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MERCAPTOPURINE Drug Record

  • Summary
  • Interactions
  • Claims
  • MERCAPTOPURINE chembl:CHEMBL1425 ApprovedAntineoplasticImmunotherapy

    Alternate Names:

    MERCAPTOPURINE ANHYDROUS
    MERCAPTOPURINE
    6-THIOXOPURINE
    MERCAPURIN
    6-MP
    MERCAPTOPURINUM
    PURINETHOL®
    6-MERCAPTOPURINE
    6-THIOHYPOXANTHINE
    MERCAPTOPURINA
    6 MP
    chembl:CHEMBL1425
    drugbank:01033
    pubchem.compound:667490
    rxcui:1546028
    chemidplus:50-44-2

    Drug Info:

    FDA Approval 1953
    Drug Class small molecule
    Drug Indications Antineoplastic Agents
    Drug Class antineoplastic agents
    Year of Approval 1953
    Drug Categories drugs for obstructive airway diseases
    Drug Categories heterocyclic compounds, fused-ring
    Drug Categories narrow therapeutic index drugs
    Drug Categories nucleoside metabolic inhibitor
    Drug Categories oat3/slc22a8 inhibitors
    Drug Categories oat3/slc22a8 substrates
    Drug Categories xanthine derivatives
    (8 More Sources)

    Publications:

