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
NCT05584228 Medical Treatment Versus Surgery in Stricturing Small Bowel Crohn's Disease NA NOT_YET_RECRUITING Nantes University Hospital Crohn Disease DRUG: Azathioprine + infliximab|PROCEDURE: Intest… Details
NCT05456776 Azathioprine Linked With Impaired Intestinal Epithelial Postoperative Regeneration in Crohn's Disease NULL COMPLETED Centre of Postgraduate Medical Education Inflammatory Bowel Diseases None Details
NCT05321485 The Effect of MedicijnWijs on Adherence to Azathioprine Therapy in Adolescents With IBD NA UNKNOWN Maxima Medical Center Inflammatory Bowel Diseases|Crohn Disease|Ulcerat… OTHER: MedicijnWijs Details
NCT07138898 Immunosuppressant Management in Rheumatology Patients Undergoing Elective Total Shoulder Arthroplasty PHASE2 NOT_YET_RECRUITING NYU Langone Health Rheumatic Disease DRUG: Methotrexate|DRUG: Sulfasalazine|DRUG: Hydr… Details
NCT05040464 Comparison of Azathioprine to Methotrexate in Combination Therapy With Adalimumab in Crohn's Disease: an Open-label Randomized Controlled Trial PHASE3 RECRUITING Centre Hospitalier Universitaire, Amiens Crohn Disease|Azathioprine|Methotrexate DRUG: AZA capsules|DRUG: MTX|BIOLOGICAL: blood sa… Details
NCT04882683 Clinical Study of Cord Blood Mononuclear Cells on Treatment of Hormone-resistant or Hormone-dependent Ulcerative Colitis NA UNKNOWN Shandong Qilu Stem Cells Engineering Co., Ltd. Ulcerative Colitis DRUG: Prednisone|DRUG: Azathioprine|DRUG: Adalimu… Details
NCT04761952 N-3 Polyunsaturated Fatty Acids Prevent Postoperative Recurrence of Crohn's Disease NA UNKNOWN Sixth Affiliated Hospital, Sun Yat-sen University Inflammatory Bowel Diseases|Crohn Disease|Polyuns… DRUG: azathioprine|DRUG: infliximab|DRUG: N-3 Pol… Details
NCT04160325 Effect of the Exclusive Enteral Nutrition Combined With Azathioprine for Remission of Crohn's Diseases After Surgery NA UNKNOWN Zhu Weiming Crohn Disease DIETARY_SUPPLEMENT: postoperative 3-month exclusi… Details
NCT03681652 Post-Operative Crohn's Disease Outcome in Children NULL RECRUITING Schneider Children's Medical Center, Israel Crohn Disease DRUG: Azathioprine|DRUG: Anti-TNF Drug Details
NCT03580876 Addition of Azathioprine in IBD Patients With Immunogenic Failure PHASE4 UNKNOWN Védrines, Philippe, M.D. Clinical Failure After Switch DRUG: addition of azathioprine|DRUG: Switch to a … Details
NCT03393247 The Therapy Effect of Azathioprine Initial or 14 Weeks After Combined With Infliximab on CD NA UNKNOWN Sixth Affiliated Hospital, Sun Yat-sen University Crohn Disease DRUG: infliximab and azathioprine combination at … Details
NCT03370601 Evaluation of the Clinical and Immunological Impact of Two Therapeutic Strategies in Chronic Inflammatory Diseases NA TERMINATED University Hospital, Lille Inflammatory Bowel Diseases DRUG: Infliximab|DRUG: Mercaptopurine|DRUG: Azath… Details
NCT03185611 Effectiveness of Rifaximin Combined With Thiopurine on Preventing Postoperative Recurrence in Crohn's Disease PHASE3 UNKNOWN Sixth Affiliated Hospital, Sun Yat-sen University Crohn Disease DRUG: Rifaximin|DRUG: Azathioprine 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
NCT03101800 Beneficial and Harmful Effects of Azathioprine and Allopurinol Versus Standard Azathioprine Therapy for Patients With Ulcerative Colitis PHASE3 UNKNOWN Hvidovre University Hospital Colitis, Ulcerative|Colitis Ulcerative Exacerbati… DRUG: Azathioprine and Allopurinol|DRUG: Azathiop… Details
NCT02998827 Thalidomide Results in Diminished Ovarian Reserve in Reproductive Age Female IBD Patients NA UNKNOWN Sixth Affiliated Hospital, Sun Yat-sen University Crohn Disease DRUG: Thalidomide|DRUG: infliximab, azathioprine|… Details
NCT02929706 Pre-genotype NUDT 15 R139C on Reducing Thiopurine-induced Leucopenia in Inflammatory Bowel Disease NA UNKNOWN Sixth Affiliated Hospital, Sun Yat-sen University Thiopurine-induced Leukopenia GENETIC: Pre-genotype NUDT15 and optimize azathio… Details
NCT02852694 Reduce Risk for Crohn's Disease Patients PHASE4 COMPLETED PIBD-Net Crohn's Disease DRUG: Methotrexate|DRUG: Adalimumab|DRUG: Azathio… 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
NCT02517684 Top-down Infliximab Study in Kids With Crohn's Disease PHASE4 COMPLETED Erasmus Medical Center Crohn's Disease DRUG: Infliximab|DRUG: Prednisolone|OTHER: Exclus… 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

