General Information of Drug Therapeutic Target (DTT) (ID: TT3OT40)

DTT Name Multidrug resistance protein 1 (ABCB1)
Synonyms PGY1; P-glycoprotein 1; MDR1; CD243 antigen; CD243; ATP-binding cassette sub-family B member 1
Gene Name ABCB1
DTT Type
Successful target
[1]
BioChemical Class
ABC transporter
UniProt ID
MDR1_HUMAN
TTD ID
T25258
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 7.6.2.2
Sequence
MDLEGDRNGGAKKKNFFKLNNKSEKDKKEKKPTVSVFSMFRYSNWLDKLYMVVGTLAAII
HGAGLPLMMLVFGEMTDIFANAGNLEDLMSNITNRSDINDTGFFMNLEEDMTRYAYYYSG
IGAGVLVAAYIQVSFWCLAAGRQIHKIRKQFFHAIMRQEIGWFDVHDVGELNTRLTDDVS
KINEGIGDKIGMFFQSMATFFTGFIVGFTRGWKLTLVILAISPVLGLSAAVWAKILSSFT
DKELLAYAKAGAVAEEVLAAIRTVIAFGGQKKELERYNKNLEEAKRIGIKKAITANISIG
AAFLLIYASYALAFWYGTTLVLSGEYSIGQVLTVFFSVLIGAFSVGQASPSIEAFANARG
AAYEIFKIIDNKPSIDSYSKSGHKPDNIKGNLEFRNVHFSYPSRKEVKILKGLNLKVQSG
QTVALVGNSGCGKSTTVQLMQRLYDPTEGMVSVDGQDIRTINVRFLREIIGVVSQEPVLF
ATTIAENIRYGRENVTMDEIEKAVKEANAYDFIMKLPHKFDTLVGERGAQLSGGQKQRIA
IARALVRNPKILLLDEATSALDTESEAVVQVALDKARKGRTTIVIAHRLSTVRNADVIAG
FDDGVIVEKGNHDELMKEKGIYFKLVTMQTAGNEVELENAADESKSEIDALEMSSNDSRS
SLIRKRSTRRSVRGSQAQDRKLSTKEALDESIPPVSFWRIMKLNLTEWPYFVVGVFCAII
NGGLQPAFAIIFSKIIGVFTRIDDPETKRQNSNLFSLLFLALGIISFITFFLQGFTFGKA
GEILTKRLRYMVFRSMLRQDVSWFDDPKNTTGALTTRLANDAAQVKGAIGSRLAVITQNI
ANLGTGIIISFIYGWQLTLLLLAIVPIIAIAGVVEMKMLSGQALKDKKELEGSGKIATEA
IENFRTVVSLTQEQKFEHMYAQSLQVPYRNSLRKAHIFGITFSFTQAMMYFSYAGCFRFG
AYLVAHKLMSFEDVLLVFSAVVFGAMAVGQVSSFAPDYAKAKISAAHIIMIIEKTPLIDS
YSTEGLMPNTLEGNVTFGEVVFNYPTRPDIPVLQGLSLEVKKGQTLALVGSSGCGKSTVV
QLLERFYDPLAGKVLLDGKEIKRLNVQWLRAHLGIVSQEPILFDCSIAENIAYGDNSRVV
SQEEIVRAAKEANIHAFIESLPNKYSTKVGDKGTQLSGGQKQRIAIARALVRQPHILLLD
EATSALDTESEKVVQEALDKAREGRTCIVIAHRLSTIQNADLIVVFQNGRVKEHGTHQQL
LAQKGIYFSMVSVQAGTKRQ
Function Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
KEGG Pathway
ABC transporters (hsa02010 )
Bile secretion (hsa04976 )
MicroRNAs in cancer (hsa05206 )
Reactome Pathway
ABC-family proteins mediated transport (R-HSA-382556 )
BioCyc Pathway
MetaCyc:HS01500-MON

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
2 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
EDP-322 DMWTVM1 Bacterial infection 1A00-1C4Z Phase 1 [2]
W-198 DMJ2R69 Solid tumour/cancer 2A00-2F9Z Phase 1 [3]
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8 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
CBT-1 DM097UP Non-small-cell lung cancer 2C25.Y Discontinued in Phase 3 [4]
LY335979 DM2KITF Acute myeloid leukaemia 2A60 Discontinued in Phase 3 [5]
Biricodar DM65JCM Ovarian cancer 2C73 Discontinued in Phase 2 [6]
S-9788 DMER3I9 Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 2 [7]
Tariquidar DMJG7VP Adrenocortical carcinoma 2D11.Z Discontinued in Phase 2 [8]
Elacridar DMURVE8 Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1 [9]
ONT-093 DMB8T5U Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1 [10]
XR-9051 DMCK210 Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1 [11]
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⏷ Show the Full List of 8 Discontinued Drug(s)
8 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
4,3'',5''-trimethoxy-[1,1':2',1'']-terphenyl DMBN4G6 Discovery agent N.A. Investigative [12]
6-(3,5-dimethoxy-phenyl)-naphthalen-2-ol DMIXT2L Discovery agent N.A. Investigative [12]
TRISMETHOXYRESVERATROL DM6USPC Discovery agent N.A. Investigative [12]
XR-9456 DMTUFI1 Discovery agent N.A. Investigative [13]
XR-9504 DMIQP69 Discovery agent N.A. Investigative [13]
XR-9544 DM1OZPN Discovery agent N.A. Investigative [13]
XR-9577 DMIZV6T Discovery agent N.A. Investigative [13]
[1,1':2',1'']-terphenyl-4,3'',5''-triol DMVOY4D Discovery agent N.A. Investigative [12]
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⏷ Show the Full List of 8 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Lung cancer 2C82 Lung tissue 3.12E-33 -0.83 -1.04
Ovarian cancer 2C82 Ovarian tissue 1.53E-04 -0.69 -2.04
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The Drug Transporter (DTP) Role of This DTT

DTT DTP Name P-glycoprotein 1 (ABCB1) DTP Info
Gene Name ABCB1
339 Approved Drug(s) Transported by This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Abacavir DMMN36E Human immunodeficiency virus infection 1C62 Approved [14]
Acebutolol DM0TI4U Hypertension BA00-BA04 Approved [15]
Acrivastine DMTIGA0 Allergic rhinitis CA08.0 Approved [16]
Ajmaline DMDJW5K Atrial fibrillation BC81.3 Approved [17]
Albendazole DMYZ57N Echinococcus granulosus infectious disease Approved [18]
Aldosterone DM9S2JW Hypertension BA00-BA04 Approved [19]
Aliskiren DM1BV7W Hypertension BA00-BA04 Approved [20]
Ambrisentan DMD1QXW Pulmonary arterial hypertension BB01.0 Approved [21]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [22]
Amisulpride DMSJVAM Schizophrenia 6A20 Approved [23]
Amitriptyline DMK7F9S Depression 6A70-6A7Z Approved [24]
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [15]
Amphotericin B DMTAJQE Acne vulgaris ED80 Approved [25]
Amprenavir DMLMXE0 Human immunodeficiency virus infection 1C62 Approved [22]
Apixaban DM89JLN Thrombosis DB61-GB90 Approved [26]
Apremilast DMTWS9E Psoriasis vulgaris EA90 Approved [27]
Aprepitant DM053KT Depression 6A70-6A7Z Approved [28]
ARRY-162 DM1P6FR Melanoma 2C30 Approved [29]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [30]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [24]
Atenolol DMNKG1Z Angina pectoris BA40 Approved [31]
Atomoxetine DM5L6HI Attention deficit hyperactivity disorder 6A05.Z Approved [28]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [27]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [32]
Azathioprine DMMZSXQ Lupus nephritis 4A40.0Y Approved [24]
Baloxavir marboxil DM1UV7F Influenza virus infection 1E30-1E32 Approved [33]
Baricitinib DM4ONW5 Rheumatoid arthritis FA20 Approved [34]
Beclomethasone DMZPHIK Allergic rhinitis CA08.0 Approved [35]