    Perez-Andreu V et al., 2013, Inherited GATA3 variants are associated with Ph-like childhood acute lymphoblastic leukemia and risk of relapse., Nat Genet
    Kim HS et al., 2017, A coding variant in <i>FTO</i> confers susceptibility to thiopurine-induced leukopenia in East Asian patients with IBD., Gut
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Sahasranaman et al., 2008, Clinical pharmacology and pharmacogenetics of thiopurines., Eur. J. Clin. Pharmacol.
    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for &gt;200 compounds., Chem Res Toxicol
    Dorababu P et al., 2012, Genetic variants of thiopurine and folate metabolic pathways determine 6-MP-mediated hematological toxicity in childhood ALL., Pharmacogenomics
    Brouwer C et al., 2005, Role of 5'-nucleotidase in thiopurine metabolism: enzyme kinetic profile and association with thio-GMP levels in patients with acute lymphoblastic leukemia during 6-mercaptopurine treatment., Clin Chim Acta
    Meyer JA et al., 2013, Relapse-specific mutations in NT5C2 in childhood acute lymphoblastic leukemia., Nat Genet
    Tzoneva et al., 2013, Activating mutations in the NT5C2 nucleotidase gene drive chemotherapy resistance in relapsed ALL., Nat. Med.
    Ban H et al., 2010, The multidrug-resistance protein 4 polymorphism is a new factor accounting for thiopurine sensitivity in Japanese patients with inflammatory bowel disease., J Gastroenterol
    Valerie NC et al., 2016, NUDT15 Hydrolyzes 6-Thio-DeoxyGTP to Mediate the Anticancer Efficacy of 6-Thioguanine., Cancer Res
    Liang DC et al., 2016, NUDT15 gene polymorphism related to mercaptopurine intolerance in Taiwan Chinese children with acute lymphoblastic leukemia., Pharmacogenomics J
    Soler AM et al., 2018, TPMT and NUDT15 genes are both related to mercaptopurine intolerance in acute lymphoblastic leukaemia patients from Uruguay., Br J Haematol
    Tsujimoto S et al., 2018, Diplotype analysis of NUDT15 variants and 6-mercaptopurine sensitivity in pediatric lymphoid neoplasms., Leukemia
    Shih YC et al., 2019, Azathioprine-induced myelosuppression in two pemphigus vulgaris patients with homozygous polymorphism of NUDT15., J Dermatol
    Kakuta Y et al., 2018, NUDT15 codon 139 is the best pharmacogenetic marker for predicting thiopurine-induced severe adverse events in Japanese patients with inflammatory bowel disease: a multicenter study., J Gastroenterol
    Moriyama T et al., 2017, Novel variants in <i>NUDT15</i> and thiopurine intolerance in children with acute lymphoblastic leukemia from diverse ancestry., Blood
    Ailing Z et al., 2016, Further evidence that a variant of the gene NUDT15 may be an important predictor of azathioprine-induced toxicity in Chinese subjects: a case report., J Clin Pharm Ther
    Asada A et al., 2016, NUDT15 R139C-related thiopurine leukocytopenia is mediated by 6-thioguanine nucleotide-independent mechanism in Japanese patients with inflammatory bowel disease., J Gastroenterol
    Suzuki H et al., 2016, Genotyping NUDT15 can predict the dose reduction of 6-MP for children with acute lymphoblastic leukemia especially at a preschool age., J Hum Genet
    Moriyama T et al., 2016, NUDT15 polymorphisms alter thiopurine metabolism and hematopoietic toxicity., Nat Genet
    Cargnin S et al., 2018, Diagnostic accuracy of NUDT15 gene variants for thiopurine-induced leukopenia: a systematic review and meta-analysis., Pharmacol Res
    Moriyama T et al., 2017, The effects of inherited NUDT15 polymorphisms on thiopurine active metabolites in Japanese children with acute lymphoblastic leukemia., Pharmacogenet Genomics
    Tanaka Y et al., 2015, Susceptibility to 6-MP toxicity conferred by a NUDT15 variant in Japanese children with acute lymphoblastic leukaemia., Br J Haematol
    Shah SA et al., 2017, Nucleoside diphosphate-linked moiety X-type motif 15 C415T variant as a predictor for thiopurine-induced toxicity in Indian patients., J Gastroenterol Hepatol
    Kakuta Y et al., 2016, NUDT15 R139C causes thiopurine-induced early severe hair loss and leukopenia in Japanese patients with IBD., Pharmacogenomics J
    Zhu X et al., 2016, NUDT15 polymorphisms are better than thiopurine S-methyltransferase as predictor of risk for thiopurine-induced leukopenia in Chinese patients with Crohn's disease., Aliment Pharmacol Ther
    Lee YJ et al., 2016, NUDT15 variant is the most common variant associated with thiopurine-induced early leukopenia and alopecia in Korean pediatric patients with Crohn's disease., Eur J Gastroenterol Hepatol
    Zgheib NK et al., 2017, NUDT15 and TPMT genetic polymorphisms are related to 6-mercaptopurine intolerance in children treated for acute lymphoblastic leukemia at the Children's Cancer Center of Lebanon., Pediatr Blood Cancer
    Kishibe M et al., 2018, Severe thiopurine-induced leukocytopenia and hair loss in Japanese patients with defective NUDT15 variant: Retrospective case-control study., J Dermatol
    Wong FC et al., 2016, NUDT15 variant and thiopurine-induced leukopenia in Hong Kong., Hong Kong Med J
    Heap GA et al., 2014, HLA-DQA1-HLA-DRB1 variants confer susceptibility to pancreatitis induced by thiopurine immunosuppressants., Nat Genet
    Hareedy MS et al., 2015, Genetic variants in 6-mercaptopurine pathway as potential factors of hematological toxicity in acute lymphoblastic leukemia patients., Pharmacogenomics
    Stocco G et al., 2009, Genetic polymorphism of inosine triphosphate pyrophosphatase is a determinant of mercaptopurine metabolism and toxicity during treatment for acute lymphoblastic leukemia., Clin Pharmacol Ther
    Adam de Beaumais T et al., 2011, Determinants of mercaptopurine toxicity in paediatric acute lymphoblastic leukemia maintenance therapy., Br J Clin Pharmacol
    Sugita et al., 1992, [Analysis of lymphocyte surface markers in childhood acute lymphoblastic leukemia during maintenance chemotherapy]., Gan To Kagaku Ryoho
    Smid A et al., 2016, PACSIN2 polymorphism is associated with thiopurine-induced hematological toxicity in children with acute lymphoblastic leukaemia undergoing maintenance therapy., Sci Rep
    López-López E et al., 2014, Pharmacogenetics of microRNAs and microRNAs biogenesis machinery in pediatric acute lymphoblastic leukemia., PLoS One
    Gaulton et al., 2012, ChEMBL: a large-scale bioactivity database for drug discovery., Nucleic Acids Res.
    Dubinsky, 2004, Azathioprine, 6-mercaptopurine in inflammatory bowel disease: pharmacology, efficacy, and safety., Clin. Gastroenterol. Hepatol.
    Pikman et al., 2017, Synergistic Drug Combinations with a CDK4/6 Inhibitor in T-cell Acute Lymphoblastic Leukemia., Clin. Cancer Res.
    Eldem İ et al., 2018, SLCO1B1 Polymorphisms are Associated With Drug Intolerance in Childhood Leukemia Maintenance Therapy., J Pediatr Hematol Oncol
    Stocco G et al., 2012, PACSIN2 polymorphism influences TPMT activity and mercaptopurine-related gastrointestinal toxicity., Hum Mol Genet
    Li B et al., 2015, Negative feedback-defective PRPS1 mutants drive thiopurine resistance in relapsed childhood ALL., Nat Med
  • MERCAPTOPURINE   NUDT15

