| Drug ID: | Drug79 |
|---|---|
| Drug Name: | Mercaptopurine |
| CID: | 667490 |
| DrugBank ID: | DB01033 |
| Modality: | Small Molecule |
| Groups: | approved |
| US Approved: | YES |
| Other Approved: | YES |
| Identifier: | NCT02413047, , NCT00514982, , NCT03370601 |
| Molecular Formula: | C5H4N4S |
| Molecular Weight: | 152.18 g/mol |
| Isomeric SMILES: | C1=NC2=C(N1)C(=S)N=CN2 |
| Synonyms: | 6-Mercaptopurine; mercaptopurine; 50-44-2; Purinethol; Mercapurin; 6-Thiopurine; 7H-purine-6-thiol; Mercaleukin; Leukerin; Leupurin |
| Phase 0: | 0 |
| Phase 1: | 26 |
| Phase 2: | 90 |
| Phase 3: | 87 |
| Phase 4: | 24 |
| Description: | An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia. [PubChem] |
Molecular Structure
Knowledge Graph
| dtID | CID | Compound Name | Gene ID | Gene Name | Species | PubMed IDs | Action |
|---|---|---|---|---|---|---|---|
| dt665 | 667490 | Mercaptopurine | 3251 | HPRT1 | Homo sapiens (human) | 15354273 | Inhibitor |
| dt666 | 667490 | Mercaptopurine | 3614 | IMPDH1 | Homo sapiens (human) | 37713619 | Inhibitor |
| dt667 | 667490 | Mercaptopurine | 5471 | PPAT | Homo sapiens (human) | Inhibitor | |
| dt668 | 667490 | Mercaptopurine | 3614 | IMPDH1 | Homo sapiens (human) | Inhibitor | |
| dt669 | 667490 | Mercaptopurine | 3615 | IMPDH2 | Homo sapiens (human) | Inhibitor | |
| dt670 | 667490 | Mercaptopurine | 316 | AOX1 | Homo sapiens (human) | Substrate | |
| dt671 | 667490 | Mercaptopurine | 7172 | TPMT | Homo sapiens (human) | 15354273 | Substrate |
| dt672 | 667490 | Mercaptopurine | 7498 | XDH | Homo sapiens (human) | 15354273 | Substrate |
| dt673 | 667490 | Mercaptopurine | 9376 | SLC22A8 | Homo sapiens (human) | Substrate|Inhibitor | |
| dt674 | 667490 | Mercaptopurine | 10257 | ABCC4 | Homo sapiens (human) | 11447229 | Substrate |
- 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 | |
|---|---|---|---|---|---|---|---|
| NCT00514982 | Medical Treatment of Colitis in Patients With Hermansky-Pudlak Syndrome | PHASE2 | WITHDRAWN | National Institute of Allergy and Infectious Diseases (NIAID) | Hermanski-Pudlak Syndrome|Colitis|Cytokines|Lymph… | DRUG: Mesalamine|DRUG: Infliximab|DRUG: Corticost… | 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 |
| 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 |
| 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 |
| ACTRN12612001107819 | Febuxostat-thiopurine combination therapy in patients with moderately severe inflammatory bowel disease (IBD): a pilot study of a novel drug combination that may influence thiopurine bioavailability | PHASE1 | Not Recruiting | Prof Tim Florin | inflammatory bowel disease; inflammatory bowel d… | To use the combination of febuxostat and 6-mercap… | 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 |
| NCT02413047 | Evaluate if Response to Infliximab or Adalimumab May be Regained With an Immunomodulator | None | TERMINATED | Indiana University | Inflammatory Bowel Disease|Ulcerative Colitis|Cro… | DRUG: Azathioprine|DRUG: 6 mercaptopurine|DRUG: M… | Details |
| NCT02910245 | Mercaptopurine Therapy in Ulcerative Colitis | PHASE3 | UNKNOWN | Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA) | Colitis, Ulcerative | DRUG: Mercaptopurine (Purinethol)|DRUG: Placebo|D… | Details |
| NCT00521950 | Cost-effectiveness of TPMT Pharmacogenetics | None | COMPLETED | ZonMw: The Netherlands Organisation for Health Research and Development | Inflammatory Bowel Diseases|Crohn Disease|Ulcerat… | GENETIC: TPMT genotyping; Drug: azathioprine or 6… | Details |
| NCT03370601 | Evaluation of the Clinical and Immunological Impact of Two Therapeutic Strategies in Chronic Inflammatory Diseases | None | TERMINATED | University Hospital, Lille | Inflammatory Bowel Diseases | DRUG: Infliximab|DRUG: Mercaptopurine|DRUG: Azath… | 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 |
Does lymphopenia or macrocytosis reflect 6-thioguanine levels in patients with …
PMID: 26425841
Year: 2016
Relationship Type:
Association
Score: 6.3
Comment in Am J Gastroenterol. 2015 Aug;110(8):1242-3. Am J Gastroenterol. 2015 Aug;110(8):1243-4. Am J Gastroenterol. 2015 Dec;110(12):1…
Concomitant use of azathioprine/6-mercaptopurine decreases the risk of anti-TNF…
