Drug/Small Molecule:
tamoxifen

2D structure

Overview

Generic Names: Tamoxifen Citrate; Tamoxifene [INN-French]; Tamoxifeno [INN-Spanish]; Tamoxifenum [INN-Latin]; Trans-Tamoxifen
Trade Names: Apo-Tamox; Citofen; Crisafeno; Diemon; Gen-Tamoxifen; Istubol; Kessar; Noltam; Nolvadex; Nolvadex-D; Nourytam; Novo-Tamoxifen; Oncomox; PMS-Tamoxifen; Retaxim; Tamizam; Tamofen; Tamone; Tamoxasta; Tamoxen; Valodex; Zemide
PharmGKB Accession Id: PA451581

Description

One of the selective estrogen receptor modulators with tissue-specific activities. Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue, but as an estrogen (stimulating agent) in cholesterol metabolism, bone density, and cell proliferation in the endometrium. PubChem (source: Drug Bank)

Indication

Used for the treatment and prevention of breast cancer. (source: Drug Bank)

ATC Therapeutic Category

  • L02BA:Anti-estrogens

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Tamoxifen binds to estrogen receptors (ER), inducing a conformational change in the receptor. This results in a blockage or change in the expression of estrogen dependent genes. The prolonged binding of tamoxifen to the nuclear chromatin of these results in reduced DNA polymerase activity, impaired thymidine utilization, blockade of estradiol uptake, and decreased estrogen response. It is likely that tamoxifen interacts with other coactivators or corepressors in the tissue and binds with different estrogen receptors, ER-alpha or ER-beta, producing both estrogenic and antiestrogenic effects. (source: Drug Bank)

Pharmacology

Tamoxifen belongs to a class of drugs called selective estrogen receptor modulators (SERMs), which have both estrogenic and antiestrogenic effects. Tamoxifen has the same nucleus as diethylstilbestrol but possesses an additional side chain (<i>trans</i> isomer) which accounts for its antiestrogenic activity. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. Tamoxifen is extensively metabolized after oral administration. N-desmethyl tamoxifen is the major metabolite found in plasma. N-desmethyl tamoxifen activity is similar to tamoxifen. 4-Hydroxytamoxifen and a side chain primary alcohol derivative of tamoxifen have been identified as minor metabolites in plasma. Tamoxifen is a substrate of cytochrome P450 CYP3A4, CYP2C9 and CYP2D6, and an inhibitor of P-glycoprotein. (source: Drug Bank)

Toxicity

Signs observed at the highest doses following studies to determine LD50 in animals were respiratory difficulties and convulsions. (source: Drug Bank)

Isomeric SMILES Code:

CC/C(=C(\c1ccccc1)/c2ccc(cc2)OCCN(C)C)/c3ccccc3 (source: Drug Bank)

In-Depth Annotations (In-Depth Annotation)

  1. rs6025 at chr1:167785673 in F5
    Associated with risk of venous thromboembolism (VTE).
    Variant Name:
    F5:Factor V Leiden (FVL)
    Related Drugs:
    drotrecogin alfa, estrogens, hormonal contraceptives for systemic use, tamoxifen
    Related Diseases:
    Thromboembolism, venous thromboembolism
    Evidence:
    http://www.pharmgkb.org/.../variant.jsp
  2. rs2740574 at chr7:99220032 in CYP3A, CYP3A4
    Defining variant for CYP3A4*1B; well studied, conflicting results on effect on gene transcription, no clear consensus on its significance for drug disposition, may be assocated with an increased risk of developing endometrial cancer after tamoxifen treatment.
    Variant Name:
    CYP3A4:-392A>G; CYP3A4*1B
    Related Drugs:
    tamoxifen
    Related Diseases:
    Endometrial Neoplasms
    Evidence:
    http://www.pharmgkb.org/.../variant.jsp

Curated Annotations (Curated Annotation)