Commensal bacteria promote azathioprine therapy failure in inflammatory bowel d…

PMID: 37586320
Year: 2023
Relationship Type: Treatment Score: 9.5

Azathioprine (AZA) therapy failure, though not the primary cause, contributes to disease relapse and progression in inflammatory bowel disease (IBD).…

Acute myeloid leukemia after 10 years of azathioprine treatment for Crohn's dis…

PMID: 37548454
Year: 2023
Relationship Type: Treatment Score: 9.5

BACKGROUND: Azathioprine, which is an immunosuppressive agent commonly used for chronic inflammatory bowel disease, may be associated with an increas…

Azathioprine monotherapy withdrawal in inflammatory bowel diseases: A retrospec…

PMID: 37545640
Year: 2023
Relationship Type: Treatment Score: 9.5

BACKGROUND: There is no consensus on the recommended duration of and optimal time to stop azathioprine (AZA) therapy in inflammatory bowel disease (I…

Analysis of the NUDT15 gene and metabolites of azathioprine in Japanese patient…

PMID: 37454061
Year: 2023
Relationship Type: Treatment Score: 9.5

BACKGROUND: Thiopurines continue to play an important role in the treatment of inflammatory bowel disease (IBD). It is well known that thiopurines ca…

Case report: NUDT15 polymorphism and severe azathioprine-induced myelosuppressi…

PMID: 37229272
Year: 2023
Relationship Type: Treatment Score: 9.5

Azathioprine is clinically used as an immunosuppressant for treating autoimmune diseases. However it has narrow therapeutic indices due to frequent m…

Diffuse large B-cell lymphoma in a patient treated with azathioprine for ulcera…

PMID: 37229049
Year: 2023
Relationship Type: Treatment Score: 9.5

Azathioprine (AZA) used as an immunomodulator agent in the management of inflammatory bowel disease (IBD) increases the risk of the development of ly…

Evaluation of the mTORC activity in the presence of Toxoplasma gondii and azath…

PMID: 36941573
Year: 2023
Relationship Type: Treatment Score: 9.5

BACKGROUND: Autophagy is an important part of pathogenesis of IBD. Thiopurines such as azathioprine (AZA) are approved drugs for clinical practices i…

Development and validation of a novel HPLC-UV method for simultaneous determina…

PMID: 36895397
Year: 2023
Relationship Type: Treatment Score: 9.5

A rapid, specific and accurate high-performance liquid chromatography with tunable ultraviolet detection method was developed to simultaneously deter…

