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

General Information of Drug (ID: DM4KI7O)

Drug Name

Zidovudine Drug Info

Synonyms

zidovudine; Azidothymidine; 30516-87-1; 3'-Azido-3'-deoxythymidine; Retrovir; AZT; Zidovudinum; Compound S; Thymidine, 3'-azido-3'-deoxy-; ZIDOVUDINE [AZT]; zidovudin; BW A509U; Zidovudinum [Latin]; Zidovudina [Spanish]; BWA509U; DRG-0004; 3'-Azido-2',3'-Dideoxythymidine; ZDV; UNII-4B9XT59T7S; 3'-Deoxy-3'-azidothymidine; CCRIS 105; Aztec; BW-A509U; BW-A-509U; HSDB 6515; 3'-Azido-3'-deoxythymidine (AIDS); CHEMBL129; NSC 602670; BW-A 509U; MLS000028548; 4B9XT59T7S; AZT; Antiviral; Azidodeoxythymidine; ZVD; Zidovudin; Zidovudina; AZT Antiviral; AZT TRANSPLACENTAL CARCINOGENESIS STUDY; Antiviral AZT; Cpd S; Racemic Liposomal AZT; Zidovudine EP III; BWA 509U; K7 [P Ti2 W10 O40]; AZT & EPO; AZT & HPA; AZT & Lymphoblastoid Interferon; AZT & SST; AZT & rsT4; AZT & sCD4; AZT & srCD4; AZT (Antiviral); AZT+PRO 140; AZT, Antiviral; Apo-Zidovudine; BWA-509U; Intron A & AZT; Novo-Azt; Propolis+AZT; Retrovir (TN); Retrovir(TM); Retrovis (TN); Zidovudine+PRO 140; AZT & Colony-stimulating factor 2; AZT & Concanavalin A (ConA); AZT & GM-CSF; AZT & IFN-alpha; AZT & IL-1; AZT & IL-2; AZT & IL-6; AZT & Li & EPO; AZT & NP (from PHCA or HSA); AZT & PM-19; DS-4152 & AZT; Liposomal AZT-SN-1; Liposomal AZT-SN-3; PC-SOD+AZT;RIFN-beta seron & AZT; AZT & CD4(178)-PE 40; AZT & Li & GM-CSF; AZT & Li & IL-1; AZT & Li & IL-6; AZT & rIFNalpha2; Racemic-dipalmitoylglycerophospho-AZT (in a lipid vesicle); Zidovudine (JAN/USP/INN); Zidovudine [USAN:INN:BAN:JAN]; AZT & rsCD4 & rIFNalphaA; SN-1-dipalmitoylglycerophospho-AZT (in a lipid vesicle); SN-3-dipalmitoylglycerophospho-AZT (in a lipid vesicle); AZT & Interferon-alpha-2; Met-SDF-1beta & AZT; Met-SDF-1beta & Zidovudine; Interferon AD + 3'-azido-3'-deoxythymidine; 1-(3-Azido-2,3-dideoxy-beta-D-ribofuranosyl)thymine; 3′-Azido-3′-deoxythymidine; 3' Azido 2',3' Dideoxythymidine; 3' Azido 3' deoxythymidine; 3'-Azido-3'-deoxythymidine & Concanavalin A; 3'-Azido-3'-deoxythymidine & Erythropoietin; 3'-Azido-3'-deoxythymidine & Heteropolyoxotungstate PM-19; 3'-Azido-3'-deoxythymidine & Interleukin-1; 3'-Azido-3'-deoxythymidine & Interleukin-2; 3'-Azido-3'-deoxythymidine & Interleukin-6; 3'-Azido-3'-deoxythymidine & Lithium & Erythropoietin; 3'-Azido-3'-deoxythymidine & Lithium & Interleukin-1; 3'-Azido-3'-deoxythymidine & Lithium & Interleukin-6; 3'-Azido-3'-deoxythymidine & Lymphoblastoid Interferon; 3'-Azido-3'-deoxythymidine & Sho-Saiko-To; 3'-Azido-3'deoxythymidine & Interferon-alpha; 3'-Azidothymidine; 3'-azido-3'-deoxythymidine, AZT; 3-Azido-3-deoxythymidine; Dendrigen; CTCE-0422

Indication

Disease Entry	ICD 11	Status	REF
Human immunodeficiency virus infection	1C62	Approved	[1]
Diarrhea	ME05.1	Investigative	[2]
Nephropathy	GC2Z	Investigative	[2]
Virus infection	1A24-1D9Z	Investigative	[3]

Therapeutic Class

Anti-HIV Agents

Cross-matching ID

PubChem CID: 35370
ChEBI ID: CHEBI:10110
CAS Number: CAS 30516-87-1
TTD Drug ID: DM4KI7O
VARIDT Drug ID: DR00296
INTEDE Drug ID: DR1729
ACDINA Drug ID: D00739

