General Information of Drug (ID: DMSWLM5)

Drug Name
CP-122721 Drug Info
Synonyms
CP-122721; UNII-R7OYP6N58F; R7OYP6N58F; CHEMBL319118; CHEMBL1917847; DSSTox_CID_27251; DSSTox_RID_82210; DSSTox_GSID_47251; SCHEMBL156646; DTXSID9047251; Tox21_300205; BDBM50067935; ZINC22441997; AKOS030542331; DB05421; NCGC00254228-01; NCGC00247927-01; CAS-145742-28-5; (2S,3S)-N-(2-methoxy-5-(trifluoromethoxy)benzyl)-2-phenylpiperidin-3-amine
Indication
Disease Entry ICD 11 Status REF
Major depressive disorder 6A70.3 Phase 2 [1]
Cross-matching ID
PubChem CID
9821217
CAS Number
CAS 145742-28-5
TTD Drug ID
DMSWLM5
VARIDT Drug ID
DR01429
INTEDE Drug ID
DR1849

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Substance-P receptor (TACR1) TTZPO1L NK1R_HUMAN Antagonist [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Phase 2 [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Phase 2 [4]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Phase 2 [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
Substance-P receptor (TACR1) DTT TACR1 3.597 4.186 4.271 5.113
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
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 Major depressive disorder
ICD Disease Classification 6A70.3
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Substance-P receptor (TACR1) DTT TACR1 7.40E-01 0.02 0.07
Substance-P receptor (TACR1) DTT TACR1 8.57E-01 -0.02 -0.18
P-glycoprotein 1 (ABCB1) DTP P-GP 1.19E-01 -1.32E-01 -2.77E-01
P-glycoprotein 1 (ABCB1) DTP P-GP 1.65E-01 -1.47E-01 -4.48E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 2.59E-01 6.29E-02 3.14E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 4.84E-01 -8.38E-02 -8.46E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 4.66E-01 4.25E-02 1.20E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 4.75E-01 5.15E-02 3.64E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007429)
2 A review of drug options in age-related macular degeneration therapy and potential new agents. Expert Opin Pharmacother. 2006 Dec;7(17):2355-68.
3 P-glycoprotein efflux at the blood-brain barrier mediates differences in brain disposition and pharmacodynamics between two structurally related neurokinin-1 receptor antagonists. J Pharmacol Exp Ther. 2001 Sep;298(3):1252-9.
4 In vitro metabolism of CP-122,721 ((2S,3S)-2-phenyl-3-[(5-trifluoromethoxy-2-methoxy)benzylamino]piperidine), a non-peptide antagonist of the substance P receptor. Drug Metab Pharmacokinet. 2007 Oct;22(5):336-49.