Organic anion transporting polypeptide 2B1 is a high-affinity transporter for atorvastatin and is expressed in the human heart

Grube, Markus; Köck, Kathleen; Oswald, Stefan; Draber, Katrin; Meissner, Konrad; Eckel, Lothar; Böhm, Michael; Felix, Stephan B.; Vogelgesang, Silke; Jedlitschky, Gabriele

doi:10.1016/j.clpt.2006.09.010

Cited by 196 publications

(163 citation statements)

References 41 publications

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“…Atorvastatin [164] 0.2 Atazanavir [165] 3.6 a Estriol [158] Benzylpenicillin [35] Atorvastatin [164] 0.7 Pregnenolone sulfate [158] Estrone [158] Bosentan [166] 202 Benzylpenicillin [36] 16 000 a Prostaglandin E2 [35] Pregnenolone sulfate [157,158] 3.5 a Fexofenadine [41] Cerivastatin [164] 66 a Taurocholate [41] 72 Testosterone [158] 15 a /21 a Fluvastatin [162,167] 0.7 Cimetidine [36] Glibenclamide [163] 6.3 Ciclosporin [154] 0.07 a Pitavastatin [161] 1.2 Darunavir [165] 26 a Pravastatin [37,41] 2250 Digoxin [164] Rosuvastatin [87,154] 2.4/6.4 Efavirenz [165] 9.6 a Tebipenem pivoxil [156] >1000 Gemfibrozil [154,162,164] 8 a Glibenclamide [164] Indinavir [168] 3.0 Indometacin [36,164] Lopinavir [165] 0.7 a Lovastatin [164] Memantine [164] Mifepristone [158] 2.2 a /4.7 a Nelfinavir [165] 0.9 a Pravastatin [36,37] 5 500 a /1 020 a Probenecid …”

Section: Oatp1a2 (Oatp-a)mentioning

confidence: 99%

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Intestinal transporters for endogenic and pharmaceutical organic anions: the challenges of deriving in-vitro kinetic parameters for the prediction of clinically relevant drug–drug interactions

Grandvuinet

Vestergaard

Rapin³

et al. 2012

Journal of Pharmacy and Pharmacology

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Objectives This review provides an overview of intestinal human transporters for organic anions and stresses the need for standardization of the various in‐vitro methods presently employed in drug–drug interaction (DDI) investigations. Key findings Current knowledge on the intestinal expression of the apical sodium‐dependent bile acid transporter (ASBT), the breast cancer resistance protein (BCRP), the monocarboxylate transporters (MCT) 1, MCT3‐5, the multidrug resistance associated proteins (MRP) 1–6, the organic anion transporting polypetides (OATP) 2B1, 1A2, 3A1 and 4A1, and the organic solute transporter α/β (OSTα/β) has been covered along with an overview of their substrates and inhibitors. Furthermore, the many challenges in predicting clinically relevant DDIs from in‐vitro studies have been discussed with focus on intestinal transporters and the various methods for deducting in‐vitro parameters for transporters (Km/Ki/IC50, efflux ratio). The applicability of using a cut‐off value (estimated based on the intestinal drug concentration divided by the Ki or IC50) has also been considered. Summary A re‐evaluation of the current approaches for the prediction of DDIs is necessary when considering the involvement of other transporters than P‐glycoprotein. Moreover, the interplay between various processes that a drug is subject to in‐vivo such as translocation by several transporters and dissolution should be considered.

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Section: Oatp1a2 (Oatp-a)mentioning

confidence: 99%

“…[178,179] Thus, the inhibition of the enterocytic influx via OSTa/b is probably not of concern with regards to DDIs. However, OSTa/b is also an intestinal basolateral absorptive transporter (along [165,168] 4.0/4.6 a Simvastatin [164] 85 a Tipranavir [165] 0.9 a OATP3A1_v1 (OATP-D)…”

Section: Oatp1a2 (Oatp-a)mentioning

confidence: 99%

Intestinal transporters for endogenic and pharmaceutical organic anions: the challenges of deriving in-vitro kinetic parameters for the prediction of clinically relevant drug–drug interactions

