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

2D Molecular Structure

Knowledge Graph

dtIDCIDCompound NameGene IDGene NameSpeciesPubMed IDsAction
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 IDTitlePhaseStatusSponsorIndicationsInterventions
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 IDDisease NameDefinitionCategoryRelated DrugsMechanism
No data available

Strategy IDTherapeutic StrategySynonymsRelated DrugsMechanism
S02 Immunosuppression Classic immunosuppressive drugs azathioprine; 6-mercaptopurine; methotrexate; ciclosporin-A; tacrolimus Ciclosporin-A and tacrolimus bind to specific intracellular… Details

[Nodular regenerative hyperplasia: azathioprine-induced hepatotoxicity in a pat…

PMID: 21168244
Year: 2011
Relationship Type: Treatment Score: 9.1

We report the case of a 53-year-old man with Crohn's disease who developed azathioprine-induced nodular regenerative hyperplasia of the liver. The di…

Infliximab and/or azathioprine in the treatment of Crohn's disease-like complic…

PMID: 21160308
Year: 2011
Relationship Type: Treatment Score: 9.1

PURPOSE: Ileal pouch-anal anastomosis continues to be confounded by Crohn's disease-like complications after surgery. Such patients experience signif…

Usefulness of the measurement of azathioprine metabolites in the assessment of …

PMID: 21122567
Year: 2010
Relationship Type: Treatment Score: 9.1

Azathioprine is a thiopurine immunosuppressive antimetabolite used to chronically treat inflammatory bowel disease and autoimmune hepatitis. Azathiop…

Increased proportion of CD16(+) NK cells in the colonic lamina propria of infla…

PMID: 21083588
Year: 2011
Relationship Type: Treatment Score: 9.1

AIM: To investigate variants of immunity-related GTPase family M (IRGM) and NKX2-3 genes and genotype-phenotype in Eastern European patients with i…

Nodular regenerative liver hyperplasia as a complication of azathioprine-contai…

PMID: 20726808
Year: 2011
Relationship Type: Treatment Score: 9.1

Nodular regenerative liver hyperplasia (NRH) is a very rare but potentially severe complication of thiopurine-containing immunosuppressive therapy fo…

Predictive factors of azathioprine prescription in adult patients with Crohn's …

PMID: 20583428
Year: 2010
Relationship Type: Treatment Score: 9.1

BACKGROUND/AIMS: Azathioprine is the most commonly used immunomodulator in Crohn's disease. The aims of the study are to determine the cumulative fre…

Nodular regenerative hyperplasia of the liver secondary to azathioprine in a pa…

PMID: 20581898
Year: 2010
Relationship Type: Treatment Score: 9.1

A case of dramatic portal hypertension with massive ascites and splenomegaly is described in a patient with inflammatory bowel disease receiving azat…

Azathioprine versus mesalazine for prevention of postoperative clinical recurre…

PMID: 20551460
Year: 2010
Relationship Type: Treatment Score: 9.1

OBJECTIVE: The aim of the study was to compare azathioprine versus mesalazine tablets for the prevention of clinical recurrence in patients with post…

Azathioprine-induced liver injury in a patient with multiple autoimmune syndrome

PMID: 20443662
Year: 2010
Relationship Type: Treatment Score: 9.1

Extraintestinal manifestations are frequent in patients with ulcerative colitis. They are most commonly associated with active bowel disease but can …

Predictors of infliximab failure after azathioprine withdrawal in Crohn's disea…

PMID: 20389296
Year: 2010
Relationship Type: Treatment Score: 9.1

OBJECTIVES: Whether all Crohn's disease (CD) patients should maintain long-term azathioprine treatment in combination with infliximab remains controv…

Early onset steroid-dependent ulcerative colitis is a predictor of azathioprine…

PMID: 20110928
Year: 2010
Relationship Type: Treatment Score: 9.1

BACKGROUND: Studies assessing the efficacy of azathioprine (AZA) in steroid-dependent ulcerative colitis (UC) are scarce. The aim of this study was t…

Efficacy of azathioprine in mild or moderate relapse in Crohn's disease: clinic…

PMID: 20078661
Year: 2010
Relationship Type: Treatment Score: 9.1

AIM: The present study was aimed at evaluating the efficacy of azathioprine (AZA) in patients with active and relapsing Crohn's disease (CD) and the …

Low-dose azathioprine or mercaptopurine in combination with allopurinol can byp…

PMID: 20015102
Year: 2010
Relationship Type: Treatment Score: 9.1

Joint involvement associated with inflammatory bowel disease (IBD) belongs to the concept of spondyloarthritis (SpA) and includes two types of arthr…

Azathioprine, mucosal healing in ulcerative colitis, and the chemoprevention of…

PMID: 19906011
Year: 2010
Relationship Type: Treatment Score: 9.1

The development of colorectal cancer in ulcerative colitis is a function of disease duration, with the risk approaching 14% at 25 years. Colitic canc…

Mercaptopurine rescue after azathioprine-induced liver injury in inflammatory b…

PMID: 19709096
Year: 2010
Relationship Type: Treatment Score: 9.1

BACKGROUND: Azathioprine (AZA) liver toxicity arises in approximately 3% of inflammatory bowel disease patients and may result in treatment discontin…

Azathioprine maintains long-term steroid-free remission through 3 years in pati…

PMID: 19705415
Year: 2010
Relationship Type: Treatment Score: 9.1

BACKGROUND: Studies assessing the efficacy of azathioprine (AZA) in steroid-dependent ulcerative colitis (SD-UC) are scarce. The purpose of this tria…

Azathioprine or 6-mercaptopurine for maintenance of remission in Crohn's disease

PMID: 19160175
Year: 2009
Relationship Type: Treatment Score: 9.1

Update in Cochrane Database Syst Rev. 2005;(1):CD003459. BACKGROUND: Although corticosteroids are effective for induction of remission of Crohn…

Pharmacogenomic studies of the anticancer and immunosuppressive thiopurines mer…

PMID: 18662289
Year: 2008
Relationship Type: Adverse Effect Score: 9.1

BACKGROUND: 6-Mercaptopurine (6-MP) and its prodrug azathioprine (AZA) are effective for the induction and maintenance of remission and reduction of…

Pharmacoeconomic analyses of azathioprine, methotrexate and prospective pharmac…

PMID: 16898847
Year: 2006
Relationship Type: Treatment Score: 9.1

The thiopurine drugs azathioprine and 6-mercaptopurine (6-MP) are well-established in the treatment of inflammatory bowel disease (IBD). However, t…

High-dose azathioprine in children with inflammatory bowel disease

PMID: 12656694
Year: 2003
Relationship Type: Treatment Score: 9.1

The only therapy in inflammatory bowel disease (IBD), which up to the mid-1990s was disease modifying, was immunosuppression with azathioprine. Othe…

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