| 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 |
Discontinuation rate of azathioprine
PMID: 32744415
Year: 2020
Relationship Type:
Association
Score: 6.5
Combination therapy in inflammatory bowel disease patients: do we need to maxim…
PMID: 32689833
Year: 2020
Relationship Type:
Treatment
Score: 6.5
Coalescent simulations are widely used to examine the effects of evolution and demographic history on the genetic makeup of populations. Thanks to r…
Microbial Butyrate Synthesis Indicates Therapeutic Efficacy of Azathioprine in …
PMID: 32687146
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Inflammatory bowel diseases (IBD) are chronic, relapsing-remitting inflammatory conditions with a substantial negative impact on health-…
Discontinuation rate of azathioprine
PMID: 32627355
Year: 2020
Relationship Type:
Association
Score: 6.5
Adjustment of azathioprine dose should be based on a lower 6-TGN target level t…
PMID: 32598049
Year: 2020
Relationship Type:
Association
Score: 6.5
BACKGROUND: The causes of chronic antibiotic refractory pouchitis (CARP) and pouch failure in inflammatory bowel disease (IBD) patients remain unkno…
[Isolated Crohn's disease of the vulva with rapid clinical response to inflixim…
PMID: 32505375
Year: 2020
Relationship Type:
Association
Score: 6.5
Azathioprine-Induced Tremor: A Rare, Dose-Dependent Side Effect of Azathioprine…
PMID: 32444877
Year: 2020
Relationship Type:
Adverse Effect
Score: 6.5
Azathioprine-induced cholestasis of pregnancy-A new insight on azathioprine saf…
PMID: 32439244
Year: 2020
Relationship Type:
Association
Score: 6.5
[Duration of sustained remission after treatment by induction with exclusive en…
PMID: 32430216
Year: 2021
Relationship Type:
Treatment
Score: 6.5
Severe Necrotising Toxoplasmic Retinochoroiditis in a Patient With Crohn's Dise…
PMID: 32415301
Year: 2020
Relationship Type:
Association
Score: 6.5
AOX1 and XDH Enzymes Genotyping and its Effect on Clinical Response to Azathiop…
PMID: 32282298
Year: 2020
Relationship Type:
Mechanism
Score: 6.5
Interleukin-33 (IL-33) has emerged as a critical regulator in a variety of diseases, including inflammatory bowel disease (IBD). IL-33 can be produc…
How Does It Look in an Autopsy? Hepatosplenic T-Cell Lymphoma in a Patient with…
PMID: 32270949
Year: 2020
Relationship Type:
Association
Score: 6.5
Adherence to Azathioprine/6-Mercaptopurine in Children and Adolescents with Inf…
PMID: 32185153
Year: 2020
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: No conclusive treatment is available for irritable bowel disease (IBD). Adherence to a diet low in fermentable oligosaccharides, disacch…
New role for azathioprine in case of switching anti-TNFs in IBD
PMID: 32075889
Year: 2020
Relationship Type:
Treatment
Score: 6.5
Anti- tumor Necrosis Factor (anti-TNF) agents are the backbone treatment of moderate to severe cases of inflammatory bowel disease. One of the main …
Addition of azathioprine to the switch of anti-TNF in patients with IBD in clin…
PMID: 31980448
Year: 2020
Relationship Type:
Association
Score: 6.5
BACKGROUND: Interleukin 10 receptor alpha subunit (IL10RA) dysfunction is the main cause of very early-onset inflammatory bowel disease (VEO-IBD) in…
Azathioprine Has a Deleterious Effect on the Bone Health of Mice with DSS-Induc…
PMID: 31816823
Year: 2019
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: There is limited information regarding the impact of patients' perception of injection pain on adherence to treatments, specifically in …
The potential application of human PIG-A assay on azathioprine-treated inflamma…
PMID: 31743483
Year: 2020
Relationship Type:
Treatment
Score: 6.5
Inflammatory bowel disease (IBD) is a chronic disease that occurs in the intestinal tract. Phyto-ingredients have been evaluated for their ability t…
Determination of azathioprine/6-mercaptopurine metabolites in dried blood spots…
PMID: 31685266
Year: 2020
Relationship Type:
Association
Score: 6.5
Comment in Aliment Pharmacol Ther. 2019 Nov;50(10):1137-1138. Aliment Pharmacol Ther. 2020 Feb;51(3):405. BACKGROUND: Obesity is associated …
TPMT Genotype and Adverse Effects of Azathioprine among Jordanian Group
PMID: 31631819
Year: 2019
Relationship Type:
Treatment
Score: 6.5
Thiopurines are central to inflammatory bowel disease (IBD) therapeutics, either as monotherapy or in combination with newer biologic therapies, how…
Azathioprine and 6-mercaptopurine for maintenance of surgically-induced remissi…
PMID: 31425621
Year: 2019
Relationship Type:
Treatment
Score: 6.5
G protein-coupled receptor (GPR) 40 is a receptor for long-chain free fatty acids that enhances glucagon-like peptide (GLP)-2 production in intestin…