Grandvuinet

Vestergaard

Rapin³

et al. 2012

Journal of Pharmacy and Pharmacology

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“…A c c e p t e d M a n u s c r i p t 13 The quantitation of fexofenadine by LC-MS/MS was performed as previously described [25]. …”

Section: Quantitation Of Fexofenadine By Lc-ms/msmentioning

confidence: 99%

“…OATP1A2 mediates the intracellular uptake of drugs such as fexofenadine [10] as well as of endogenous compounds such as taurocholate [11]. OATP2B1 mediates the cellular uptake of drugs such as fluvastatin [12], atorvastatin [13] and of endogenous compounds such as estrone-3-sulfate [14].…”

Section: Introductionmentioning

confidence: 99%

Influence of the flavonoids apigenin, kaempferol, and quercetin on the function of organic anion transporting polypeptides 1A2 and 2B1

Mandery

Bujok

Schmidt

et al. 2010

Biochemical Pharmacology

124

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Influence of the flavonoids apigenin; kaempferol and quercetin on the function of organic anion transporting polypeptides 1A2 and 2B1, Biochemical Pharmacology (2010), doi:10.1016/j.bcp.2010 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.Page 1 of 37 A c c e p t e d M a n u s c r i p t 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 61 62 63 64 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 61 62 63 64 A c c e p t e d M a n u s c r i p t 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 61 62 63 64 A c c e p t e d M a n u s c r i p t 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 61 62 63 64 65 4 modification of OATP1A2 and OATP2B1 transport activity by apigenin, kaempferol, and quercetin may be a mechanism for food-drug or drug-drug interactions in humans.Page 5 of 37A c c e p t e d M a n u s c r i p t 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 61 62 63 64 A c c e p t e d M a n u s c r i p t Generation of a HEK293 cell line stably expressing OATP1A2The SLCO1A2 coding sequence (NM_134431. 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 61 62 63 64 65 10 subcloned into the retroviral vector pQCXIN (Takara Bio Europe/Clontech, SaintGermain-en-Laye, France). Human embryonic kidney cells (HEK293) were transfected with the plasmid pQCXIN-OATP1A2 using a retroviral gene transfer and expression kit (Takara Bio Europe/Clontech, Saint-Germain-en-Laye, France). After geneticin (G-418; 500 µg/ml) treatment, single colonies were selected and characterized for OATP1A2 mRNA and protein expression using ...

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“…A pravastatina, rosuvastatina, fluvastatina e atorvastatina também são substratos de alta afinidade dos transportadores de captação da família dos solutecarriers (SLC), tais como SLCO1B1 e SLCO2B1 (NEUVONEN; NIEMI; BACKMAN, 2006;GRUBE et al, 2006). Estes transportadores estão envolvidos na captação hepática e intestinal e facilitam a translocação do fármaco para dentro da célula.…”

Section: Estatinasunclassified

Efeitos de hipolipemiantes sobre a expressão de CYP3A4 e CYP3A5 in vitro e in vivo

Willrich¹

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Organic anion transporting polypeptide 2B1 is a high-affinity transporter for atorvastatin and is expressed in the human heart

Abstract: OATP2B1 is a high-affinity uptake transporter for atorvastatin and is expressed in the vascular endothelium of the human heart, suggesting its involvement in cardiac uptake of atorvastatin.

Cited by 196 publications

References 41 publications

Intestinal transporters for endogenic and pharmaceutical organic anions: the challenges of deriving in-vitro kinetic parameters for the prediction of clinically relevant drug–drug interactions

Intestinal transporters for endogenic and pharmaceutical organic anions: the challenges of deriving in-vitro kinetic parameters for the prediction of clinically relevant drug–drug interactions

Influence of the flavonoids apigenin, kaempferol, and quercetin on the function of organic anion transporting polypeptides 1A2 and 2B1

Efeitos de hipolipemiantes sobre a expressão de CYP3A4 e CYP3A5 in vitro e in vivo

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