  1. rs351855 at chr5:176452849 in FGFR4
    This variant is associated with cancer progression and tumor cell motility. Patients carrying arg388 allele was associated with metastasis and poor prognosis in breast cancer and in colon cancer as well as poor clinical outcome for head and neck squamous cell carcinoma. possible association with sensitivity to cisplatin. It is associated with resistence to adjuvent systemic therapy in primary breast cancer.
    Variant Name:
    FGFR4:GLY388ARG; FGFR4:Arg388
    Related Drugs:
    cisplatin, cyclophosphamide, fluorouracil, methotrexate, tamoxifen
    Related Diseases:
    Breast Neoplasms
    Evidence:
    PMID:11830541
    PMID:15197773
    PMID:16822847
    PMID:17084840
    PMID:18487077
  2. rs9340799 at chr6:152205074 in ESR1
    SNP is associated with tamoxifen-induced changes in total cholesterol and triglycerides in postmenopausal woman.
    Variant Name:
    ESR1:c.454-351A>G; ESR1:XbaI; ESR1:rs9340799
    Related Drugs:
    tamoxifen
    Evidence:
    PMID:17713466
  3. rs11188072 at chr10:96509051 in CYP2C19
    This promoter variant is part of CYP2C19*17 haplotype, which causes increased acitivity and increased transcription of CYP2C19. Patients carrying this allele may exhibit a lack of response to commonly prescribed dosages of certain proton pump inhibitors (PPIs) and antidepressants, due to ultrarapid clearance of these drugs. CYP2C19*17 carriers are more likely to benifit from tamoxifen treatment.
    Variant Name:
    CYP2C19: -3402C>T
    Related Drugs:
    amitriptyline, citalopram, clomipramine, escitalopram, omeprazole, proguanil, tamoxifen
    Evidence:
    PMID:16413245
    PMID:17625515
    PMID:18294333
  4. rs12248560 at chr10:96511647 in CYP2C19
    This promoter variant is part of CYP2C19*17 haplotype, which causes increased acitivity and increased transcription of CYP2C19. Patients carrying this allele may exhibit a lack of response to commonly prescribed dosages of certain proton pump inhibitors (PPIs) and antidepressants, due to ultrarapid clearance of these drugs. CYP2C19*17 carriers are more likely to benifit from tamoxifen treatment.
    Variant Name:
    CYP2C19: -806C>T
    Related Drugs:
    amitriptyline, citalopram, clomipramine, escitalopram, omeprazole, proguanil, tamoxifen
    Evidence:
    PMID:16413245
    PMID:18024866
  5. rs11023197 at chr11:14337574 in RRAS2
    In a study of tamoxifen treated breat cancer patients, carrying the T variant of RRAS2:(-582)C>T was associated with a higher frequency of relapse.
    Variant Name:
    TC21 (RRAS2) -582C>T, RRAS2:(-582)C>T
    Related Drugs:
    tamoxifen
    Related Diseases:
    Breast Neoplasms
    Evidence:
    PMID:19047159
  6. rs4986938 at chr14:63769569 in ESR2
    SNP is associated with tamoxifen-induced changes in total cholesterol and triglycerides in postmenopausal woman.
    Variant Name:
    ESR2-02
    Related Drugs:
    tamoxifen
    Evidence:
    PMID:17713466
  7. rs1135840 at chr22:40852557 in CYP2D6
    Risk or phenotype-associated allele: T. Phenotype: The CYP2D6*2A haplotype was associated with lower incidence of breast cancer on tamoxifen compared to placebo in a prevention study. The CYP2D6*2A allele may be associated with increased efficacy of tamoxifen. Study size: 182. Study population/ethnicity: Women in the Italian Tamoxifen Prevention trial, Caucasian, Italy. Significance metric(s): p = 0.0001. Type of association: CO.
    Variant Name:
    CYP2D6:4180G>C, part of CYP2D6*2A an extensive metabolizer haplotype.
    Related Drugs:
    tamoxifen
    Related Diseases:
    Breast Neoplasms
    Evidence:
    PMID:20309015
  8. rs16947 at chr22:40853887 in CYP2D6
    Risk or phenotype-associated allele: T. Phenotype: The CYP2D6*2A haplotype was associated with lower incidence of breast cancer on tamoxifen compared to placebo in a prevention study. The CYP2D6*2A allele may be associated with increased efficacy of tamoxifen. Study size: 182. Study population/ethnicity: Women in the Italian Tamoxifen Prevention trial, Caucasian, Italy. Significance metric(s): p = 0.0001. Type of association: CO.
    Variant Name:
    CYP2D6:2850C>T, part of CYP2D6*2A an extensive metabolizer haplotype.
    Related Drugs:
    tamoxifen
    Related Diseases:
    Breast Neoplasms
    Evidence:
    PMID:20309015
  9. rs3892097 at chr22:40854891 in CYP2D6
    In tamoxifen-treated patients, women with the CYP2D6 *4/*4 genotype tended to have a higher risk of disease relapse and a lower incidence of hot flashes.
    Variant Name:
    CYP2D6:1846G>A, part of CYP2D6*4
    Related Drugs:
    tamoxifen
    Evidence:
    PMID:16361630
    http://preview.pharmgkb.org/.../variant.jsp
