General Information of Drug (ID: DMRTD16)

Drug Name
Talinolol Drug Info
Synonyms
Talinolol; 57460-41-0; Cordanum; Racemic talinolol; 1-(4-(3-(TERT-BUTYLAMINO)-2-HYDROXYPROPOXY)PHENYL)-3-CYCLOHEXYLUREA; Talinolol [INN]; (+-)-Talinolol; Talinololum [INN-Latin]; 38649-73-9; 1-(4-Cyclohexylureidophenoxy)-2-hydroxy-3-tert-butylaminopropane; Talinolol (INN); (+-)-N-Cyclohexyl-N'-(4-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy)phenyl)urea; NCGC00164542-01; 1-(4-(cyclohexylureido)phenoxy)-3-(tert-butylamino)-2-propanol; 1-(3-(3-Cyclohexylureido)phenoxy)-3-(tert-butylamino)-2-propanol
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
68770
ChEBI ID
CHEBI:135533
CAS Number
CAS 57460-41-0
TTD Drug ID
DMRTD16
VARIDT Drug ID
DR00401
INTEDE Drug ID
DR1527

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTP
DME
Drug Status:
Approved Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [7]
Progesterone DMUY35B Premature labour JB00 Approved [8]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [9]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [10]
Acetaminophen DMUIE76 Pain MG30-MG3Z Approved [11]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [12]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [13]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [14]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [8]
Verapamil DMA7PEW Hypertension BA00-BA04 Approved [15]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [16]
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [17]
Folic acid DMEMBJC Folate-deficiency anemia 3A02.Y Approved [18]
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [19]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [20]
Cisplatin DMRHGI9 Solid tumour/cancer 2A00-2F9Z Approved [21]
Acetaminophen DMUIE76 Pain MG30-MG3Z Approved [22]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [23]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [24]
Oxaliplatin DMQNWRD Colorectal cancer 2B91.Z Approved [25]
⏷ 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 Bacterial infection 1A00-1C4Z Approved [26]
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [27]
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [28]
Folic acid DMEMBJC Folate-deficiency anemia 3A02.Y Approved [29]
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [28]
Cisplatin DMRHGI9 Solid tumour/cancer 2A00-2F9Z Approved [28]
Progesterone DMUY35B Premature labour JB00 Approved [30]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [28]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [31]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [32]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [33]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [34]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [35]
Atorvastatin DMF28YC Cardiovascular disease BA00-BE2Z Approved [36]
Pitavastatin calcium DM1UJO0 Dyslipidemia 5C80-5C81 Approved [37]
Rosuvastatin DMMIQ7G Hypercholesterolaemia 5C80.0 Approved [38]
Saquinavir DMG814N Human immunodeficiency virus infection 1C62 Approved [39]
Enalapril DMNFUZR Hypertension BA00-BA04 Approved [40]
Cholic acid DM7OKQV Peroxisomal disorder 5C57 Approved [41]
Liothyronine DM6IR3P Hypothyroidism 5A00 Approved [42]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [43]
L-glutamic acid DM4PUDW Schizophrenia 6A20 Approved [44]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [45]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [46]
Pravastatin DM6A0X7 Hypercholesterolaemia 5C80.0 Approved [47]
Atorvastatin DMF28YC Cardiovascular disease BA00-BE2Z Approved [48]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [49]
Pitavastatin calcium DM1UJO0 Dyslipidemia 5C80-5C81 Approved [50]
Digoxin DMQCTIH Arrhythmia BC9Z Approved [51]
Rosuvastatin DMMIQ7G Hypercholesterolaemia 5C80.0 Approved [52]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [2]
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Substrate [3]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Substrate [4]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [6]

