Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMCBJSR)

Drug Name

Sunitinib Drug Info

Synonyms

Sunitanib; Sunitinibum; Sutent; PDGF TK antagonist; SU 11248; SU11248; KS-5022; SU-11248; SU-11248J; SU-12662; Su-011248; Sunitinib (INN); Sunitinib (free base); Sutent (TN); N-(2-diethylaminoethyl)-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide; N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide; 5-(5-FLUORO-2-OXO-1,2-DIHYDRO-INDOL-3-YLIDENEMETHYL)-2,4-DIMETHYL-1H-PYRROLE-3-CARBOXYLIC ACID (2-DIETHYLAMINO-ETHYL)-AMIDE; Sunitinib (Pan-TK inhibitor)

Indication

Disease Entry	ICD 11	Status	REF
Acute undifferentiated leukemia		Approved	[1]
Chronic myelomonocytic leukemia		Approved	[1]
Classic Kaposi sarcoma		Approved	[1]
Gastrointestinal cancer	2C11	Approved	[2]
Gastrointestinal stromal tumour	2B5B	Approved	[3]
Large granular lymphocytic leukemia	2A90.1	Approved	[1]
Lung cancer	2C25.0	Approved	[1]
Mast cell leukaemia	2A21.00	Approved	[1]
Non-small-cell lung cancer	2C25.Y	Approved	[1]
Pancreatic cancer	2C10	Approved	[1]
Primary myelofibrosis	2A20.2	Approved	[1]
Prolymphocytic leukaemia	2A82.1	Approved	[1]
Prostate adenocarcinoma		Approved	[1]
Refractory chronic myeloid leukaemia	2A20	Approved	[1]
Salivary gland squamous cell carcinoma		Approved	[1]
Plexiform neurofibroma		Investigative	[1]

Therapeutic Class

Anticancer Agents

Cross-matching ID

PubChem CID: 5329102
ChEBI ID: CHEBI:38940
CAS Number: CAS 557795-19-4
TTD Drug ID: DMCBJSR
VARIDT Drug ID: DR00454
INTEDE Drug ID: DR1519
ACDINA Drug ID: D00646

Molecule-Related Drug Atlas

Molecule Type:

DTT

DTP

DME

DOT

Drug Status:

Approved Drug(s)

Download the Complete Related Drug List

Drug(s) Targeting Vascular endothelial growth factor receptor 2 (KDR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[13]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[14]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[15]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[16]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[17]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[18]
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[19]
Cabozantinib	DMIYDT4	Medullary thyroid gland carcinoma		Approved	[20]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[21]
Lenvatinib	DMB1IU4	Thyroid cancer	2D10	Approved	[22]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

Drug(s) Transported By P-glycoprotein 1 (ABCB1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Amoxicillin	DMUYNEI	Acute otitis media	AB00	Approved	[23]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[24]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[25]
Folic Acid	DMEMBJC	Colorectal carcinoma		Approved	[26]
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[25]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[25]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[27]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[25]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[28]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[29]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

Drug(s) Transported By Breast cancer resistance protein (ABCG2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[30]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[31]
Folic Acid	DMEMBJC	Colorectal carcinoma		Approved	[32]
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[33]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[34]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[35]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[36]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[35]
Sulfasalazine	DMICA9H	Irritable bowel syndrome	DD91.0	Approved	[37]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[38]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

Drug(s) Transported By Organic anion transporting polypeptide 1B1 (SLCO1B1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[39]
Dinoprostone	DMTYOPD	Medical abortion	JA00.1Z	Approved	[40]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[7]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[41]
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[7]
Pravastatin	DM6A0X7	Adult acute monocytic leukemia		Approved	[42]
Mycophenolate mofetil	DMPQAGE	Hepatosplenic T-cell lymphoma		Approved	[43]
Atorvastatin	DMF28YC	Acute coronary syndrome	BA41	Approved	[44]
Cerivastatin	DMXCM7H	Hyperlipidaemia	5C80	Approved	[45]
PITAVASTATIN CALCIUM	DM1UJO0	Dyslipidemia	5C80-5C81	Approved	[42]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

Drug(s) Transported By Organic anion transporting polypeptide 1B3 (SLCO1B3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[46]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[7]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[47]
Diclofenac	DMPIHLS	Chronic renal failure	GB61.Z	Approved	[48]
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[7]
Pravastatin	DM6A0X7	Adult acute monocytic leukemia		Approved	[49]
Mycophenolate mofetil	DMPQAGE	Hepatosplenic T-cell lymphoma		Approved	[43]
Atorvastatin	DMF28YC	Acute coronary syndrome	BA41	Approved	[45]
Erythromycin	DM4K7GQ	Acne vulgaris	ED80	Approved	[50]
Cerivastatin	DMXCM7H	Hyperlipidaemia	5C80	Approved	[45]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

Drug(s) Transported By RalBP1-associated Eps domain-containing protein 2 (RALBP1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[5]
------------------------------------------------------------------------------------

Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[51]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[52]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[53]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[54]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[55]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[56]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[57]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[58]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[52]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[59]
Eplerenone	DMF0NQR	Heart failure	BD10-BD13	Approved	[72]
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[73]
Isotretinoin	DM4QTBN	Acne vulgaris	ED80	Approved	[74]
Voriconazole	DMAOL2S	Aspergillosis	1F20	Approved	[75]
Proguanil	DMBL79I	Malaria	1F40-1F45	Approved	[76]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[76]
Loratadine	DMF3AN7	Allergy	4A80-4A85	Approved	[77]
Nelfinavir mesylate	DMFX6G8	N. A.	N. A.	Approved	[78]
Capsaicin	DMGMF6V	Back pain	ME84.Z	Approved	[79]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[80]
------------------------------------------------------------------------------------


⏷ Show the Full List of 20 Drug(s)

Drug(s) Metabolized By Cytochrome P450 3A5 (CYP3A5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[60]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[61]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[62]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[10]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[63]
Sulfasalazine	DMICA9H	Irritable bowel syndrome	DD91.0	Approved	[64]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[65]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[66]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[67]
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[10]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

Drug(s) Metabolized By Cytochrome P450 3A7 (CYP3A7)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[68]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[10]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[10]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[10]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[69]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[70]
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[10]
Quinine	DMSWYF5	Malaria	1F40-1F45	Approved	[10]
Irinotecan	DMP6SC2	Adenocarcinoma	2D40	Approved	[10]
Metronidazole	DMTIVEN	Abscess		Approved	[71]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

Drug(s) Affected By Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[81]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[81]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[82]
Rosuvastatin	DMMIQ7G	Arteriosclerosis	BD40	Approved	[83]
Ciprofloxacin XR	DM2NLS9	Acute gonococcal cervicitis		Approved	[84]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[85]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[86]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[87]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[88]
Folic Acid	DMEMBJC	Colorectal carcinoma		Approved	[89]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Modulator	[4]

------------------------------------------------------------------------------------

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
RalBP1-associated Eps domain-containing protein 2 (RALBP1)	DTYEM9B	REPS2_HUMAN	Substrate	[5]
Breast cancer resistance protein (ABCG2)	DTI7UX6	ABCG2_HUMAN	Substrate	[6]
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DT3D8F0	SO1B1_HUMAN	Substrate	[7]
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DT9C1TS	SO1B3_HUMAN	Substrate	[7]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[8]

------------------------------------------------------------------------------------

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)^{Main DME}	DE4LYSA	CP3A4_HUMAN	Substrate	[9]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Substrate	[10]
Cytochrome P450 3A7 (CYP3A7)	DERD86B	CP3A7_HUMAN	Substrate	[10]

------------------------------------------------------------------------------------

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2)	OTW8V2V1	ABCG2_HUMAN	Drug Response	[11]
Cytochrome P450 3A4 (CYP3A4)	OTQGYY83	CP3A4_HUMAN	Drug Response	[12]

------------------------------------------------------------------------------------