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ABCB1
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
ABCC2
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Has annotations
BRCA1
  • CO
  •   
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  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
BRCA2
  • CO
  •   
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CDKN1B
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP1A2
  • CO
  • PD
  • PK
  •   
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Has annotations
CYP2A6
  • CO
  • PD
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2B6
  • CO
  • PD
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C19
  • CO
  • PD
  • PK
  • FA
  • GN
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP2C8
  •   
  •   
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C9
  • CO
  • PD
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2D6
  • CO
  • PD
  • PK
  • FA
  • GN
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP3A
  •   
  •   
  • PK
  •   
  •   
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
  • CO
  • PD
  • PK
  • FA
  •   
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A5
  • CO
  •   
  • PK
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
ERBB2
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  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
ESR1
  • CO
  • PD
  •   
  • FA
  • GN
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Not annotated
ESR2
  • CO
  • PD
  •   
  •   
  • GN
Publications, Variants
No phenotype data Genotype Data Available Literature annotations available Has annotations
F5
  •   
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  •   
  •   
  •   
Variants
No phenotype data No genotype data Literature annotations available Not annotated
FGFR4
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  •   
Variants
Phenotype data available No genotype data Literature annotations available Not annotated
G6PD
  •   
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  •   
  • FA
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
GPX1
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
HOXB13
  • CO
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
IL17RB
  • CO
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
JAG1
  •   
  • PD
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
KRT13
  •   
  • PD
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
MECP2
  •   
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  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
NOS3
  • CO
  • PD
  • PK
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
NR1I2
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
OGG1
  •   
  • PD
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
PAX2
  •   
  • PD
  •   
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  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
RRAS2
  • CO
  •   
  •   
  • FA
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SLC7A11
  •   
  • PD
  •   
  • FA
  •   
Publications
Phenotype data available No genotype data Literature annotations available Not annotated
SOD1
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SOD2
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SP1
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SPINK4
  •   
  • PD
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
SULT1A1
  • CO
  •   
  •   
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
SULT1A2
  •   
  •   
  •   
  • FA
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
SULT1A3
  •   
  •   
  •   
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
SULT1A4
  •   
  •   
  •   
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
SULT1B1
  •   
  •   
  •   
  • FA
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SULT1C4
  •   
  •   
  •   
  • FA
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
SULT1E1
  •   
  •   
  •   
  • FA
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
SULT2A1
  •   
  •   
  •   
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
SULT2B1
  •   
  •   
  •   
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
SULT4A1
  •   
  •   
  •   
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
SULT6B1
  •   
  •   
  •   
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
UGT1A4
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
XRCC4
  •   
  • PD
  •   
  • FA
  •   
Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
ABCB1 Uncurated Annotation (source: Drug Bank)
ECGF1 Uncurated Annotation (source: Drug Bank)
EPHX2 Uncurated Annotation (source: Drug Bank)
ESR1 Uncurated Annotation (source: Drug Bank)
ESR2 Uncurated Annotation (source: Drug Bank)

