General Information of Drug Transporter (DTP) (ID: DT9C1TS)

DTP Name Organic anion transporting polypeptide 1B3 (SLCO1B3)
Gene Name SLCO1B3
UniProt ID
Q9NPD5 (SO1B3_HUMAN)
VARIDT ID
DTD0030
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Synonyms
LST-2; LST-3TM13; LST2; LST3; Liver-specific organic anion transporter 2; OATP-8; OATP1B3; OATP8; Organic anion transporter 8; Organic anion-transporting polypeptide 8; SLC21A8; SLCO1B3; Solute carrier family 21 member 8; Solute carrier organic anion transporter family member 1B3
DTP Family Organo Anion Transporter (OAT) Family ;
Tissue Specificity Highly expressed in liver, in particular atthe basolateral membrane of hepatocytes near the central vein. Notdetected in other tissues. Highly expressed in some cancer celllines derived from colon, pancreas, liver and gall bladder.
Sequence
MDQHQHLNKTAESASSEKKKTRRCNGFKMFLAALSFSYIAKALGGIIMKISITQIERRFD
ISSSLAGLIDGSFEIGNLLVIVFVSYFGSKLHRPKLIGIGCLLMGTGSILTSLPHFFMGY
YRYSKETHINPSENSTSSLSTCLINQTLSFNGTSPEIVEKDCVKESGSHMWIYVFMGNML
RGIGETPIVPLGISYIDDFAKEGHSSLYLGSLNAIGMIGPVIGFALGSLFAKMYVDIGYV
DLSTIRITPKDSRWVGAWWLGFLVSGLFSIISSIPFFFLPKNPNKPQKERKISLSLHVLK
TNDDRNQTANLTNQGKNVTKNVTGFFQSLKSILTNPLYVIFLLLTLLQVSSFIGSFTYVF
KYMEQQYGQSASHANFLLGIITIPTVATGMFLGGFIIKKFKLSLVGIAKFSFLTSMISFL
FQLLYFPLICESKSVAGLTLTYDGNNSVASHVDVPLSYCNSECNCDESQWEPVCGNNGIT
YLSPCLAGCKSSSGIKKHTVFYNCSCVEVTGLQNRNYSAHLGECPRDNTCTRKFFIYVAI
QVINSLFSATGGTTFILLTVKIVQPELKALAMGFQSMVIRTLGGILAPIYFGALIDKTCM
KWSTNSCGAQGACRIYNSVFFGRVYLGLSIALRFPALVLYIVFIFAMKKKFQGKDTKASD
NERKVMDEANLEFLNNGEHFVPSAGTDSKTCNLDMQDNAAAN
Function
This transporter involved in the clearance of bile acids and organic anions from the liver. Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP).
Endogenous Substrate(s) Cholate; Cholecystokinin; 17Beta-glucuronosyl estradiol; Cholecystokinin 8; Monoglucuronosyl bilirubin; Tauroursodeoxycholate
TCDB ID
2.A.60.1.12
Gene ID
28234
KEGG Pathway
Bile secretion (hsa04976 )
Reactome Pathway
Heme degradation (R-HSA-189483 )
Defective SLCO1B3 causes hyperbilirubinemia, Rotor type (HBLRR) (R-HSA-5619058 )
Transport of organic anions (R-HSA-879518 )
Atorvastatin ADME (R-HSA-9754706 )
Recycling of bile acids and salts (R-HSA-159418 )

Molecular Interaction Atlas (MIA) of This DTP

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTP
51 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acocantherin DM7JT24 Atrial fibrillation BC81.3 Approved [2]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [3]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [4]
Cefmetazole DM42W1B Bacterial infection 1A00-1C4Z Approved [5]
Cefoperazone DM53PV8 Bacterial infection 1A00-1C4Z Approved [5]
Ceftriaxone DMCEW64 Acute gonococcal cervicitis Approved [5]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [3]
Cilostazol DMZMSCT Intermittent claudication BD40.00 Approved [6]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [7]
