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

General Information of Drug (ID: DMT5GNL)

Drug Name

Romidepsin Drug Info

Synonyms

Chromadax; Istodax; Antibiotic FR 901228; FK 228; FK228; FR 901228; FR901228; HDInhib_000006; Chromadax (TN); FK-228; FK-901228; FR-901228; Istodax (TN); Romidepsin (USAN); Cyclo((2Z)-2-amino-2-butenoyl-L-valyl-(3S,4E)-3-hydroxy-7-mercapto-4-heptenoyl-D-valyl-D-cysteinyl), cyclic (35)-disulfide; L-Valine, N-((3S,4E)-3-hydroxy-7-mercapto-1-oxo-4-heptenyl)-D-valyl-D-cysteinyl-(2Z)-2-amino-2-butenoxyl-, (4-1)-lactone, cyclic (1-2)-disulfide; (1S,4S,7Z,10S,16E,21R)-7-Ethylidene-4,21-bis(1-methylethyl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo(8.7.6)tricos-16-ene-3,6,9,19,22-pentone; (1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone; (1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone

Indication

Disease Entry	ICD 11	Status	REF
Cutaneous T-cell lymphoma	2B01	Approved	[1]
Gastrin-producing neuroendocrine tumor		Approved	[2]
Glucagonoma		Approved	[2]
Insulinoma	2C10.1	Approved	[2]
Lung carcinoid tumor		Approved	[2]
Melanoma	2C30	Approved	[2]
Primary cutaneous peripheral T-cell lymphoma not otherwise specified		Approved	[2]
Primary cutaneous T-cell lymphoma		Approved	[2]
Urethral cancer	2C93	Approved	[2]
Peripheral T-cell lymphoma	2A90.C	Phase 3	[3]
Renal cell carcinoma	2C90	Phase 3	[1]

Cross-matching ID

PubChem CID: 5352062
ChEBI ID: CHEBI:61080
CAS Number: CAS 128517-07-7
TTD Drug ID: DMT5GNL
VARIDT Drug ID: DR00233
INTEDE Drug ID: DR1438
ACDINA Drug ID: D01401

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histone deacetylase 1 (HDAC1)	TT6R7JZ	HDAC1_HUMAN	Inhibitor	[4]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DT9C1TS	SO1B3_HUMAN	Approved	[5]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_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 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Approved	[7]
Cytochrome P450 2B6 (CYP2B6)	DEPKLMQ	CP2B6_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
Histone deacetylase 1 (HDAC1)	DTT	HDAC1	6.206	8.094	7.236	7.56
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DTP	OATP1B3	8.873	2.17	2.485	3.322
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

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

Cutaneous T-cell lymphoma

ICD Disease Classification

2B01

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Histone deacetylase 1 (HDAC1)	DTT	HDAC1	1.91E-11	0.44	1.3
P-glycoprotein 1 (ABCB1)	DTP	P-GP	5.54E-01	1.87E-01	4.30E-01
Organic anion transporting polypeptide 1B3 (SLCO1B3)	DTP	OATP1B3	1.48E-59	-3.95E+00	-5.81E+00
Cytochrome P450 2B6 (CYP2B6)	DME	CYP2B6	2.38E-13	-2.40E+00	-1.69E+00
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	4.87E-05	-5.90E-01	-7.24E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	1.02E-14	-3.12E+00	-2.25E+00

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: 7006).
2	Romidepsin FDA Label
3	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4	Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
5	Population pharmacokinetics of romidepsin in patients with cutaneous T-cell lymphoma and relapsed peripheral T-cell lymphoma. Clin Cancer Res. 2009 Feb 15;15(4):1496-503.
6	A phase I/II trial of the histone deacetylase inhibitor romidepsin for adults with recurrent malignant glioma: North American Brain Tumor Consortium Study 03-03. Neuro Oncol. 2011 May;13(5):509-16.
7	Population pharmacokinetics of romidepsin in patients with cutaneous T-cell lymphoma and relapsed peripheral T-cell lymphoma. Clin Cancer Res. 2009 Feb 15;15(4):1496-503.
8	FDA Label of Romidepsin. The 2020 official website of the U.S. Food and Drug Administration.