The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
amiodarone
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
amitriptyline
  •   
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
amlodipine
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  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
anastrozole
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
bupropion
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
celecoxib
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  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
cetirizine
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  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
chloroquine
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
chlorpheniramine
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
chlorpromazine
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Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
cimetidine
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
cinacalcet
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
citalopram
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
clemastine
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  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
clomipramine
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
clozapine
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  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
delavirdine
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  •   
Publications
Phenotype data available No genotype data Literature annotations available Not annotated
desipramine
  •   
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  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
diphenylpyraline
  •   
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  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
doxepin
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
duloxetine
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
efavirenz
  •   
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  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
escitalopram
  •   
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  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
estradiol
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
felodipine
  •   
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  •   
  •   
  •   
Publications
Phenotype data available No genotype data Literature annotations available Not annotated
fluoxetine
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
fluphenazine
  •   
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  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
fluvoxamine
  •   
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  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
gabapentin
  •   
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
halofantrine
  •   
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  •   
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  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
haloperidol
  •   
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  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
hydroxyzine
  •   
  •   
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  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
imipramine
  •   
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
indinavir
  •   
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
letrozole
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
loratadine
  •   
  •   
  •   
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
metoclopramide
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
mirtazapine
  •   
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
nelfinavir
  •   
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
nevirapine
  •   
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
nicardipine
  •   
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  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
nifedipine
  •   
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  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
nortriptyline
  •   
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
olanzapine
  •   
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
paroxetine
  • CO
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
perphenazine
  •   
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
pimozide
  •   
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
promethazine
  •   
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
quetiapine
  •   
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  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
quinidine
  •   
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
ranitidine
  •   
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
reboxetine
  •   
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
risperidone
  •   
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
ritonavir
  •   
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Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
saquinavir
  •   
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
sertraline
  •   
  •   
  • PK
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
terbinafine
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Publications
Phenotype data available No genotype data Literature annotations available Not annotated
thioridazine
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
thiothixene
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
ticlopidine
  •   
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
trastuzumab
  •   
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  • FA
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
tripelennamine
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
venlafaxine
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  • PK
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
verapamil
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Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
warfarin
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
ziprasidone
  •   
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Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
Nilotinib Uncurated Annotation Nilotinib may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
acenocoumarol Uncurated Annotation Tamoxifen may increase the serum concentration of Acenocoumarol increasing the risk of bleeding. Concomitant therapy should be avoided. (source: Drug Bank)
aminoglutethimide Uncurated Annotation Aminoglutethimide may increase Tamoxifen clearance decreasing its therapeutic effect. Consider alternate therapy or monitor for changes in Tamoxifen effects when Aminoglutethimide is initiated, discontinued or dose changed. (source: Drug Bank)
amiodarone Uncurated Annotation Amiodarone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
amprenavir Uncurated Annotation Amprenavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
atazanavir Uncurated Annotation Atazanavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
capecitabine Uncurated Annotation Capecitabine may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Capecitabine is initiated, discontinued or dose changed. (source: Drug Bank)
chloroquine Uncurated Annotation Chloroquine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
chlorpromazine Uncurated Annotation Chlorpromazine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
cimetidine Uncurated Annotation Cimetidine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
cinacalcet Uncurated Annotation Cinacalcet may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
clarithromycin Uncurated Annotation Clarithromycin may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
clomipramine Uncurated Annotation Clomipramine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
clozapine Uncurated Annotation Clozapine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
cocaine Uncurated Annotation Cocaine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
conivaptan Uncurated Annotation Conivaptan may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
darifenacin Uncurated Annotation Darifenacin may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
darunavir Uncurated Annotation Darunavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
delavirdine Uncurated Annotation Delavirdine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
desipramine Uncurated Annotation Desipramine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
diphenhydramine Uncurated Annotation Diphenhydramine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
duloxetine Uncurated Annotation Duloxetine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
