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LETROZOLE Drug Record

  • Summary
  • Interactions
  • Claims
  • LETROZOLE chembl:CHEMBL1444 ApprovedAntineoplastic

    Alternate Names:

    LETROZOLE
    FEMARA
    CGS-20267
    FEM345
    FEMARA®
    LETROZOL
    rxcui:72965
    drugbank:01006
    chemidplus:112809-51-5
    chembl:CHEMBL1444
    pubchem.compound:3902

    Drug Info:

    Year of Approval 1997
    Drug Class antineoplastic agents
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications antineoplastic agent
    (8 More Sources)

    Publications:

    Ferlin MG et al., 2013, Design, synthesis, and structure-activity relationships of azolylmethylpyrroloquinolines as nonsteroidal aromatase inhibitors., J Med Chem
    Oesterreich S et al., 2015, Associations between genetic variants and the effect of letrozole and exemestane on bone mass and bone turnover., Breast Cancer Res Treat
    Santa-Maria CA et al., 2016, Association of Variants in Candidate Genes with Lipid Profiles in Women with Early Breast Cancer on Adjuvant Aromatase Inhibitor Therapy., Clin Cancer Res
    Wang L et al., 2010, Functional genetic polymorphisms in the aromatase gene CYP19 vary the response of breast cancer patients to neoadjuvant therapy with aromatase inhibitors., Cancer Res
    Long et al., 2004, Therapeutic strategies using the aromatase inhibitor letrozole and tamoxifen in a breast cancer model., J. Natl. Cancer Inst.
    Murphy, 1998, Molecular Action and Clinical Relevance of Aromatase Inhibitors., Oncologist
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Ebert et al., [Aromatase inhibitors--theoretical concept and present experiences in the treatment of endometriosis]., Zentralbl Gynakol
    Finn et al., 2015, The cyclin-dependent kinase 4/6 inhibitor palbociclib in combination with letrozole versus letrozole alone as first-line treatment of oestrogen receptor-positive, HER2-negative, advanced breast cancer (PALOMA-1/TRIO-18): a randomised phase 2 study., Lancet Oncol.
    Johnston et al., 2009, Lapatinib combined with letrozole versus letrozole and placebo as first-line therapy for postmenopausal hormone receptor-positive metastatic breast cancer., J. Clin. Oncol.
    Gao et al., 2015, Does CDKN2A loss predict palbociclib benefit?, Curr Oncol
    Mayer et al., 2017, A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2- Metastatic Breast Cancer., Clin. Cancer Res.
    Borrie AE et al., 2018, Letrozole concentration is associated with CYP2A6 variation but not with arthralgia in patients with breast cancer., Breast Cancer Res Treat
    Desta Z et al., 2011, Plasma letrozole concentrations in postmenopausal women with breast cancer are associated with CYP2A6 genetic variants, body mass index, and age., Clin Pharmacol Ther
    Kitagawa K et al., 1999, The significance of the homozygous CYP2A6 deletion on nicotine metabolism: a new genotyping method of CYP2A6 using a single PCR-RFLP., Biochem Biophys Res Commun
    Oscarson M et al., 1998, Genotyping of human cytochrome P450 2A6 (CYP2A6), a nicotine C-oxidase., FEBS Lett
    Wang H et al., 2011, Association analysis of CYP2A6 genotypes and haplotypes with 5-fluorouracil formation from tegafur in human liver microsomes., Pharmacogenomics
    Tanii H et al., 2011, Population pharmacokinetic analysis of letrozole in Japanese postmenopausal women., Eur J Clin Pharmacol
    Elens L et al., 2010, Influence of host genetic factors on efavirenz plasma and intracellular pharmacokinetics in HIV-1-infected patients., Pharmacogenomics
    Hirose T et al., 2010, Pharmacokinetics of S-1 and CYP2A6 genotype in Japanese patients with advanced cancer., Oncol Rep