Bepridil DM0RKS4 Chronic/stable angina BA40.1 Approved [22]
Beta-acetyldigoxin DMI6GKT Cardiovascular disease BA00-BE2Z Approved [36]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [25]
Betamethasone DMAHJEF Acute adrenal insufficiency Approved [37]
BETRIXABAN DM2C4RF Venous thromboembolism BD72 Approved [38]
BIBW 2992 DMTKD7Q Non-small-cell lung cancer 2C25.Y Approved [39]
Bicalutamide DMZMSPF Prostate cancer 2C82.0 Approved [40]
BOCEPREVIR DMBSHMF Hepatitis C virus infection 1E51.1 Approved [41]
Bortezomib DMNO38U Leukemia Approved [42]
Bosutinib DMTI8YE Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [43]
Brilinta DMBR01X Acute coronary syndrome BA41 Approved [44]
Bromocriptine DMVE3TK Acromegaly 5A60.0 Approved [28]
Bupropion DM5PCS7 Depression 6A70-6A7Z Approved [45]
Cabergoline DMQ4HIN Hyperprolactinaemia 5A60.1 Approved [46]
Canagliflozin DMFRM1I Non-insulin dependent diabetes 5A11 Approved [47]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [44]
Carfilzomib DM48K0X Multiple myeloma 2A83 Approved [48]
Carvedilol DMHTEAO Chronic heart failure BD1Z Approved [27]
Cefoperazone DM53PV8 Bacterial infection 1A00-1C4Z Approved [22]
Cefotetan DM07TX3 Bacteremia 1A73 Approved [15]
Ceftriaxone DMCEW64 Acute gonococcal cervicitis Approved [22]
Celiprolol hcl DMD5LBX Hypertension BA00-BA04 Approved [49]
Cepharanthine DM9Y5JB N. A. N. A. Approved [50]
Ceritinib DMB920Z Non-small-cell lung cancer 2C25.Y Approved [51]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [52]
Cetirizine DMOMP9U Allergic rhinitis CA08.0 Approved [53]
Chlorambucil DMRKE63 Chronic lymphocytic leukaemia 2A82.0 Approved [22]
Chloramphenicol DMFXEWT Bacterial infection 1A00-1C4Z Approved [54]
Chloroquine DMSI5CB Malaria 1F40-1F45 Approved [28]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [22]
Ciclesonide DM2NA4K Allergic rhinitis CA08.0 Approved [35]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [55]
Cimetidine DMH61ZB Acid-reflux disorder DA22 Approved [22]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [22]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [56]
Clarithromycin DM4M1SG Acute maxillary sinusitis Approved [22]
Clobazam - Lundbeck DMW1OQ0 Anxiety disorder 6B00-6B0Z Approved [27]
Clofazimine DMEBOFW Crohn disease DD70 Approved [57]
Clomifene DMKI7RB Female infertility GA31.Z Approved [58]
Clomiphene Citrate DMS51VC Female infertility GA31.Z Approved [58]
Clomipramine DMINRKW Depression 6A70-6A7Z Approved [28]
Clonidine DM6RZ9Q Attention deficit hyperactivity disorder 6A05.Z Approved [24]
Clopidogrel DMOL54H Acute coronary syndrome BA41 Approved [59]
Clozapine DMFC71L Schizophrenia 6A20 Approved [23]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [60]
cortisone DMU5QZX Atopic dermatitis EA80 Approved [37]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [61]
Cytarabine DMZD5QR Acute lymphoblastic leukaemia 2A85 Approved [22]
Dabigatran DMDI6R4 Stroke 8B20 Approved [62]
Dabrafenib DMX6OE3 Melanoma 2C30 Approved [63]
Daclatasvir DMSFK9V Hepatitis C virus infection 1E51.1 Approved [62]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [64]
Darunavir DMN3GCH Human immunodeficiency virus infection 1C62 Approved [65]
Dasatinib DMJV2EK Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [66]
Daunorubicin DMQUSBT Acute monocytic leukemia Approved [22]
Debrisoquin DMC50ME Hypertension BA00-BA04 Approved [67]
Deflazacort DMV0RNS Duchenne dystrophy 8C70 Approved [44]
Delavirdine DM3NF5G Human immunodeficiency virus infection 1C62 Approved [14]
Desipramine DMT2FDC Attention deficit hyperactivity disorder 6A05.Z Approved [68]
Desloratadine DM56YN7 Allergic rhinitis CA08.0 Approved [69]
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [70]
Dexlansoprazole DM1DBV5 Erosive esophagitis DA25.0 Approved [68]
Diazepam DM08E9O Alcohol withdrawal Approved [71]
Dicloxacillin DM8EU0Z Bacterial infection 1A00-1C4Z Approved [72]
Diethylstilbestrol DMN3UXQ Gonorrheal vaginitis GA02 Approved [58]
Digitoxin DMWVIGP Arrhythmia BC9Z Approved [73]
Digoxin DMQCTIH Arrhythmia BC9Z Approved [74]
Dihydroergocristine DM5SQ1G Alcohol dependence 6C40.2 Approved [75]
Diltiazem DMAI7ZV Angina pectoris BA40 Approved [22]
Dipyridamole DMXY30O Atrial fibrillation BC81.3 Approved [28]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [76]
Dolutegravir DMCZGRE Human immunodeficiency virus infection 1C62 Approved [27]
Domperidone DMBDPY0 Gastrointestinal disease DE2Z Approved [23]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [77]
Doxycycline DM7ICNU Acne vulgaris ED80 Approved [22]
DU-176b DMCIJBH Atrial fibrillation BC81.3 Approved [78]
Efavirenz DMC0GSJ Human immunodeficiency virus infection 1C62 Approved [15]
Eletriptan DMW649X Migraine 8A80 Approved [28]
Eliglustat tartrate DMSRZAO Metabolic disorder 5C50-5D2Z Approved [44]
Emetine DMCT2YF Hepatitis virus infection 1E50-1E51 Approved [64]
Empagliflozin DMRF9YK Type-1 diabetes 5A10 Approved [44]
Epinastine DMX0K3Q Allergic conjunctivitis 9A60.02 Approved [79]
Epirubicin DMPDW6T Solid tumour/cancer 2A00-2F9Z Approved [22]
Ergotamine DMKR3C5 Cluster headache 8A81.0 Approved [28]
Erlotinib DMCMBHA Adrenal gland neoplasm Approved [80]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [81]
Eslicarbazepine acetate DMREUZV N. A. N. A. Approved [82]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [58]
Estriol DMOEM2I Hormone deficiency 5A61.1 Approved [83]
Estrone DM5T6US Acne vulgaris ED80 Approved [83]
Estrone sulfate DMVBIZL Atrophic vaginitis GA30.2 Approved [52]
Ethinyl Estradiol DMODJ40 Acne vulgaris ED80 Approved [83]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [84]
Everolimus DM8X2EH Advanced cancer 2A00-2F9Z Approved [85]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [86]
Famciclovir DMJHLSD Meniere disease AB31.0 Approved [16]
Felodipine DMOSW35 Hypertension BA00-BA04 Approved [87]