PMID: 25789922
Year: 2015
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: Chronic periodontitis (CP) is an inflammatory condition affecting tooth-supporting tissues and alveolar bone that surround the tooth, le…
6-mercaptopurine-induced hepatotoxicity during the treatment of ulcerative coli…
PMID: 25636015
Year: 2015
Relationship Type:
Treatment
Score: 6.3
Update 2014: advances to optimize 6-mercaptopurine and azathioprine to reduce t…
PMID: 25248004
Year: 2015
Relationship Type:
Adverse Effect
Score: 6.3
Not found
[6-mercaptopurine as a safe therapeutic alternative for patients with inflammat…
PMID: 25198089
Year: 2014
Relationship Type:
Treatment
Score: 6.3
UPLC-MS/MS method for quantification of the azathioprine metabolites 6-mercapto…
PMID: 24960235
Year: 2014
Relationship Type:
Treatment
Score: 6.3
In the treatment of inflammatory bowel diseases, the use of azathioprine is increasing over the time. It has been demonstrated that the effectiveness…
Risk of lymphoma in patients with inflammatory bowel disease treated with azath…
PMID: 24879926
Year: 2015
Relationship Type:
Association
Score: 6.3
OBJECTIVES: Antibodies to infliximab (ATIs) have been associated with loss of clinical response and lower serum infliximab (IFX) levels in some stud…
Non-cirrhotic portal hypertension due to 6-mercaptopurine use for Crohn's disea…
PMID: 24535249
Year: 2014
Relationship Type:
Association
Score: 6.3
6-Mercaptopurine/Azathioprine remains an important contributor in managing Croh…
PMID: 24462321
Year: 2014
Relationship Type:
Treatment
Score: 6.3
Two large studies concluded that AZA started early after diagnosis of Crohn's disease have no late maintenance value. This is contrary to previous st…
Can azathioprine 6-mercaptopurine treatment be withdrawn in patients with respo…
PMID: 23576085
Year: 2012
Relationship Type:
Treatment
Score: 6.1
How long should we treat patients with azathioprine/6-mercaptopurine before dec…
PMID: 23576084
Year: 2012
Relationship Type:
Treatment
Score: 6.1
[Immunomodulator: azathioprine and 6-mercaptopurine]
PMID: 23126110
Year: 2012
Relationship Type:
Association
Score: 6.1
Comment to 'Nutritional therapy versus 6-mercaptopurine as maintenance therapy …
PMID: 22981244
Year: 2013
Relationship Type:
Treatment
Score: 6.1
Mercaptopurine-induced hepatoportal sclerosis in a patient with Crohn's disease
PMID: 22841133
Year: 2013
Relationship Type:
Treatment
Score: 6.1
Thiopurines play a pivotal role in the management of inflammatory bowel disease. Azathioprine and mercaptopurine have been associated with a number o…
Intermittent granulocyte and monocyte apheresis versus mercaptopurine for maint…
PMID: 22607563
Year: 2012
Relationship Type:
Treatment
Score: 6.1
The effect of granulocyte and monocyte adsorption apheresis (GMA) on prevention of relapse of ulcerative colitis (UC) is not clear. This was a pilot …
High TPMT enzyme activity does not explain drug resistance due to preferential …
PMID: 22486532
Year: 2012
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: Up to 20% of patients on thiopurine therapy fail to achieve adequate drug response. Many of these patients preferentially produce the tox…
Hepatotoxicity associated with 6-methyl mercaptopurine formation during azathio…
PMID: 22261533
Year: 2012
Relationship Type:
Treatment
Score: 6.1
Comment in Gastroenterology. 2015 Nov;149(6):1302-4. Gastroenterology. 2015 Nov;149(6):1323-6. BACKGROUND & AIMS: Inflammatory bowel disease…
6-Mercaptopurine transport in human lymphocytes: correlation with drug-induced …
PMID: 22257476
Year: 2012
Relationship Type:
Adverse Effect
Score: 6.1
Not found
Prognosis of lymphoma in patients following treatment with 6-mercaptopurine/aza…
PMID: 22241664
Year: 2012
Relationship Type:
Treatment
Score: 6.1
Inflammatory bowel disease (IBD) is characterized by chronic relapsing inflammatory disorders of the gastrointestinal tract, and includes two major …
Optimizing 6-mercaptopurine and azathioprine therapy in the management of infla…
PMID: 22072847
Year: 2011
Relationship Type:
Treatment
Score: 6.1
Infliximab is a monoclonal antibody against tumor necrosis factor alpha (TNF-α), which is approved for the treatment of chronic inflammatory bowel d…