Physiologically Based Pharmacokinetic Modeling of Tamoxifen and its Metabolites in Women of Different CYP2D6 Phenotypes Provides New Insight into the Tamoxifen Mass Balance. (Q35975826)

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English	Physiologically Based Pharmacokinetic Modeling of Tamoxifen and its Metabolites in Women of Different CYP2D6 Phenotypes Provides New Insight into the Tamoxifen Mass Balance.	scientific article

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scholarly article

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3 February 2020

Physiologically Based Pharmacokinetic Modeling of Tamoxifen and its Metabolites in Women of Different CYP2D6 Phenotypes Provides New Insight into the Tamoxifen Mass Balance (English)

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3 February 2020

mass-balance modelling

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based on heuristic

inferred from title

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based on heuristic

inferred from title

pharmacokinetics

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based on heuristic

inferred from title

4

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3 February 2020

author name string

Kristin Dickschen

1

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3 February 2020

Stefan Willmann

2

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3 February 2020

Kirstin Thelen

3

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3 February 2020

Georg Hempel

5

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3 February 2020

Thomas Eissing

6

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publication date

21 May 2012

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3 February 2020

Frontiers in Pharmacology

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3 February 2020

3

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3 February 2020

92

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Europe PubMed Central

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3 February 2020

The clinical effectiveness and cost-effectiveness of genotyping for CYP2D6 for the management of women with breast cancer treated with tamoxifen: a systematic review

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

Genotype-guided tamoxifen dosing increases active metabolite exposure in women with reduced CYP2D6 metabolism: a multicenter study

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

Tamoxifen metabolite concentrations, CYP2D6 genotype, and breast cancer outcomes.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

CYP2C19*2 polymorphism is associated with increased survival in breast cancer patients using tamoxifen

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

Endoxifen, a new cornerstone of breast cancer therapy: demonstration of safety, tolerability, and systemic bioavailability in healthy human subjects

1 reference

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2 October 2017

The impact of CYP2D6-predicted phenotype on tamoxifen treatment outcome in patients with metastatic breast cancer

1 reference

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2 October 2017

Associations between tamoxifen, estrogens, and FSH serum levels during steady state tamoxifen treatment of postmenopausal women with breast cancer

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

Effects of silybinin on the pharmacokinetics of tamoxifen and its active metabolite, 4-hydroxytamoxifen in rats

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

Genotype-guided tamoxifen therapy: time to pause for reflection?

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

CYP2D6 and tamoxifen: DNA matters in breast cancer

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

Tamoxifen pharmacogenomics: the role of CYP2D6 as a predictor of drug response

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

New insights into the metabolism of tamoxifen and its role in the treatment and prevention of breast cancer

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

Glucuronidation of active tamoxifen metabolites by the human UDP glucuronosyltransferases

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

The impact of cytochrome P450 2D6 metabolism in women receiving adjuvant tamoxifen

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

Endoxifen, a secondary metabolite of tamoxifen, and 4-OH-tamoxifen induce similar changes in global gene expression patterns in MCF-7 breast cancer cells

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

Tamoxifen (ICI46,474) as a targeted therapy to treat and prevent breast cancer

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

Pharmacogenetics of tamoxifen biotransformation is associated with clinical outcomes of efficacy and hot flashes

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

CYP2D6 genotype, antidepressant use, and tamoxifen metabolism during adjuvant breast cancer treatment

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

A physiological model for the estimation of the fraction dose absorbed in humans.

1 reference

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2 October 2017

Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

The influence of CYP2B6, CYP2C9 and CYP2D6 genotypes on the formation of the potent antioestrogen Z-4-hydroxy-tamoxifen in human liver

1 reference

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2 October 2017

Pharmacokinetics of anastrozole and tamoxifen alone, and in combination, during adjuvant endocrine therapy for early breast cancer in postmenopausal women: a sub-protocol of the 'Arimidex and tamoxifen alone or in combination' (ATAC) trial

1 reference

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2 October 2017

The effect of anastrozole on the pharmacokinetics of tamoxifen in post-menopausal women with early breast cancer

1 reference

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2 October 2017

Clinical pharmacology of tamoxifen in patients with breast cancer: correlation with clinical data

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

2 October 2017

A comparison of two doses of tamoxifen (Nolvadex) in postmenopausal women with advanced breast cancer: 10 mg bd versus 20 mg bd.

1 reference

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2 October 2017

Tamoxifen. A reappraisal of its pharmacodynamic and pharmacokinetic properties, and therapeutic use.

1 reference

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2 October 2017

A computational systems biology software platform for multiscale modeling and simulation: integrating whole-body physiology, disease biology, and molecular reaction networks.

1 reference

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11 July 2018

Tamoxifen metabolite isomer separation and quantification by liquid chromatography-tandem mass spectrometry

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

11 July 2018

Comprehensive analysis of the genetic factors determining expression and function of hepatic CYP2D6.

1 reference

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11 July 2018

Correlation between tamoxifen elimination and biomarker recovery in a primary prevention trial.

1 reference

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11 July 2018

A comparative study of tamoxifen metabolism in female rat, mouse and human liver microsomes.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

11 July 2018

The metabolism of tamoxifen (I.C.I. 46,474). I. In laboratory animals.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

11 July 2018

Tamoxifen metabolism: pharmacokinetic and in vitro study

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

11 July 2018

Binding of antitumor tamoxifen and its metabolites 4-hydroxytamoxifen and endoxifen to human serum albumin.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Dissolution rate and apparent solubility of poorly soluble drugs in biorelevant dissolution media.

