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-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Aprepitant DM053KT Depression 6A70-6A7Z Approved [5]
Selegiline DM6034S Major depressive disorder 6A70.3 Approved [6]
Rolapitant DM8XP26 Chemotherapy-induced nausea MD90 Approved [2]
Serlopitant DM5VH6U Prurigo nodularis EC91.0 Phase 3 [7]
LY-686017 DM7WORZ Atopic dermatitis EA80 Phase 3 [8]
Elinzanetant DMC6EFI Hot flushes GA30 Phase 3 [9]
CP-122721 DMSWLM5 Major depressive disorder 6A70.3 Phase 2 [10]
FR139317 DMEL5SV Hypertension BA00-BA04 Phase 2 [6]
VOFOPITANT HYDROCHLORIDE DMQMYP5 Vomiting MD90 Phase 2 [11]
LY-2590443 DM81UJW Migraine 8A80 Phase 2 [12]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [13]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [14]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [15]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [16]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [17]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [18]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [19]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [20]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [14]
Verapamil DMA7PEW Angina pectoris BA40 Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2D6 (CYP2D6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [22]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [23]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [24]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [17]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [21]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [25]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [26]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [27]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [28]
Propranolol DM79NTF Angina pectoris BA40 Approved [29]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2C9 (CYP2C9)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Progesterone DMUY35B Amenorrhea GA20.0 Approved [30]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [31]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [32]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [33]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [34]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [33]
Verapamil DMA7PEW Angina pectoris BA40 Approved [35]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [36]
Estrone DM5T6US Acne vulgaris ED80 Approved [37]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [38]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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 MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [3]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [4]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Substrate [4]

References

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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.
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6 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
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9 Elinzanetant (NT-814), a Neurokinin 1,3 Receptor Antagonist, Reduces Estradiol and Progesterone in Healthy Women. J Clin Endocrinol Metab. 2021 Jul 13;106(8):e3221-e3234.
10 A review of drug options in age-related macular degeneration therapy and potential new agents. Expert Opin Pharmacother. 2006 Dec;7(17):2355-68.
11 Efficacy and safety of casopitant mesylate, a neurokinin 1 (NK1)-receptor antagonist, in prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based highly emetogenicchemotherapy: a randomised, double-blind, placebo-controlled trial. Lancet Oncol. 2009 Jun;10(6):549-58.
12 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. (Target id: 360).
13 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
14 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
15 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
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17 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
18 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
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20 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
21 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
22 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
23 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
24 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
25 Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
26 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
27 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
28 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
29 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
30 Progesterone and testosterone hydroxylation by cytochromes P450 2C19, 2C9, and 3A4 in human liver microsomes. Arch Biochem Biophys. 1997 Oct 1;346(1):161-9.
31 Tamoxifen inhibits cytochrome P450 2C9 activity in breast cancer patients. J Chemother. 2006 Aug;18(4):421-4.
32 Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98.
33 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
34 Drug-drug interactions with imatinib: an observational study. Medicine (Baltimore). 2016 Oct;95(40):e5076.
35 Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30.
36 New insights into the structural features and functional relevance of human cytochrome P450 2C9. Part I. Curr Drug Metab. 2009 Dec;10(10):1075-126.
37 A potential role for the estrogen-metabolizing cytochrome P450 enzymes in human breast carcinogenesis. Breast Cancer Res Treat. 2003 Dec;82(3):191-7.
38 A mechanistic approach to antiepileptic drug interactions. Ann Pharmacother. 1998 May;32(5):554-63.