| 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 |
Synthesis of pro-prodrugs L-lysine based for 5-aminosalicylic acid and 6-mercap…
PMID: 21925255
Year: 2011
Relationship Type:
Association
Score: 6.1
BACKGROUND: Host-intestinal microbial interaction plays an important role in the pathogenesis of inflammatory bowel diseases (IBDs). The surface mol…
Azathioprine and mercaptopurine: lymphoma
PMID: 21648178
Year: 2011
Relationship Type:
Treatment
Score: 6.1
Prospective follow-up for a median of 35 months of a French cohort of 19 486 patients with inflammatory bowel disease showed a nearly 4-fold increase…
Varicella zoster meningoradiculitis in Crohn's disease treated with 6-mercaptop…
PMID: 21618366
Year: 2011
Relationship Type:
Association
Score: 6.1
Long term efficacy and safety of allopurinol and azathioprine or 6-mercaptopuri…
PMID: 21172265
Year: 2009
Relationship Type:
Association
Score: 6.1
Not found
Lower doses of 6-mercaptopurine/azathioprine bring enough clinical efficacy and…
PMID: 21172230
Year: 2008
Relationship Type:
Treatment
Score: 6.1
Erratum in Inflamm Bowel Dis. 2009 Sep;15(9):1438-47.
A prospective evaluation of the impact of allopurinol in pediatric and adult IB…
PMID: 21122558
Year: 2010
Relationship Type:
Association
Score: 6.1
BACKGROUND: Interleukin (IL)-17F, produced in IL-23R-expressing Th17 cells, is a novel member of the IL-17 cytokine family. Given the association of…
Azathioprine or 6-mercaptopurine for induction of remission in Crohn's disease
PMID: 20556747
Year: 2010
Relationship Type:
Treatment
Score: 6.1
Erratum in Gastroenterology. 2009 May;136(5):1844. Fernadez-Hernando, Carlos [corrected to Fernandez-Hernando, Carlos]. BACKGROUND & AIMS: Incr…
Azathioprine-induced hypersensitivity hepatitis: tolerance to 6-mercaptopurine
PMID: 20196148
Year: 2010
Relationship Type:
Association
Score: 6.1
Treatment-associated acute myeloid leukemia in a patient with Crohn's disease o…
PMID: 20128002
Year: 2010
Relationship Type:
Treatment
Score: 6.1
Mercaptopurine-induced fever: hypersensitivity reaction in a patient with acute…
PMID: 20030482
Year: 2010
Relationship Type:
Treatment
Score: 6.1
The antimetabolite mercaptopurine is commonly used as part of treatment regimens for acute lymphoblastic leukemia and as treatment for inflammatory b…
Azathioprine or 6-mercaptopurine for induction of remission in Crohn's disease
PMID: 19821270
Year: 2009
Relationship Type:
Association
Score: 6.1
Not found
Mercaptopurine rescue after azathioprine-induced liver injury in inflammatory b…
PMID: 19709096
Year: 2010
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: Azathioprine (AZA) liver toxicity arises in approximately 3% of inflammatory bowel disease patients and may result in treatment discontin…
Thiopurine S-methyltransferase and inosine triphosphate pyrophosphohydrolase ge…
PMID: 19214663
Year: 2009
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: Patient information has been viewed as a key component of self-management. However, little attention has been given to methods of disse…
Azathioprine or 6-mercaptopurine for maintenance of remission in Crohn's disease
PMID: 19160175
Year: 2009
Relationship Type:
Treatment
Score: 6.1
Update in Cochrane Database Syst Rev. 2005;(1):CD003459. BACKGROUND: Although corticosteroids are effective for induction of remission of Crohn…
Increased dosing requirements for 6-mercaptopurine and azathioprine in inflamma…
PMID: 18266236
Year: 2008
Relationship Type:
Association
Score: 6.1
To investigate the basis for the LEDGF/p75 dependence of HIV-1 integrase (IN) nuclear localization and chromatin association, we used cell lines mad…
[Optimization of immunomodulatory treatment with azathioprine or 6-mercaptopuri…
PMID: 17980127
Year: 2007
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: Inflammatory bowel disease (IBD) is proposed to result from a dysregulated mucosal immune response to the colonic flora in genetically …
Hepatotoxicity of 6-mercaptopurine (6-MP) and Azathioprine (AZA) in adult IBD p…
PMID: 17764490
Year: 2007
Relationship Type:
Adverse Effect
Score: 6.1
BACKGROUND: NOD2 mutations are associated with Crohn's disease (CD) in Caucasian clinic-based cohorts. Data from population-based cohorts are limite…
Squamous dysplasia of the rectum in a patient with ulcerative colitis treated w…
PMID: 17717741
Year: 2008
Relationship Type:
Association
Score: 6.1
PURPOSE: To evaluate the quantity and severity of bone disorders in children and adolescents with inflammatory bowel diseases (IBD) and to examine t…
Severe pulmonary toxicity after azathioprine/6-mercaptopurine initiation for th…
PMID: 17667053
Year: 2007
Relationship Type:
Treatment
Score: 6.1
Inflammatory bowel disease (IBD) is a chronic inflammatory disorder of the gastrointestinal tract involving aberrant activation of innate and adapti…
Effect of allopurinol on clinical outcomes in inflammatory bowel disease nonres…
PMID: 17296529
Year: 2007
Relationship Type:
Association
Score: 6.1
AIM: To understand the local pathophysiological alterations and gene ontology-based functional classification of colonic biopsies into inflammatory …