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Fms-like tyrosine kinase 3 (FLT-3)	TTGJCWZ	FLT3_HUMAN	Binder	[4]
Human immunodeficiency virus Reverse transcriptase (HIV RT)	TT84ETX	POL_HV1B1	Inhibitor	[5]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
Organic anion transporter 2 (SLC22A7)	DT0OC1Q	S22A7_HUMAN	Approved	[6]
Organic anion transporter 4 (SLC22A11)	DT06JWZ	S22AB_HUMAN	Approved	[6]
Multidrug resistance-associated protein 4 (ABCC4)	DTCSGPB	MRP4_HUMAN	Approved	[7]
Organic cation transporter 1 (SLC22A1)	DTT79CX	S22A1_HUMAN	Approved	[7]
Breast cancer resistance protein (ABCG2)	DTI7UX6	ABCG2_HUMAN	Approved	[8]
Organic anion transporter 1 (SLC22A6)	DTQ23VB	S22A6_HUMAN	Approved	[6]
Organic anion transporter 3 (SLC22A8)	DTVP67E	S22A8_HUMAN	Approved	[6]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[9]

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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	[10]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Approved	[11]
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DEYGVN4	UD11_HUMAN	Approved	[12]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Approved	[11]
Cytochrome P450 2A6 (CYP2A6)	DEJVYAZ	CP2A6_HUMAN	Approved	[11]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Approved	[11]
UDP-glucuronosyltransferase 2B7 (UGT2B7)	DEB3CV1	UD2B7_HUMAN	Approved	[13]

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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
Organic anion transporter 3 (SLC22A8)	DTP	OAT3	2.722	2.07	8.103	3.597
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Organic cation transporter 1 (SLC22A1)	DTP	`OCT1	10.261	4.162	4.07	3.797
Organic anion transporter 1 (SLC22A6)	DTP	OAT1	4.413	2.233	7.194	4.655
Breast cancer resistance protein (ABCG2)	DTP	BCRP	6.732	7.513	6.326	9.277
Multidrug resistance-associated protein 4 (ABCC4)	DTP	MRP4	4.797	7.054	6.875	5.42
Organic anion transporter 2 (SLC22A7)	DTP	OAT2	6.588	1.202	4.42	4.07
Organic anion transporter 4 (SLC22A11)	DTP	OAT4	1.926	2.585	6.595	3.336
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	9.791	3.744	3.413	1.609
Cytochrome P450 2A6 (CYP2A6)	DME	CYP2A6	10.644	6.631	6.598	6.937
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	7.867	5.142	5.52	7.08
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	11.76	5.931	6.164	9.423
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

Human immunodeficiency virus infection

ICD Disease Classification

1C62

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Fms-like tyrosine kinase 3 (FLT-3)	DTT	FLT3	2.11E-01	-0.05	-0.16
Organic anion transporter 3 (SLC22A8)	DTP	OAT3	5.19E-01	-8.88E-03	-2.08E-02
P-glycoprotein 1 (ABCB1)	DTP	P-GP	9.39E-02	1.07E-01	2.80E-01
Organic cation transporter 1 (SLC22A1)	DTP	SLC22A1	8.54E-01	1.24E-02	7.20E-02
Organic anion transporter 1 (SLC22A6)	DTP	OAT1	7.18E-01	-4.56E-02	-1.42E-01
Breast cancer resistance protein (ABCG2)	DTP	BCRP	9.45E-01	-5.34E-02	-9.01E-02
Multidrug resistance-associated protein 4 (ABCC4)	DTP	MRP4	3.73E-06	2.82E-01	7.01E-01
Organic anion transporter 2 (SLC22A7)	DTP	OAT2	5.96E-02	-5.09E-02	-3.48E-01
Organic anion transporter 4 (SLC22A11)	DTP	OAT4	4.61E-04	-7.04E-02	-3.49E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	1.10E-01	-5.91E-02	-3.60E-01
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	1.82E-04	-1.35E-01	-5.84E-01
Cytochrome P450 2A6 (CYP2A6)	DME	CYP2A6	2.02E-01	-2.49E-02	-1.81E-01
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	2.40E-01	-3.31E-02	-1.97E-01
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	1.90E-01	-9.81E-03	-5.96E-02
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	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: 4825).
2	Zidovudine FDA Label
3	The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
4	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. (Target id: 1807).
5	Antiviral drugs in current clinical use. J Clin Virol. 2004 Jun;30(2):115-33.
6	Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. J Pharmacol Exp Ther. 2002 Mar;300(3):918-24.
7	Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
8	Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
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10	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.
11	Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
12	Interindividual variability in pharmacokinetics of generic nucleoside reverse transcriptase inhibitors in TB/HIV-coinfected Ghanaian patients: UGT2B7*1c is associated with faster zidovudine clearance and glucuronidation. J Clin Pharmacol. 2009 Sep;49(9):1079-90.
13	Determination of UDP-glucuronosyltransferase UGT2B7 activity in human liver microsomes by ultra-performance liquid chromatography with MS detection. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Jul 1;870(1):84-90.