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

General Information of Drug (ID: DMHZJCG)

Drug Name

Pentamidine Drug Info

Synonyms

Lomidine; Nebupent; PENTAM; PNT; Pentacarinat; Pentamide; Pentamidin; Pentamidina; Pentamidinum; Pneumopent; PENTAMIDINE ISETHIONATE; Pentamidina [DCIT]; Pentamidine isetionate; Pentamidine mesylate; MB 800; Pentam 300; Lomidine (TN); MB-800; Nebupent (as isethionate); Pentacarinat (as isethionate); Pentam 300 (as isethionate); Pentamidine (INN); Pentamidinum [INN-Latin]; RP-2512; Nebupent (*Isethionate); Pentacarinat (*Isethionate); Pentam 300 (*Isethionate); Pentamidine Isethionate 2-Hydroxy-Ethanesulfonic Acid;Pentamidine [INN:BAN:DCF]; RP 2512 (*Isethionate); P,p'-(Pentamethylenedioxy)bis[benzamidine]; P,p'-(Pentamethylenedioxy)dibenzamidine; P,p'-(Pentamethylene-dioxy)bis-benzamidine; Benzenecarboximidamide, 4,4'-(1,5-pentanediylbis(oxy))bis-(9CI); 1,3-BIS(4-AMIDINOPHENOXY)PENTANE; 4, 4'-Diamidinodiphenoxypentane; 4,4'-(1,5-Pentanediylbis(oxy))bis-benzenecarboximidamide; 4,4'-(Pentamethylenedioxy)dibenzamide; 4,4'-(Pentamethylenedioxy)dibenzamidine; 4,4'-Diamidino-.alpha.,.omega.-diphenoxypentane; 4,4'-Diamidinodiphenoxypentane; 4,4'-[pentane-1,5-diylbis(oxy)]dibenzenecarboximidamide; 4-[5-(4-Carbamimidoylphenoxy)pentoxy]benzenecarboximidamide

Indication

Disease Entry	ICD 11	Status	REF
African trypanosomiasis	1F51	Approved	[1]
Fungal infection	1F29-1F2F	Approved	[2]
Pneumocystis pneumonia	CA40.20	Approved	[1]
Human immunodeficiency virus infection	1C62	Withdrawn from market	[3]

Therapeutic Class

Antifungal Agents

Cross-matching ID

PubChem CID: 4735
ChEBI ID: CHEBI:45081
CAS Number: CAS 100-33-4
TTD Drug ID: DMHZJCG
VARIDT Drug ID: DR00085
INTEDE Drug ID: DR1252

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Tryptase alpha/beta-1 (Tryptase)	TTM1TDX	TRYB1_HUMAN	Inhibitor	[4]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
Organic cation transporter 1 (SLC22A1)	DTT79CX	S22A1_HUMAN	Approved	[5]

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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	[6]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Approved	[6]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Approved	[7]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Approved	[6]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Approved	[6]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_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
Tryptase alpha/beta-1 (Tryptase)	DTT	TPSAB1	4.146	8.091	5.053	6.282
Organic cation transporter 1 (SLC22A1)	DTP	`OCT1	10.261	4.162	4.07	3.797
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	9.791	3.744	3.413	1.609
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 2D6 (CYP2D6)	DME	CYP2D6	3.307	5.005	3.921	5.327
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

African trypanosomiasis

ICD Disease Classification

1F51

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Tryptase alpha/beta-1 (Tryptase)	DTT	TPSAB1	3.09E-07	1.07	0.89
Organic cation transporter 1 (SLC22A1)	DTP	SLC22A1	8.27E-06	1.93E-01	5.03E-01
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	2.93E-03	-2.19E-01	-4.49E-01
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	7.57E-07	-1.95E-01	-4.24E-01
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	3.85E-05	8.08E-01	6.07E-01
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	1.65E-02	-4.37E-02	-7.84E-02
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	1.21E-04	-2.33E-01	-5.09E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	6.90E-01	2.35E-02	7.88E-02

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Pentamidine FDA Label
2	Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40.
3	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
4	Inhibitors of tryptase for the treatment of mast cell-mediated diseases. Curr Pharm Des. 1998 Oct;4(5):381-96.
5	Transport of dicationic drugs pentamidine and furamidine by human organic cation transporters. Drug Metab Dispos. 2009 Feb;37(2):424-30.
6	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.
7	Value of preemptive CYP2C19 genotyping in allogeneic stem cell transplant patients considered for pentamidine administration. Clin Transplant. 2011 May-Jun;25(3):E271-5.