Fentanyl DM8WAHT Analgesia MB40.8 Approved [22]
Fesoterodine fumarate DM13495 Overactive bladder GC50.0 Approved [88]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [89]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [22]
Fluoxetine DM3PD2C Bipolar depression Approved [90]
Flupentixol DM0DJ9O Schizophrenia 6A20 Approved [23]
Fluphenazine DMIT8LX Psychotic disorder 6A20-6A25 Approved [23]
Fluticasone propionate DMRWLB2 Allergic asthma CA23.0 Approved [35]
Fluvastatin DM4MDJY Arteriosclerosis BD40 Approved [68]
Fluvoxamine DMQTJSX Depression 6A70-6A7Z Approved [23]
Folic Acid DMEMBJC Colorectal carcinoma Approved [91]
Fosamprenavir DM4W9B3 Human immunodeficiency virus infection 1C62 Approved [27]
Gatifloxacin DMSL679 Acute gonococcal cervicitis Approved [92]
Gefitinib DM15F0X Colon adenocarcinoma Approved [93]
Gemcitabine DMSE3I7 Anterior urethra cancer Approved [94]
Gepirone DMGX5Q0 Major depressive disorder 6A70.3 Approved [15]
Gilteritinib DMTI0ZO Acute myeloid leukaemia 2A60 Approved [44]
Glecaprevir DM31YVO N. A. N. A. Approved [27]
Glutathione DMAHMT9 Human immunodeficiency virus infection 1C62 Approved [95]
Gramicidin D DMPT74U Bacterial infection 1A00-1C4Z Approved [22]
Grepafloxacin DMGLX0T Chronic bronchitis CA20.1 Approved [22]
Guanabenz DM5QWEL High blood pressure BA00 Approved [68]
Guggulsterone DMP7LK1 Osteoarthritis FA00-FA05 Approved [96]
Haloperidol DM96SE0 Delirium Approved [23]
Hydrocortisone DMGEMB7 Acne vulgaris ED80 Approved [35]
Hydroxyurea DMOQVU9 Chronic myelogenous leukaemia 2A20.0 Approved [22]
Ibrutinib DMHZCPO Mantle cell lymphoma 2A85.5 Approved [97]
Idarubicin DMM0XGL Acute myelogenous leukaemia 2A41 Approved [98]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [99]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [24]
Indacaterol DMQJHR7 Chronic obstructive pulmonary disease CA22 Approved [44]
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [100]
Indomethacin DMSC4A7 Bursitis Approved [101]
Ingenol mebutate DMK1CZJ Actinic keratosis EK90.0 Approved [102]
Intedanib DMSTA36 Colorectal cancer 2B91.Z Approved [103]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [104]
Itraconazole DMCR1MV Aspergillosis 1F20 Approved [22]
Ivacaftor DMZC1HS Cystic fibrosis CA25 Approved [105]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [106]
Ivosidenib DM8S6T7 Acute myeloid leukaemia 2A60 Approved [107]
Ixabepilone DM2OZ3G Breast cancer 2C60-2C65 Approved [108]
Ketoconazole DMPZI3Q Blastomycosis 1F22 Approved [22]
L-Tryptophan DMIBH7M Depression 6A70-6A7Z Approved [109]
Labetalol DMK8U72 Hypertension BA00-BA04 Approved [15]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [110]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [27]
Lenalidomide DM6Q7U4 Adult T-cell leukemia/lymphoma Approved [111]
Lenvatinib DMB1IU4 Thyroid cancer 2D10 Approved [112]
Levetiracetam DMTGDN8 Epilepsy 8A60-8A68 Approved [113]
Levodopa DMN3E57 Parkinson disease 8A00.0 Approved [15]
Levofloxacin DMS60RB Acute maxillary sinusitis Approved [22]
Levomepromazine DMIKFEL Bipolar disorder 6A60 Approved [23]
Levomilnacipran DMV26S8 Fibromyalgia MG30.01 Approved [114]
Lidocaine DML4ZOT Anaesthesia 9A78.6 Approved [22]
Linagliptin DMWFJTR Non-insulin dependent diabetes 5A11 Approved [27]
Loperamide DMOJZQ9 Diarrhea ME05.1 Approved [115]
Lopinavir DMITQS0 Human immunodeficiency virus infection 1C62 Approved [116]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [69]
Losartan DM72JXH Diabetic kidney disease GB61.Z Approved [117]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [22]
Lovastatin acid DMGCQ4E N. A. N. A. Approved [15]
Maraviroc DMTL94F Human immunodeficiency virus infection 1C62 Approved [27]
Mefloquine DMWT905 Malaria 1F40-1F45 Approved [118]
Melphalan DMOLNHF Hematologic disease 3C0Z Approved [119]
Meperidine DMX4GND Pain MG30-MG3Z Approved [120]
Mequitazine DMAFBCY Allergic rhinitis CA08.0 Approved [16]
Methadone DMTW6IU Advanced cancer 2A00-2F9Z Approved [121]
Methotrexate DM2TEOL Anterior urethra cancer Approved [22]
Methylprednisolone DM4BDON Acute adrenal insufficiency Approved [122]
Methysergide DM1EF73 Migraine 8A80 Approved [16]
Midazolam DMXOELT Agitation 6A70.3 Approved [68]
Midostaurin DMI6E0R Acute myeloid leukaemia 2A60 Approved [15]
Mitomycin DMH0ZJE Breast cancer 2C60-2C65 Approved [123]
Mitoxantrone DMM39BF Acute myelogenous leukaemia 2A41 Approved [22]
Morphine DMRMS0L Advanced cancer 2A00-2F9Z Approved [124]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [125]
Nadolol DMW6GVL Angina pectoris BA40 Approved [27]
Nalbuphine DMOSQGU Pain MG30-MG3Z Approved [16]
Naloxegol DML0B41 Opioid-induced constipation DB32.1 Approved [27]
Neostigmine DM6T2J3 Myasthenia gravis 8C6Y Approved [28]
Nevirapine DM6HX9B Human immunodeficiency virus infection 1C62 Approved [15]
Nicardipine DMCDYW7 High blood pressure BA00 Approved [70]
Nifedipine DMSVOZT Angina pectoris BA40 Approved [22]
Nilotinib DM7HXWT Chronic myelogenous leukaemia 2A20.0 Approved [44]
Nimodipine DMQ0RKZ Cerebral vasospasm BA85.Z Approved [15]
Nisoldipine DM7ISKJ Hypertension BA00-BA04 Approved [22]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [22]
Nizatidine DMGFV3Z Acid-reflux disorder DA22 Approved [126]
Norfloxacin DMIZ6W2 Acute gonococcal cervicitis Approved [15]
Olanzapine DMPFN6Y Bipolar depression Approved [23]
Olaparib DM8QB1D Ovarian cancer 2C73 Approved [127]
Olmesartan medoxomil DMWBHRY High blood pressure BA00 Approved [44]
Olopatadine DMKMWQG Allergic conjunctivitis 9A60.02 Approved [15]
Omadacycline DMR2J95 Acute bacterial skin infection 1C41 Approved [128]
Omeprazole DM471KJ Cystic fibrosis CA25 Approved [68]
Ondansetron DMOTQ1I Chemotherapy-induced nausea MD90 Approved [118]
Oseltamivir DMGO72P Influenza 1E30-1E32 Approved [129]
Oxcarbazepine DM5PU6O Epilepsy 8A60-8A68 Approved [130]
Paclitaxel DMLB81S Breast carcinoma Approved [131]