Normal Ranges of Thiopurine Methyltransferase Activity Do Not Affect Thioguanin…

PMID: 36776499
Year: 2020
Relationship Type: Treatment Score: 9.5

BACKGROUND: Thiopurine methyltransferase (TPMT) activity influences azathioprine conversion into active metabolite 6-thioguanine nucleotide (6-TGN). …

Azathioprine Withdrawal Is Cost-Effective in Patients with Crohn's Disease in R…

PMID: 36512266
Year: 2023
Relationship Type: Treatment Score: 9.5

BACKGROUND: In Crohn's disease, combination therapy with infliximab and azathioprine is more effective than either drug alone but is associated with …

DNA methylation of the TPMT gene and azathioprine pharmacokinetics in children …

PMID: 36462311
Year: 2023
Relationship Type: Pharmacology Score: 9.5

BACKGROUND: Thiopurine methyltransferase (TPMT) is a crucial enzyme for azathioprine biotransformation and its activity is higher in very early onset…

An older patient with active ulcerative colitis and coronavirus disease 2019 (C…

PMID: 36417106
Year: 2023
Relationship Type: Treatment Score: 9.5

A 77-year-old patient with ulcerative colitis (UC) was transferred to our department because of worsening bloody diarrhea and abdominal pain, which w…

Low-Dose Azathioprine in Combination with Allopurinol: The Past, Present and Fu…

PMID: 36242689
Year: 2022
Relationship Type: Treatment Score: 9.5

The inflammatory bowel diseases (IBD) are complex immune-mediated inflammatory diseases that are associated with significant morbidity around the wor…

On-demand reconstitutable hyaluronic acid-doped azathioprine microcrystals effe…

PMID: 36178247
Year: 2022
Relationship Type: Treatment Score: 9.5

Although CD44-targeted delivery of pure drug microcrystals of azathioprine (AZA) could be a desirable approach to treat ulcerative colitis (UC), prem…

[Metabolism and therapeutic monitoring of azathioprine in gastroenterology and …

PMID: 36047549
Year: 2022
Relationship Type: Treatment Score: 9.5

Azathioprine keeps an important place in the treatment of inflammatory bowel disease and autoimmune hepatitis. This molecule has a narrow therapeutic…

Alopecia and colon ulcers following azathioprine use in a patient with myasthen…

PMID: 35984164
Year: 2022
Relationship Type: Treatment Score: 9.5

RATIONALE: Azathioprine is a purine analog (PA) used to treat myasthenia gravis (MG). However, some patients are sensitive to azathioprine and develo…

Management of Idiopathic Pyoderma Gangrenosum With Azathioprine As the Primary …

PMID: 35746991
Year: 2022
Relationship Type: Treatment Score: 9.5

Pyoderma gangrenosum (PG) is a very rare, non-infectious, progressive inflammatory condition falling under the umbrella of neutrophilic dermatoses. I…

Use of Azathioprine in Ulcerative Colitis: A Comprehensive Review

PMID: 35698683
Year: 2022
Relationship Type: Treatment Score: 9.5

Ulcerative colitis (UC) is a relapsing and remitting chronic inflammatory disease of the large intestine characterized by bloody diarrhea, abdominal …

Imputability of Azathioprine in the Occurrence of Chronic Myeloid Leukemia in C…

PMID: 35676842
Year: 2023
Relationship Type: Treatment Score: 9.5

BACKGROUND: Patients with Cohn's disease (CD) treated with thiopurines are at an increased risk of developing cancer. Leukemias are less frequent tha…

C-reactive protein levels and prevalence of leukopenia in patients with inflamm…

PMID: 35584442
Year: 2022
Relationship Type: Treatment Score: 9.5

OBJECTIVE: To examine serum C-reactive protein levels and the prevalence of leukopenia in patients with Crohn's disease or ulcerative colitis undergo…

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