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2020 0
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The use of aromatase inhibitors in boys with short stature: what to know before prescribing?
Linardi A, et al. Arch Endocrinol Metab 2017 - Review. PMID 28977209 Free article.
The use of aromatase inhibitors (AI) in boys with short stature has showed its capability to improve the predicted final height. ...Therefore, it is important to understand the pharmacokinetics of AIs, recognizing and avoiding possible drug interactions and offering a safer prescription profile of this class of aromatase inhibitors. ...
The use of aromatase inhibitors (AI) in boys with short stature has showed its capability to improve the predicted final heigh …
Comparison of pharmacokinetics of newly discovered aromatase inhibitors by a cassette microdosing approach in healthy Japanese subjects.
Kusuhara H, et al. Drug Metab Pharmacokinet 2017 - Clinical Trial. PMID 29137842
The aim of the present study is to investigate the pharmacokinetics of our newly developed aromatase inhibitors (cetrozole and TMD-322) in healthy subjects by a cassette microdose strategy. ...We report the first clinical investigation of our aromatase inhibitors by a cassette microdose strategy in healthy Japanese subjects. ...
The aim of the present study is to investigate the pharmacokinetics of our newly developed aromatase inhibitors (cetroz …
Anastrozole
Kelly CM and Buzdar AU. Expert Opin Drug Saf 2010 - Review. PMID 20923259
IMPORTANCE OF THE FIELD: Anastrozole is a third-generation aromatase inhibitor used in the adjuvant setting for the treatment of hormone receptor-positive breast cancer. ...AREAS COVERED IN THIS REVIEW: This review discusses the mechanism of action of anastrozole; pharmacokinetic and pharmacodynamic characteristics; results of randomized controlled trials of anastrozole compared to tamoxifen in the adjuvant treatment of postmenopausal women with hormone receptor-positive breast cancer and the safety profile of anastrozole compared to tamoxifen. ...
IMPORTANCE OF THE FIELD: Anastrozole is a third-generation aromatase inhibitor used in the adjuvant setting for the treatment of horm …
Investigation of the effect of active efflux at the blood-brain barrier on the distribution of nonsteroidal aromatase inhibitors in the central nervous system.
Miyajima M, et al. J Pharm Sci 2013. PMID 23712697
The brain distribution of nonsteroidal aromatase inhibitors was investigated in mice to understand their interactions with brain aromatase. ...IC50 (nM) of anastrozole and letrozole against human aromatase was 12.9 ± 0.7 and 3.59 ± 0.75, respectively. Taken together, these results suggest that active efflux mediated by P-gp at the blood-brain barrier limits the effect of anastrozole in the central nervous system, whereas vorozole and letrozole easily traverse the barrier....
The brain distribution of nonsteroidal aromatase inhibitors was investigated in mice to understand their interactions with bra …
Impact of the OATP1B1 c.521T>C single nucleotide polymorphism on the pharmacokinetics of exemestane in healthy post-menopausal female volunteers.
Gregory BJ, et al. J Clin Pharm Ther 2017. PMID 28868654 Free PMC article.
This retrospective pharmacogenetic study was conducted to assess the impact of the OATP1B1 c.521T>C single nucleotide polymorphism (SNP) on the pharmacokinetics of the steroidal aromatase inhibitor drug exemestane in healthy volunteers. ...WHAT IS NEW AND CONCLUSION: Our data suggest that the OAPTP1B1 c.521T>C SNP may influence exemestane pharmacokinetics in humans....
This retrospective pharmacogenetic study was conducted to assess the impact of the OATP1B1 c.521T>C single nucleotide polymorphism (SNP) …
Variable aromatase inhibitor plasma concentrations do not correlate with circulating estrogen concentrations in post-menopausal breast cancer patients.
Hertz DL, et al. Breast Cancer Res Treat 2017. PMID 28643023 Free PMC article.
PURPOSE: The aromatase inhibitors (AI) exemestane (EXE), letrozole (LET), and anastrozole suppress estrogen biosynthesis, and are effective treatments for estrogen receptor (ER)-positive breast cancer. ...
PURPOSE: The aromatase inhibitors (AI) exemestane (EXE), letrozole (LET), and anastrozole suppress estrogen biosynthesis, and …
Anastrozole: a review of its use in postmenopausal women with early-stage breast cancer
Sanford M and Plosker GL. Drugs 2008 - Review. PMID 18547136
Ongoing head-to-head trials against other third-generation aromatase inhibitors will provide data as to its relative efficacy against these agents. ...Like other aromatase inhibitors, its most important adverse effect was an increased risk of bone fractures, which for anastrozole was restricted to the treatment period. ...
Ongoing head-to-head trials against other third-generation aromatase inhibitors will provide data as to its relative efficacy …
Impact of UGT2B17 Gene Deletion on the Pharmacokinetics of 17-Hydroexemestane in Healthy Volunteers.
Chen SM, et al. J Clin Pharmacol 2016. PMID 26608382 Free PMC article.
Exemestane is an aromatase inhibitor drug used for the treatment of hormone-dependent breast cancer. 17-Hydroexemestane, the major and biologically active metabolite of exemestane in humans, is eliminated via glucuronidation by the polymorphic UGT2B17 phase II drug-metabolizing enzyme. ...Our data suggest that UGT2B17 gene deletion influences 17-hydroexemestane pharmacokinetics in humans....
Exemestane is an aromatase inhibitor drug used for the treatment of hormone-dependent breast cancer. 17-Hydroexemestane, the major an …
Pharmacokinetics and pharmacodynamics of anastrozole in pubertal boys with recent-onset gynecomastia.
Mauras N, et al. J Clin Endocrinol Metab 2009. PMID 19470631
CONTEXT: Use of aromatase inhibitors to suppress estrogen production is being actively investigated in a variety of experimental conditions in both females and males. Anastrozole (Arimidex) is a potent and selective reversible inhibitor of the aromatase enzyme in females. OBJECTIVE: Our objective was to characterize the pharmacokinetics (PK) and pharmacodynamics (PD) of anastrozole in adolescent males with gynecomastia of less than 1 yr duration. ...
CONTEXT: Use of aromatase inhibitors to suppress estrogen production is being actively investigated in a variety of experiment …
Effect of simvastatin on the pharmacokinetics of anastrozole.
Bao T, et al. Breast Cancer Res Treat 2012. PMID 22089963
We have prospectively tested the effects of simvastatin on the pharmacokinetics of anastrozole and on estrogen concentrations in postmenopausal women with hormone receptor-positive breast cancer who were receiving adjuvant anastrozole. ...Pharmacokinetic results suggest that simvastatin is not likely to compromise the activity of anastrozole....
We have prospectively tested the effects of simvastatin on the pharmacokinetics of anastrozole and on estrogen concentrations in post …
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