Palbociclib DMD7L94 Breast cancer 2C60-2C65 Approved [132]
Paliperidone DM7NPJS Psychotic disorder 6A20-6A25 Approved [133]
Panobinostat DM58WKG Chronic graft versus host disease Approved [134]
Pantoprazole DMSVOCZ Gastrinoma 2C10.1 Approved [68]
Paroxetine DM5PVQE Anxiety disorder 6B00-6B0Z Approved [28]
Pazopanib HCl DM6U9CQ Renal cell carcinoma 2C90 Approved [135]
Pemirolast DML97WV Allergic conjunctivitis 9A60.02 Approved [15]
Pentazocine DM1XBHS Pain MG30-MG3Z Approved [22]
Perazine DM2AOTZ Psychotic disorder 6A20-6A25 Approved [23]
Perphenazine DMA4MRX Schizophrenia 6A20 Approved [23]
Phenobarbital DMXZOCG Cluster headache 8A81.0 Approved [130]
Phenprocoumon DMDO279 Myocardial infarction BA41-BA43 Approved [136]
Phenytoin DMNOKBV Epilepsy 8A60-8A68 Approved [130]
Pibrentasvir DM27BL1 N. A. N. A. Approved [27]
Pimozide DMW83TP Schizophrenia 6A20 Approved [15]
Pirarubicin DMGTW1I Breast cancer 2C60-2C65 Approved [15]
Pirenzepine DMP6M1N Peptic ulcer DA61 Approved [16]
Pomalidomide DMTGBAX Plasma cell myeloma 2A83.1 Approved [137]
Ponatinib DMYGJQO Acute lymphoblastic leukaemia 2A85 Approved [138]
Posaconazole DMUL5EW Aspergillosis 1F20 Approved [44]
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [27]
Prazosin DMCD9YG Benign prostatic hyperplasia GA90 Approved [139]
Prednisolone DMQ8FR2 Acute adrenal insufficiency Approved [140]
Prednisone DM2HG4X Acute asthma CA23 Approved [37]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [71]
Propafenone DMPIBJK Tachyarrhythmias BC71 Approved [22]
Propranolol DM79NTF Angina pectoris BA40 Approved [27]
Protriptyline DMNHTZI Depression 6A70-6A7Z Approved [16]
Quercetin DM3NC4M Obesity 5B81 Approved [141]
Quetiapine DM1N62C Anorexia nervosa cachexia 6B80 Approved [23]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [22]
R0-93877 DMM4U9G Constipation DD91.1 Approved [142]
Raloxifene DMDKF3M Osteoporosis FB83.0 Approved [143]
Ramosetron DMH7GN8 Diarrhea-predominant irritable bowel syndrome DD91.01 Approved [144]
Ranitidine DM0GUSX Gastric ulcer DA60 Approved [22]
Ranolazine DM0C9IL Acute coronary syndrome BA41 Approved [145]
Regorafenib DMHSY1I Gastrointestinal stromal tumour 2B5B Approved [146]
Relugolix DMK7IWL Prostate cancer 2C82.0 Approved [44]
Reserpine DM6VM38 Hypertension BA00-BA04 Approved [28]
Rifampin DMA8J1G Tuberculosis 1B10-1B1Z Approved [22]
Rifaximin DMW1TV2 Bacterial infection 1A00-1C4Z Approved [147]
Riociguat DMXBLMP Chronic thromboembolic pulmonary hypertension Approved [148]
Risperidone DMN6DXL Bipolar I disorder Approved [149]
Ritonavir DMU764S Human immunodeficiency virus infection 1C62 Approved [150]
Rivaroxaban DMQMBZ1 Deep vein thrombosis BD71 Approved [151]
Romidepsin DMT5GNL Cutaneous T-cell lymphoma 2B01 Approved [152]
Rosuvastatin DMMIQ7G Arteriosclerosis BD40 Approved [153]
S-licarbazepine DMDIZCS N. A. N. A. Approved [82]
Saphris DM5VP0F N. A. N. A. Approved [15]
Saquinavir DMG814N Human immunodeficiency virus infection 1C62 Approved [154]
Saxagliptin DMGXENV Type-2 diabetes 5A11 Approved [27]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [28]
SILODOSIN DMJSBT6 Benign prostatic hyperplasia GA90 Approved [155]
Simeprevir DMLUA9D Chronic HCV-1 infection 1E51.1 Approved [44]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [22]
Sirolimus DMGW1ID Advanced cancer 2A00-2F9Z Approved [156]
Sitagliptin DMGDKXN Cystic fibrosis CA25 Approved [27]
Sofosbuvir DMQI86A Hepatitis C 1E51 Approved [157]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [158]
Sparfloxacin DMB4HCT Bacterial infection 1A00-1C4Z Approved [22]
Sumatriptan DMVYXR8 Cluster headache 8A81.0 Approved [159]
Sunitinib DMCBJSR Acute undifferentiated leukemia Approved [160]
Sunitinib malate DMN8E5D N. A. N. A. Approved [161]
Tacrine DM51FY6 Alzheimer disease 8A20 Approved [162]
Tacrolimus DMZ7XNQ Graft-versus-host disease 4B24 Approved [22]
Tadalafil DMJZHT1 Benign prostatic hyperplasia GA90 Approved [163]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [164]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [22]
Telaprevir DMMRV29 Hepatitis C virus infection 1E51.1 Approved [41]
Telithromycin DMZ4P3A Bacterial infection 1A00-1C4Z Approved [165]
Temsirolimus DMS104F Renal cell carcinoma 2C90 Approved [166]
Teniposide DMLW57T Acute lymphoblastic leukaemia 2A85 Approved [22]
Tenofovir DM1IS6U Chronic hepatitis B virus infection Approved [44]
Tenofovir alafenamide DMTQF4A Hiv infectious disease Approved [167]
Tenoxicam DMVAZP9 Rheumatoid arthritis FA20 Approved [15]
Testosterone DM7HUNW Hot flushes GA30 Approved [68]
Tetracycline DMZA017 Acne vulgaris ED80 Approved [22]
Thiamphenicol DMDRKH2 Bacterial infection 1A00-1C4Z Approved [54]
Thioridazine DM35M8J Schizophrenia 6A20 Approved [28]
Timolol DM3NXRU High blood pressure BA00 Approved [49]
Tolvaptan DMIWFRL Autosomal dominant polycystic kidney disease GB81 Approved [168]
Topiramate DM82Z30 Alcohol dependence 6C40.2 Approved [169]
Topotecan DMP6G8T Central nervous system neoplasm Approved [170]
Toremifene DMQYUWG Breast cancer 2C60-2C65 Approved [58]
Tramadol DMRQD04 Osteoarthritis FA00-FA05 Approved [171]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [25]
Trifluoperazine DMKBYWI Anxiety Approved [22]
Triflupromazine DMKFQJP Nausea MD90 Approved [15]
Trimethoprim DMM7CHK Acute otitis media AB00 Approved [28]
Triprolidine DM7SWIA Allergic rhinitis CA08.0 Approved [172]
Trospium chloride DM32XZT Discovery agent N.A. Approved [173]
Vecuronium DMP0UK2 Spasm MB47.3 Approved [118]
Velpatasvir DMGF8ZQ N. A. N. A. Approved [27]
Vemurafenib DM62UG5 Melanoma 2C30 Approved [174]
Venetoclax DM8I94Y Chronic lymphocytic leukaemia 2A82.0 Approved [175]
Verapamil DMA7PEW Angina pectoris BA40 Approved [176]
Vibegron DMFR201 Overactive bladder GC50.0 Approved [44]
Vildagliptin DMYN59P Type-2 diabetes 5A11 Approved [177]