References

1	Sunitinib FDA Label
2	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. (Ligand id: 5713).
3	The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
4	2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
5	Rlip76 transports sunitinib and sorafenib and mediates drug resistance in kidney cancer. Int J Cancer. 2010 Mar 15;126(6):1327-38.
6	Double-transduced MDCKII cells to study human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) interplay in drug transport across the blood-brain barrier. Mol Pharm. 2011 Apr 4;8(2):571-82.
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	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.
9	In vitro assessment of time-dependent inhibitory effects on CYP2C8 and CYP3A activity by fourteen protein kinase inhibitors. Drug Metab Dispos. 2014 Jul;42(7):1202-9.
10	Drug Interactions Flockhart Table
11	ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
12	Sunitinib-induced hypertension in CYP3A4 rs4646437 A-allele carriers with metastatic renal cell carcinoma. Pharmacogenomics J. 2017 Jan;17(1):42-46. doi: 10.1038/tpj.2015.100. Epub 2016 Jan 26.
13	Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40.
14	Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
15	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
16	Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
17	A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
18	Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
19	Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.
20	Clinical pipeline report, company report or official report of Exelixis (2011).
21	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
22	Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.
23	Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
24	MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
25	Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
26	Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
27	Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
28	Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
29	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.
30	Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
31	Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
32	The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. Mol Pharmacol. 2007 Jan;71(1):240-9.
33	Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
34	Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
35	Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
36	The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters. Cancer Lett. 2016 Jun 28;376(1):165-72.
37	Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
38	Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
39	Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo. Mol Pharm. 2015 Dec 7;12(12):4259-69.
40	Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
41	Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells. Br J Pharmacol. 2012 Mar;165(6):1836-1847.
42	The effect of SLCO1B115 on the disposition of pravastatin and pitavastatin is substrate dependent: the contribution of transporting activity changes by SLCO1B115. Pharmacogenet Genomics. 2008 May;18(5):424-33.
43	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.
44	Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
45	FDA Drug Development and Drug Interactions
46	LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers. Gastroenterology. 2001 Jun;120(7):1689-99.
47	Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3. Eur J Pharmacol. 2008 Apr 14;584(1):57-65.
48	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.
49	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.
50	Impact of OATP transporters on pharmacokinetics. Br J Pharmacol. 2009 Oct;158(3):693-705.
51	Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
52	Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
53	Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
54	Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
55	Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
56	Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
57	Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
58	The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
59	Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
60	Drug related genetic polymorphisms affecting adverse reactions to methotrexate, vinblastine, doxorubicin and cisplatin in patients with urothelial cancer. J Urol. 2008 Dec;180(6):2389-95.
61	Human prostate CYP3A5: identification of a unique 5'-untranslated sequence and characterization of purified recombinant protein. Biochem Biophys Res Commun. 1999 Jul 14;260(3):676-81.
62	Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett. 2005 Jan 10;217(1):61-72.
63	Induction of hepatic CYP2E1 by a subtoxic dose of acetaminophen in rats: increase in dichloromethane metabolism and carboxyhemoglobin elevation. Drug Metab Dispos. 2007 Oct;35(10):1754-8.
64	Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
65	Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
66	Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
67	Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
68	The role of cytochrome P450 3A (CYP3A) isoform(s) in oxidative metabolism of testosterone and benzphetamine in human adult and fetal liver. J Steroid Biochem Mol Biol. 1993 Jan;44(1):61-7.
69	Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
70	Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites. Drug Metab Dispos. 2004 Feb;32(2):259-66.
71	The role of human cytochrome P450 enzymes in the formation of 2-hydroxymetronidazole: CYP2A6 is the high affinity (low Km) catalyst. Drug Metab Dispos. 2013 Sep;41(9):1686-94.
72	The relative role of CYP3A4 and CYP3A5 in eplerenone metabolism. Toxicol Lett. 2019 Oct 15;315:9-13.
73	Characterization of the structural determinants required for potent mechanism-based inhibition of human cytochrome P450 1A1 by cannabidiol. Chem Biol Interact. 2014 May 25;215:62-8.
74	Retinoids activate the RXR/SXR-mediated pathway and induce the endogenous CYP3A4 activity in Huh7 human hepatoma cells. Toxicol Sci. 2006 Jul;92(1):51-60.
75	The novel azole R126638 is a selective inhibitor of ergosterol synthesis in Candida albicans, Trichophyton spp., and Microsporum canis. Antimicrob Agents Chemother. 2004 Sep;48(9):3272-8.
76	Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s. Drug Metab Dispos. 2001 Jan;29(1):30-5.
77	Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5591-4.
78	Mechanism-based inactivation of CYP3A by HIV protease inhibitors. J Pharmacol Exp Ther. 2005 Feb;312(2):583-91.
79	Studies of the toxicological potential of capsinoids, XIII: inhibitory effects of capsaicin and capsinoids on cytochrome P450 3A4 in human liver microsomes. Int J Toxicol. 2010 Mar;29(2 Suppl):22S-6S.
80	Investigation of the effects of axitinib on the pharmacokinetics of loperamide and its main metabolite N-demethylated loperamide in rats by UPLC-MS/MS. Chem Biol Interact. 2019 Sep 1;310:108744. doi: 10.1016/j.cbi.2019.108744. Epub 2019 Jul 9.
81	Localization of breast cancer resistance protein (Bcrp) in endocrine organs and inhibition of its transport activity by steroid hormones. Cell Tissue Res. 2012 Aug;349(2):551-63. doi: 10.1007/s00441-012-1417-5. Epub 2012 May 13.
82	Pharmacogenetics of ABCG2 and adverse reactions to gefitinib. J Natl Cancer Inst. 2006 Dec 6;98(23):1739-42.
83	ABCG2 polymorphism is associated with the low-density lipoprotein cholesterol response to rosuvastatin. Clin Pharmacol Ther. 2010 May;87(5):558-62.
84	Ciprofloxacin mediates cancer stem cell phenotypes in lung cancer cells through caveolin-1-dependent mechanism. Chem Biol Interact. 2016 Apr 25;250:1-11.
85	Proteomic identification of differentially expressed proteins associated with the multiple drug resistance in methotrexate-resistant human breast cancer cells. Int J Oncol. 2014 Jul;45(1):448-58.
86	Activation of beta-catenin signalling by GSK-3 inhibition increases p-glycoprotein expression in brain endothelial cells. J Neurochem. 2008 Aug;106(4):1855-65. doi: 10.1111/j.1471-4159.2008.05537.x. Epub 2008 Jul 4.
87	Differential gene expression in human hepatocyte cell lines exposed to the antiretroviral agent zidovudine. Arch Toxicol. 2014 Mar;88(3):609-23. doi: 10.1007/s00204-013-1169-3. Epub 2013 Nov 30.
88	Chronic imatinib mesylate exposure leads to reduced intracellular drug accumulation by induction of the ABCG2 (BCRP) and ABCB1 (MDR1) drug transport pumps. Cancer Biol Ther. 2005 Jul;4(7):747-52.
89	Folate deprivation induces BCRP (ABCG2) expression and mitoxantrone resistance in Caco-2 cells. Int J Cancer. 2008 Oct 1;123(7):1712-20.