    Djordjevic N et al., 2010, In vivo evaluation of CYP2A6 and xanthine oxidase enzyme activities in the Serbian population., Eur J Clin Pharmacol
    Tan L et al., 2010, The influence of cytochrome oxidase CYP2A6, CYP2B6, and CYP2C9 polymorphisms on the plasma concentrations of valproic acid in epileptic patients., Clin Neurol Neurosurg
    Ishii Y et al., 2010, Can the 2-(13)C-uracil breath test be used to predict the effect of the antitumor drug S-1?, Cancer Chemother Pharmacol
    Murai K et al., 2009, Deactivation of anti-cancer drug letrozole to a carbinol metabolite by polymorphic cytochrome P450 2A6 in human liver microsomes., Xenobiotica
    Kong SY et al., 2009, Association of CYP2A6 polymorphisms with S-1 plus docetaxel therapy outcomes in metastatic gastric cancer., Pharmacogenomics
    di Iulio J et al., 2009, In vivo analysis of efavirenz metabolism in individuals with impaired CYP2A6 function., Pharmacogenet Genomics
    Arab-Alameddine M et al., 2009, Pharmacogenetics-based population pharmacokinetic analysis of efavirenz in HIV-1-infected individuals., Clin Pharmacol Ther
    Endo T et al., 2008, Genetic polymorphisms of CYP2A6 affect the in-vivo pharmacokinetics of pilocarpine., Pharmacogenet Genomics
    Fujita K et al., 2008, CYP2A6 and the plasma level of 5-chloro-2, 4-dihydroxypyridine are determinants of the pharmacokinetic variability of tegafur and 5-fluorouracil, respectively, in Japanese patients with cancer given S-1., Cancer Sci
    Kaida Y et al., 2008, The CYP2A6*4 allele is determinant of S-1 pharmacokinetics in Japanese patients with non-small-cell lung cancer., Clin Pharmacol Ther
    Peamkrasatam S et al., 2006, In vivo evaluation of coumarin and nicotine as probe drugs to predict the metabolic capacity of CYP2A6 due to genetic polymorphism in Thais., Drug Metab Pharmacokinet
    Audrain-McGovern J et al., 2007, The role of CYP2A6 in the emergence of nicotine dependence in adolescents., Pediatrics
    Benowitz NL et al., 2006, CYP2A6 genotype and the metabolism and disposition kinetics of nicotine., Clin Pharmacol Ther
    Nakajima M et al., 2006, Comprehensive evaluation of variability in nicotine metabolism and CYP2A6 polymorphic alleles in four ethnic populations., Clin Pharmacol Ther
    Nurfadhlina M et al., 2006, CYP2A6 polymorphisms in Malays, Chinese and Indians., Xenobiotica
    Minematsu N et al., 2006, Limitation of cigarette consumption by CYP2A6*4, *7 and *9 polymorphisms., Eur Respir J
    Malaiyandi V et al., 2006, Impact of CYP2A6 genotype on pretreatment smoking behaviour and nicotine levels from and usage of nicotine replacement therapy., Mol Psychiatry
    Wang J et al., 2006, 3'-UTR polymorphism in the human CYP2A6 gene affects mRNA stability and enzyme expression., Biochem Biophys Res Commun
    Huang S et al., 2005, CYP2A6, MAOA, DBH, DRD4, and 5HT2A genotypes, smoking behaviour and cotinine levels in 1518 UK adolescents., Pharmacogenet Genomics
    Kimura M et al., 2005, Cyp2a6 is a principal enzyme involved in hydroxylation of 1,7-dimethylxanthine, a main caffeine metabolite, in humans., Drug Metab Dispos
    Gambier N et al., 2005, Association of CYP2A6*1B genetic variant with the amount of smoking in French adults from the Stanislas cohort., Pharmacogenomics J
    Fukami T et al., 2005, Characterization of novel CYP2A6 polymorphic alleles (CYP2A6*18 and CYP2A6*19) that affect enzymatic activity., Drug Metab Dispos
    Gyamfi MA et al., 2005, High prevalence of cytochrome P450 2A6*1A alleles in a black African population of Ghana., Eur J Clin Pharmacol
    Fukami T et al., 2004, A novel polymorphism of human CYP2A6 gene CYP2A6*17 has an amino acid substitution (V365M) that decreases enzymatic activity in vitro and in vivo., Clin Pharmacol Ther