Vinblastine DM5TVS3 Advanced cancer 2A00-2F9Z Approved [178]
Vincristine DMINOX3 Acute lymphoblastic leukaemia 2A85 Approved [179]
Vindesine DMVR628 Acute lymphoblastic leukaemia 2A85 Approved [15]
Vinorelbine DMVXFYE Advanced cancer 2A00-2F9Z Approved [180]
Voxilaprevir DMAI83D N. A. N. A. Approved [27]
VRX496 DMIO4V5 Acquired immune deficiency syndrome 1C62.3 Approved [181]
Y-25130 DMDPM7R Nausea and vomiting MD90 Approved [15]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [14]
Ziprasidone DMM58JY Bipolar disorder 6A60 Approved [28]
Zolmitriptan DM1IB4Q Migraine 8A80 Approved [28]
Beclomethasone dipropionate DM5NW1E Allergic rhinitis CA08.0 Phase 4 [35]
Berberine DMC5Q8X N. A. N. A. Phase 4 [182]
Dihydrotestosterone DM3S8XC Prostate hyperplasia GA90 Phase 4 [183]
Ebastine DMH21D9 N. A. N. A. Phase 4 [15]
Guanfacine DMPN5IH Attention deficit hyperactivity disorder 6A05.Z Phase 4 [184]
Ombitasvir DMQIMTK Hepatitis C 1E51 Phase 4 [27]
Tenofovir disoproxil DM62IPN N. A. N. A. Phase 4 [15]
------------------------------------------------------------------------------------
⏷ Show the Full List of 339 Approved Drug(s)
29 Clinical Trial Drug(s) Transported by This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
ABT-263 DMNE56X Myelofibrosis 2A20.2 Phase 3 [185]
Asimadoline DMND3AB Diarrhea-predominant irritable bowel syndrome DD91.01 Phase 3 [22]
Crocin DM5F24X N. A. N. A. Phase 3 [25]
Curcumin DMQPH29 Solid tumour/cancer 2A00-2F9Z Phase 3 [22]
MELAGATRAN DM4W8RE N. A. N. A. Phase 3 [15]
Morphine-6-glucuronide DMPVW6H Pain MG30-MG3Z Phase 3 [15]
Pazufloxacin DMHXTAQ Conjunctivitis 9A60 Phase 3 [186]
Simvastatin acid DM18QHT N. A. N. A. Phase 3 [187]
Sitafloxacin DMTV5XC Escherichia coli infection 1A03 Phase 2/3 [15]
(Z)-endoxifen DMGDOS2 N. A. N. A. Phase 2 [188]
Afimoxifene DMFORDT Breast cancer 2C60-2C65 Phase 2 [58]
Arverapamil DML27AE Irritable bowel syndrome DD91.0 Phase 2 [189]
Bisantrene DMW76V0 N. A. N. A. Phase 2 [22]
BMS 650032 DMQI43G Hepatitis C virus infection 1E51.1 Phase 2 [44]
CKD602 DMW9F1G Solid tumour/cancer 2A00-2F9Z Phase 2 [15]
CP-122721 DMSWLM5 Major depressive disorder 6A70.3 Phase 2 [190]
Dolastatin 10 DM0QDC9 N. A. N. A. Phase 2 [191]
Fucoxanthin DMPQFTA Metabolic syndrome x 5C50-5D2Z Phase 2 [25]
Gallopamil DMXBR27 Asthma CA23 Phase 2 [15]
GS-5885 DMSL3DX Hepatitis C virus infection 1E51.1 Phase 2 [27]
ONO-6126 DMRT28X Chronic obstructive pulmonary disease CA22 Phase 2 [192]
Paritaprevir DM4N7BT Hepatitis C 1E51 Phase 2 [27]
R-roscovitine DMSH108 Non-small-cell lung cancer 2C25.Y Phase 2 [193]
ABT-333 DM7TOWX Hepatitis C virus infection 1E51.1 Phase 1 [27]
Genz 644282 DMTGN0U N. A. N. A. Phase 1 [194]
Mibefradil DMU9VDS Glioblastoma multiforme 2A00.0 Phase 1 [15]
NARINGENIN DMHAZLM N. A. N. A. Phase 1 [141]
Norbuprenorphine DM2ILSJ N. A. N. A. Phase 1 [195]
Sphingosine-1-phosphate DMJCQKA Acne vulgaris ED80 Phase 1 [196]
------------------------------------------------------------------------------------
⏷ Show the Full List of 29 Clinical Trial Drug(s)
20 Discontinued Drug(s) Transported by This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Alprenolol DMYJ8Z3 Hypertension BA00-BA04 Withdrawn from market [68]
Astemizole DM2HN6Q Allergic rhinitis CA08.0 Withdrawn from market [28]
Isoxicam DMMS2J5 Osteoarthritis FA00-FA05 Withdrawn from market [15]
Roxithromycin DMVMIK2 Bacterial infection 1A00-1C4Z Withdrawn from market [165]
Terfenadine DM4KLPT Allergy 4A80-4A85 Withdrawn from market [22]
Ximelagatran DMABRJL Coagulation defect 3B10.0 Withdrawn from market [15]
Flesinoxan DMOIP7R Anxiety disorder 6B00-6B0Z Discontinued in Phase 3 [197]
Valspodar DMXRU9M Acute myeloid leukaemia 2A60 Discontinued in Phase 3 [22]
DE-081 DM3AVO1 Conjunctivitis 9A60 Discontinued in Phase 2 [198]
Dexniguldipine DMLZIT2 Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 2 [192]
Droloxifene DM9JPUD Breast cancer 2C60-2C65 Discontinued in Phase 2 [15]
Radafaxine DMARQE0 Major depressive disorder 6A70.3 Discontinued in Phase 2 [45]
S-9788 DMER3I9 Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 2 [15]
Tolafentrine DMEROU4 Chronic obstructive pulmonary disease CA22 Discontinued in Phase 2 [68]
PAFENOLOL DM6LQGO Hypertension BA00-BA04 Discontinued in Phase 1 [15]
Rhodamine-123 DMQAK6T Prostate cancer 2C82.0 Discontinued in Phase 1 [70]
ABT-737 DML0DBV N. A. N. A. Terminated [185]
Bisbenzimide (Hoechst 33258) DMKRBL2 Solid tumour/cancer 2A00-2F9Z Terminated [22]
Calphostin C DM9X2D0 N. A. N. A. Terminated [15]
NIGULDIPINE DMSPWMF N. A. N. A. Terminated [15]
------------------------------------------------------------------------------------
⏷ Show the Full List of 20 Discontinued Drug(s)
15 Preclinical Drug(s) Transported by This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Abamectin B1A DMRSATG N. A. N. A. Preclinical [199]
BMS-3870032 DMCWIBU N. A. N. A. Preclinical [15]
Bouvardin DM5O3HC N. A. N. A. Preclinical [192]
Bunitrolol DMT4532 N. A. N. A. Preclinical [200]
Cephaeline DM1ZFCS N. A. N. A. Preclinical [192]
Coelenterazine DMG3BE1 N. A. N. A. Preclinical [201]
Desmethylsertraline DM2I76R N. A. N. A. Preclinical [45]
Epothilone A DMX2FZS N. A. N. A. Preclinical [15]
Metildigoxin DMDPV82 N. A. N. A. Preclinical [44]
Metkephamid DMDU8KC N. A. N. A. Preclinical [192]
MG-132 DMKA2YS N. A. N. A. Preclinical [202]
N-desethyl sunitinib DM5ATJ0 N. A. N. A. Preclinical [203]
Nonactin DMKF2H0 N. A. N. A. Preclinical [64]
Puromycin DMDKLB5 N. A. N. A. Preclinical [204]
Selamectin DM5LU3N N. A. N. A. Preclinical [199]
------------------------------------------------------------------------------------
⏷ Show the Full List of 15 Preclinical Drug(s)
22 Investigative Drug(s) Transported by This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(11-BETA)-11,21-DIHYDROXY-PREGN-4-ENE-3,20-DIONE DMTPQ84 Discovery agent N.A. Investigative [58]