    Interaction Score: 13.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27530327 26503813 28146264 27558924 29967377 30035323 29923122 28659275 27381176 26590936 27193222 26878724 30048756 28445187 26033531 27416873 26076924 27604507 26735160 27577869 30101994 27095468


    Sources:
    FDA PharmGKB CIViC

  • MERCAPTOPURINE   PACSIN2

    Interaction Score: 2.37

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22846425 27452984


    Sources:
    PharmGKB

  • MERCAPTOPURINE   HPRT1

    Interaction Score: 2.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    15354273


    Sources:
    TEND TdgClinicalTrial DrugBank

  • MERCAPTOPURINE   ITPA

    Interaction Score: 1.58

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26237184 18685564 21395650


    Sources:
    PharmGKB

  • MERCAPTOPURINE   NT5C2

    Interaction Score: 1.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15990089 23377183 23377281


    Sources:
    PharmGKB CIViC

  • MERCAPTOPURINE   PRPS1

    Interaction Score: 1.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25962120


    Sources:
    CIViC

  • MERCAPTOPURINE   PPAT

    Interaction Score: 1.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    21948594 18506437


    Sources:
    TTD DrugBank

  • MERCAPTOPURINE   HLA-DQA1

    Interaction Score: 0.79

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25217962


    Sources:
    PharmGKB

  • MERCAPTOPURINE   GNMT

    Interaction Score: 0.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27452984


    Sources:
    PharmGKB

  • MERCAPTOPURINE   IMPDH1

    Interaction Score: 0.53

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    11752352 18506437


    Sources:
    TTD DrugBank

  • MERCAPTOPURINE   FTO

    Interaction Score: 0.53

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27558924


    Sources:
    PharmGKB

  • MERCAPTOPURINE   DROSHA

    Interaction Score: 0.45

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24614921


    Sources:
    PharmGKB

  • MERCAPTOPURINE   TPMT

    Interaction Score: 0.32

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Alteration TPMT:A80P,Y240C,A154T,A167G
    Alteration TPMT:.
    Drug family Purine analog

    PMIDs:
    None found


    Sources:
    FDA CGI

  • MERCAPTOPURINE   FOLH1

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22838948


    Sources:
    PharmGKB

  • MERCAPTOPURINE   GATA3

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24141364


    Sources:
    PharmGKB

  • MERCAPTOPURINE   NOTCH1

    Interaction Score: 0.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Ribociclib + Mercaptopurine
    Indication/Tumor Type T-cell adult acute lymphocytic leukemia
    Response Type decreased response

    PMIDs:
    28151717


    Sources:
    JAX-CKB

  • MERCAPTOPURINE   RB1

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Ribociclib + Mercaptopurine
    Indication/Tumor Type T-cell adult acute lymphocytic leukemia
    Response Type decreased response

