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

General Information of Drug (ID: DM15F0X)

Drug Name

Gefitinib Drug Info

Synonyms

Gefitini; IRE; Iressa; Irressat; Gefitinib [USAN]; ZD 1839; ZD1839; Iressa (TN); Iressa(TM); ZD-1839; CU-00000000396-1; Gefitinib,Iressa, ZD1839; Gefitinib (JAN/USAN/INN); ZD-1839, Iressa, Gefitinib; N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine; N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(4-morpholinyl)propoxy)-4-quinazolinamide; N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine; N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine; N-(3-Chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine; 4-(3'-Chloro-4'-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline; 6-(3-morpholinopropoxy)-N-(3-chloro-4-fluorophenyl)-7-methoxyquinazolin-4-amine

Indication

Disease Entry	ICD 11	Status	REF
Colon adenocarcinoma		Approved	[1]
Glioblastoma	2A00	Approved	[1]
Lung cancer	2C25.0	Approved	[1]
Non-small-cell lung cancer	2C25.Y	Approved	[1]
Rectal adenocarcinoma	2B92	Approved	[1]
Rectum mucinous adenocarcinoma		Approved	[1]
Solid tumour/cancer	2A00-2F9Z	Approved	[2]
Head and neck cancer	2D42	Phase 3	[2]
Urethral cancer	2C93	Phase 2	[2]
Colon cancer	2B90.Z	Investigative	[1]
Colon mucinous adenocarcinoma		Investigative	[1]

Therapeutic Class

Anticancer Agents

Cross-matching ID

PubChem CID: 123631
ChEBI ID: CHEBI:49668
CAS Number: CAS 184475-35-2
TTD Drug ID: DM15F0X
VARIDT Drug ID: DR00423
INTEDE Drug ID: DR0764
ACDINA Drug ID: D00299

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Epidermal growth factor receptor (EGFR)	TTGKNB4	EGFR_HUMAN	Inhibitor	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
Breast cancer resistance protein (ABCG2)	DTI7UX6	ABCG2_HUMAN	Approved	[4]
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DT3D8F0	SO1B1_HUMAN	Approved	[5]
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DT9C1TS	SO1B3_HUMAN	Approved	[5]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[6]

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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	[7]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Approved	[8]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Approved	[7]

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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
Epidermal growth factor receptor (EGFR)	DTT	EGFR	6.045	4.991	5.317	5.252
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Breast cancer resistance protein (ABCG2)	DTP	BCRP	6.732	7.513	6.326	9.277
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DTP	OATP1B3	8.873	2.17	2.485	3.322
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DTP	OATP1B1	9.79	0.485	3.511	2.07
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	10.08	7.207	5.403	9.211
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

Colon adenocarcinoma

ICD Disease Classification

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Epidermal growth factor receptor (EGFR)	DTT	EGFR	1.04E-65	-0.89	-1.53
P-glycoprotein 1 (ABCB1)	DTP	P-GP	3.61E-73	-1.15E+00	-1.66E+00
Breast cancer resistance protein (ABCG2)	DTP	BCRP	1.46E-65	-1.41E+00	-1.41E+00
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DTP	OATP1B3	4.86E-01	-5.39E-02	-2.84E-01
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DTP	OATP1B1	9.12E-01	9.67E-03	3.43E-02
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	2.56E-19	-3.06E-01	-6.18E-01
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	6.51E-02	-2.38E-02	-9.58E-02
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	1.87E-03	-6.67E-02	-2.12E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Gefitinib FDA Label
2	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: 4941).
3	Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
4	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.
5	Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
6	Gefitinib-phenytoin interaction is not correlated with the C-erythromycin breath test in healthy male volunteers. Br J Clin Pharmacol. 2009 Aug;68(2):226-37.
7	Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes. Clin Cancer Res. 2007 Jun 15;13(12):3731-7.
8	Pharmacokinetic drug interactions of gefitinib with rifampicin, itraconazole and metoprolol. Clin Pharmacokinet. 2005;44(10):1067-81.