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

General Information of Drug (ID: DM2POTE)

Drug Name

Colchicine Drug Info

Synonyms

Colchicin; Colchicina; Colchicinum; Colchineos; Colchisol; Colchysat; Colcin; Colcrys; Colsaloid; Colstat; Condylon; Goutnil; Kolkicin; LOC; Binds to tubulin; Colchicin [German]; Colchicina [Italian]; Colchicine [JAN]; Inhibits microtubular assembly; Spindle poison; C 9754; Colchicine (TN); Colchicine, Colchicum autumnale; MPC-004; N-Acetyl trimethylcolchicinic acid methylether; Colchicine (JP15/USP); Colchicine, (R)-Isomer; Benzo(a)heptalen-9(5H)-one; Colchicine, (+-)-Isomer; N-(5,6,7,9-Tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo(a)heptalen-7-yl)acetamide; N-[(7S)-1,2,3,10-tetramethoxy-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]acetamide; N-[(7S)-1,2,3,10-tetramethoxy-9-oxo-6,7-dihydro-5H-benzo[a]heptalen-7-yl]acetamide; N-[(7S)-5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo[a]heptalen-7-yl]acetamide; N-(5,6,7,9-Tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo[.alpha.]heptalen-7-yl)-acetamide; N-((7S)-5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo(a)heptalen-7-yl)-acetamide; (S)-N-(5,6,7,9-Tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo[a]heptalen-7-yl)acetamide; 7-alpha-H-Colchicine; 7.alpha.H-Colchicine; 7alphaH-Colchicine

Indication

Disease Entry	ICD 11	Status	REF
Acute gout flare	FA25.0	Approved	[1]
Acute gouty arthritis	FA25.0	Approved	[2]
Gout	FA25	Approved	[3]
Coronavirus Disease 2019 (COVID-19)	1D6Y	Phase 2	[4]
Familial Mediterranean fever		Investigative	[3]

Therapeutic Class

Gout Suppressants

Cross-matching ID

PubChem CID: 6167
ChEBI ID: CHEBI:27882
CAS Number: CAS 64-86-8
TTD Drug ID: DM2POTE
VARIDT Drug ID: DR00135
INTEDE Drug ID: DR0372
ACDINA Drug ID: D00149

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Tubulin (TUB)	TTML2WA	NOUNIPROTAC	Binder	[5]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
Multidrug resistance-associated protein 1 (ABCC1)	DTSYQGK	MRP1_HUMAN	Approved	[6]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[7]

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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	[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
Tubulin (TUB)	DTT	TUB	7.743	8.411	8.625	8.347
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Multidrug resistance-associated protein 1 (ABCC1)	DTP	MRP1	4.838	6.296	5.935	6.146
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

Acute gout flare

ICD Disease Classification

FA25.0

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Tubulin (TUB)	DTT	NO-GeName	7.94E-02	0.35	0.43
P-glycoprotein 1 (ABCB1)	DTP	P-GP	1.53E-04	-6.93E-01	-2.04E+00
Multidrug resistance-associated protein 1 (ABCC1)	DTP	MRP1	1.01E-02	8.86E-01	1.34E+00
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	2.96E-01	-3.35E-01	-1.10E+00

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	FDA Approved Drug Products from FDA Official Website. 2019. Application Number: (NDA) 022351
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: 7526).
3	Colchicine FDA Label
4	ClinicalTrials.gov (NCT04322565) Colchicine Counteracting Inflammation in COVID-19 Pneumonia. U.S. National Institutes of Health.
5	Vitamin K3 disrupts the microtubule networks by binding to tubulin: a novel mechanism of its antiproliferative activity. Biochemistry. 2009 Jul 28;48(29):6963-74.
6	Pharmacological characterization of the murine and human orthologs of multidrug-resistance protein in transfected human embryonic kidney cells. Mol Pharmacol. 1997 Sep;52(3):344-53.
7	Nilotinib (AMN107, Tasigna) reverses multidrug resistance by inhibiting the activity of the ABCB1/Pgp and ABCG2/BCRP/MXR transporters. Biochem Pharmacol. 2009 Jul 15;78(2):153-61.
8	Colchicine down-regulates cytochrome P450 2B6, 2C8, 2C9, and 3A4 in human hepatocytes by affecting their glucocorticoid receptor-mediated regulation. Mol Pharmacol. 2003 Jul;64(1):160-9.