General Information of Drug (ID: DMU79X2)

Drug Name
YM-758 Drug Info
Synonyms
YM 758 Phosphate; (R)-(-)-N-[2-[3-[(6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)carbonyl]piperidino]ethyl]-4-fluorobenzamide monophosphate; YM 758; N-[2-[(3R)-3-[(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)carbonyl]-1-piperidinyl]ethyl]-4-fluorobenzamide Phosphate
Indication
Disease Entry ICD 11 Status REF
Angina pectoris BA40 Phase 2 [1]
Cross-matching ID
PubChem CID
9894205
CAS Number
CAS 312752-85-5
TTD Drug ID
DMU79X2
VARIDT Drug ID
DR01466

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTP
DOT
Drug Status:
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [4]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [2]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [5]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [6]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [5]
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [7]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [8]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [9]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [10]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [7]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Eplerenone DMF0NQR Heart failure BD10-BD13 Approved [11]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [12]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [13]
Voriconazole DMAOL2S Aspergillosis 1F20 Approved [14]
Proguanil DMBL79I Malaria 1F40-1F45 Approved [15]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [15]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [16]
Nelfinavir mesylate DMFX6G8 N. A. N. A. Approved [17]
Capsaicin DMGMF6V Back pain ME84.Z Approved [18]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [19]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Cytochrome P450 2D6 (CYP2D6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [20]
Paliperidone DM7NPJS Psychotic disorder 6A20-6A25 Approved [21]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [22]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [23]
Oxatomide DM1F42Z Hay fever CA08.00 Approved [24]
Cinacalcet DMCX0K3 Hyperparathyroidism 5A51 Approved [25]
Capsaicin DMGMF6V Back pain ME84.Z Approved [26]
Pentamidine DMHZJCG African trypanosomiasis 1F51 Approved [15]
Quinidine DMLPICK N. A. N. A. Approved [27]
Buprenorphine DMPRI8G Opioid dependence 6C43.2Z Approved [28]
⏷ 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
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cytochrome P450 2D6 (CYP2D6) OTZJC802 CP2D6_HUMAN Regulation of Drug Effects [3]
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Gene/Protein Processing [3]

References

1 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024920)
2 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
3 Evaluation of the inhibitory and induction potential of YM758, a novel If channel inhibitor, for human P450-mediated metabolism. Eur J Drug Metab Pharmacokinet. 2008 Oct-Dec;33(4):211-23. doi: 10.1007/BF03190875.
4 Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo. Mol Pharm. 2015 Dec 7;12(12):4259-69.
5 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
6 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.
7 The effect of SLCO1B1*15 on the disposition of pravastatin and pitavastatin is substrate dependent: the contribution of transporting activity changes by SLCO1B1*15. Pharmacogenet Genomics. 2008 May;18(5):424-33.
8 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.
9 Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
10 FDA Drug Development and Drug Interactions
11 The relative role of CYP3A4 and CYP3A5 in eplerenone metabolism. Toxicol Lett. 2019 Oct 15;315:9-13.
12 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.
13 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.
14 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.
15 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.
16 Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5591-4.
17 Mechanism-based inactivation of CYP3A by HIV protease inhibitors. J Pharmacol Exp Ther. 2005 Feb;312(2):583-91.
18 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.
19 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.
20 Human recombinant cytochrome P450 enzymes display distinct hydrogen peroxide generating activities during substrate independent NADPH oxidase reactions. Toxicol Sci. 2014 Oct;141(2):344-52. doi: 10.1093/toxsci/kfu133. Epub 2014 Jul 24.
21 Cytochrome P450 2D6 genotype and steady state plasma levels of risperidone and 9-hydroxyrisperidone. Psychopharmacology (Berl). 1999 Dec;147(3):300-5. doi: 10.1007/s002130051171.
22 Effect of penicillin-based antibiotics, amoxicillin, ampicillin, and piperacillin, on drug-metabolizing activities of human hepatic cytochromes P450. J Toxicol Sci. 2016 Feb;41(1):143-6.
23 Cannabidiol, a major phytocannabinoid, as a potent atypical inhibitor for CYP2D6. Drug Metab Dispos. 2011 Nov;39(11):2049-56. doi: 10.1124/dmd.111.041384. Epub 2011 Aug 5.
24 Identification of human P450 isoforms involved in the metabolism of the antiallergic drug, oxatomide, and its kinetic parameters and inhibition constants. Biol Pharm Bull. 2005 Feb;28(2):328-34.
25 Pharmacokinetics of desipramine HCl when administered with cinacalcet HCl. Eur J Clin Pharmacol. 2007 Feb;63(2):159-63.
26 Effects of capsaicin and dihydrocapsaicin on human and rat liver microsomal CYP450 enzyme activities in vitro and in vivo. J Asian Nat Prod Res. 2012;14(4):382-95.
27 Inhibition of cytochrome P4502D6 activity with paroxetine normalizes the ultrarapid metabolizer phenotype as measured by nortriptyline pharmacokinetics and the debrisoquin test. Clin Pharmacol Ther. 2001 Oct;70(4):327-35.
28 Interaction of buprenorphine and its metabolite norbuprenorphine with cytochromes p450 in vitro. Drug Metab Dispos. 2003 Jun;31(6):768-72.