Pharmacokinetics and Pharmacodynamics of Anastrozole in Pubertal Boys with Recent-Onset Gynecomastia
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 wa...
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| Veröffentlicht in: | The journal of clinical endocrinology and metabolism 2009-08, Vol.94 (8), p.2975-2978 |
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| creator | Mauras, Nelly Bishop, Kim Merinbaum, Debbie Emeribe, Ugochi Agbo, Felix Lowe, Elizabeth |
| description | 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. The effect of anastrozole on breast size was also assessed as an exploratory aim.
Design: We conducted a PK/PD open-label study.
Setting: This clinical research center study was undertaken at pediatric academic centers.
Patients: Forty-two boys with gynecomastia (mean age 13 ± 1.8 yr; duration of gynecomastia 7.0 ± 2.5 months; body mass index 28.3 ± 5.9 kg/m2) were recruited.
Interventions: Anastrozole, 1 mg, was given daily for 6 months.
Main Outcomes: We assessed PK/PD of anastrozole after 14 d daily dosing and changes in breast size (exploratory aim) by manual tape measurements (area) and ultrasound (volume) after 6 months.
Results: Anastrozole was rapidly absorbed orally (time to reach maximum concentration, 1 h) with a slow apparent clearance of 1.54 liters/h and a terminal half-life of 46.8 h. Testosterone/estradiol ratios increased significantly with concomitant increase in LH/FSH concentrations indicating aromatase blockade. There was a reduction in breast area (∼63%) and breast volume (∼57%) in the study group as compared with baseline (P = 0.004). The drug was well tolerated.
Conclusions: Anastrozole is a potent aromatase inhibitor in adolescent males, with rapid absorption and slow elimination kinetics after oral dosing. Exploratory analysis of changes in breast size showed breast reduction in the cohort; this deserves further study.
Pharmacokinetics of oral anastrozole in adolescent males with gynecomastia show rapid absorption and slow elimination kinetics; an observed reduction in breast size deserves further study. |
| doi_str_mv | 10.1210/jc.2008-2527 |
| format | Article |
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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. The effect of anastrozole on breast size was also assessed as an exploratory aim.
Design: We conducted a PK/PD open-label study.
Setting: This clinical research center study was undertaken at pediatric academic centers.
Patients: Forty-two boys with gynecomastia (mean age 13 ± 1.8 yr; duration of gynecomastia 7.0 ± 2.5 months; body mass index 28.3 ± 5.9 kg/m2) were recruited.
Interventions: Anastrozole, 1 mg, was given daily for 6 months.
Main Outcomes: We assessed PK/PD of anastrozole after 14 d daily dosing and changes in breast size (exploratory aim) by manual tape measurements (area) and ultrasound (volume) after 6 months.
Results: Anastrozole was rapidly absorbed orally (time to reach maximum concentration, 1 h) with a slow apparent clearance of 1.54 liters/h and a terminal half-life of 46.8 h. Testosterone/estradiol ratios increased significantly with concomitant increase in LH/FSH concentrations indicating aromatase blockade. There was a reduction in breast area (∼63%) and breast volume (∼57%) in the study group as compared with baseline (P = 0.004). The drug was well tolerated.
Conclusions: Anastrozole is a potent aromatase inhibitor in adolescent males, with rapid absorption and slow elimination kinetics after oral dosing. Exploratory analysis of changes in breast size showed breast reduction in the cohort; this deserves further study.
Pharmacokinetics of oral anastrozole in adolescent males with gynecomastia show rapid absorption and slow elimination kinetics; an observed reduction in breast size deserves further study.</description><identifier>ISSN: 0021-972X</identifier><identifier>EISSN: 1945-7197</identifier><identifier>DOI: 10.1210/jc.2008-2527</identifier><identifier>PMID: 19470631</identifier><identifier>CODEN: JCEMAZ</identifier><language>eng</language><publisher>Bethesda, MD: Endocrine Society</publisher><subject>Adolescent ; Aromatase Inhibitors - pharmacokinetics ; Aromatase Inhibitors - therapeutic use ; Biological and medical sciences ; Breast - drug effects ; Breast - growth & development ; Child ; Endocrinopathies ; Feeding. Feeding behavior ; Fundamental and applied biological sciences. Psychology ; Gynecomastia - drug therapy ; Humans ; Male ; Medical sciences ; Nitriles - adverse effects ; Nitriles - pharmacokinetics ; Nitriles - therapeutic use ; Puberty - metabolism ; Triazoles - adverse effects ; Triazoles - pharmacokinetics ; Triazoles - therapeutic use ; Vertebrates: anatomy and physiology, studies on body, several organs or systems ; Vertebrates: endocrinology</subject><ispartof>The journal of clinical endocrinology and metabolism, 2009-08, Vol.94 (8), p.2975-2978</ispartof><rights>2009 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c401t-f5f9fbbf55b84fa7f6f0dd77d74872a4f554c89f2a9cc72a6323fc17a85694023</citedby><cites>FETCH-LOGICAL-c401t-f5f9fbbf55b84fa7f6f0dd77d74872a4f554c89f2a9cc72a6323fc17a85694023</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=21816341$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19470631$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Mauras, Nelly</creatorcontrib><creatorcontrib>Bishop, Kim</creatorcontrib><creatorcontrib>Merinbaum, Debbie</creatorcontrib><creatorcontrib>Emeribe, Ugochi</creatorcontrib><creatorcontrib>Agbo, Felix</creatorcontrib><creatorcontrib>Lowe, Elizabeth</creatorcontrib><title>Pharmacokinetics and Pharmacodynamics of Anastrozole in Pubertal Boys with Recent-Onset Gynecomastia</title><title>The journal of clinical endocrinology and metabolism</title><addtitle>J Clin Endocrinol Metab</addtitle><description>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. The effect of anastrozole on breast size was also assessed as an exploratory aim.