Dasatinib DMJV2EK Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [7]
Dehydroepiandrosterone sulfate DM4Q80H N. A. N. A. Approved [8]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [9]
Digoxin DMQCTIH Arrhythmia BC9Z Approved [2]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [10]
Enalapril DMNFUZR Congestive heart failure BD10 Approved [11]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [12]
Estrone sulfate DMVBIZL Atrophic vaginitis GA30.2 Approved [13]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [13]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [14]
FLUORESCEIN DMQTFAO Ocular disease 1F00.1Z Approved [15]
Fluvastatin DM4MDJY Arteriosclerosis BD40 Approved [16]
Gadobenate Dimeglumine DM4VAOG Schizophrenia 6A20 Approved [17]
Gefitinib DM15F0X Colon adenocarcinoma Approved [7]
Glutathione DMAHMT9 Human immunodeficiency virus infection 1C62 Approved [18]
Hydroxyurea DMOQVU9 Chronic myelogenous leukaemia 2A20.0 Approved [19]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [7]
Indocyanine green DM2NQUY Gastrointestinal disease DE2Z Approved [20]
Liothyronine DM6IR3P Congenital hypothyroidism Approved [8]
Mesalazine DMOL5IU Diverticulitis Approved [21]
Methotrexate DM2TEOL Anterior urethra cancer Approved [8]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [22]
Nateglinide DMLK2QH Diabetic complication 5A2Y Approved [3]
Nilotinib DM7HXWT Chronic myelogenous leukaemia 2A20.0 Approved [7]
Olmesartan medoxomil DMWBHRY High blood pressure BA00 Approved [23]
Paclitaxel DMLB81S Breast carcinoma Approved [24]
Pitavastatin DMJH792 Hypercholesterolaemia 5C80.0 Approved [12]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [25]
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [26]
Rifampin DMA8J1G Tuberculosis 1B10-1B1Z Approved [27]
Romidepsin DMT5GNL Cutaneous T-cell lymphoma 2B01 Approved [28]
Rosuvastatin DMMIQ7G Arteriosclerosis BD40 Approved [29]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [7]
Sunitinib DMCBJSR Acute undifferentiated leukemia Approved [7]
Technetium (99MTC) mebrofenin DMUEWM3 N. A. N. A. Approved [30]
Telmisartan DMS3GX2 Hypertension BA00-BA04 Approved [31]
Testosterone DM7HUNW Hot flushes GA30 Approved [32]
Valsartan DMREUQ6 Chronic heart failure BD1Z Approved [33]
Vandetanib DMRICNP Solid tumour/cancer 2A00-2F9Z Approved [7]
Vemurafenib DM62UG5 Melanoma 2C30 Approved [7]
Warfarin DMJYCVW Atrial fibrillation BC81.3 Approved [4]
Primovist DM37FKA N. A. N. A. Phase 4 [34]
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⏷ Show the Full List of 51 Approved Drug(s)
7 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Atrasentan DMM74PK Diabetic nephropathy GB61.Z Phase 3 [35]
Benzylpenicillin DMS9503 Actinomycosis Phase 3 [36]
BQ-123 DM0MO8I Pulmonary arterial hypertension BB01.0 Phase 2 [2]
Danoprevir DM20MDU Hepatitis C virus infection 1E51.1 Phase 2 [3]
LE-SN38 DMW50NF Colorectal cancer 2B91.Z Phase 2 [10]