azidopine DMD0LCA Discovery agent N.A. Investigative [22]
Bcecf-Am DMPG1LJ N. A. N. A. Investigative [22]
biotin DMKMCE1 Discovery agent N.A. Investigative [205]
Cholesterol DMR3J6S Discovery agent N.A. Investigative [206]
cycloheximide DMGDA3C Discovery agent N.A. Investigative [25]
FLUPENTIXOLE DMELB5S Discovery agent N.A. Investigative [22]
G418 DMKTJBU Discovery agent N.A. Investigative [204]
GNF-PF-5411 DMZNAEQ Discovery agent N.A. Investigative [15]
Leupeptin DMU075F Malaria 1F40-1F45 Investigative [22]
Nafoxidine DM0FROP Discovery agent N.A. Investigative [58]
Nogalamycin DM50TCG Discovery agent N.A. Investigative [192]
Okadaic acid DM47CO1 Discovery agent N.A. Investigative [192]
paraquat DMR8O3X Discovery agent N.A. Investigative [22]
prostaglandin A2 DMWC4X8 Discovery agent N.A. Investigative [207]
Staurosporine DM0E9BR Discovery agent N.A. Investigative [15]
Substance P DMQ6W4I Discovery agent N.A. Investigative [209]
talinolol DMRTD16 Discovery agent N.A. Investigative [210]
Tiapamil DMWSI0H Cardiovascular disease BA00-BE2Z Investigative [22]
Tyrphostin ag-1478 DM87ZIH Discovery agent N.A. Investigative [211]
Valinomycin DMW4TYV N. A. N. A. Investigative [70]
[3H]spiperone DMWHEV8 Discovery agent N.A. Investigative [15]
------------------------------------------------------------------------------------
⏷ Show the Full List of 22 Investigative Drug(s)
1 Investigative Agents Transported by This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Silvestrol DM5JKNF Middle East Respiratory Syndrome (MERS) 1D64 Investigative [208]
------------------------------------------------------------------------------------

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87 The influence of CYP3A5*3 and BCRPC421A genetic polymorphisms on the pharmacokinetics of felodipine in healthy Chinese volunteers. J Clin Pharm Ther. 2017 Jun;42(3):345-349.
88 Blood-brain barrier permeation and efflux exclusion of anticholinergics used in the treatment of overactive bladder. Drugs Aging. 2012 Apr 1;29(4):259-73.
89 Effect of itraconazole on the pharmacokinetics and pharmacodynamics of fexofenadine in relation to the MDR1 genetic polymorphism. Clin Pharmacol Ther. 2005 Aug;78(2):191-201.
90 Fluoxetine and reversal of multidrug resistance. Cancer Lett. 2006 Jun 18;237(2):180-7.
91 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
92 Interaction of gatifloxacin with efflux transporters: a possible mechanism for drug resistance. Int J Pharm. 2010 Aug 16;395(1-2):114-21.
93 Gefitinib-phenytoin interaction is not correlated with the C-erythromycin breath test in healthy male volunteers. Br J Clin Pharmacol. 2009 Aug;68(2):226-37.
94 Increased sensitivity to gemcitabine of P-glycoprotein and multidrug resistance-associated protein-overexpressing human cancer cell lines. Br J Cancer. 2003 Jun 16;88(12):1963-70.
95 Upregulation of cellular glutathione levels in human ABCB5- and murine Abcb5-transfected cells. BMC Pharmacol Toxicol. 2015 Dec 15;16:37.
96 Effects of plant sterols on human multidrug transporters ABCB1 and ABCC1. Biochem Biophys Res Commun. 2008 May 2;369(2):363-8.
97 P-Glycoprotein (MDR1/ABCB1) Restricts Brain Penetration of the Bruton's Tyrosine Kinase Inhibitor Ibrutinib, While Cytochrome P450-3A (CYP3A) Limits Its Oral Bioavailability. Mol Pharm. 2018 Nov 5;15(11):5124-5134.
98 Amonafide L-malate is not a substrate for multidrug resistance proteins in secondary acute myeloid leukemia. Leukemia. 2008 Nov;22(11):2110-5.
99 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
100 HIV-1 protease inhibitors are substrates for the MDR1 multidrug transporter. Biochemistry. 1998 Mar 17;37(11):3594-601.
101 Indomethacin induces apoptosis via a MRP1-dependent mechanism in doxorubicin-resistant small-cell lung cancer cells overexpressing MRP1. Br J Cancer. 2007 Oct 22;97(8):1077-83.
102 The skin cancer chemotherapeutic agent ingenol-3-angelate (PEP005) is a substrate for the epidermal multidrug transporter (ABCB1) and targets tumor vasculature. Cancer Res. 2010 Jun 1;70(11):4509-19.
103 Effects of Ketoconazole and Rifampicin on the Pharmacokinetics of Nintedanib in Healthy Subjects. Eur J Drug Metab Pharmacokinet. 2018 Oct;43(5):533-541.
104 Intestinal transport of irinotecan in Caco-2 cells and MDCK II cells overexpressing efflux transporters Pgp, cMOAT, and MRP1. Drug Metab Dispos. 2002 Jul;30(7):763-70.
105 Investigation of the effects of the CFTR potentiator ivacaftor on human P-glycoprotein (ABCB1). Sci Rep. 2017 Dec 13;7(1):17481.
106 MDR1-deficient genotype in Collie dogs hypersensitive to the P-glycoprotein substrate ivermectin. Eur J Pharmacol. 2003 Jan 24;460(2-3):85-91.
107 DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB14568)
108 Ixabepilone, a novel microtubule-targeting agent for breast cancer, is a substrate for P-glycoprotein (P-gp/MDR1/ABCB1) but not breast cancer resistance protein (BCRP/ABCG2). J Pharmacol Exp Ther. 2011 May;337(2):423-32.
109 Pharmacogenetics of antidepressants. Front Pharmacol. 2011 Feb 16;2:6.
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112 Influence of CYP3A4/5 and ABC transporter polymorphisms on lenvatinib plasma trough concentrations in Japanese patients with thyroid cancer. Sci Rep. 2019 Apr 1;9(1):5404.
113 Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein. Neuropharmacology. 2007 Feb;52(2):333-46.
114 P-glycoprotein differentially affects escitalopram, levomilnacipran, vilazodone and vortioxetine transport at the mouse blood-brain barrier inivo. Neuropharmacology. 2016 Apr;103:104-11.
115 In vitro P-glycoprotein assays to predict the in vivo interactions of P-glycoprotein with drugs in the central nervous system. Drug Metab Dispos. 2008 Feb;36(2):268-75.
116 Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir. Br J Pharmacol. 2010 Jul;160(5):1224-33.
