General Information of Drug Transporter (DT)
DT ID	DTD0031 Transporter Info
Gene Name	SLCO2B1
Protein Name	Organic anion transporting polypeptide 2B1
Gene ID	11309
UniProt ID	O94956
Genetic Polymorphisms of DT (GPD)
Genetic Polymorphism	rs12422149
Site of GPD	chr11:75172532 (GRCh38.p12)
GPD Type	SNP
Allele(s) in dbSNP	G>A / G>T
Minor Allele Frequency	A=0.2099/1051 (Global)
Allele A	Click to Show/Hide the Full List of Affected Drugs:           5 Drugs in Total
Montelukast	Drug Info	Healthy Individuals	Irrelevant to the drug clearance in healthy individuals (compare with allele G)		[ 1]
Estrone Sulfate	N.A.	Diabetes Mellitus	Allele A is not associated with decreased transport of SLCO2B1 when assayed with estrone sulfate or rosuvastatin HEK293 cells expressing OATP2B1 variants as compared to allele G.		[ 2]
Rosuvastatin	N.A.	Diabetes Mellitus	Allele A is not associated with decreased transport of SLCO2B1 when assayed with estrone sulfate or rosuvastatin HEK293 cells expressing OATP2B1 variants as compared to allele G.		[ 2]
Montelukast	N.A.	Parasitemia	Allele A is not associated with clearance of montelukast in healthy individuals as compared to allele G.		[ 1]
Montelukast	N.A.	Asthma	Allele A is not associated with clearance of montelukast in healthy individuals as compared to allele G.		[ 1]
Genotype AG	Click to Show/Hide the Full List of Affected Drugs:           6 Drugs in Total
Montelukast	Drug Info	Asthma	Correlated with the decreased drug response in patients (compare with genotype GG)		[ 3]
Montelukast	N.A.	Parasitemia	Genotype AG is associated with decreased response to montelukast in people with Asthma as compared to genotype GG.		[ 3]
4-hydroxyatorvastatin	N.A.	Parasitemia	Genotype AG is associated with increased concentrations of 4-hydroxyatorvastatin and 4-hydroxyatorvastatin lactone in people with Coronary Disease as compared to genotype GG.		[ 4]
4-hydroxyatorvastatin Lactone	N.A.	Parasitemia	Genotype AG is associated with increased concentrations of 4-hydroxyatorvastatin and 4-hydroxyatorvastatin lactone in people with Coronary Disease as compared to genotype GG.		[ 4]
Montelukast	N.A.	Asthma	Genotype AG is associated with decreased response to montelukast in people with Asthma as compared to genotype GG.		[ 3]
Rosuvastatin	N.A.	Asthma	Patients with the rs12422149 AG genotype may have decreased LDL lowering effect as compared to patients with the GG genotype. Other genetic and clinical factors may also influence a patient's response to rosuvasatin.		[ 5]
Genotype GG	Click to Show/Hide the Full List of Affected Drugs:           4 Drugs in Total
Chloroquine	N.A.	Parasitemia	Genotype GG is associated with increased severity of Parasitemia when treated with chloroquine and primaquine in people with Malaria as compared to genotypes AA + AG.		[ 6]
Primaquine	N.A.	Parasitemia	Genotype GG is associated with increased severity of Parasitemia when treated with chloroquine and primaquine in people with Malaria as compared to genotypes AA + AG.		[ 6]
Montelukast	N.A.	Asthma	Patients with the GG genotype and Asthma treated with montelukast may have higher plasma concentration of montelukast and better response to montelukast compared to patients with the GA genotype. Other genetic and clinical factors may also influence a patient's response to montelukast.		[ 3]
Rosuvastatin	N.A.	Asthma	Patients with the rs12422149 GG genotype may have increased LDL lowering effect as compared to patients with the AA or AG genotype. Other genetic and clinical factors may also influence a patient's response to rosuvasatin.		[ 5]
Genotypes AA + AG	Click to Show/Hide the Full List of Affected Drugs:           3 Drugs in Total