    Schoedel KA et al., 2004, Ethnic variation in CYP2A6 and association of genetically slow nicotine metabolism and smoking in adult Caucasians., Pharmacogenetics
    Fujieda M et al., 2004, Evaluation of CYP2A6 genetic polymorphisms as determinants of smoking behavior and tobacco-related lung cancer risk in male Japanese smokers., Carcinogenesis
    Yamanaka H et al., 2004, Metabolic profile of nicotine in subjects whose CYP2A6 gene is deleted., Eur J Pharm Sci
    Nakajima M et al., 2004, Novel human CYP2A6 alleles confound gene deletion analysis., FEBS Lett
    Iwahashi K et al., 2004, Whole deletion of CYP2A6 gene (CYP2A6AST;4C) and smoking behavior., Neuropsychobiology
    Yoshida R et al., 2003, Effects of polymorphism in promoter region of human CYP2A6 gene (CYP2A6*9) on expression level of messenger ribonucleic acid and enzymatic activity in vivo and in vitro., Clin Pharmacol Ther
    Smith IE et al., 2003, Aromatase inhibitors in breast cancer., N Engl J Med
    Ando M et al., 2003, Association of CYP2A6 gene deletion with cigarette smoking status in Japanese adults., J Epidemiol
    Oscarson M et al., 2002, Characterization of a novel CYP2A7/CYP2A6 hybrid allele (CYP2A6*12) that causes reduced CYP2A6 activity., Hum Mutat
    Ariyoshi N et al., 2002, Genetic polymorphism of CYP2A6 gene and tobacco-induced lung cancer risk in male smokers., Cancer Epidemiol Biomarkers Prev
    Daigo S et al., 2002, A novel mutant allele of the CYP2A6 gene (CYP2A6*11 ) found in a cancer patient who showed poor metabolic phenotype towards tegafur., Pharmacogenetics
    Xu C et al., 2002, An in vivo pilot study characterizing the new CYP2A6*7, *8, and *10 alleles., Biochem Biophys Res Commun
    Zhang X et al., 2001, Lack of association between smoking and CYP2A6 gene polymorphisms in A Japanese population., Nihon Arukoru Yakubutsu Igakkai Zasshi
    Paschke T et al., 2001, Comparison of cytochrome P450 2A6 polymorphism frequencies in Caucasians and African-Americans using a new one-step PCR-RFLP genotyping method., Toxicology
    Kwon JT et al., 2001, Nicotine metabolism and CYP2A6 allele frequencies in Koreans., Pharmacogenetics
    Pitarque M et al., 2001, Identification of a single nucleotide polymorphism in the TATA box of the CYP2A6 gene: impairment of its promoter activity., Biochem Biophys Res Commun
    Tan W et al., 2001, Frequency of CYP2A6 gene deletion and its relation to risk of lung and esophageal cancer in the Chinese population., Int J Cancer
    Ariyoshi N et al., 2001, A novel single nucleotide polymorphism altering stability and activity of CYP2a6., Biochem Biophys Res Commun
    Nakajima M et al., 2001, Relationship between interindividual differences in nicotine metabolism and CYP2A6 genetic polymorphism in humans., Clin Pharmacol Ther
    Rao Y et al., 2000, Duplications and defects in the CYP2A6 gene: identification, genotyping, and in vivo effects on smoking., Mol Pharmacol
    Oscarson M et al., 1999, Identification and characterisation of novel polymorphisms in the CYP2A locus: implications for nicotine metabolism., FEBS Lett
    Mitropoulou et al., 2003, Letrozole as a potent inhibitor of cell proliferation and expression of metalloproteinases (MMP-2 and MMP-9) by human epithelial breast cancer cells., Int. J. Cancer
    Rahman et al., 2008, CYP1B1 is not a major determinant of the disposition of aromatase inhibitors in epithelial cells of invasive ductal carcinoma., Drug Metab. Dispos.
    Gala K et al., 2018, KMT2C mediates the estrogen dependence of breast cancer through regulation of ERα enhancer function., Oncogene
  • LETROZOLE   CYP2A6

