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

General Information of Drug (ID: DMCX0K3)

Drug Name

Cinacalcet Drug Info

Synonyms

Cinacalcet [INN]; AMG 073; AMG073; Cinacalcet (USAN); Mimpara (TN); Sensipar (TN); N-[(1R)-1-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)phenyl]propan-1-amine; N-[(1R)-1-naphthalen-1-ylethyl]-3-[3-(trifluoromethyl)phenyl]propan-1-amine; N-((1R)-1-(1-Naphthyl)ethyl)-3-(3-(trifluoromethyl)phenyl)propan-1-amine; N-((1R)-1-(Naphthalen-1-yl)ethyl)-3-(3-(trifluoromethyl)phenyl)propan-1-amine; (R)-N-(1-(Naphthalen-1-yl)ethyl)-3-(3-(trifluoromethyl)phenyl)propan-1-amine; (R)-alpha-methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-naphthalenemethane amine

Indication

Disease Entry	ICD 11	Status	REF
Hyperparathyroidism	5A51	Approved	[1]
Kidney disease	GC2Z	Phase 3	[1]

Therapeutic Class

Calcimimetics

Cross-matching ID

PubChem CID: 156419
ChEBI ID: CHEBI:48390
CAS Number: CAS 226256-56-0
TTD Drug ID: DMCX0K3
INTEDE Drug ID: DR0326
ACDINA Drug ID: D00131

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Extracellular calcium-sensing receptor (CASR)	TTBUYHA	CASR_HUMAN	Agonist	[2]

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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	[3]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Approved	[3]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Approved	[4]

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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
Extracellular calcium-sensing receptor (CASR)	DTT	CASR	4.966	4.892	5.342	5.37
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	10.036	5.779	6.508	6.481
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	3.307	5.005	3.921	5.327
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

Hyperparathyroidism

ICD Disease Classification

5A51

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Extracellular calcium-sensing receptor (CASR)	DTT	CASR	5.81E-02	-0.03	-0.19
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	8.12E-01	3.88E-03	1.91E-02
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	4.26E-01	5.09E-02	2.01E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	4.73E-01	-1.99E-02	-1.18E-01

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: 3308).
2	Clinical pipeline report, company report or official report of Amgen (2009).
3	Clinical pharmacokinetic and pharmacodynamic profile of cinacalcet hydrochloride. Clin Pharmacokinet. 2009;48(5):303-11.
4	Effects of CYP3A inhibition on the metabolism of cilostazol. Clin Pharmacokinet. 1999;37 Suppl 2:61-8.