117 Active transport of the angiotensin-II antagonist losartan and its main metabolite EXP 3174 across MDCK-MDR1 and caco-2 cell monolayers. Br J Pharmacol. 2000 Mar;129(6):1235-43.
118 Polymorphisms in human MDR1 (P-glycoprotein): recent advances and clinical relevance. Clin Pharmacol Ther. 2004 Jan;75(1):13-33.
119 Multidrug resistance protein-mediated transport of chlorambucil and melphalan conjugated to glutathione. Br J Cancer. 1998;77(2):201-9.
120 Opioids and efflux transporters. Part 3: P-glycoprotein substrate activity of 3-hydroxyl addition to meperidine analogs. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3638-40.
121 In vitro P-glycoprotein-mediated transport of (R)-, (S)-, (R,S)-methadone, LAAM and their main metabolites. Pharmacology. 2007;80(4):304-11.
122 Secretory transport of methylprednisolone possibly mediated by P-glycoprotein in Caco-2 cells. Biol Pharm Bull. 2002 Mar;25(3):393-6.
123 In vivo expansion of MDR1-transduced cells accompanied by a post-transplantation chemotherapy regimen with mitomycin C and methotrexate. J Gene Med. 2010 Jul;12(7):596-603.
124 Genetic variability and clinical efficacy of morphine. Acta Anaesthesiol Scand. 2005 Aug;49(7):902-8.
125 Influence of drug transporters and UGT polymorphisms on pharmacokinetics of phenolic glucuronide metabolite of mycophenolic acid in Japanese renal transplant recipients. Ther Drug Monit. 2008 Oct;30(5):559-64.
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127 Overexpressed ABCB1 Induces Olaparib-Taxane Cross-Resistance in Advanced Prostate Cancer. Transl Oncol. 2019 May 7;12(7):871-878.
128 DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB12455)
129 Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system. Antimicrob Agents Chemother. 2009 Nov;53(11):4753-61.
130 The transport of antiepileptic drugs by P-glycoprotein. Adv Drug Deliv Rev. 2012 Jul;64(10):930-42.
131 Kinetics of P-glycoprotein-mediated efflux of paclitaxel. J Pharmacol Exp Ther. 2001 Sep;298(3):1236-42.
132 Efflux transporters at the blood-brain barrier limit delivery and efficacy of cyclin-dependent kinase 4/6 inhibitor palbociclib (PD-0332991) in an orthotopic brain tumor model. J Pharmacol Exp Ther. 2015 Nov;355(2):264-71.
133 Invega (paliperidone) extended release tablets FDA Label
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135 Bioavailability, metabolism and disposition of oral pazopanib in patients with advanced cancer. Xenobiotica. 2013 May;43(5):443-53.
136 Role of P-glycoprotein in the uptake/efflux transport of oral vitamin K antagonists and rivaroxaban through the Caco-2 cell model. Basic Clin Pharmacol Toxicol. 2013 Oct;113(4):259-65.
137 DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB08910)
138 DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB08901)
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140 The role of the efflux transporter P-glycoprotein in brain penetration of prednisolone. J Endocrinol. 2002 Oct;175(1):251-60.
141 Flavonoid permeability across an in situ model of the blood-brain barrier. Free Radic Biol Med. 2004 Mar 1;36(5):592-604.
142 Resolor, INN-prucalopride
143 Influence of hepatic and intestinal efflux transporters and their genetic variants on the pharmacokinetics and pharmacodynamics of raloxifene in osteoporosis treatment. Transl Res. 2012 Oct;160(4):298-308.
144 Contribution of P-glycoprotein to efflux of ramosetron, a 5-HT3 receptor antagonist, across the blood-brain barrier. J Pharm Pharmacol. 2002 Aug;54(8):1055-63.
145 Ranolazine-tacrolimus interaction. Ann Pharmacother. 2010 Nov;44(11):1844-9.
146 Brain and Testis Accumulation of Regorafenib is Restricted by Breast Cancer Resistance Protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1). Pharm Res. 2015 Jul;32(7):2205-16.
147 Advantageous Solubility-Permeability Interplay When Using Amorphous Solid Dispersion (ASD) Formulation for the BCS Class IV P-gp Substrate Rifaximin: Simultaneous Increase of Both the Solubility and the Permeability. AAPS J. 2017 May;19(3):806-813.
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149 Effect of verapamil on pharmacokinetics and pharmacodynamics of risperidone: in vivo evidence of involvement of P-glycoprotein in risperidone disposition. Clin Pharmacol Ther. 2005 Jul;78(1):43-51.
150 MDR1 G1199A polymorphism alters permeability of HIV protease inhibitors across P-glycoprotein-expressing epithelial cells. AIDS. 2005 Oct 14;19(15):1617-25.
151 Downregulation of ABCB1 gene in patients with total hip or knee arthroplasty influences pharmacokinetics of rivaroxaban: a population pharmacokinetic-pharmacodynamic study. Eur J Clin Pharmacol. 2019 Feb 6.
152 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.
153 Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos. 2008 Oct;36(10):2014-23.
154 Predicting P-glycoprotein effects on oral absorption: correlation of transport in Caco-2 with drug pharmacokinetics in wild-type and mdr1a(-/-) mice in vivo. Pharm Res. 2004 May;21(5):819-26.
155 The influence of UGT2B7, UGT1A8, MDR1, ALDH, ADH, CYP3A4 and CYP3A5 genetic polymorphisms on the pharmacokinetics of silodosin in healthy Chinese volunteers. Drug Metab Pharmacokinet. 2013;28(3):239-43.
156 Pharmacogenetics of tacrolimus and sirolimus in renal transplant patients: from retrospective analyses to prospective studies. Transplant Proc. 2007 Sep;39(7):2142-4.
157 Cytochrome P450 3A Induction Predicts P-glycoprotein Induction; Part 2: Prediction of Decreased Substrate Exposure After Rifabutin or Carbamazepine. Clin Pharmacol Ther. 2018 Dec;104(6):1191-1198.
158 Breast cancer resistance protein and P-glycoprotein limit sorafenib brain accumulation. Mol Cancer Ther. 2010 Feb;9(2):319-26.
159 HT29-MTX and Caco-2/TC7 monolayers as predictive models for human intestinal absorption: role of the mucus layer. J Pharm Sci. 2001 Oct;90(10):1608-19. Comparative Study
160 Interaction of the multikinase inhibitors sorafenib and sunitinib with solute carriers and ATP-binding cassette transporters. Clin Cancer Res. 2009 Oct 1;15(19):6062-9.
161 JNK-AKT-NF-kB controls P-glycoprotein expression to attenuate the cytotoxicity of deoxynivalenol in mammalian cells. Biochem Pharmacol. 2018 Oct;156:120-134.
162 Tacrine sinusoidal uptake and biliary excretion in sandwich-cultured primary rat hepatocytes. J Pharm Pharm Sci. 2014;17(3):427-38.
163 In Vitro P-Glycoprotein-Mediated Transport of Tadalafil: A Comparison with Sildenafil. Biol Pharm Bull. 2017;40(8):1314-1319.
164 DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB11760)
165 Differences in assessment of macrolide interaction with human MDR1 (ABCB1, P-gp) using rhodamine-123 efflux, ATPase activity and cellular accumulation assays. Eur J Pharm Sci. 2010 Sep 11;41(1):86-95.
166 Association of NR1I2, CYP3A5 and ABCB1 genetic polymorphisms with variability of temsirolimus pharmacokinetics and toxicity in patients with metastatic bladder cancer. Cancer Chemother Pharmacol. 2017 Sep;80(3):653-659.
