Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism
Both atorvastatin and rifampicin are substrates of OATP1B1 (organic anion transporting polypeptide 1B1) encoded by SLCO1B1 gene. Rifampicin is a potent inhibitor of SLCO1B1 (IC50 1.5 umol/l) and SLCO1B1 521T>C functional genetic polymorphism alters the kinetics of atorvastatin in vivo. We hypothe...
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| Veröffentlicht in: | Clinica chimica acta 2009-07, Vol.405 (1), p.49-52 |
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| creator | He, Yi-Jing Zhang, Wei Chen, Yao Guo, Dong Tu, Jiang-Hua Xu, Lin-Yong Tan, Zhi-Rong Chen, Bi-Lian Li, Zhi Zhou, Gan Yu, Bang-Ning Kirchheiner, Julia Zhou, Hong-Hao |
| description | Both atorvastatin and rifampicin are substrates of OATP1B1 (organic anion transporting polypeptide 1B1) encoded by
SLCO1B1 gene. Rifampicin is a potent inhibitor of
SLCO1B1 (IC50 1.5 umol/l) and
SLCO1B1 521T>C functional genetic polymorphism alters the kinetics of atorvastatin
in vivo. We hypothesize that rifampicin might influence atorvastatin kinetics in a
SLCO1B1 polymorphism dependent manner.
Sixteen subjects with known
SLCO1B1 genotypes (6 c.521TT, 6 c.521TC and 4 c.521CC) were divided into 2 groups (atorvastatin–placebo group,
n
=
8; atorvastatin–rifampicin group,
n
=
8) randomly. In this 2-phase crossover study, atorvastatin (40 mg single-oral dose) pharmacokinetics after co-administration of placebo and rifampicin (600 mg single-oral dose) were measured for up to 48 h by liquid chromatography–mass spectrometry (LC–MS). In the third phase, rifampicin (450 mg single-oral dose) pharmacokinetics was measured additionally.
Rifampicin increased atorvastatin plasma concentration in accordance with
SLCO1B1 521T>C genotype while the increasing percentage of AUC
(0–48) among c.521TT, c.521TC and c.521CC individuals were 833
±
245%
vs 468
±
233%
vs 330
±
223% (
P
=
0.007). However,
SLCO1B1 521T>C exerted no impact on rifampicin pharmacokinetics (
P
>
0.05).
These results suggested that rifampicin elevated the plasma concentration of atorvastatin depending on
SLCO1B1 genotype and rifampicin pharmacokinetics were not altered by
SLCO1B1 genotype. |
| doi_str_mv | 10.1016/j.cca.2009.04.003 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_67318593</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0009898109001740</els_id><sourcerecordid>67318593</sourcerecordid><originalsourceid>FETCH-LOGICAL-c442t-60d89d404d79e0a5700cd52382e88aa577a7230d5041db0508af804ec47fec123</originalsourceid><addsrcrecordid>eNp9kFtrGzEQhUVISdwkP6AvRU952-3osl4thUJj0gsYDI3zLGRplsjsrraSHMi_j4INeQsMDHPmzIH5CPnCoGbAlt_2tbWm5gBdDbIGEGdkwVQrKiE7fk4WUDaV6hS7JJ9T2pdRwpJdkEvWiVaqji-I_ud7M87e-omaIWNM1OQQn03KJhdtHkwaDbVhsjjlWLQw0VL5CenOJJ9o6OnDerVhd4w2nG1_rOgchpcxxPnJp_GafOrNkPDm1K_I46_77epPtd78_rv6ua6slDxXS3CqcxKkazsE07QA1jVcKI5KmTK3puUCXAOSuR00oEyvQKKVbY-WcXFFbo-5cwz_D5iyHn2yOAxmwnBIetkKpppOFCM7Gm0MKUXs9Rz9aOKLZqDfqOq9LlT1G1UNUheq5ebrKfywG9G9X5wwFsP3owHLi88eo07WY0HmfESbtQv-g_hXGHiGvw</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>67318593</pqid></control><display><type>article</type><title>Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism</title><source>MEDLINE</source><source>Elsevier ScienceDirect Journals Complete</source><creator>He, Yi-Jing ; Zhang, Wei ; Chen, Yao ; Guo, Dong ; Tu, Jiang-Hua ; Xu, Lin-Yong ; Tan, Zhi-Rong ; Chen, Bi-Lian ; Li, Zhi ; Zhou, Gan ; Yu, Bang-Ning ; Kirchheiner, Julia ; Zhou, Hong-Hao</creator><creatorcontrib>He, Yi-Jing ; Zhang, Wei ; Chen, Yao ; Guo, Dong ; Tu, Jiang-Hua ; Xu, Lin-Yong ; Tan, Zhi-Rong ; Chen, Bi-Lian ; Li, Zhi ; Zhou, Gan ; Yu, Bang-Ning ; Kirchheiner, Julia ; Zhou, Hong-Hao</creatorcontrib><description>Both atorvastatin and rifampicin are substrates of OATP1B1 (organic anion transporting polypeptide 1B1) encoded by
SLCO1B1 gene. Rifampicin is a potent inhibitor of
SLCO1B1 (IC50 1.5 umol/l) and
SLCO1B1 521T>C functional genetic polymorphism alters the kinetics of atorvastatin
in vivo. We hypothesize that rifampicin might influence atorvastatin kinetics in a
SLCO1B1 polymorphism dependent manner.