Sodium taurocholate DM3GO0J Type-2 diabetes 5A11 Phase 1/2 [8]
Taurocholic Acid DM2LZ8F Type-2 diabetes 5A11 Phase 1/2 [13]
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⏷ Show the Full List of 7 Clinical Trial Drug(s)
7 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
amanitin DM59IT4 Discovery agent N.A. Investigative [36]
bilirubin DMI0V4O Discovery agent N.A. Investigative [37]
bromsulphthalein DM9W2ZV N. A. N. A. Investigative [2]
CCK-8 DMN0J4W N. A. N. A. Investigative [38]
Fluo-3 DMLO9FU N. A. N. A. Investigative [13]
glycocholic acid DM0SXNM Discovery agent N.A. Investigative [2]
[3H]estradiol-17beta-glucuronide DM3KJ45 Discovery agent N.A. Investigative [39]
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⏷ Show the Full List of 7 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTP

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTP
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Acute myelocytic leukaemia 2B33.1 Bone marrow 4.93E-05 -5.25E-02 -3.14E-01
Adrenocortical carcinoma 2D11.Z Kidney 4.39E-01 -2.04E-02 -1.19E-01
Alopecia ED70 Skin from scalp 7.94E-01 -4.14E-02 -2.34E-01
Alzheimer's disease 8A20 Entorhinal cortex 9.69E-01 1.16E-03 3.56E-03
Ankylosing spondylitis FA92.0 Pheripheral blood 9.41E-01 -3.03E-02 -1.71E-01
Aortic stenosis BB70 Calcified aortic valve 5.19E-01 -4.89E-03 -2.25E-02
Apnea 7A40 Hyperplastic tonsil 2.71E-01 4.34E-02 2.21E-01
Arthropathy FA00-FA5Z Peripheral blood 7.51E-01 2.07E-02 1.29E-01
Asthma CA23 Nasal and bronchial airway 1.89E-10 2.54E+00 1.39E+00
Atopic dermatitis EA80 Skin 2.09E-03 1.23E-01 1.08E+00
Autism 6A02 Whole blood 1.91E-01 4.38E-02 2.73E-01
Autoimmune uveitis 9A96 Peripheral monocyte 3.07E-02 1.33E-01 8.39E-01
Autosomal dominant monocytopenia 4B04 Whole blood 2.73E-02 1.31E-01 1.22E+00
Bacterial infection of gingival 1C1H Gingival tissue 2.93E-03 -6.98E-02 -3.12E-01
Batten disease 5C56.1 Whole blood 6.72E-01 -1.20E-02 -1.10E-01
Behcet's disease 4A62 Peripheral blood 5.93E-01 1.43E-01 7.52E-01
Bipolar disorder 6A60-6A6Z Prefrontal cortex 2.21E-02 9.48E-02 6.45E-01
Bladder cancer 2C94 Bladder tissue 6.97E-08 9.09E-02 5.81E-01
Breast cancer 2C60-2C6Z Breast tissue 4.86E-01 -5.39E-02 -2.84E-01
Cardioembolic stroke 8B11.20 Whole blood 2.95E-01 4.49E-02 2.13E-01
Cervical cancer 2C77 Cervical tissue 6.36E-01 -3.47E-01 -2.65E-01
Childhood onset rheumatic disease FA20.Z Peripheral blood 5.36E-01 2.34E-02 1.67E-01
Chronic hepatitis C 1E51.1 Whole blood 3.27E-01 3.76E-02 2.29E-01
Chronic obstructive pulmonary disease CA22 Lung tissue 3.20E-01 2.15E-02 1.15E-01
Chronic obstructive pulmonary disease CA22 Small airway epithelium 1.40E-02 -4.58E-02 -1.12E-01
Chronic rhinosinusitis CA0A Sinus mucosa tissue 8.37E-02 6.07E-01 2.69E+00
Colon cancer 2B90 Colon tissue 1.63E-158 1.56E+00 3.75E+00
Coronary artery disease BA80-BA8Z Peripheral blood 4.71E-01 -3.34E-02 -1.22E-01
