| 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 |
PACSIN2 as a modulator of autophagy and mercaptopurine cytotoxicity: mechanisms…
PMID: 36596605
Year: 2023
Relationship Type:
Mechanism
Score: 6.5
PACSIN2 variants are associated with gastrointestinal effects of thiopurines and thiopurine methyltransferase activity through an uncharacterized mec…
Anti-inflammation and anti-aging mechanisms of mercaptopurine in vivo and in vi…
PMID: 36442232
Year: 2023
Relationship Type:
Treatment
Score: 6.5
Skin is the biggest organ of the human body, which easily gets irritated by exposure to the sun. Skin photoaging and acute photodamage are caused by …
Pancreatitis associated with azathioprine and 6-mercaptopurine use in Crohn's d…
PMID: 35401955
Year: 2020
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Our objective was to provide consensus recommendations on the optimal management of the immune-mediated inflammatory diseases (IMIDs) se…
Limited Impact of 6-Mercaptopurine on Inflammation-Induced Chemokines Expressio…
PMID: 33864170
Year: 2021
Relationship Type:
Association
Score: 6.5
OBJECTIVES: The aim of the study was to review the evidence regarding the clinical use and value of fecal calprotectin (FC) measurements in differen…
Allopurinol to Prevent Mercaptopurine Adverse Effects in Children and Young Adu…
PMID: 33750748
Year: 2021
Relationship Type:
Treatment
Score: 6.5
Mercaptopurine (6MP) is used to treat acute lymphoblastic leukemia (ALL) and is metabolized by hypoxanthine guanine phosphoribosal transferase to for…
Full Potential of 6-Mercaptopurine in IBD May Remain Untapped
PMID: 32740082
Year: 2020
Relationship Type:
Association
Score: 6.5
Comment on Dig Dis Sci. 2020 Nov;65(11):3287-3296.
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…
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 …
Determination of 6-thioguanine and 6-methylmercaptopurine in dried blood spots …
PMID: 31449774
Year: 2019
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Therapeutic drug monitoring of azathioprine metabolites is required for pharmacotherapy individualisation in patients with inflammatory b…
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…
Mercaptopurine and Metabolites in Breast Milk
PMID: 31414890
Year: 2020
Relationship Type:
Association
Score: 6.5
A 35-year-old pregnant woman visited our outpatient clinical questioning the safety of once daily 50 mg mercaptopurine (MP) during pregnancy and lact…
Emerging role of NUDT15 polymorphisms in 6-mercaptopurine metabolism and dose r…
PMID: 28963908
Year: 2017
Relationship Type:
Adverse Effect
Score: 6.3
Despite more than 80% long term survival in ALL, morbidity due to drug related myelotoxicity remains high. Germline variants of thiopurine metabolizi…
[Research advances in pharmacogenomics of mercaptopurine]
PMID: 28899477
Year: 2017
Relationship Type:
Treatment
Score: 6.3
Mercaptopurine is a common chemotherapeutic drug and immunosuppressive agent and plays an important role in the treatment of acute lymphoblastic leuk…
Safety of azathioprine and 6-mercaptopurine in patients with inflammatory bowel…
PMID: 28406092
Year: 2017
Relationship Type:
Treatment
Score: 6.3
Patients with inflammatory bowel disease [IBD] may develop, similarly to individuals from general population, rare cases of human papilloma virus […
The glutathione transferase Mu null genotype leads to lower 6-MMPR levels in pa…
PMID: 28045129
Year: 2018
Relationship Type:
Association
Score: 6.3
The conversion of azathioprine (AZA) to mercaptopurine (MP) is mediated by glutathione transferase Mu1 (GSTM1), alpha1 (GSTA1) and alpha2 (GSTA2). We…
NK cells are biologic and biochemical targets of 6-mercaptopurine in Crohn's di…
PMID: 28011186
Year: 2017
Relationship Type:
Treatment
Score: 6.3
OBJECTIVE: The aim of the study was to investigate the course of fatigue in a conventional inflammatory bowel disease treatment setting. MATERIALS A…
6-methylmercaptopurine-induced leukocytopenia during thiopurine therapy in infl…
PMID: 27859568
Year: 2017
Relationship Type:
Treatment
Score: 6.3
BACKGROUND AND AIM: Thiopurines have a favorable benefit-risk ratio in the treatment of inflammatory bowel disease. A feared adverse event of thiopur…
Mercaptopurine and inflammatory bowel disease: the other thiopurine
PMID: 27809554
Year: 2017
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: Data about use and effectiveness of mercaptopurine in inflammatory bowel disease are relatively limited. AIMS: To assess the possible the…
Reassuring results on birth outcomes in children fathered by men treated with a…
PMID: 27456154
Year: 2017
Relationship Type:
Mechanism
Score: 6.3
Inflammatory bowel disease (IBD) arises when intestinal immune homeostasis is broken, the maintenance of such homeostasis is principally controlled …
Clinical Value of Mercaptopurine After Failing Azathioprine Therapy in Patients…
PMID: 27158876
Year: 2016
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: Thiopurines have been widely accepted as immunosuppressive therapy in inflammatory bowel disease. However, many patients have to disconti…