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

General Information of Drug (ID: DMKSUOI)

Drug Name

Flavopiridol Drug Info

Synonyms

FLAVO; Alvocidib [INN]; Flavopiridol hydrochloride; L 868275; HMR-1275; L-868275; L86-8275; HMR-1275, Alvocidib, L868275, Flavopiridol; (-)-cis-5,7-Dihydroxy-2-(2-chlorophenyl)-8-(4-(3-hydroxy-1-methyl)piperidinyl)-4H-1-benzopyran-4-one; 2-(2-CHLORO-PHENYL)-5,7-DIHYDROXY-8-(3-HYDROXY-1-METHYL-PIPERIDIN-4-YL)-4H-BENZOPYRAN-4-ONE; 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one

Indication

Disease Entry	ICD 11	Status	REF
Acute myeloid leukaemia	2A60	Phase 2	[1]
Chronic lymphocytic leukaemia	2A82.0	Discontinued in Phase 3	[2]

Cross-matching ID

PubChem CID: 5287969
ChEBI ID: CHEBI:47344
CAS Number: CAS 146426-40-6
TTD Drug ID: DMKSUOI
VARIDT Drug ID: DR00235
INTEDE Drug ID: DR0079

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cyclin-dependent kinase (CDK)	TTMBO1Z	NOUNIPROTAC	Inhibitor	[3]
Cyclin-dependent kinase 9 (CDK9)	TT1LVF2	CDK9_HUMAN	Inhibitor	[4]
Myophosphorylase (PYGM)	TT31JXP	PYGM_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	Phase 2	[5]
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DT3D8F0	SO1B1_HUMAN	Phase 2	[6]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DEYGVN4	UD11_HUMAN	Phase 2	[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
Cyclin-dependent kinase 9 (CDK9)	DTT	CDK9	5.597	5.711	5.221	5.776
Breast cancer resistance protein (ABCG2)	DTP	BCRP	6.732	7.513	6.326	9.277
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DTP	OATP1B1	9.79	0.485	3.511	2.07

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 myeloid leukaemia

ICD Disease Classification

2A60

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Cyclin-dependent kinase 9 (CDK9)	DTT	CDK9	4.38E-01	-0.04	-0.1
Breast cancer resistance protein (ABCG2)	DTP	BCRP	3.87E-47	-1.28E+00	-1.63E+00
Organic anion transporting polypeptide 1B1 (SLCO1B1)	DTP	OATP1B1	2.80E-34	1.44E-01	9.71E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	2.33E-02	1.75E-02	8.91E-02

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
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: 5680).
3	Pharma & Vaccines. Product Development Pipeline. April 29 2009.
4	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5	The novel BCR-ABL and FLT3 inhibitor ponatinib is a potent inhibitor of the MDR-associated ATP-binding cassette transporter ABCG2. Mol Cancer Ther. 2012 Sep;11(9):2033-44.
6	Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
7	Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8.