Tamoxifen	N.A.	Parasitemia	Genotypes AA + AG is associated with increased concentrations of tamoxifen in women with Breast Neoplasms as compared to genotype GG.		[ 7]
Atorvastatin	N.A.	Parasitemia	Genotypes AA + AG are not associated with exposure to atorvastatin as compared to genotype GG.		[ 8]
Rosuvastatin	N.A.	Parasitemia	Genotypes AA + AG are associated with decreased response to rosuvastatin in healthy individuals as compared to genotype GG.		[ 5]
Genotype AA	Click to Show/Hide the Full List of Affected Drugs:           3 Drugs in Total
Simvastatin	N.A.	Parasitemia	Genotype AA is associated with increased clearance of simvastatin as compared to genotypes AG + GG.		[ 9]
Montelukast	N.A.	Asthma	No AA genotype carrier was found in the study. But patients with the AG genotype and Asthma treated with montelukast may have significantly reduced plasma concentration of montelukast and poorer response to montelukast compared to patients with the GG genotype. Other genetic and clinical factors may also influence a patient's response to montelukast.		[ 3]
Rosuvastatin	N.A.	Asthma	Patients with the rs12422149 AA genotype may have decreased LDL lowering effect as compared to patients with the GG genotype. Other genetic and clinical factors may also influence a patient's response to rosuvasatin.		[ 5]
Genetic Polymorphism	rs2306168
Site of GPD	chr11:75196537 (GRCh38.p12)
GPD Type	SNP
Allele(s) in dbSNP	C>T
Minor Allele Frequency	T=0.1803/903 (Global)
Allele T	Click to Show/Hide the Full List of Affected Drugs:           4 Drugs in Total
Fexofenadine	Drug Info	Healthy Individuals	Correlated with the decreased area under the plasma concentration-time curve (AUC) in healthy individuals (compare with genotype CC)		[ 10]
Estrone Sulfate	N.A.	Diabetes Mellitus	Allele T is associated with decreased transport of SLCO2B1 when assayed with estrone sulfate HEK293 cells expressing OATP2B1 variants as compared to allele C.		[ 2]
Fexofenadine	N.A.	Parasitemia	Allele T is associated with decreased area under the plasma concentration-time curve when treated with fexofenadine in healthy individuals as compared to genotype CC.		[ 10]
Rosuvastatin	N.A.	Parasitemia	Allele T is associated with decreased uptake of rosuvastatin in transfected HEK293T cells as compared to allele C.		[ 12]
Genotype TT	Click to Show/Hide the Full List of Affected Drugs:           5 Drugs in Total
Atenolol	N.A.	Diabetes Mellitus	Genotype TT is not associated with increased exposure to atenolol in healthy individuals as compared to genotype CC.		[ 12]
Glyburide	N.A.	Parasitemia	Genotype TT is not associated with concentrations of glibenclamide, rosuvastatin or sulfasalazine in healthy individuals as compared to genotype CC.		[ 13]
Rosuvastatin	N.A.	Parasitemia	Genotype TT is not associated with concentrations of glibenclamide, rosuvastatin or sulfasalazine in healthy individuals as compared to genotype CC.		[ 13]
Sulfasalazine	N.A.	Parasitemia	Genotype TT is not associated with concentrations of glibenclamide, rosuvastatin or sulfasalazine in healthy individuals as compared to genotype CC.		[ 13]
Fexofenadine	N.A.	Asthma	Patients with the TT genotype who are treated with fexofenadine may have decreased area under the plasma concentration-time curve as compared to patients with the CC genotype. Other genetic and clinical factors may also influence a patient's metabolism of fexofenadine.		[ 10]
Allele C	Click to Show/Hide the Full List of Affected Drugs:           2 Drugs in Total
Montelukast	N.A.	Parasitemia	Allele C is not associated with clearance of montelukast in healthy individuals as compared to allele T.		[ 1]
Montelukast	N.A.	Parasitemia	Allele C is not associated with response to montelukast in people with Asthma as compared to allele T.		[ 3]
