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

General Information of Drug (ID: DMZ7XNQ)

Drug Name

Tacrolimus Drug Info

Synonyms

Advagraf; Fujimycin; Graceptor; Modigraf; Prograf; Protopic; Protopy; Tacarolimus; Tsukubaenolide; Tacrolimus anhydrous; FK 506; FK5; FK506; FR 900506; FR900506; K506; L 679934; Advagraf (TN); FR-900506; Fk-506; L-679934; LCP-Tacro; Prograf (TN); Protopic (TN); Tacrolimus (INN); Tacrolimus (Prograf); Tacrolimus (anhydrous); (-)-FK 506; 15,19-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(23H)-tetrone; 8-DEETHYL-8-[BUT-3-ENYL]-ASCOMYCIN

Indication

Disease Entry	ICD 11	Status	REF
Graft-versus-host disease	4B24	Approved	[1]
Hepatosplenic T-cell lymphoma		Approved	[1]
Kidney transplant rejection	NE84	Approved	[1]
Large granular lymphocytic leukemia	2A90.1	Approved	[1]
Leukemia		Approved	[1]
Lupus nephritis	4A40.0Y	Approved	[1]
MALT lymphoma		Approved	[1]
Myeloproliferative neoplasm	2A20	Approved	[1]
Nodal marginal zone lymphoma	2A85.0	Approved	[1]
Organ transplant rejection	NE84	Approved	[2]
Primary cutaneous peripheral T-cell lymphoma not otherwise specified		Approved	[1]
Recurrent adult burkitt lymphoma	2A85.6	Approved	[1]
Small intestine lymphoma		Approved	[1]
Splenic marginal zone lymphoma		Approved	[1]
Testicular lymphoma		Approved	[1]
Ocular allergy	4A81	Phase 3	[2]
Classic Hodgkin lymphoma		Investigative	[1]

Therapeutic Class

Immunosuppressive Agents

Cross-matching ID

PubChem CID: 445643
ChEBI ID: CHEBI:61049
CAS Number: CAS 104987-11-3
TTD Drug ID: DMZ7XNQ
VARIDT Drug ID: DR00406
INTEDE Drug ID: DR1524
ACDINA Drug ID: D00648

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Calcineurin (PPP3CA)	TTA4LDE	PP2BA_HUMAN	Inhibitor	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[4]

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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	[5]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Approved	[6]
NADPH-cytochrome P450 reductase (CPR)	DE3N2FM	NCPR_HUMAN	Approved	[7]
Ribosomal 23S RNA methyltransferase Erm (erm)	DEW6V07	A0A5N1AHF6_CORAY	Approved	[8]
Ribosomal 23S RNA methyltransferase Erm (erm)	DEA65D8	A0A381KDL2_CORJE	Approved	[8]

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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
Calcineurin (PPP3CA)	DTT	PPP3CA	6.282	7.43	6.685	6.815
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	10.08	7.207	5.403	9.211
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	11.692	6.58	4.984	9.089
NADPH-cytochrome P450 reductase (CPR)	DME	POR	9.429	6.313	7.325	7.047

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

Graft-versus-host disease

ICD Disease Classification

4B24

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Calcineurin (PPP3CA)	DTT	PPP3CA	5.29E-01	1.74E-03	9.99E-03
P-glycoprotein 1 (ABCB1)	DTP	P-GP	2.00E-01	2.57E-02	6.18E-02
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	5.05E-02	4.52E-01	5.39E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	8.67E-01	-3.83E-03	-1.24E-02
NADPH-cytochrome P450 reductase (CPR)	DME	POR	8.69E-02	-1.76E-01	-3.46E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Tacrolimus 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: 6784).
3	Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20.
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	Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
6	Tacrolimus pharmacokinetics and pharmacogenetics: influence of adenosine triphosphate-binding cassette B1 (ABCB1) and cytochrome (CYP) 3A polymorphisms. Fundam Clin Pharmacol. 2007 Aug;21(4):427-35.
7	Polymorphisms in cytochrome P450 oxidoreductase and its effect on drug metabolism and efficacy. Pharmacogenet Genomics. 2017 Sep;27(9):337-346.
8	High frequency of macrolide resistance mechanisms in clinical isolates of Corynebacterium species. Microb Drug Resist. 2010 Dec;16(4):273-7.