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 6.64E-01 -9.32E-03 -4.05E-02
Endometriosis GA10 Endometrium tissue 7.75E-01 3.79E-03 1.43E-02
Familial hypercholesterolemia 5C80.00 Peripheral blood 1.88E-01 6.89E-02 7.14E-01
Familial hypercholesterolemia 5C80.00 Whole blood 1.65E-01 -6.07E-02 -3.77E-01
Gastric cancer 2B72 Gastric tissue 8.76E-03 4.48E-01 1.50E+00
Glioblastopma 2A00.00 Nervous tissue 1.59E-10 1.01E-01 3.62E-01
Glioma 2A00.0Y-2A00.0Z White matter tissue 2.96E-02 -1.22E-01 -6.03E-01
Head and neck cancer 2D42 Head and neck tissue 1.86E-13 4.08E-01 7.55E-01
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 4.96E-01 -3.44E-02 -2.84E-01
Huntington's disease 8A01.10 Whole blood 4.28E-02 -6.30E-02 -5.39E-01
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 8.11E-02 8.89E-02 5.62E-01
Immunodeficiency 4A00-4A20 Peripheral blood 7.48E-01 5.71E-02 5.27E-01
Influenza 1.00E+30 Whole blood 6.10E-01 5.26E-02 8.59E-01
Interstitial cystitis GC00.3 Bladder tissue 5.99E-01 -4.97E-03 -8.00E-02
Intracranial aneurysm 8B01.0 Intracranial artery 1.18E-02 -1.16E-01 -5.16E-01
Irritable bowel syndrome DD91.0 Rectal colon tissue 4.25E-02 9.85E-02 2.50E-01
Ischemic stroke 8B11 Peripheral blood 2.24E-01 1.24E-02 7.67E-02
Juvenile idiopathic arthritis FA24 Peripheral blood 5.72E-01 1.95E-02 6.17E-02
Lateral sclerosis 8B60.4 Cervical spinal cord 4.11E-01 4.27E-02 2.48E-01
Lateral sclerosis 8B60.4 Skin 9.37E-01 1.31E-02 6.46E-02
Liver cancer 2C12.0 Liver tissue 1.48E-59 -3.95E+00 -5.81E+00
Liver failure DB99.7-DB99.8 Liver tissue 7.11E-04 -4.42E+00 -8.15E+00
Lung cancer 2C25 Lung tissue 3.46E-61 1.83E-01 7.90E-01
Lupus erythematosus 4A40 Whole blood 9.22E-01 -7.31E-02 -1.96E-01
Major depressive disorder 6A70-6A7Z Whole blood 1.00E+00 1.02E-02 5.01E-02
Major depressive disorder 6A70-6A7Z Hippocampus 3.85E-03 1.01E-01 7.72E-01
Melanoma 2C30 Skin 1.98E-01 -7.45E-02 -3.24E-01
Multiple myeloma 2A83.1 Bone marrow 2.19E-02 4.44E-02 4.09E-01
Multiple myeloma 2A83.1 Peripheral blood 6.12E-01 1.16E-01 7.74E-01
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 9.32E-01 -1.68E-02 -1.21E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 9.92E-01 -7.89E-03 -5.24E-02
Myelofibrosis 2A20.2 Whole blood 5.08E-04 1.95E-01 1.57E+00
Myocardial infarction BA41-BA50 Peripheral blood 2.17E-01 1.81E-01 3.61E-01
Myopathy 8C70.6 Muscle tissue 3.21E-01 5.75E-02 2.16E-01
Neonatal sepsis KA60 Whole blood 1.20E-02 -5.15E-02 -2.71E-01
Neuroectodermal tumour 2A00.11 Brain stem tissue 1.45E-02 9.14E-02 6.66E-01
Non-alcoholic fatty liver disease DB92 Liver tissue 6.32E-01 -6.16E-02 -8.28E-02
Obesity related type 2 diabetes 5A11 Omental adipose tissue 8.12E-01 2.69E-02 2.21E-01
Olive pollen allergy CA08.00 Peripheral blood 1.19E-01 -2.74E-02 -4.39E-01
Oral cancer 2B6E Oral tissue 7.27E-35 1.22E+00 7.24E+00
Osteoarthritis FA00-FA0Z Synovial tissue 1.49E-01 8.37E-03 9.66E-02
