General Information of Drug (ID: DMH6NG5)

Drug Name
FENDILINE Drug Info
Synonyms
fendiline; Fendilin; 13042-18-7; Fendilinum; Fendilinum [INN-Latin]; Fendilina [INN-Spanish]; Fendiline [INN]; EINECS 235-915-6; CHEMBL254832; Fendiline (INN); Benzenepropanamine, gamma-phenyl-N-(1-phenylethyl)-; Benzenepropanamine, .gamma.-phenyl-N-(1-phenylethyl)-; 3,3-diphenyl-N-(1-phenylethyl)propan-1-amine; Phendilin; Fendilina; Senzit; NCGC00018223-06; SPBio_001131; Spectrum_000443; AC1L1FPB; Spectrum5_001302; Spectrum2_001006; Prestwick1_000270; Spectrum4_000417; Prestwick3_000270; Spectrum3_001436; Prestwick2_000270
Indication
Disease Entry ICD 11 Status REF
Coronary artery disease BA80 Withdrawn from market [1]
Cross-matching ID
PubChem CID
3336
ChEBI ID
CHEBI:94434
CAS Number
CAS 13042-18-7
TTD Drug ID
DMH6NG5
VARIDT Drug ID
DR00949
INTEDE Drug ID
DR0686

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Drug(s) Targeting 5-HT 2B receptor (HTR2B)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [5]
Triflupromazine DMKFQJP Nausea MD90 Approved [6]
Minaprine DM0EP7M Depression 6A70-6A7Z Approved [7]
SPN-812 DMTV7XH Attention deficit hyperactivity disorder 6A05.Z Phase 4 [8]
Vabicaserin DM9GZW6 Psychotic disorder 6A20-6A25 Phase 2 [9]
PRX-08066 DMR7H2V Pulmonary arterial hypertension BB01.0 Phase 2 [10]
Pyrimidine derivative 29 DMVOYJ8 N. A. N. A. Patented [11]
Pyrimidine derivative 26 DM90WKN N. A. N. A. Patented [11]
Pyrimidine derivative 23 DM5MLQU N. A. N. A. Patented [11]
Pyrimidine derivative 25 DM51MFS N. A. N. A. Patented [11]
⏷ Show the Full List of 10 Drug(s)
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 [12]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [13]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [14]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [15]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [16]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [17]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [18]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [19]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [13]
Verapamil DMA7PEW Angina pectoris BA40 Approved [20]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metoclopramide DMFA5MY Nausea MD90 Approved [21]
Quinidine DMLPICK N. A. N. A. Approved [22]
Verapamil DMA7PEW Angina pectoris BA40 Approved [23]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [24]
Clarithromycin DM4M1SG Acute maxillary sinusitis Approved [24]
Disopyramide DM5SYZP Long QT syndrome BC65.0 Approved [25]
Propranolol DM79NTF Angina pectoris BA40 Approved [26]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [27]
Dofetilide DMPN1TW Sinus rhythm disorder BC9Y Approved [28]
Flecainide DMSQDLE Tachyarrhythmias BC71 Approved [24]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 2B receptor (HTR2B) TT0K1SC 5HT2B_HUMAN Inhibitor [2]

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

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Potassium voltage-gated channel subfamily H member 2 (KCNH2) OTZX881H KCNH2_HUMAN Gene/Protein Processing [4]

References

1 Value of fendiline in the treatment of patients with stable angina pectoris. Pol Tyg Lek. 1987 Nov 16;42(46):1456-8.
2 Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify no... J Med Chem. 2010 Nov 11;53(21):7573-86.
3 Integrated analysis on the physicochemical properties of dihydropyridine calcium channel blockers in grapefruit juice interactions. Curr Pharm Biotechnol. 2012 Jul;13(9):1705-17.
4 Why are most phospholipidosis inducers also hERG blockers?. Arch Toxicol. 2017 Dec;91(12):3885-3895. doi: 10.1007/s00204-017-1995-9. Epub 2017 May 27.
5 Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23.
6 Some properties of 5-hydroxytryptamine receptors in the hindquarters of the rat. Br J Pharmacol. 1979 Sep;67(1):79-85.
7 Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
8 New Insights into the Mechanism of Action of Viloxazine: Serotonin and Norepinephrine Modulating Properties. J Exp Pharmacol. 2020 Aug 25;12:285-300.
9 Prediction of Efficacy of Vabicaserin, a 5-HT2C Agonist, for the Treatment of Schizophrenia Using a Quantitative Systems Pharmacology Model.CPT Pharmacometrics Syst Pharmacol.2014 Apr 23;3:e111.
10 Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
11 Novel serotonin receptor 2 (5-HT2R) agonists and antagonists: a patent review (2004-2014).Expert Opin Ther Pat. 2016;26(1):89-106.
12 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.
13 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
14 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.
15 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
16 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.
17 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.
18 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
19 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.
20 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.
21 Comparison of the effects of metoclopramide and domperidone on HERG channels. Pharmacology. 2005 Apr;74(1):31-6. doi: 10.1159/000083234. Epub 2005 Jan 7.
22 Further insights into the effect of quinidine in short QT syndrome caused by a mutation in HERG. J Cardiovasc Electrophysiol. 2005 Jan;16(1):54-8. doi: 10.1046/j.1540-8167.2005.04470.x.
23 Automated tight seal electrophysiology for assessing the potential hERG liability of pharmaceutical compounds. Assay Drug Dev Technol. 2004 Oct;2(5):497-506. doi: 10.1089/adt.2004.2.497.
24 Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model. Toxicol Sci. 2013 Dec;136(2):581-94. doi: 10.1093/toxsci/kft205. Epub 2013 Sep 19.
25 Pharmacology of the short QT syndrome N588K-hERG K+ channel mutation: differential impact on selected class I and class III antiarrhythmic drugs. Br J Pharmacol. 2008 Nov;155(6):957-66. doi: 10.1038/bjp.2008.325. Epub 2008 Aug 25.
26 Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy. Br J Pharmacol. 2006 Mar;147(6):642-52. doi: 10.1038/sj.bjp.0706508.
27 Inhibitory effects of the class III antiarrhythmic drug amiodarone on cloned HERG potassium channels. Naunyn Schmiedebergs Arch Pharmacol. 1999 Mar;359(3):212-9. doi: 10.1007/pl00005344.
28 Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation. FEBS Lett. 2000 May 26;474(1):111-5. doi: 10.1016/s0014-5793(00)01586-6.