Sixteen subjects with known
SLCO1B1 genotypes (6 c.521TT, 6 c.521TC and 4 c.521CC) were divided into 2 groups (atorvastatin–placebo group,
n
=
8; atorvastatin–rifampicin group,
n
=
8) randomly. In this 2-phase crossover study, atorvastatin (40 mg single-oral dose) pharmacokinetics after co-administration of placebo and rifampicin (600 mg single-oral dose) were measured for up to 48 h by liquid chromatography–mass spectrometry (LC–MS). In the third phase, rifampicin (450 mg single-oral dose) pharmacokinetics was measured additionally.
Rifampicin increased atorvastatin plasma concentration in accordance with
SLCO1B1 521T>C genotype while the increasing percentage of AUC
(0–48) among c.521TT, c.521TC and c.521CC individuals were 833
±
245%
vs 468
±
233%
vs 330
±
223% (
P
=
0.007). However,
SLCO1B1 521T>C exerted no impact on rifampicin pharmacokinetics (
P
>
0.05).
These results suggested that rifampicin elevated the plasma concentration of atorvastatin depending on
SLCO1B1 genotype and rifampicin pharmacokinetics were not altered by
SLCO1B1 genotype.</description><identifier>ISSN: 0009-8981</identifier><identifier>EISSN: 1873-3492</identifier><identifier>DOI: 10.1016/j.cca.2009.04.003</identifier><identifier>PMID: 19374892</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Atorvastatin Calcium ; Genotype ; Heptanoic Acids - blood ; Humans ; Kinetics ; Male ; Organic Anion Transporters - genetics ; Organic Anion Transporters - metabolism ; Polymorphism, Genetic - genetics ; Pyrroles - blood ; Rifampicin ; Rifampin - blood ; Rifampin - pharmacokinetics ; SLCO1B1 ; Solute Carrier Organic Anion Transporter Family Member 1b1 ; Thymidine - genetics ; Thymidine - metabolism ; Young Adult</subject><ispartof>Clinica chimica acta, 2009-07, Vol.405 (1), p.49-52</ispartof><rights>2009 Elsevier B.V.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c442t-60d89d404d79e0a5700cd52382e88aa577a7230d5041db0508af804ec47fec123</citedby><cites>FETCH-LOGICAL-c442t-60d89d404d79e0a5700cd52382e88aa577a7230d5041db0508af804ec47fec123</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.cca.2009.04.003$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19374892$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>He, Yi-Jing</creatorcontrib><creatorcontrib>Zhang, Wei</creatorcontrib><creatorcontrib>Chen, Yao</creatorcontrib><creatorcontrib>Guo, Dong</creatorcontrib><creatorcontrib>Tu, Jiang-Hua</creatorcontrib><creatorcontrib>Xu, Lin-Yong</creatorcontrib><creatorcontrib>Tan, Zhi-Rong</creatorcontrib><creatorcontrib>Chen, Bi-Lian</creatorcontrib><creatorcontrib>Li, Zhi</creatorcontrib><creatorcontrib>Zhou, Gan</creatorcontrib><creatorcontrib>Yu, Bang-Ning</creatorcontrib><creatorcontrib>Kirchheiner, Julia</creatorcontrib><creatorcontrib>Zhou, Hong-Hao</creatorcontrib><title>Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism</title><title>Clinica chimica acta</title><addtitle>Clin Chim Acta</addtitle><description>Both atorvastatin and rifampicin are substrates of OATP1B1 (organic anion transporting polypeptide 1B1) encoded by
SLCO1B1 gene. Rifampicin is a potent inhibitor of
SLCO1B1 (IC50 1.5 umol/l) and
SLCO1B1 521T>C functional genetic polymorphism alters the kinetics of atorvastatin
in vivo. We hypothesize that rifampicin might influence atorvastatin kinetics in a
SLCO1B1 polymorphism dependent manner.