Osteoporosis FB83.1 Bone marrow 6.27E-02 1.74E-01 2.30E+00
Ovarian cancer 2C73 Ovarian tissue 4.48E-08 2.47E-01 1.40E+00
Pancreatic cancer 2C10 Pancreas 2.10E-05 -2.39E-02 -3.15E-02
Parkinson's disease 8A00.0 Substantia nigra tissue 8.56E-01 3.16E-02 2.99E-01
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 8.29E-01 -5.97E-03 -4.70E-02
Pituitary cancer 2D12 Pituitary tissue 7.96E-01 2.13E-03 4.75E-03
Pituitary gonadotrope tumour 2D12 Pituitary tissue 7.13E-01 4.25E-02 2.01E-01
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 2.10E-01 3.36E-02 3.86E-01
Polycythemia vera 2A20.4 Whole blood 6.00E-03 5.21E-02 4.46E-01
Pompe disease 5C51.3 Biceps muscle 1.92E-01 -5.10E-02 -1.12E+00
Preterm birth KA21.4Z Myometrium 7.67E-01 0.00E+00 0.00E+00
Prostate cancer 2C82 Prostate 2.08E-04 3.94E-02 1.17E-01
Psoriasis EA90 Skin 1.60E-03 -7.70E-02 -3.78E-01
Rectal cancer 2B92 Rectal colon tissue 3.97E-10 1.24E+00 3.81E+00
Renal cancer 2C90-2C91 Kidney 5.58E-04 1.35E-01 1.08E+00
Retinoblastoma 2D02.2 Uvea 8.32E-03 1.35E-01 1.39E+00
Rheumatoid arthritis FA20 Synovial tissue 7.74E-01 -2.06E-02 -1.41E-01
Rhinovirus infection CA42.1 Nasal epithelium tissue 9.78E-01 -2.44E-01 -3.05E-01
Schizophrenia 6A20 Prefrontal cortex 4.67E-01 7.28E-03 4.43E-02
Schizophrenia 6A20 Superior temporal cortex 4.47E-03 4.60E-02 6.32E-01
Scleroderma 4A42.Z Whole blood 5.46E-02 6.67E-02 4.39E-01
Seizure 8A60-8A6Z Whole blood 4.65E-01 -3.40E-02 -1.53E-01
Sensitive skin EK0Z Skin 8.21E-01 -8.15E-02 -5.34E-01
Sepsis with septic shock 1G41 Whole blood 2.84E-01 -4.40E-02 -1.85E-01
Shwachman-Diamond syndrome 3A70.0 Bone marrow 1.20E-01 2.94E-01 2.91E+00
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 7.21E-01 5.01E-03 5.22E-02
Simpson golabi behmel syndrome LD2C Adipose tissue 4.56E-01 3.96E-02 7.74E-01
Sjogren's syndrome 4A43.2 Salivary gland tissue 9.13E-01 2.35E-01 3.97E-01
Skin cancer 2C30-2C3Z Skin 2.61E-01 -1.13E-02 -5.09E-02
Thrombocythemia 3B63 Whole blood 4.64E-01 3.84E-02 2.91E-01
Thrombocytopenia 3B64 Whole blood 9.38E-01 -1.40E-01 -6.03E-01
Thyroid cancer 2D10 Thyroid 7.57E-04 7.55E-03 3.42E-02
Tibial muscular dystrophy 8C75 Muscle tissue 1.74E-03 -8.06E-02 -4.03E-01
Tuberous sclerosis complex LD2D.2 Perituberal tissue 3.66E-02 3.18E-01 4.81E+00
Type 2 diabetes 5A11 Liver tissue 5.85E-01 1.81E-01 6.68E-01
Ureter cancer 2C92 Urothelium 8.54E-01 2.15E-02 1.03E-01
Uterine cancer 2C78 Endometrium tissue 8.39E-02 -6.52E-02 -8.24E-02
Vitiligo ED63.0 Skin 5.52E-01 4.27E-02 2.79E-01
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⏷ Show the Full List of Expression Under 107 Diseases

Drug Affinity of This DTP Assessed by Cell Line

Approved Drug(s)
Drug Name Highest Status Cell Line Affinity REF
Atorvastatin Approved Human embryonic kidney cells (HEK293)-OATP1B3 Km = 0.73 microM [38]
Bosentan Approved Chinese hamster ovary (CHO) cells-OATP1B3 Km = 141.0 microM [4]