167 Pharmacokinetics of Tenofovir Alafenamide When Coadministered With Other HIV Antiretrovirals. J Acquir Immune Defic Syndr. 2018 Aug 1;78(4):465-472.
168 In vitro P-glycoprotein interactions and steady-state pharmacokinetic interactions between tolvaptan and digoxin in healthy subjects. J Clin Pharmacol. 2011 May;51(5):761-9.
169 The antiepileptic drug topiramate is a substrate for human P-glycoprotein but not multidrug resistance proteins. Pharm Res. 2009 Nov;26(11):2464-70.
170 Involvement of P-glycoprotein, multidrug resistance protein 2 and breast cancer resistance protein in the transport of belotecan and topotecan in Caco-2 and MDCKII cells. Pharm Res. 2008 Nov;25(11):2601-12.
171 Tramadol hydrochloride: pharmacokinetics, pharmacodynamics, adverse side effects, co-administration of drugs and new drug delivery systems. Biomed Pharmacother. 2015 Mar;70:234-8.
172 Central nervous system pharmacokinetics of the Mdr1 P-glycoprotein substrate CP-615,003: intersite differences and implications for human receptor occupancy projections from cerebrospinal fluid exposures. Drug Metab Dispos. 2007 Aug;35(8):1341-9.
173 Expression of drug transporters and drug metabolizing enzymes in the bladder urothelium in man and affinity of the bladder spasmolytic trospium chloride to transporters likely involved in its pharmacokinetics. Mol Pharm. 2015 Jan 5;12(1):171-8.
174 Differential effects of the oncogenic BRAF inhibitor PLX4032 (vemurafenib) and its progenitor PLX4720 on ABCB1 function. J Pharm Pharm Sci. 2014;17(1):154-68.
175 Venclexta FDA label
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177 Pharmacokinetics of dipeptidylpeptidase-4 inhibitors. Diabetes Obes Metab. 2010 Aug;12(8):648-58.
178 Xenopus laevis oocytes expressing human P-glycoprotein: probing trans- and cis-inhibitory effects on [3H]vinblastine and [3H]digoxin efflux. Pharmacol Res. 2010 Jan;61(1):76-84.
179 L-type calcium channel blockers reverse docetaxel and vincristine-induced multidrug resistance independent of ABCB1 expression in human lung cancer cell lines. Toxicol Lett. 2010 Feb 15;192(3):408-18.
180 Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8.
181 Pharmacogenetics of long-term responses to antiretroviral regimens containing Efavirenz and/or Nelfinavir: an Adult Aids Clinical Trials Group Study. J Infect Dis. 2005 Dec 1;192(11):1931-42.
182 P-glycoprotein-mediated transport of berberine across Caco-2 cell monolayers. J Pharm Sci. 2002 Dec;91(12):2614-21.
183 P-glycoprotein increases the efflux of the androgen dihydrotestosterone and reduces androgen responsive gene activity in prostate tumor cells. Prostate. 2004 Apr 1;59(1):77-90.
184 An in vitro evaluation of guanfacine as a substrate for P-glycoprotein. Neuropsychiatr Dis Treat. 2011;7:501-5.
185 The B-cell lymphoma 2 (BCL2)-inhibitors, ABT-737 and ABT-263, are substrates for P-glycoprotein. Biochem Biophys Res Commun. 2011 May 6;408(2):344-9.
186 Possible involvement of P-glycoprotein in renal excretion of pazufloxacin in rats. Eur J Pharmacol. 2004 Oct 6;501(1-3):151-9.
187 Interactions of human P-glycoprotein with simvastatin, simvastatin acid, and atorvastatin. Pharm Res. 2004 Sep;21(9):1686-91.
188 P-glycoprotein (ABCB1) transports the primary active tamoxifen metabolites endoxifen and 4-hydroxytamoxifen and restricts their brain penetration. J Pharmacol Exp Ther. 2011 Jun;337(3):710-7.
189 Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoprotein. J Pharmacol Exp Ther. 2000 May;293(2):376-82.
190 P-glycoprotein efflux at the blood-brain barrier mediates differences in brain disposition and pharmacodynamics between two structurally related neurokinin-1 receptor antagonists. J Pharmacol Exp Ther. 2001 Sep;298(3):1252-9.
191 Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity. J Biol Chem. 1996 Feb 9;271(6):3163-71.
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193 ATP-binding cassette B1 transports seliciclib (R-roscovitine), a cyclin-dependent kinase inhibitor. Drug Metab Dispos. 2010 Nov;38(11):2000-6.
194 Molecular and cellular pharmacology of the novel noncamptothecin topoisomerase I inhibitor Genz-644282. Mol Cancer Ther. 2011 Aug;10(8):1490-9.
195 Interaction of drugs of abuse and maintenance treatments with human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2). Int J Neuropsychopharmacol. 2010 Aug;13(7):905-15.
196 Lipid dependence of ABC transporter localization and function. Chem Phys Lipids. 2009 Oct;161(2):57-64.
197 Active efflux of the 5-HT(1A) receptor agonist flesinoxan via P-glycoprotein at the blood-brain barrier. Eur J Pharm Sci. 2001 Aug;14(1):81-6.
198 Altered drug disposition of the platelet activating factor antagonist apafant in mdr1a knockout mice. Eur J Pharm Sci. 2002 Aug;16(3):119-28.
199 Interaction of macrocyclic lactones with P-glycoprotein: structure-affinity relationship. Eur J Pharm Sci. 2007 Jan;30(1):84-94.
200 Contribution of P-glycoprotein to bunitrolol efflux across blood-brain barrier. Biopharm Drug Dispos. 1999 Mar;20(2):85-90.
201 Imaging reversal of multidrug resistance in living mice with bioluminescence: MDR1 P-glycoprotein transports coelenterazine. Proc Natl Acad Sci U S A. 2004 Feb 10;101(6):1702-7.
202 Increased ABCB1 expression in TP-110-resistant RPMI-8226 cells. Biosci Biotechnol Biochem. 2010;74(9):1913-9.
203 P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) restrict brain accumulation of the active sunitinib metabolite N-desethyl sunitinib. J Pharmacol Exp Ther. 2012 Apr;341(1):164-73.
204 ATP-binding cassette transporters as pitfalls in selection of transgenic cells. Anal Biochem. 2010 Apr 15;399(2):246-50.
205 Functional characterization of sodium-dependent multivitamin transporter in MDCK-MDR1 cells and its utilization as a target for drug delivery. Mol Pharm. 2006 May-Jun;3(3):329-39.
206 Cholesterol interaction with the daunorubicin binding site of P-glycoprotein. Biochem Biophys Res Commun. 2000 Oct 5;276(3):909-16.
207 Unveiling the role of multidrug resistance proteins in hypertension. Hypertension. 2009 Aug;54(2):210-6.
208 Resistance to the translation initiation inhibitor silvestrol is mediated by ABCB1/P-glycoprotein overexpression in acute lymphoblastic leukemia cells. AAPS J. 2011 Sep;13(3):357-64.
209 Transport of somatostatin and substance P by human P-glycoprotein. FEBS Lett. 2004 Sep 10;574(1-3):55-61.
210 Grapefruit juice-drug interactions: Grapefruit juice and its components inhibit P-glycoprotein (ABCB1) mediated transport of talinolol in Caco-2 cells. J Pharm Sci. 2007 Oct;96(10):2808-17.
211 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.