Sixteen subjects with known
SLCO1B1 genotypes (6 c.521TT, 6 c.521TC and 4 c.521CC) were divided into 2 groups (atorvastatin–placebo group,
n
=
8; atorvastatin–rifampicin group,
n
=
8) randomly. In this 2-phase crossover study, atorvastatin (40 mg single-oral dose) pharmacokinetics after co-administration of placebo and rifampicin (600 mg single-oral dose) were measured for up to 48 h by liquid chromatography–mass spectrometry (LC–MS). In the third phase, rifampicin (450 mg single-oral dose) pharmacokinetics was measured additionally.
Rifampicin increased atorvastatin plasma concentration in accordance with
SLCO1B1 521T>C genotype while the increasing percentage of AUC
(0–48) among c.521TT, c.521TC and c.521CC individuals were 833
±
245%
vs 468
±
233%
vs 330
±
223% (
P
=
0.007). However,
SLCO1B1 521T>C exerted no impact on rifampicin pharmacokinetics (
P
>
0.05).
These results suggested that rifampicin elevated the plasma concentration of atorvastatin depending on
SLCO1B1 genotype and rifampicin pharmacokinetics were not altered by
SLCO1B1 genotype.</description><subject>Atorvastatin Calcium</subject><subject>Genotype</subject><subject>Heptanoic Acids - blood</subject><subject>Humans</subject><subject>Kinetics</subject><subject>Male</subject><subject>Organic Anion Transporters - genetics</subject><subject>Organic Anion Transporters - metabolism</subject><subject>Polymorphism, Genetic - genetics</subject><subject>Pyrroles - blood</subject><subject>Rifampicin</subject><subject>Rifampin - blood</subject><subject>Rifampin - pharmacokinetics</subject><subject>SLCO1B1</subject><subject>Solute Carrier Organic Anion Transporter Family Member 1b1</subject><subject>Thymidine - genetics</subject><subject>Thymidine - metabolism</subject><subject>Young Adult</subject><issn>0009-8981</issn><issn>1873-3492</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kFtrGzEQhUVISdwkP6AvRU952-3osl4thUJj0gsYDI3zLGRplsjsrraSHMi_j4INeQsMDHPmzIH5CPnCoGbAlt_2tbWm5gBdDbIGEGdkwVQrKiE7fk4WUDaV6hS7JJ9T2pdRwpJdkEvWiVaqji-I_ud7M87e-omaIWNM1OQQn03KJhdtHkwaDbVhsjjlWLQw0VL5CenOJJ9o6OnDerVhd4w2nG1_rOgchpcxxPnJp_GafOrNkPDm1K_I46_77epPtd78_rv6ua6slDxXS3CqcxKkazsE07QA1jVcKI5KmTK3puUCXAOSuR00oEyvQKKVbY-WcXFFbo-5cwz_D5iyHn2yOAxmwnBIetkKpppOFCM7Gm0MKUXs9Rz9aOKLZqDfqOq9LlT1G1UNUheq5ebrKfywG9G9X5wwFsP3owHLi88eo07WY0HmfESbtQv-g_hXGHiGvw</recordid><startdate>20090701</startdate><enddate>20090701</enddate><creator>He, Yi-Jing</creator><creator>Zhang, Wei</creator><creator>Chen, Yao</creator><creator>Guo, Dong</creator><creator>Tu, Jiang-Hua</creator><creator>Xu, Lin-Yong</creator><creator>Tan, Zhi-Rong</creator><creator>Chen, Bi-Lian</creator><creator>Li, Zhi</creator><creator>Zhou, Gan</creator><creator>Yu, Bang-Ning</creator><creator>Kirchheiner, Julia</creator><creator>Zhou, Hong-Hao</creator><general>Elsevier B.V</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20090701</creationdate><title>Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism</title><author>He, Yi-Jing ; Zhang, Wei ; Chen, Yao ; Guo, Dong ; Tu, Jiang-Hua ; Xu, Lin-Yong ; Tan, Zhi-Rong ; Chen, Bi-Lian ; Li, Zhi ; Zhou, Gan ; Yu, Bang-Ning ; Kirchheiner, Julia ; Zhou, Hong-Hao</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c442t-60d89d404d79e0a5700cd52382e88aa577a7230d5041db0508af804ec47fec123</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Atorvastatin Calcium</topic><topic>Genotype</topic><topic>Heptanoic Acids - blood</topic><topic>Humans</topic><topic>Kinetics</topic><topic>Male</topic><topic>Organic Anion Transporters - genetics</topic><topic>Organic Anion Transporters - metabolism</topic><topic>Polymorphism, Genetic - genetics</topic><topic>Pyrroles - blood</topic><topic>Rifampicin</topic><topic>Rifampin - blood</topic><topic>Rifampin - pharmacokinetics</topic><topic>SLCO1B1</topic><topic>Solute Carrier