Cilostazol Approved Human embryonic kidney cells (HEK293)-OATP1B3 Km = 2.7 microM [6]
Fexofenadine Approved Human embryonic kidney cells (HEK293)-OATP1B3 Km = 108.0 microM [14]
Fluvastatin Approved Madin-Darby canine kidney cells (MDCKII)-OATP1B3 Km = 7.0 microM [40]
Liothyronine Approved Oocytes-OATP1B3 Km = 6.4 microM [8]
Mesalazine Approved Human embryonic kidney cells (HEK293)-OATP1B3 Km = 77.4 microM [21]
Methotrexate Approved Madin-Darby canine kidney (MDCK) cells-OATP1B3 Km = 39.4 microM [8]
Methotrexate Approved Oocytes-OATP1B3 Km = 24.7 microM [8]
Olmesartan medoxomil Approved Human embryonic kidney cells (HEK293)-OATP1B3 Km = 44.2 microM [23]
Olmesartan medoxomil Approved Oocytes-OATP1B3 Km = 71.8 microM [41]
PITAVASTATIN CALCIUM Approved Human embryonic kidney cells (HEK293)-OATP1B3 Km = 3.25 microM [25]
PITAVASTATIN CALCIUM Approved Oocytes-OATP1B3 Km = 3.8 microM [42]
Rifampin Approved Oocytes-OATP1B3 Km = 2.3 microM [27]
Rosuvastatin Approved Human cervical cancer cell line (Hela)-OATP1B3 Km = 9.8 microM [43]
Rosuvastatin Approved Human embryonic kidney cells (HEK293)-OATP1B3 Km = 14.2 microM [29]
Telmisartan Approved Human embryonic kidney cells (HEK293)-OATP1B3 Km = 0.81 microM [31]
Telmisartan Approved Human embryonic kidney cells (HEK293)-OATP1B3 Km = 3.4 microM [44]
Valsartan Approved Chinese hamster ovary (CHO) cells-OATP1B3 Km = 23.5 microM [45]
Valsartan Approved Human embryonic kidney cells (HEK293)-OATP1B3 Km = 18.2 microM [33]
⏷ Show the Full List of 20 Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Highest Status Cell Line Affinity REF
Sodium taurocholate Phase 1/2 Oocytes-OATP1B3 Km = 5.8 microM [8]
Investigative Drug(s)
Drug Name Highest Status Cell Line Affinity REF
amanitin Investigative Madin-Darby canine kidney cells (MDCKII)-OATP1B3 Km = 3.7 microM [36]
bilirubin Investigative Human embryonic kidney cells (HEK293)-OATP1B3 Km = 0.5 microM [46]
bilirubin Investigative Oocytes-OATP1B3 Km = 0.0391 microM [37]
bromsulphthalein Investigative Human embryonic kidney cells (HEK293)-OATP1B3 Km = 3.3 microM [46]
bromsulphthalein Investigative Oocytes-OATP1B3 Km = 0.4 microM [2]
CCK-8 Investigative Oocytes-OATP1B3 Km = 11.1 microM [47]
[3H]estradiol-17beta-glucuronide Investigative Chinese hamster ovary (CHO) cells-OATP1B3 Km = 15.8 microM [13]
[3H]estradiol-17beta-glucuronide Investigative Human embryonic kidney cells (HEK293)-OATP1B3 Km = 24.6 microM [25]
⏷ Show the Full List of 8 Investigative Drug(s)

The Drug Therapeutic Target (DTT) Role of This DTP

DTP DTT Name Liver organic anion transporter 2 (SLCO1B3) DTT Info
DTP DTT Type Literature-reported
1 Investigative Drug(s) Targeting This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
[3H]estradiol-17beta-glucuronide DM3KJ45 Discovery agent N.A. Investigative [1]
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References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1221).