Design: We conducted a PK/PD open-label study.
Setting: This clinical research center study was undertaken at pediatric academic centers.
Patients: Forty-two boys with gynecomastia (mean age 13 ± 1.8 yr; duration of gynecomastia 7.0 ± 2.5 months; body mass index 28.3 ± 5.9 kg/m2) were recruited.
Interventions: Anastrozole, 1 mg, was given daily for 6 months.
Main Outcomes: We assessed PK/PD of anastrozole after 14 d daily dosing and changes in breast size (exploratory aim) by manual tape measurements (area) and ultrasound (volume) after 6 months.
Results: Anastrozole was rapidly absorbed orally (time to reach maximum concentration, 1 h) with a slow apparent clearance of 1.54 liters/h and a terminal half-life of 46.8 h. Testosterone/estradiol ratios increased significantly with concomitant increase in LH/FSH concentrations indicating aromatase blockade. There was a reduction in breast area (∼63%) and breast volume (∼57%) in the study group as compared with baseline (P = 0.004). The drug was well tolerated.
Conclusions: Anastrozole is a potent aromatase inhibitor in adolescent males, with rapid absorption and slow elimination kinetics after oral dosing. Exploratory analysis of changes in breast size showed breast reduction in the cohort; this deserves further study.
Pharmacokinetics of oral anastrozole in adolescent males with gynecomastia show rapid absorption and slow elimination kinetics; an observed reduction in breast size deserves further study.</description><subject>Adolescent</subject><subject>Aromatase Inhibitors - pharmacokinetics</subject><subject>Aromatase Inhibitors - therapeutic use</subject><subject>Biological and medical sciences</subject><subject>Breast - drug effects</subject><subject>Breast - growth & development</subject><subject>Child</subject><subject>Endocrinopathies</subject><subject>Feeding. Feeding behavior</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Gynecomastia - drug therapy</subject><subject>Humans</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Nitriles - adverse effects</subject><subject>Nitriles - pharmacokinetics</subject><subject>Nitriles - therapeutic use</subject><subject>Puberty - metabolism</subject><subject>Triazoles - adverse effects</subject><subject>Triazoles - pharmacokinetics</subject><subject>Triazoles - therapeutic use</subject><subject>Vertebrates: anatomy and physiology, studies on body, several organs or systems</subject><subject>Vertebrates: endocrinology</subject><issn>0021-972X</issn><issn>1945-7197</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNptkMFLwzAUh4Mobk5vniUXb3Ymadq0xzl0CsKGKHgrr2nCWtdkJB1S_3pTNvXi6cHvfe893ofQJSVTyii5beSUEZJFLGHiCI1pzpNI0FwcozEhjEa5YO8jdOZ9QwjlPIlP0ShAgqQxHaNqtQbXgrQftVFdLT0GU-GfsOoNtENoNZ4Z8J2zX3ajcG3walcq18EG39ne48-6W-MXJZXpoqXxqsOL3ihp2zBTwzk60bDx6uJQJ-jt4f51_hg9LxdP89lzJDmhXaQTneuy1ElSZlyD0KkmVSVEJXgmGPDQ4DLLNYNcyhCkMYu1pAKyJM05YfEE3ez3Sme9d0oXW1e34PqCkmKQVTSyGGQVg6yAX-3x7a5sVfUHH-wE4PoAgJew0Q6MrP0vx2hG05gPXLznlKmsdMHk1invi8bunAkP_3_-G7pjhK0</recordid><startdate>20090801</startdate><enddate>20090801</enddate><creator>Mauras, Nelly</creator><creator>Bishop, Kim</creator><creator>Merinbaum, Debbie</creator><creator>Emeribe, Ugochi</creator><creator>Agbo, Felix</creator><creator>Lowe, Elizabeth</creator><general>Endocrine Society</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>20090801</creationdate><title>Pharmacokinetics and Pharmacodynamics of Anastrozole in Pubertal Boys with Recent-Onset Gynecomastia</title><author>Mauras, Nelly ; Bishop, Kim ; Merinbaum, Debbie ; Emeribe, Ugochi ; Agbo, Felix ; Lowe, Elizabeth</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c401t-f5f9fbbf55b84fa7f6f0dd77d74872a4f554c89f2a9cc72a6323fc17a85694023</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Adolescent</topic><topic>Aromatase Inhibitors - pharmacokinetics</topic><topic>Aromatase Inhibitors - therapeutic use</topic><topic>Biological and medical sciences</topic><topic>Breast - drug effects</topic><topic>Breast - growth & development</topic><topic>Child</topic><topic>Endocrinopathies</topic><topic>Feeding. Feeding behavior</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Gynecomastia - drug therapy</topic><topic>Humans</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Nitriles - adverse