improve Clinical Outcomes in Patients with Inflammatory Bowel Disease (IBD). | PHASE3|PHASE4 | Not Recruiting | The Alfred Hospital | Inflammatory Bowel Disease (IBD); Inflammatory B… | Eligible IBD patients will be randomly allocated … | Details |
| NL-OMON22783 | Long term hepatotoxicity of azathioprine, 6-mercaptopurine and 6-thioguanine in inflammatory bowel disease. | Not Available | Not Recruiting | Department of Gastroenterology and Hepatology, VU University Medical Center, Amsterdam, The Netherlands | Inflammatory bowel disease, azathioprine, 6-merca… | 1. Liver biopsy; 2. Venapuncture; 3. Abdominal … | Details |
| Disease ID | Disease Name | Definition | Category | Related Drugs | Mechanism | |
|---|---|---|---|---|---|---|
| No data available | ||||||
| Strategy ID | Therapeutic Strategy | Synonyms | Related Drugs | Mechanism | |
|---|---|---|---|---|---|
| S02 | Immunosuppression | Classic immunosuppressive drugs | azathioprine; 6-mercaptopurine; methotrexate; ciclosporin-A; tacrolimus | Ciclosporin-A and tacrolimus bind to specific intracellular… | Details |
Immunomodulatory Agents for Treatment of Patients with Inflammatory Bowel Disea…
PMID: 34913108
Year: 2021
Relationship Type:
Treatment
Score: 6.5
At the beginning of the coronavirus disease 2019 (COVID-19) pandemic, there were many unknowns: transmission vectors of the virus, appropriate inter…
Frequency, Predisposing Factors, and Clinical Outcome of Azathioprine-Induced P…
PMID: 34860811
Year: 2021
Relationship Type:
Association
Score: 6.5
BACKGROUND: Faecal calprotectin (FC) testing to detect inflammatory bowel disease (IBD) was recommended for use in UK general practice in 2013. The …
A novel NUDT15 variant identified in Caucasian TPMT wild type patients with inf…
PMID: 34751173
Year: 2022
Relationship Type:
Adverse Effect
Score: 6.5
Azathioprine with Allopurinol Is a Promising First-Line Therapy for Inflammator…
PMID: 34729677
Year: 2022
Relationship Type:
Treatment
Score: 6.5
Decision makers are used to consider Out-of-Pocket Expenditure (OOPE) within a health technology assessment framework in order to account for an ind…
Idiopathic non-cirrhotic portal hypertension (INCPH) during azathioprine treatm…
PMID: 34454746
Year: 2022
Relationship Type:
Treatment
Score: 6.5
Cost-effectiveness analysis of genotype screening and therapeutic drug monitori…
PMID: 34430579
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: One goal of multi-omic studies is to identify interpretable predictive models for outcomes of interest, with analytes drawn from multipl…
Usefulness of Measuring Thiopurine Metabolites in Children with Inflammatory Bo…
PMID: 34239556
Year: 2021
Relationship Type:
Association
Score: 6.5
Clinicians may be hesitant to prescribe biologics or immunomodulators to individuals with familial adenomatous polyposis (FAP) and comorbid inflamma…
Real-World Use of Azathioprine Metabolites Changes Clinical Management of Infla…
PMID: 34056527
Year: 2020
Relationship Type:
Association
Score: 6.5
Eltrombopag can be used safely as upfront medication in the management of ulcerative colitis as well as ITP, and it showed a beneficial effect in bo…
Azathioprine-induced Myelotoxicity After Switching Mesalazine Compound
PMID: 33999201
Year: 2021
Relationship Type:
Adverse Effect
Score: 6.5
Importance of NUDT15 c.415C>T phenotype in treatment of inflammatory bowel dise…
PMID: 33860754
Year: 2021
Relationship Type:
Treatment
Score: 6.5
Worldwide incidence of inflammatory bowel disease (IBD) is stable in developed countries, but rising in developing countries. Presenting symptoms of…
Pretreatment HLADQA1-HLADRB1 Testing for the Prevention of Azathioprine-Induced…
PMID: 33821842
Year: 2021
Relationship Type:
Treatment
Score: 6.5
Comment in Clin Gastroenterol Hepatol. 2022 Feb;20(2):e28-e30. BACKGROUND & AIMS: The risk of serious infections associated with vedolizumab in …
Impact of Inflammatory Bowel Disease and Azathioprine on Long-Term Outcomes Aft…
PMID: 33569894
Year: 2021
Relationship Type:
Association
Score: 6.5
NUDT15 genotyping during azathioprine treatment in patients with inflammatory b…
PMID: 33442476
Year: 2020
Relationship Type:
Treatment
Score: 6.5
Comment in Rev Esp Enferm Dig. 2021 Feb;113(2):153-154. INTRODUCTION AND OBJECTIVES: the SARS-COV-2 pandemic has forced a substantial change in…
Optimization of azathioprine dose in combined treatment with anti-TNF-alpha in …
PMID: 33272733
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Colitis-associated cancer (CAC) accounts for 2%-3% of colorectal cancer (CRC) cases preceded by inflammatory bowel diseases (IBD) such a…
Editorial: methotrexate vs azathioprine-do differential rates of discontinuatio…
PMID: 33263380
Year: 2020
Relationship Type:
Association
Score: 6.5
Methotrexate or azathioprine-do differing rates of discontinuation settle the d…
PMID: 33263378
Year: 2020
Relationship Type:
Association
Score: 6.5
Azathioprine for prevention of clinical recurrence in Crohn's disease patients …
PMID: 33215456
Year: 2020
Relationship Type:
Association
Score: 6.5
Nerve injury-induced protein 1 (Ninjurin1, Ninj1) is a cell-surface adhesion molecule that regulates cell migration and attachment. This study demon…
Population pharmacokinetics of azathioprine active metabolite in patients with …
PMID: 33150655
Year: 2021
Relationship Type:
Treatment
Score: 6.5
Biogenic amines (BA) are a broad group of biologically active substances, the presence of which in the human body can provide important diagnostic i…
NUDT15 C415T variant compared with TPMT genotyping in predicting azathioprine-i…
PMID: 33111378
Year: 2020
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Disease heterogeneity, according to the age at onset, has been reported in Crohn's disease (CD). OBJECTIVE: This study aimed to compare …
Azathioprine-Induced Acute Submandibular Sialadenitis in a Crohn's Disease Pati…
PMID: 32999909
Year: 2020
Relationship Type:
Treatment
Score: 6.5
Inflammatory bowel disease (IBD), consisting of ulcerative colitis (UC) and Crohn's disease (CD), is featured by overactive immune response and endu…