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

General Information of Drug (ID: DMEKAYI)

Drug Name
Netupitant Drug Info
Synonyms R-1124; NK1 antagonist (emesis), Roche; Ro-67-3189
Indication
Disease Entry ICD 11 Status REF
Chemotherapy-induced nausea MD90 Phase 3 [1]
Cross-matching ID
PubChem CID
6451149
ChEBI ID
CHEBI:85155
CAS Number
CAS 290297-26-6
TTD Drug ID
DMEKAYI
INTEDE Drug ID
DR1141

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-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Phase 3 [3]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Phase 3 [4]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Phase 3 [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
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 3.307 5.005 3.921 5.327
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 11.76 5.931 6.164 9.423
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 Chemotherapy-induced nausea
ICD Disease Classification MD90
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
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 2C9 (CYP2C9) DME CYP2C9 8.99E-01 -6.93E-03 -1.36E-02
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 9.21E-01 7.31E-03 6.10E-02
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 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: 5742).
2 Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells. Exp Brain Res. 2014 Aug;232(8):2637-44.
3 Complementary pharmacokinetic profiles of netupitant and palonosetron support the rationale for their oral fixed combination for the prevention of chemotherapy-induced nausea and vomiting. J Clin Pharmacol. 2019 Apr;59(4):472-487.
4 Effect of netupitant, a highly selective NK?receptor antagonist, on the pharmacokinetics of palonosetron and impact of the fixed dose combination of netupitant and palonosetron when coadministered with ketoconazole, rifampicin, and oral contraceptives. Support Care Cancer. 2013 Oct;21(10):2879-87.