effects</topic><topic>Nitriles - pharmacokinetics</topic><topic>Nitriles - therapeutic use</topic><topic>Puberty - metabolism</topic><topic>Triazoles - adverse effects</topic><topic>Triazoles - pharmacokinetics</topic><topic>Triazoles - therapeutic use</topic><topic>Vertebrates: anatomy and physiology, studies on body, several organs or systems</topic><topic>Vertebrates: endocrinology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Mauras, Nelly</creatorcontrib><creatorcontrib>Bishop, Kim</creatorcontrib><creatorcontrib>Merinbaum, Debbie</creatorcontrib><creatorcontrib>Emeribe, Ugochi</creatorcontrib><creatorcontrib>Agbo, Felix</creatorcontrib><creatorcontrib>Lowe, Elizabeth</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>The journal of clinical endocrinology and metabolism</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Mauras, Nelly</au><au>Bishop, Kim</au><au>Merinbaum, Debbie</au><au>Emeribe, Ugochi</au><au>Agbo, Felix</au><au>Lowe, Elizabeth</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pharmacokinetics and Pharmacodynamics of Anastrozole in Pubertal Boys with Recent-Onset Gynecomastia</atitle><jtitle>The journal of clinical endocrinology and metabolism</jtitle><addtitle>J Clin Endocrinol Metab</addtitle><date>2009-08-01</date><risdate>2009</risdate><volume>94</volume><issue>8</issue><spage>2975</spage><epage>2978</epage><pages>2975-2978</pages><issn>0021-972X</issn><eissn>1945-7197</eissn><coden>JCEMAZ</coden><abstract>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. The effect of anastrozole on breast size was also assessed as an exploratory aim.
Design: We conducted a PK/PD open-label study.
Setting: This clinical research center study was undertaken at pediatric academic centers.
Patients: Forty-two boys with gynecomastia (mean age 13 ± 1.8 yr; duration of gynecomastia 7.0 ± 2.5 months; body mass index 28.3 ± 5.9 kg/m2) were recruited.
Interventions: Anastrozole, 1 mg, was given daily for 6 months.
Main Outcomes: We assessed PK/PD of anastrozole after 14 d daily dosing and changes in breast size (exploratory aim) by manual tape measurements (area) and ultrasound (volume) after 6 months.
Results: Anastrozole was rapidly absorbed orally (time to reach maximum concentration, 1 h) with a slow apparent clearance of 1.54 liters/h and a terminal half-life of 46.8 h. Testosterone/estradiol ratios increased significantly with concomitant increase in LH/FSH concentrations indicating aromatase blockade. There was a reduction in breast area (∼63%) and breast volume (∼57%) in the study group as compared with baseline (P = 0.004). The drug was well tolerated.
Conclusions: Anastrozole is a potent aromatase inhibitor in adolescent males, with rapid absorption and slow elimination kinetics after oral dosing. Exploratory analysis of changes in breast size showed breast reduction in the cohort; this deserves further study.
Pharmacokinetics of oral anastrozole in adolescent males with gynecomastia show rapid absorption and slow elimination kinetics; an observed reduction in breast size deserves further study.</abstract><cop>Bethesda, MD</cop><pub>Endocrine Society</pub><pmid>19470631</pmid><doi>10.1210/jc.2008-2527</doi><tpages>4</tpages><oa>free_for_read</oa></addata></record> |
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| source | Oxford University Press Journals All Titles (1996-Current); MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Alma/SFX Local Collection |
| subjects | Adolescent Aromatase Inhibitors - pharmacokinetics Aromatase Inhibitors - therapeutic use Biological and medical sciences Breast - drug effects Breast - growth & development Child Endocrinopathies Feeding. Feeding behavior Fundamental and applied biological sciences. Psychology Gynecomastia - drug therapy Humans Male Medical sciences Nitriles - adverse effects Nitriles - pharmacokinetics Nitriles - therapeutic use Puberty - metabolism Triazoles - adverse effects Triazoles - pharmacokinetics Triazoles - therapeutic use Vertebrates: anatomy and physiology, studies on body, several organs or systems Vertebrates: endocrinology |
| title | Pharmacokinetics and Pharmacodynamics of Anastrozole in Pubertal Boys with Recent-Onset Gynecomastia |
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