    PMIDs:
    28151717


    Sources:
    JAX-CKB

  • MERCAPTOPURINE   TYMSOS

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • MERCAPTOPURINE   IL2RA

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    1580639


    Sources:
    NCI

  • MERCAPTOPURINE   ABCC4

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20393862


    Sources:
    PharmGKB

  • MERCAPTOPURINE   HLA-DRB1

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25217962


    Sources:
    PharmGKB

  • MERCAPTOPURINE   SLCO1B1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29683944


    Sources:
    PharmGKB

  • MERCAPTOPURINE   HBB

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MERCAPTOPURINE   TDP1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MERCAPTOPURINE   CYP2C9

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • MERCAPTOPURINE   CYP2C19

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • MERCAPTOPURINE   KDM4E

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MERCAPTOPURINE   CYP1A2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • MERCAPTOPURINE   CYP2D6

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • MERCAPTOPURINE   BAZ2B

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MERCAPTOPURINE   TP53

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MERCAPTOPURINE   IDH1

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MERCAPTOPURINE   ALDH1A1

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MERCAPTOPURINE   KDM4A

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • MERCAPTOPURINE   CYP3A4

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • MERCAPTOPURINE   NFE2L2

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DrugBank: DB01033

    • Version: 5.1.7

    Alternate Names:
    50-44-2 CAS Number
    Leukerin Drug Brand
    Mercaptopurine Tablets USP Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Categories antimetabolites

    Publications:
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Sahasranaman et al., 2008, Clinical pharmacology and pharmacogenetics of thiopurines., Eur. J. Clin. Pharmacol.
    Dubinsky, 2004, Azathioprine, 6-mercaptopurine in inflammatory bowel disease: pharmacology, efficacy, and safety., Clin. Gastroenterol. Hepatol.

  • TdgClinicalTrial: MERCAPTOPURINE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications Antineoplastic Agents
    Drug Class small molecule
    FDA Approval 1953

    Publications:

  • TEND: MERCAPTOPURINE

    • Version: 01-August-2011

    Alternate Names:

    Drug Info:
    Year of Approval 1953
    Drug Class antineoplastic agents

    Publications:

  • DTC: MERCAPTOPURINE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL1425 ChEMBL Drug ID

    Drug Info:

    Publications:
    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for &gt;200 compounds., Chem Res Toxicol

  • NCI: 6-MP

    • Version: 14-September-2017

    Alternate Names:
    C195 NCI drug code

    Drug Info:

    Publications:
    Sugita et al., 1992, [Analysis of lymphocyte surface markers in childhood acute lymphoblastic leukemia during maintenance chemotherapy]., Gan To Kagaku Ryoho

  • JAX-CKB: Mercaptopurine

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Pikman et al., 2017, Synergistic Drug Combinations with a CDK4/6 Inhibitor in T-cell Acute Lymphoblastic Leukemia., Clin. Cancer Res.

  • PharmGKB: mercaptopurine

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Perez-Andreu V et al., 2013, Inherited GATA3 variants are associated with Ph-like childhood acute lymphoblastic leukemia and risk of relapse., Nat Genet
    Kim HS et al., 2017, A coding variant in <i>FTO</i> confers susceptibility to thiopurine-induced leukopenia in East Asian patients with IBD., Gut
    Dorababu P et al., 2012, Genetic variants of thiopurine and folate metabolic pathways determine 6-MP-mediated hematological toxicity in childhood ALL., Pharmacogenomics

  • CIViC: MERCAPTOPURINE

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Meyer JA et al., 2013, Relapse-specific mutations in NT5C2 in childhood acute lymphoblastic leukemia., Nat Genet
    Tzoneva et al., 2013, Activating mutations in the NT5C2 nucleotidase gene drive chemotherapy resistance in relapsed ALL., Nat. Med.
    Moriyama T et al., 2016, NUDT15 polymorphisms alter thiopurine metabolism and hematopoietic toxicity., Nat Genet

  • TTD: Mercaptopurine

    • Version: 2020.06.01

    Alternate Names:
    D09UZO TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1425

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Mercaptopurine

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

  • CGI: Mercaptopurine

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21