floxuridine Uncurated Annotation Floxuridine may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Floxiridine is initiated, discontinued or dose changed. (source: Drug Bank)
fluconazole Uncurated Annotation Fluconzole may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Fluconazole is initiated, discontinued or dose changed. (source: Drug Bank)
fluorouracil Uncurated Annotation Fluorouracil may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Fluorouracil is initiated, discontinued or dose changed. (source: Drug Bank)
fluoxetine Uncurated Annotation Fluoxetine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
flurbiprofen Uncurated Annotation Flurbiprofen may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Flurbiprofen is initiated, discontinued or dose changed. (source: Drug Bank)
fosamprenavir Uncurated Annotation Fosmprenavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
gemfibrozil Uncurated Annotation Gemfibrozil may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Gemfibrozil is initiated, discontinued or dose changed. (source: Drug Bank)
haloperidol Uncurated Annotation Haloperidol may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
ibuprofen Uncurated Annotation Ibuprofen may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Ibuprofen is initiated, discontinued or dose changed. (source: Drug Bank)
imatinib Uncurated Annotation Imatinib may increase the serum concentration of Tamoxifen by decreasing its metabolism and clearance. Imatinib may also decrease the therapeutic effect of Tamoxifen by decreasing active metabolite production. Monitor for changes in the therapeutic/adverse effects of Tamoxifen if Imatinib is initiated, discontinued or dose changed. (source: Drug Bank)
imipramine Uncurated Annotation Imipramine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
indinavir Uncurated Annotation Indinavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
indomethacin Uncurated Annotation Indomethacin may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Indomethacin is initiated, discontinued or dose changed. (source: Drug Bank)
isoniazid Uncurated Annotation Isoniazid may increase the serum concentration of Tamoxifen by decreasing its metabolism and clearance. Isoniazid may also decrease the therapeutic effect of Tamoxifen by decreasing active metabolite production. Monitor for changes in the therapeutic/adverse effects of Tamoxifen if Isoniazid is initiated, discontinued or dose changed. (source: Drug Bank)
itraconazole Uncurated Annotation Itraconazole may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
ketoconazole Uncurated Annotation Ketoconazole may increase the serum concentration of Tamoxifen by decreasing its metabolism and clearance. Ketoconazole may also decrease the therapeutic effect of Tamoxifen by decreasing active metabolite production. Monitor for changes in the therapeutic/adverse effects of Tamoxifen if Ketoconazole is initiated, discontinued or dose changed. (source: Drug Bank)
lidocaine Uncurated Annotation Lidocaine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
lopinavir Uncurated Annotation Lopinavir may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
methadone Uncurated Annotation Methadone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
methimazole Uncurated Annotation Methimazole may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
miconazole Uncurated Annotation Miconazole may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
nefazodone Uncurated Annotation Nefazodone may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
nelfinavir Uncurated Annotation Nelfinavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
nicardipine Uncurated Annotation Nicardipine may increase the serum concentration of Tamoxifen by decreasing its metabolism and clearance. Nicardipine may also decrease the therapeutic effect of Tamoxifen by decreasing active metabolite production. Monitor for changes in the therapeutic/adverse effects of Tamoxifen if Nicardipine is initiated, discontinued or dose changed. (source: Drug Bank)
paroxetine Uncurated Annotation Paroxetine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
pergolide Uncurated Annotation Pergolide may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
pioglitazone Uncurated Annotation Pioglitazone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
piroxicam Uncurated Annotation Piroxicam may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Piroxicam is initiated, discontinued or dose changed. (source: Drug Bank)
posaconazole Uncurated Annotation Posaconazole may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
pyrimethamine Uncurated Annotation Pyrimethamine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
quinidine Uncurated Annotation Quinidine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
quinine Uncurated Annotation Quinine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
ranolazine Uncurated Annotation Ranolazine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
ritonavir Uncurated Annotation Ritonavir may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
saquinavir Uncurated Annotation Saquinavir may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
sertraline Uncurated Annotation Sertraline may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
sulfadiazine Uncurated Annotation Sulfadiazine may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Sulfadiazine is initiated, discontinued or dose changed. (source: Drug Bank)
sulfisoxazole Uncurated Annotation Sulfisoxazole may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Sulfisoxazole is initiated, discontinued or dose changed. (source: Drug Bank)
telithromycin Uncurated Annotation Telithromycin may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
terbinafine Uncurated Annotation Terbinafine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Concomitant therapy should be avoided. (source: Drug Bank)
thioridazine Uncurated Annotation Thioridazine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
ticlopidine Uncurated Annotation Ticlopidine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
tolbutamide Uncurated Annotation Tolbutamide may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Tolbutamide is initiated, discontinued or dose changed. (source: Drug Bank)
topotecan Uncurated Annotation Tamoxifen may increase serum concentrations of oral Topotecan. Concomitant therapy should be avoided. (source: Drug Bank)
tranylcypromine Uncurated Annotation Tranylcypromine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
trazodone Uncurated Annotation Trazodone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy. (source: Drug Bank)
voriconazole Uncurated Annotation Voriconazole may increase the serum concentration of Tamoxifen by decreasing its metabolism. Monitor for increased adverse/toxic effects of Tamoxifen. (source: Drug Bank)
warfarin Uncurated Annotation Tamoxifen may increase the serum concentration of Warfarin increasing the risk of bleeding. Concomitant therapy should be avoided. (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Breast Neoplasms
  • CO
  • PD
  • PK
  • FA
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
Death
  • CO
  •   
  •   
  •   
  •   
Publications
Phenotype data available No genotype data Literature annotations available Not annotated
Depression
  • CO
  • PD
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
estrogen-dependent carcinogenesis
  •   
  •   
  •   
  • FA
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Heart Diseases
  • CO
  • PD
  • PK
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Hot Flashes
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Lung Neoplasms
  • CO
  • PD
  • PK
  • FA
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Neoplasms
  • CO
  • PD
  • PK
  • FA
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Ovarian Neoplasms
  • CO
  • PD
  • PK
  • FA
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Rett Syndrome
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Schizophrenia
  • CO
  • PD
  • PK
  •   
  •   
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Curated Phenotype Datasets

These datasets are sorted alphabetically by title.

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. Bone mineral density in tamoxifen patients
  2. ELPh Trial Sample-Demographic
  3. Lipid Profiles for subjects in a Tamoxifen Trial
  4. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

Downloads

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LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00675
ChEBI ID:
9396
KEGG Compound ID:
C07108
KEGG Drug ID:
D00966
PubChem Compound ID:
2733526
PubChem Substance ID:
9319
IUPHAR Ligand ID:
1016

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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