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

General Information of Drug (ID: DM9CIUW)

Drug Name

Ribociclib Succinate Drug Info

Synonyms

1374639-75-4; LEE011 succinate; LEE011 (succinate); UNII-BG7HLX2919; LEE011-BBA; Ribociclib succinate [USAN]; BG7HLX2919; Kisqali (TN); Ribociclib succinate (USAN); LEE-011 succinate; SCHEMBL2684999; EX-A1586; HY-15777B; 1374639-75-4 (succinate); AKOS030526460; CS-2277; ACN-040739

Indication

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Approved	[1]
Hormone receptor positive and HER2-negative advanced or metastatic breast cancer	2C60-2C65	Approved	[2]

Cross-matching ID

PubChem CID: 57334219
CAS Number: CAS 1374639-75-4
TTD Drug ID: DM9CIUW
INTEDE Drug ID: DR1415
ACDINA Drug ID: D01386

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cyclin-dependent kinase 4 (CDK4)	TT0PG8F	CDK4_HUMAN	Modulator	[3]
Cyclin-dependent kinase 6 (CDK6)	TTO0FDJ	CDK6_HUMAN	Modulator	[3]

------------------------------------------------------------------------------------

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Approved	[4]

------------------------------------------------------------------------------------

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 6 (CDK6)	DTT	CDK6	5.142	3.087	4.307	3.406
Cyclin-dependent kinase 4 (CDK4)	DTT	CDK4	7.414	7.821	7.812	7.719
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

Breast cancer

ICD Disease Classification

2C60-2C65

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Cyclin-dependent kinase 4 (CDK4)	DTT	CDK4	3.30E-72	0.65	2.39
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	5.59E-39	-3.76E-01	-1.64E+00

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
2	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2018
3	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
4	P-glycoprotein limits ribociclib brain exposure and CYP3A4 restricts its oral bioavailability. Mol Pharm. 2019 Sep 3;16(9):3842-3852.