Genotype CT	Click to Show/Hide the Full List of Affected Drugs:           2 Drugs in Total
Rosuvastatin	N.A.	Parasitemia	Genotype CT is not associated with decreased response to rosuvastatin in healthy individuals as compared to genotype CC.		[ 5]
Fexofenadine	N.A.	Asthma	Patients with the CT genotype who are treated with fexofenadine may have decreased area under the plasma concentration-time curve as compared to patients with the CC genotype. Other genetic and clinical factors may also influence a patient's metabolism of fexofenadine.		[ 10]
Genotype CC	Click to Show/Hide the Full List of Affected Drugs:           1 Drugs in Total
Fexofenadine	N.A.	Asthma	Patients with the CC genotype who are treated with fexofenadine may have increased area under the plasma concentration-time curve as compared to patients with the TT or CT genotype. Other genetic and clinical factors may also influence a patient's metabolism of fexofenadine.		[ 10]
Genetic Polymorphism	rs1621378
Site of GPD	chr11:75193317 (GRCh38.p12)
GPD Type	SNP
Allele(s) in dbSNP	C>A / C>T
Allele T	Click to Show/Hide the Full List of Affected Drugs:           2 Drugs in Total
Estrone Sulfate	N.A.	Diabetes Mellitus	Allele T is associated with decreased transport of SLCO2B1 when assayed with estrone sulfate or rosuvastatin HEK293 cells expressing OATP2B1 variants as compared to allele C.		[ 2]
Rosuvastatin	N.A.	Diabetes Mellitus	Allele T is associated with decreased transport of SLCO2B1 when assayed with estrone sulfate or rosuvastatin HEK293 cells expressing OATP2B1 variants as compared to allele C.		[ 2]
Genetic Polymorphism	rs1009122956
Site of GPD	chr11:75196639 (GRCh38.p12)
GPD Type	SNP
Allele(s) in dbSNP	G>C
Allele C	Click to Show/Hide the Full List of Affected Drugs:           2 Drugs in Total
Estrone Sulfate	N.A.	Diabetes Mellitus	Allele C is associated with decreased transport of SLCO2B1 when assayed with estrone sulfate or rosuvastatin HEK293 cells expressing OATP2B1 variants as compared to allele G.		[ 2]
Rosuvastatin	N.A.	Diabetes Mellitus	Allele C is associated with decreased transport of SLCO2B1 when assayed with estrone sulfate or rosuvastatin HEK293 cells expressing OATP2B1 variants as compared to allele G.		[ 2]
Genetic Polymorphism	rs199654337
Site of GPD	chr11:75172550 (GRCh38.p12)
GPD Type	SNP
Allele(s) in dbSNP	C>T
Allele T	Click to Show/Hide the Full List of Affected Drugs:           2 Drugs in Total
Estrone Sulfate	N.A.	Diabetes Mellitus	Allele T is associated with decreased transport of SLCO2B1 when assayed with estrone sulfate or rosuvastatin HEK293 cells expressing OATP2B1 variants as compared to allele C.		[ 2]
Rosuvastatin	N.A.	Diabetes Mellitus	Allele T is associated with decreased transport of SLCO2B1 when assayed with estrone sulfate or rosuvastatin HEK293 cells expressing OATP2B1 variants as compared to allele C.		[ 2]
Genetic Polymorphism	rs61555831
Site of GPD	chr11:75196676 (GRCh38.p12)
GPD Type	SNP
Allele(s) in dbSNP	C>A / C>T
Minor Allele Frequency	C=0.9240/1828 (Global)
Allele A	Click to Show/Hide the Full List of Affected Drugs:           2 Drugs in Total
Estrone Sulfate	N.A.	Diabetes Mellitus	Allele A is not associated with decreased transport of SLCO2B1 when assayed with estrone sulfate or rosuvastatin HEK293 cells expressing OATP2B1 variants as compared to allele C.		[ 2]
Rosuvastatin	N.A.	Diabetes Mellitus	Allele A is not associated with decreased transport of SLCO2B1 when assayed with estrone sulfate or rosuvastatin HEK293 cells expressing OATP2B1 variants as compared to allele C.		[ 2]
Genetic Polymorphism	rs142693902
Site of GPD	chr11:75165833 (GRCh38.p12)