2 Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33.
3 FDA Drug Development and Drug Interactions
4 Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil. Drug Metab Dispos. 2007 Aug;35(8):1400-7.
5 Screening of antibiotics that interact with organic anion-transporting polypeptides 1B1 and 1B3 using fluorescent probes. Biol Pharm Bull. 2011;34(3):389-95.
6 Organic Anion-Transporting Polypeptide and Efflux Transporter-Mediated Hepatic Uptake and Biliary Excretion of Cilostazol and Its Metabolites in Rats and Humans. J Pharm Sci. 2017 Sep;106(9):2515-2523.
7 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
8 LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers. Gastroenterology. 2001 Jun;120(7):1689-99.
9 Influence of non-steroidal anti-inflammatory drugs on organic anion transporting polypeptide (OATP) 1B1- and OATP1B3-mediated drug transport. Drug Metab Dispos. 2011 Jun;39(6):1047-53.
10 Rapid screening of antineoplastic candidates for the human organic anion transporter OATP1B3 substrates using fluorescent probes. Cancer Lett. 2008 Feb 18;260(1-2):163-9.
11 Vectorial transport of enalapril by Oatp1a1/Mrp2 and OATP1B1 and OATP1B3/MRP2 in rat and human livers. J Pharmacol Exp Ther. 2006 Jul;318(1):395-402.
12 Impact of OATP transporters on pharmacokinetics. Br J Pharmacol. 2009 Oct;158(3):693-705.
13 Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3. Eur J Pharmacol. 2008 Apr 14;584(1):57-65.
14 Contribution of OATP (organic anion-transporting polypeptide) family transporters to the hepatic uptake of fexofenadine in humans. Drug Metab Dispos. 2005 Oct;33(10):1477-81.
15 Development of a cell-based high-throughput assay to screen for inhibitors of organic anion transporting polypeptides 1B1 and 1B3. Curr Chem Genomics. 2010 Mar 1;4:1-8.
16 Substrate-dependent drug-drug interactions between gemfibrozil, fluvastatin and other organic anion-transporting peptide (OATP) substrates on OATP1B1, OATP2B1, and OATP1B3. Drug Metab Dispos. 2007 Aug;35(8):1308-14.
17 Liver Perfusion Modifies Gd-DTPA and Gd-BOPTA Hepatocyte Concentrations Through Transfer Clearances Across Sinusoidal Membranes. Eur J Drug Metab Pharmacokinet. 2017 Aug;42(4):657-667.
18 Regulation of Organic Anion Transporting Polypeptides (OATP) 1B1- and OATP1B3-Mediated Transport: An Updated Review in the Context of OATP-Mediated Drug-Drug Interactions. Int J Mol Sci. 2018 Mar 14;19(3). pii: E855.
19 Transcellular movement of hydroxyurea is mediated by specific solute carrier transporters. Exp Hematol. 2011 Apr;39(4):446-56.
20 Primovist, Eovist: what to expect? J Hepatol. 2012 Aug;57(2):421-9.
21 Role of organic anion-transporting polypeptides for cellular mesalazine (5-aminosalicylic acid) uptake. Drug Metab Dispos. 2011 Jun;39(6):1097-102.
22 Influence of SLCO1B1, 1B3, 2B1 and ABCC2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients. Eur J Clin Pharmacol. 2007 Dec;63(12):1161-9.
23 Multiple human isoforms of drug transporters contribute to the hepatic and renal transport of olmesartan, a selective antagonist of the angiotensin II AT1-receptor. Drug Metab Dispos. 2007 Dec;35(12):2166-76.
