Details of the Drug

General Information of Drug (ID: DMOMBJW)

Drug Name

Moricizine

Synonyms

Moracizin; Moracizina; Moracizine; Moracizinum; Moricizine [USAN]; G 214; EN-313; Moracizina [INN-Spanish]; Moracizine (INN); Moracizinum [INN-Latin]; Moricizine (USAN); Ethyl 10-(3-morpholinopropionyl)phenothiazine-2-carbamate; Ethyl 10-(beta-N-morpholinylpropionyl)phenothiazine-2-carbamate; Ethyl N-[10-(3-morpholin-4-ylpropanoyl)phenothiazin-2-yl]carbamate; Phenothiazine-2-carbamic acid, 10-(3-morpholinopropionyl)-, ethyl ester; Ethyl [10-(3-morpholin-4-ylpropanoyl)-10H-phenothiazin-2-yl]carbamate; Ethyl {10-[3-(morpholin-4-yl)propanoyl]-10H-phenothiazin-2-yl}carbamate; Ethyl N-{10-[3-(morpholin-4-yl)propanoyl]-10H-phenothiazin-2-yl}carbamate; Ethyl (10-(3-(4-morpholinyl)-1-oxopropyl)-10H-phenothiazin-2-yl)carbamate; Carbamic acid, (10-(3-(4-morpholinyl)-1-oxopropyl)-10H-phenothiazin-2-yl)-, ethyl ester

Indication

Disease Entry	ICD 11	Status	REF
Arrhythmia	BC9Z	Approved	[1]
Long QT syndrome	BC65.0	Approved	[2]
Heart arrhythmia	BC65	Withdrawn from market	[3]
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Therapeutic Class

Antiarrhythmic Agents

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

427.5

Logarithm of the Partition Coefficient (xlogp)

3

Rotatable Bond Count (rotbonds)

6

Hydrogen Bond Donor Count (hbonddonor)

1

Hydrogen Bond Acceptor Count (hbondacc)

6

ADMET Property

Half-life: The concentration or amount of drug in body reduced by one-half in 2 (range 1.5 - 3.5) hours [4]
Metabolism: The drug is metabolized via the hepatic []
Vd: The volume of distribution (Vd) of drug is 300 L []

Chemical Identifiers

Formula: C22H25N3O4S
IUPAC Name: ethyl N-[10-(3-morpholin-4-ylpropanoyl)phenothiazin-2-yl]carbamate
Canonical SMILES: CCOC(=O)NC1=CC2=C(C=C1)SC3=CC=CC=C3N2C(=O)CCN4CCOCC4
InChI: InChI=1S/C22H25N3O4S/c1-2-29-22(27)23-16-7-8-20-18(15-16)25(17-5-3-4-6-19(17)30-20)21(26)9-10-24-11-13-28-14-12-24/h3-8,15H,2,9-14H2,1H3,(H,23,27)
InChIKey: FUBVWMNBEHXPSU-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 34633
ChEBI ID: CHEBI:6997
CAS Number: 31883-05-3
DrugBank ID: DB00680
TTD ID: D04VPA
ACDINA ID: D00446

Combinatorial Drugs (CBD)

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Repurposed Drugs (RPD)

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Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Voltage-gated sodium channel alpha Nav1.5 (SCN5A)	TTZOVE0	SCN5A_HUMAN	Blocker	[5]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Cytochrome P450 2B6 (CYP2B6)	OTOYO4S7	CP2B6_HUMAN	Gene/Protein Processing	[6]
Cytochrome P450 3A4 (CYP3A4)	OTQGYY83	CP3A4_HUMAN	Gene/Protein Processing	[6]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Moricizine (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Pasireotide	DMHM7JS	Moderate	Increased risk of bradycardia by the combination of Moricizine and Pasireotide.	Cushing syndrome [5A70]	[7]
Siponimod	DM2R86O	Major	Increased risk of atrioventricular block by the combination of Moricizine and Siponimod.	Multiple sclerosis [8A40]	[8]
Fingolimod	DM5JVAN	Moderate	Increased risk of bradycardia by the combination of Moricizine and Fingolimod.	Multiple sclerosis [8A40]	[9]
Ozanimod	DMT6AM2	Moderate	Increased risk of atrioventricular block by the combination of Moricizine and Ozanimod.	Multiple sclerosis [8A40]	[10]
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
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Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Moricizine 200 mg tablet	200 mg	Oral Tablet	Oral
Moricizine 250 mg tablet	250 mg	Oral Tablet	Oral
Moricizine 300 mg tablet	300 mg	Oral Tablet	Oral

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References

1	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2	Moricizine FDA Label
3	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: 7244).
4	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
5	From first class to third class: recent upheaval in antiarrhythmic therapy--lessons from clinical trials. Am J Cardiol. 1996 Aug 29;78(4A):28-33.
6	Comparison of immortalized Fa2N-4 cells and human hepatocytes as in vitro models for cytochrome P450 induction. Drug Metab Dispos. 2008 Jun;36(6):1046-55.
7	Canadian Pharmacists Association.
8	Cerner Multum, Inc. "Australian Product Information.".
9	Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
10	Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.