1 reference

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24 September 2018

Cytochrome P450 2D6 and outcomes of adjuvant tamoxifen therapy: results of a meta-analysis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Pharmacokinetic interaction between tamoxifen and ondansetron in rats: non-competitive (hepatic) and competitive (intestinal) inhibition of tamoxifen metabolism by ondansetron via CYP2D subfamily and 3A1/2.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Effects of epigallocatechin gallate on the oral bioavailability and pharmacokinetics of tamoxifen and its main metabolite, 4-hydroxytamoxifen, in rats.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

The CYP2D6*4 polymorphism affects breast cancer survival in tamoxifen users

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Enhanced tamoxifen bioavailability after oral administration of tamoxifen in rats pretreated with naringin

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Effects of morin on the bioavailability of tamoxifen and its main metabolite, 4-hydroxytamoxifen, in rats

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Effects of oral kaempferol on the pharmacokinetics of tamoxifen and one of its metabolites, 4-hydroxytamoxifen, after oral administration of tamoxifen to rats

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Effects of CYP2D6 and SULT1A1 genotypes including SULT1A1 gene copy number on tamoxifen metabolism

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Development of a physiology-based whole-body population model for assessing the influence of individual variability on the pharmacokinetics of drugs.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Enhanced bioavailability of tamoxifen after oral administration of tamoxifen with quercetin in rats

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Effect of exemestane on tamoxifen pharmacokinetics in postmenopausal women treated for breast cancer

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Excretion of hydroxylated metabolites of tamoxifen in human bile and urine.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Molecular properties of WHO essential drugs and provisional biopharmaceutical classification

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Medication use, tamoxifen (TAM), and TAM metabolite concentrations in women with breast cancer

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Quaternary ammonium-linked glucuronidation of tamoxifen by human liver microsomes and UDP-glucuronosyltransferase 1A4.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Pharmacological characterization of 4-hydroxy-N-desmethyl tamoxifen, a novel active metabolite of tamoxifen

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Tamoxifen and metabolite concentrations in serum and breast cancer tissue during three dose regimens in a randomized preoperative trial.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

A physiologic model for simulating gastrointestinal flow and drug absorption in rats.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Active tamoxifen metabolite plasma concentrations after coadministration of tamoxifen and the selective serotonin reuptake inhibitor paroxetine

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

A randomized trial of low-dose tamoxifen on breast cancer proliferation and blood estrogenic biomarkers

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Human variability in CYP3A4 metabolism and CYP3A4-related uncertainty factors for risk assessment

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Reverse geometrical selectivity in glucuronidation and sulfation of cis- and trans-4-hydroxytamoxifens by human liver UDP-glucuronosyltransferases and sulfotransferases

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Five versus more than five years of tamoxifen for lymph node-negative breast cancer: updated findings from the National Surgical Adjuvant Breast and Bowel Project B-14 randomized trial

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

24 September 2018

Activity Levels of Tamoxifen Metabolites at the Estrogen Receptor and the Impact of Genetic Polymorphisms of Phase I and II Enzymes on Their Concentration Levels in Plasma

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3357105

14 November 2018

Serum elimination half-life of tamoxifen and its metabolites in patients with advanced breast cancer

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

A reliable and rapid procedure to estimate drug partitioning in biomembranes

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Serum and urine levels of tamoxifen and its metabolites in patients with advanced breast cancer after a loading dose and at steady-state levels

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Absorption classification of oral drugs based on molecular surface properties

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Comparison of bioavailability in man of tamoxifen after oral and rectal administration

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The metabolism of tamoxifen (I.C.I. 46,474). II. In female patients

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Pharmacokinetics of tamoxifen in premenopausal and postmenopausal women with breast cancer

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Effects of myricetin, an anticancer compound, on the bioavailability and pharmacokinetics of tamoxifen and its main metabolite, 4-hydroxytamoxifen, in rats

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Personalized tamoxifen: what is the best way forward?

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The CYP2C19*2 genotype predicts tamoxifen treatment outcome in advanced breast cancer patients

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

CYP2D6 and tamoxifen: awaiting the denouement

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Tamoxifen metabolites in patients on long-term adjuvant therapy for breast cancer

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Distribution of 4-hydroxy-N-desmethyltamoxifen and other tamoxifen metabolites in human biological fluids during tamoxifen treatment

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identification of 4-hydroxy-N-desmethyltamoxifen as a metabolite of tamoxifen in human bile

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The steady-state pharmacokinetics of tamoxifen and its metabolites in breast cancer patients

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Effect of oestrogen receptor status and time on the intra-tumoural accumulation of tamoxifen and N-desmethyltamoxifen following short-term therapy in human primary breast cancer

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Bioequivalence of 20-mg once-daily tamoxifen relative to 10-mg twice-daily tamoxifen regimens for breast cancer

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Age-related difference in tamoxifen disposition

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Pharmacokinetics and bioavailability of tamoxifen in postmenopausal healthy women

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Quantitative effect of CYP2D6 genotype and inhibitors on tamoxifen metabolism: implication for optimization of breast cancer treatment

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Pharmacokinetics of tamoxifen after intravenous and oral dosing of tamoxifen-hydroxybutenyl-beta-cyclodextrin formulations

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

CYP2D6 worldwide genetic variation shows high frequency of altered activity variants and no continental structure

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Tamoxifen and its main metabolites serum and tissue concentrations in breast cancer women

1 reference

https://pubmed.ncbi.nlm.nih.gov/22661948

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identifiers

10.3389/FPHAR.2012.00092

1 reference

Europe PubMed Central

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3 February 2020

1 reference

Europe PubMed Central

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3 February 2020

1 reference

Europe PubMed Central

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3 February 2020

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