    Interaction Score: 9.94

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30094551 21975350 10448083 9827545 21521021 21494765 20860463 20596643 20155256 20089352 19921195 19845430 19604090 19238117 19225447 18698229 18380793 18212800 17220563 17130279 17112802 16952495 16891249 16452582 16402128 16378601 16272956 15980104 15940289 15900015 15660270 15592323 15475735 15308589 15265511 15225612 14981342 12844137 12802030 12749606 12325023 12223434 12042667 11779172 11725533 11684323 11434509 11394901 11241319 11237731 11180041 10999944 10544257


    Sources:
    PharmGKB

  • LETROZOLE   KMT2C

    Interaction Score: 2.94

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    29755131


    Sources:
    CIViC

  • LETROZOLE   CYP19A1

    Interaction Score: 1.82

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name letrozole ,Femara
    Novel drug target Established target
    Mechanism of Interaction Cytochrome P450 19A1 inhibitor

    PMIDs:
    24025069 26536870 26463708 20048079 15026471 10388095 11752352 14505258


    Sources:
    DTC TdgClinicalTrial ChemblInteractions TEND PharmGKB TTD

  • LETROZOLE   TNFSF11

    Interaction Score: 1.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • LETROZOLE   TNFRSF11B

    Interaction Score: 0.88

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • LETROZOLE   CDKN2A

    Interaction Score: 0.42

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26715889


    Sources:
    CIViC

  • LETROZOLE   MMP2

    Interaction Score: 0.37

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12569569


    Sources:
    NCI

  • LETROZOLE   CYP1B1

    Interaction Score: 0.32

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18256205


    Sources:
    NCI

  • LETROZOLE   PGR

    Interaction Score: 0.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    ClearityFoundationBiomarkers PharmGKB FDA

  • LETROZOLE   ESR2

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26536870


    Sources:
    PharmGKB

  • LETROZOLE   ESR1

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26536870 25524798


    Sources:
    ClearityFoundationBiomarkers CIViC PharmGKB FDA

  • LETROZOLE   PIK3CA

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type no benefit
    Indication/Tumor Type estrogen-receptor positive breast cancer
    combination therapy Letrozole + BYL719

    PMIDs:
    27126994


    Sources:
    JAX-CKB

  • LETROZOLE   ERBB2

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Lapatinib + Letrozole
    Indication/Tumor Type Her2-receptor positive breast cancer
    Response Type sensitive

    PMIDs:
    19786658


    Sources:
    JAX-CKB

  • LETROZOLE   CYP3A4

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TEND: LETROZOLE

    • Version: 01-August-2011

    Alternate Names:
    LETROZOLE Primary Drug Name

    Drug Info:
    Drug Class antineoplastic agents
    Year of Approval 1997

    Publications:

  • TdgClinicalTrial: LETROZOLE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antineoplastic agent
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • NCI: LETROZOLE

    • Version: 14-September-2017

    Alternate Names:
    C1527 NCI drug code

    Drug Info:

    Publications:
    Mitropoulou et al., 2003, Letrozole as a potent inhibitor of cell proliferation and expression of metalloproteinases (MMP-2 and MMP-9) by human epithelial breast cancer cells., Int. J. Cancer
    Rahman et al., 2008, CYP1B1 is not a major determinant of the disposition of aromatase inhibitors in epithelial cells of invasive ductal carcinoma., Drug Metab. Dispos.

  • DTC: LETROZOLE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL1444 ChEMBL Drug ID

    Drug Info:

    Publications:
    Ferlin MG et al., 2013, Design, synthesis, and structure-activity relationships of azolylmethylpyrroloquinolines as nonsteroidal aromatase inhibitors., J Med Chem

  • JAX-CKB: Letrozole

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Johnston et al., 2009, Lapatinib combined with letrozole versus letrozole and placebo as first-line therapy for postmenopausal hormone receptor-positive metastatic breast cancer., J. Clin. Oncol.
    Mayer et al., 2017, A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2- Metastatic Breast Cancer., Clin. Cancer Res.

  • PharmGKB: letrozole

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Oesterreich S et al., 2015, Associations between genetic variants and the effect of letrozole and exemestane on bone mass and bone turnover., Breast Cancer Res Treat
    Pitarque M et al., 2001, Identification of a single nucleotide polymorphism in the TATA box of the CYP2A6 gene: impairment of its promoter activity., Biochem Biophys Res Commun
    Malaiyandi V et al., 2006, Impact of CYP2A6 genotype on pretreatment smoking behaviour and nicotine levels from and usage of nicotine replacement therapy., Mol Psychiatry

  • CIViC: LETROZOLE

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Finn et al., 2015, The cyclin-dependent kinase 4/6 inhibitor palbociclib in combination with letrozole versus letrozole alone as first-line treatment of oestrogen receptor-positive, HER2-negative, advanced breast cancer (PALOMA-1/TRIO-18): a randomised phase 2 study., Lancet Oncol.
    Gao et al., 2015, Does CDKN2A loss predict palbociclib benefit?, Curr Oncol
    Gala K et al., 2018, KMT2C mediates the estrogen dependence of breast cancer through regulation of ERα enhancer function., Oncogene

  • TTD: Letrozole

    • Version: 2020.06.01

    Alternate Names:
    D0C1WH TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1444

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL1444

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationBiomarkers: LETROZOLE

    • Version: 26-July-2013

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Letrozole

    • Version: 04-September-2020

    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.

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