GPD Type	SNP
Allele(s) in dbSNP	G>A
Minor Allele Frequency	G=1.0000/1979 (Global)
Allele A	Click to Show/Hide the Full List of Affected Drugs:           1 Drugs in Total
Rosuvastatin	N.A.	Parasitemia	Allele A is associated with decreased uptake of rosuvastatin in transfected HEK293T cells as compared to allele G.		[ 11]
Genetic Polymorphism	rs35199625
Site of GPD	chr11:75169325 (GRCh38.p12)
GPD Type	SNP
Allele(s) in dbSNP	G>A
Minor Allele Frequency	G=0.9740/1927 (Global)
Allele A	Click to Show/Hide the Full List of Affected Drugs:           2 Drugs in Total
Rosuvastatin	N.A.	Parasitemia	Allele A is associated with decreased uptake of rosuvastatin in transfected HEK293T cells as compared to allele G.		[ 11]
Montelukast	N.A.	Parasitemia	Allele A is not associated with clearance of montelukast in healthy individuals as compared to allele G.		[ 1]
Genetic Polymorphism	rs1077858
Site of GPD	chr11:75190556 (GRCh38.p12)
GPD Type	SNP
Allele(s) in dbSNP	G>A
Minor Allele Frequency	G=0.4300/850 (Global)
Genotypes AA + AG	Click to Show/Hide the Full List of Affected Drugs:           1 Drugs in Total
Abiraterone	N.A.	Parasitemia	Genotypes AA + AG is associated with increased concentrations of abiraterone in healthy individuals as compared to genotype GG.		[ 14]
Genetic Polymorphism	rs2712807
Site of GPD	chr11:75150836 (GRCh38.p12)
GPD Type	SNP
Allele(s) in dbSNP	G>A / G>C
Minor Allele Frequency	G=0.2360/467 (Global)
Allele A	Click to Show/Hide the Full List of Affected Drugs:           1 Drugs in Total
Montelukast	N.A.	Parasitemia	Allele A is not associated with clearance of montelukast in healthy individuals as compared to allele G.		[ 1]
Genetic Polymorphism	rs3781727
Site of GPD	chr11:75204976 (GRCh38.p12)
GPD Type	SNP
Allele(s) in dbSNP	T>C / T>G
Minor Allele Frequency	T=0.8980/1777 (Global)
Genotypes CC + CT	Click to Show/Hide the Full List of Affected Drugs:           1 Drugs in Total
Voriconazole	N.A.	Parasitemia	Genotypes CC + CT are associated with decreased exposure to voriconazole in healthy individuals as compared to genotype TT.		[ 15]
Genotype CC	Click to Show/Hide the Full List of Affected Drugs:           1 Drugs in Total
Voriconazole	N.A.	Asthma	Patients with the rs3781727 CC genotype may have decreased exposure to voriconazole as compared to patients with the TT genotype. This annotation only covers the pharmacokinetic relationship between rs3781727 and voriconazole and does not include evidence about clinical outcomes. Other genetic and clinical factors may also influence exposure to voriconazole.		[ 15]
Genotype CT	Click to Show/Hide the Full List of Affected Drugs:           1 Drugs in Total
Voriconazole	N.A.	Asthma	Patients with the rs3781727 CT genotype may have decreased exposure to voriconazole as compared to patients with the TT genotype. This annotation only covers the pharmacokinetic relationship between rs3781727 and voriconazole and does not include evidence about clinical outcomes. Other genetic and clinical factors may also influence exposure to voriconazole.		[ 15]
Genotype TT	Click to Show/Hide the Full List of Affected Drugs:           1 Drugs in Total
Voriconazole	N.A.	Asthma	Patients with the rs3781727 TT genotype may have increased exposure to voriconazole as compared to patients with the CC or CT genotypes. This annotation only covers the pharmacokinetic relationship between rs3781727 and voriconazole and does not include evidence about clinical outcomes. Other genetic and clinical factors may also influence exposure to voriconazole.		[ 15]
References
1	Effects of polymorphisms of the SLCO2B1 transporter gene on the pharmacokinetics of montelukast in humans. J Clin Pharmacol. 2013 Nov;53(11):1186-93.