24 Identification of OATP1B3 as a high-affinity hepatocellular transporter of paclitaxel. Cancer Biol Ther. 2005 Aug;4(8):815-8.
25 Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther. 2004 Oct;311(1):139-46.
26 Relevance of conserved lysine and arginine residues in transmembrane helices for the transport activity of organic anion transporting polypeptide 1B3. Br J Pharmacol. 2010 Feb 1;159(3):698-708.
27 Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology. 2002 Jul;36(1):164-72.
28 Population pharmacokinetics of romidepsin in patients with cutaneous T-cell lymphoma and relapsed peripheral T-cell lymphoma. Clin Cancer Res. 2009 Feb 15;15(4):1496-503.
29 Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos. 2008 Oct;36(10):2014-23.
30 Transporters involved in the hepatic uptake of (99m)Tc-mebrofenin and indocyanine green. J Hepatol. 2011 Apr;54(4):738-45.
31 Predominant contribution of OATP1B3 to the hepatic uptake of telmisartan, an angiotensin II receptor antagonist, in humans. Drug Metab Dispos. 2006 Jul;34(7):1109-15.
32 Effect of SLCO1B3 haplotype on testosterone transport and clinical outcome in caucasian patients with androgen-independent prostatic cancer. Clin Cancer Res. 2008 Jun 1;14(11):3312-8.
33 Involvement of transporters in the hepatic uptake and biliary excretion of valsartan, a selective antagonist of the angiotensin II AT1-receptor, in humans. Drug Metab Dispos. 2006 Jul;34(7):1247-54.
34 Hepatic uptake of the magnetic resonance imaging contrast agent Gd-EOB-DTPA: role of human organic anion transporters. Drug Metab Dispos. 2010 Jul;38(7):1024-8.
35 Organic anion transporting polypeptide 1B1 activity classified by SLCO1B1 genotype influences atrasentan pharmacokinetics. Clin Pharmacol Ther. 2006 Mar;79(3):186-96.
36 Molecular characterization and inhibition of amanitin uptake into human hepatocytes. Toxicol Sci. 2006 May;91(1):140-9.
37 Role of organic anion-transporting polypeptides, OATP-A, OATP-C and OATP-8, in the human placenta-maternal liver tandem excretory pathway for foetal bilirubin. Biochem J. 2003 May 1;371(Pt 3):897-905.
38 Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63.
39 Interactions of green tea catechins with organic anion-transporting polypeptides. Drug Metab Dispos. 2011 May;39(5):920-6.
40 Human hepatobiliary transport of organic anions analyzed by quadruple-transfected cells. Mol Pharmacol. 2005 Oct;68(4):1031-8.
41 OATP1B1, OATP1B3, and mrp2 are involved in hepatobiliary transport of olmesartan, a novel angiotensin II blocker. Drug Metab Dispos. 2006 May;34(5):862-9.
42 Transporter-mediated influx and efflux mechanisms of pitavastatin, a new inhibitor of HMG-CoA reductase. J Pharm Pharmacol. 2005 Oct;57(10):1305-11.
43 Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology. 2006 May;130(6):1793-806.
44 Establishment of a set of double transfectants coexpressing organic anion transporting polypeptide 1B3 and hepatic efflux transporters for the characterization of the hepatobiliary transport of telmisartan acylglucuronide. Drug Metab Dispos. 2008 Apr;36(4):796-805.
45 Prediction of pharmacokinetic profile of valsartan in human based on in vitro uptake transport data. J Pharmacokinet Pharmacodyn. 2009 Dec;36(6):585-611.
46 Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J Biol Chem. 2001 Mar 30;276(13):9626-30.
47 Hepatic uptake of cholecystokinin octapeptide by organic anion-transporting polypeptides OATP4 and OATP8 of rat and human liver. Gastroenterology. 2001 Nov;121(5):1185-90.