References

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2 FDA Drug Development and Drug Interactions
3 Species difference in the effect of grapefruit juice on intestinal absorption of talinolol between human and rat. J Pharmacol Exp Ther. 2010 Jan;332(1):181-9.
4 Concentration-dependent effect of naringin on intestinal absorption of beta(1)-adrenoceptor antagonist talinolol mediated by p-glycoprotein and organic anion transporting polypeptide (Oatp). Pharm Res. 2009 Mar;26(3):560-7.
5 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.
6 Stereoselective disposition of talinolol in man. J Pharm Sci. 2002 Feb;91(2):303-11.
7 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.
8 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
9 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.
10 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
11 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.
12 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.
13 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
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15 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.
16 Involvement of the drug transporters p glycoprotein and multidrug resistance-associated protein Mrp2 in telithromycin transport. Antimicrob Agents Chemother. 2006 Jan;50(1):80-7.
17 Dose-dependent disposition of methotrexate in Abcc2 and Abcc3 gene knockout murine models. Drug Metab Dispos. 2011 Nov;39(11):2155-61.
18 Mammalian multidrug-resistance proteins (MRPs). Essays Biochem. 2011 Sep 7;50(1):179-207.
19 Enhancing chemosensitivity in oral squamous cell carcinoma by lentivirus vector-mediated RNA interference targeting EGFR and MRP2. Oncol Lett. 2016 Sep;12(3):2107-2114.
20 Multidrug resistance associated protein 2 mediates transport of prostaglandin E2. Liver Int. 2006 Apr;26(3):362-8.
21 Lentivirus-mediated RNAi silencing targeting ABCC2 increasing the sensitivity of a human nasopharyngeal carcinoma cell line against cisplatin. J Transl Med. 2008 Oct 4;6:55.
22 Effect of acetaminophen on expression and activity of rat liver multidrug resistance-associated protein 2 and P-glycoprotein. Biochem Pharmacol. 2004 Aug 15;68(4):791-8.
23 Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting. Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G371-7.
24 Delineating the contribution of secretory transporters in the efflux of etoposide using Madin-Darby canine kidney (MDCK) cells overexpressing P-glycoprotein (Pgp), multidrug resistance-associated protein (MRP1), and canalicular multispecific organic anion transporter (cMOAT). Drug Metab Dispos. 2002 Apr;30(4):457-63.
25 Multidrug Resistance-Associated Protein 2 (MRP2) Mediated Transport of Oxaliplatin-Derived Platinum in Membrane Vesicles. PLoS One. 2015 Jul 1;10(7):e0130727.
26 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
27 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
28 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.
29 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
30 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
31 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
32 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.
33 Interaction of methotrexate with organic-anion transporting polypeptide 1A2 and its genetic variants. J Pharmacol Exp Ther. 2006 Aug;318(2):521-9.
34 Localization of organic anion transporting polypeptide 4 (Oatp4) in rat liver and comparison of its substrate specificity with Oatp1, Oatp2 and Oatp3. Pflugers Arch. 2001 Nov;443(2):188-95.
35 Environmental and genetic factors affecting transport of imatinib by OATP1A2. Clin Pharmacol Ther. 2011 Jun;89(6):816-20.
36 Influence of the flavonoids apigenin, kaempferol, and quercetin on the function of organic anion transporting polypeptides 1A2 and 2B1. Biochem Pharmacol. 2010 Dec 1;80(11):1746-53.
37 Transporter-mediated influx and efflux mechanisms of pitavastatin, a new inhibitor of HMG-CoA reductase. J Pharm Pharmacol. 2005 Oct;57(10):1305-11.
38 Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology. 2006 May;130(6):1793-806.
39 Human organic anion-transporting polypeptide OATP-A (SLC21A3) acts in concert with P-glycoprotein and multidrug resistance protein 2 in the vectorial transport of Saquinavir in Hep G2 cells. Mol Pharm. 2004 Jan 12;1(1):49-56.
40 Uptake of enalapril and expression of organic anion transporting polypeptide 1 in zonal, isolated rat hepatocytes. Drug Metab Dispos. 2000 Jul;28(7):801-6.
41 Molecular and functional characterization of an organic anion transporting polypeptide cloned from human liver. Gastroenterology. 1995 Oct;109(4):1274-82.
42 Identification of thyroid hormone transporters in humans: different molecules are involved in a tissue-specific manner. Endocrinology. 2001 May;142(5):2005-12.
43 Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60.
44 The Transporter Classification Database (TCDB): recent advances. Nucleic Acids Res. 2016 Jan 4;44(D1):D372-9. (ID: 2.A.60.1.20)
45 Small-Dosing Clinical Study: Pharmacokinetic, Pharmacogenomic (SLCO2B1 and ABCG2), and Interaction (Atorvastatin and Grapefruit Juice) Profiles of 5 Probes for OATP2B1 and BCRP. J Pharm Sci. 2017 Sep;106(9):2688-2694.
46 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.
47 Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. J Pharmacol Exp Ther. 2004 Feb;308(2):438-45.
48 Human platelets express organic anion-transporting peptide 2B1, an uptake transporter for atorvastatin. Drug Metab Dispos. 2009 May;37(5):1129-37.
49 pH-sensitive interaction of HMG-CoA reductase inhibitors (statins) with organic anion transporting polypeptide 2B1. Mol Pharm. 2011 Aug 1;8(4):1303-13.
50 Drug-drug interaction between pitavastatin and various drugs via OATP1B1. Drug Metab Dispos. 2006 Jul;34(7):1229-36.
51 Drug Interactions in Infectious Diseases.
52 Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos. 2008 Oct;36(10):2014-23.