2	In vitro characterization of SLCO2B1 genetic variants. J Pharm Sci. 2025 Jun;114(6):103772.
3	Absorption of montelukast is transporter mediated: a common variant of OATP2B1 is associated with reduced plasma concentrations and poor response. Pharmacogenet Genomics. 2009 Feb;19(2):129-38.
4	The atorvastatin metabolite pattern in muscle tissue and blood plasma is associated with statin muscle side effects in patients with coronary heart disease; An exploratory case-control study. Atheroscler Plus. 2024 Mar;55:31-38.
5	The Effect of Genetic Polymorphisms in SLCO2B1 on the Lipid-Lowering Efficacy of Rosuvastatin in Healthy Adults with Elevated Low-Density Lipoprotein. Basic Clin Pharmacol Toxicol. 2017 Sep;121(3):195-201.
6	SLCO1A2, SLCO1B1 and SLCO2B1 polymorphisms influences chloroquine and primaquine treatment in Plasmodium vivax malaria. Pharmacogenomics. 2017 Oct;18(15):1393-1400.
7	Impact of organic anion transporting polypeptide, P-glycoprotein, and breast cancer resistance protein transporters on observed tamoxifen and endoxifen concentration and adverse effects. Pharmacogenet Genomics. 2023 Jan 01;33(1):10-18.
8	Atorvastatin Metabolite Pattern in Skeletal Muscle and Blood from Patients with Coronary Heart Disease and Statin-Associated Muscle Symptoms. Clin Pharmacol Ther. 2023 Apr;113(4):887-895.
9	Identification of the effect of multiple polymorphisms on the pharmacokinetics of simvastatin and simvastatin acid using a population-modeling approach. Clin Pharmacol Ther. 2014 Jul;96(1):90-100.
10	The effects of the SLCO2B1 c.1457C>T polymorphism and apple juice on the pharmacokinetics of fexofenadine and midazolam in humans. Pharmacogenet Genomics. 2011 Feb;21(2):84-93.
11	Organic Anion Transporting Polypeptide 2B1 (OATP2B1) Genetic Variants:. Front Pharmacol. 2021;12:713567.
12	Apple juice greatly reduces systemic exposure to atenolol. Br J Clin Pharmacol. 2013 Jan;75(1):172-9.
13	Small-Dosing Clinical Study: Pharmacokinetic, Pharmacogenomic (SLCO2B1 and ABCG2), and Interaction (Atorvastatin and Grapefruit Juice) Profiles of 5 Probes for OATP2B1 and BCRP. J Pharm Sci. 2017 Sep;106(9):2688-2694.
14	Effect of food and polymorphisms in SLCO2B1, CYP3A4 and UGT1A4 on pharmacokinetics of abiraterone and its metabolites in Chinese volunteers. Br J Clin Pharmacol. 2024 Jan;90(1):247-263.
15	Oral absorption of voriconazole is affected by SLCO2B1 c.*396T>C genetic polymorphism in CYP2C19 poor metabolizers. Pharmacogenomics J. 2020 Dec;20(6):792-800.

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