Organic Anion Transporter Family Member 1b1</topic><topic>Thymidine - genetics</topic><topic>Thymidine - metabolism</topic><topic>Young Adult</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>He, Yi-Jing</creatorcontrib><creatorcontrib>Zhang, Wei</creatorcontrib><creatorcontrib>Chen, Yao</creatorcontrib><creatorcontrib>Guo, Dong</creatorcontrib><creatorcontrib>Tu, Jiang-Hua</creatorcontrib><creatorcontrib>Xu, Lin-Yong</creatorcontrib><creatorcontrib>Tan, Zhi-Rong</creatorcontrib><creatorcontrib>Chen, Bi-Lian</creatorcontrib><creatorcontrib>Li, Zhi</creatorcontrib><creatorcontrib>Zhou, Gan</creatorcontrib><creatorcontrib>Yu, Bang-Ning</creatorcontrib><creatorcontrib>Kirchheiner, Julia</creatorcontrib><creatorcontrib>Zhou, Hong-Hao</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Clinica chimica acta</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>He, Yi-Jing</au><au>Zhang, Wei</au><au>Chen, Yao</au><au>Guo, Dong</au><au>Tu, Jiang-Hua</au><au>Xu, Lin-Yong</au><au>Tan, Zhi-Rong</au><au>Chen, Bi-Lian</au><au>Li, Zhi</au><au>Zhou, Gan</au><au>Yu, Bang-Ning</au><au>Kirchheiner, Julia</au><au>Zhou, Hong-Hao</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism</atitle><jtitle>Clinica chimica acta</jtitle><addtitle>Clin Chim Acta</addtitle><date>2009-07-01</date><risdate>2009</risdate><volume>405</volume><issue>1</issue><spage>49</spage><epage>52</epage><pages>49-52</pages><issn>0009-8981</issn><eissn>1873-3492</eissn><abstract>Both atorvastatin and rifampicin are substrates of OATP1B1 (organic anion transporting polypeptide 1B1) encoded by
SLCO1B1 gene. Rifampicin is a potent inhibitor of
SLCO1B1 (IC50 1.5 umol/l) and
SLCO1B1 521T>C functional genetic polymorphism alters the kinetics of atorvastatin
in vivo. We hypothesize that rifampicin might influence atorvastatin kinetics in a
SLCO1B1 polymorphism dependent manner.
Sixteen subjects with known
SLCO1B1 genotypes (6 c.521TT, 6 c.521TC and 4 c.521CC) were divided into 2 groups (atorvastatin–placebo group,
n
=
8; atorvastatin–rifampicin group,
n
=
8) randomly. In this 2-phase crossover study, atorvastatin (40 mg single-oral dose) pharmacokinetics after co-administration of placebo and rifampicin (600 mg single-oral dose) were measured for up to 48 h by liquid chromatography–mass spectrometry (LC–MS). In the third phase, rifampicin (450 mg single-oral dose) pharmacokinetics was measured additionally.
Rifampicin increased atorvastatin plasma concentration in accordance with
SLCO1B1 521T>C genotype while the increasing percentage of AUC
(0–48) among c.521TT, c.521TC and c.521CC individuals were 833
±
245%
vs 468
±
233%
vs 330
±
223% (
P
=
0.007). However,
SLCO1B1 521T>C exerted no impact on rifampicin pharmacokinetics (
P
>
0.05).
These results suggested that rifampicin elevated the plasma concentration of atorvastatin depending on
SLCO1B1 genotype and rifampicin pharmacokinetics were not altered by
SLCO1B1 genotype.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>19374892</pmid><doi>10.1016/j.cca.2009.04.003</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0009-8981 |
| ispartof | Clinica chimica acta, 2009-07, Vol.405 (1), p.49-52 |
| issn | 0009-8981 1873-3492 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_67318593 |
| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Atorvastatin Calcium Genotype Heptanoic Acids - blood Humans Kinetics Male Organic Anion Transporters - genetics Organic Anion Transporters - metabolism Polymorphism, Genetic - genetics Pyrroles - blood Rifampicin Rifampin - blood Rifampin - pharmacokinetics SLCO1B1 Solute Carrier Organic Anion Transporter Family Member 1b1 Thymidine - genetics Thymidine - metabolism Young Adult |
| title | Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism |
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