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

General Information of Drug (ID: DMOU1PK)

Drug Name

Praziquantel Drug Info

Synonyms

Azinox; Biliricide; Biltricide; Cesol; Cisticid; Cutter; Cysticide; Droncit; Drontsit; Prasiquantel; Praziquantelum; Pyquiton; Traziquantel; Bayer Brand of Praziquantel; Cutter Tape Tabs; Merck Brand of Praziquantel; Embay 8440; P 4668; Bay-8440; Biltricide (TN); EMBAY-8440; NPFAPI-02; Praziquantelum [INN-Latin]; Biltricide, Droncit, Praziquantel; Praziquantel (JAN/USP/INN); Praziquantel [USAN:INN:BAN:JAN]; Praziquantel, (R)-Isomer; Praziquantel, (S)-Isomer; Praziquantel, (+-)-Isomer; (+-)-2-(Cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-4H-pyrazino(2,1a)isoquinolin-4-one; (11bS)-2-(cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinolin-4-one; 2-(Cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-4H-pyrazino(2,1-a)isoquinolin-4-one; 2-(Cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]-isoquinolin-4-one; 2-(Cyclohexylcarbonyl)-1,2,3,6,7-11b-hexahydro-4H-pyrazino(2,1a)isoquinolin-4-one; 2-(Cyclohexylcarbonyl)-1,2,3,6,7-11b-hexahydro-4H-pyrazinoe(2,1a)isoquinolin-4-one; 2-(cyclohexanecarbonyl)-3,6,7,11b-tetrahydro-1H-pyrazino[2,1-a]isoquinolin-4-one; 2-(cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinolin-4-one; 2-Cyclohexanecarbonyl-1,2,3,6,7,11b-hexahydro-pyrazino[2,1-a]isoquinolin-4-one; 2-Cyclohexylcarbonyl-1,2,3,6,7,11b-hexahydro-4H-pyrazino(2,1-a) isoquinolin-4-one; 8440, EMBAY

Indication

Disease Entry	ICD 11	Status	REF
Flatworm infection	1F70-1F86	Approved	[1]
Opisthorchiasis		Approved	[2]
Schistosomiasis	1F86	Approved	[2]

Therapeutic Class

Anthelmintics

Cross-matching ID

PubChem CID: 4891
ChEBI ID: CHEBI:91583
CAS Number: CAS 55268-74-1
TTD Drug ID: DMOU1PK
INTEDE Drug ID: DR1329
ACDINA Drug ID: D00549

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Glutathione-dependent PGD synthase (HPGDS)	TTCYE56	HPGDS_HUMAN	Inhibitor	[3]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Approved	[4]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Approved	[5]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Approved	[5]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Approved	[6]
Cytochrome P450 3A7 (CYP3A7)	DERD86B	CP3A7_HUMAN	Approved	[6]
Cytochrome P450 3A43 (CYP3A43)	DEO1IE3	CP343_HUMAN	Approved	[6]

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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Glutathione-dependent PGD synthase (HPGDS)	DTT	HPGDS	6.186	5.744	5.641	7.445
Cytochrome P450 3A43 (CYP3A43)	DME	CYP3A43	8.111	5.075	4.174	6.12
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	10.036	5.779	6.508	6.481
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	10.08	7.207	5.403	9.211
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	7.867	5.142	5.52	7.08
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	11.692	6.58	4.984	9.089

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Flatworm infection

ICD Disease Classification

1F70-1F86

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Glutathione-dependent PGD synthase (HPGDS)	DTT	HPGDS	1.63E-05	0.34	0.71
Cytochrome P450 3A43 (CYP3A43)	DME	CYP3A43	1.55E-01	-2.09E-02	-1.34E-01
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	7.36E-01	1.62E-02	1.08E-01
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	9.96E-01	-3.17E-03	-1.84E-02
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	2.40E-01	-3.31E-02	-1.97E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	1.04E-02	6.29E-02	3.54E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40.
2	Praziquantel FDA Label
3	X-ray structure of glutathione S-transferase from Schistosoma japonicum in a new crystal form reveals flexibility of the substrate-binding site. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2005 Mar 1;61(Pt 3):263-5.
4	Biotransformation of praziquantel by human cytochrome p450 3A4 (CYP 3A4). Acta Pol Pharm. 2006 Sep-Oct;63(5):381-5.
5	Identification of human cytochrome P(450)s that metabolise anti-parasitic drugs and predictions of in vivo drug hepatic clearance from in vitro data. Eur J Clin Pharmacol. 2003 Sep;59(5-6):429-42.
6	Rifampin markedly decreases plasma concentrations of praziquantel in healthy volunteers. Clin Pharmacol Ther. 2002 Nov;72(5):505-13.