Details of Drug-Metabolizing Enzyme (DME)

General Information of DME (ID: DMEN229)
DME Name Esterases (ES), Homo sapiens
Gene Name ES
Lineage    Species: Homo sapiens     (Click to Show/Hide the Complete Species Lineage)
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
      Click to Show/Hide the Molecular/Functional Data (Sequence/Structure/Pathway/Function) of This DME
Full List of Drug(s) Metabolized by This DME
      Drugs Approved by FDA Click to Show/Hide the Full List of Drugs:          4 Drugs
Ibrutinib
 Drug Info Approved Mantle cell lymphoma ICD11: 2A85 [1]
Ampiroxicam
 Drug Info Approved Inflammation ICD11: 1A00-CA43 [2]
Carbenicillin Indanyl Sodium
 Drug Info Approved Bacterial infection ICD11: 1A00-1C4Z [3]
Hydroxyprogesterone caproate
 Drug Info Approved Uterine cancer ICD11: 2C76 [4], [5]
      Drugs in Phase 2 Clinical Trial Click to Show/Hide the Full List of Drugs:          3 Drugs
Remogliflozin etabonate
 Drug Info Phase 2 Type-1/2 diabetes ICD11: 5A10-5A11 [6]
ETIPREDNOL DICLOACETATE
 Drug Info Phase 2 Rheumatoid arthritis ICD11: FA20 [7]
Managlinat dialanetil
 Drug Info Phase 2 Type-2 diabetes ICD11: 5A11 [8]
      Discontinued/withdrawn Drugs Click to Show/Hide the Full List of Drugs:          2 Drugs
EMITEFUR
 Drug Info Discontinued in Preregistration Solid tumour/cancer ICD11: 2A00-2F9Z [9]
TNP-470
 Drug Info Discontinued in Phase 2 Solid tumour/cancer ICD11: 2A00-2F9Z [10]
      Preclinical/investigative Agents Click to Show/Hide the Full List of Drugs:          1 Drugs
Bopindolol
 Drug Info Investigative Discovery agent ICD: N.A. [11], [12]
Full List of Metabolic Reactions (MR) Catalyzed by This DME
MR ID Reactant Product MR Type Source Drug REF
MR014205 NUC?1031 Gemcitabine Hydrolysis - Hydrolyzation acelarin [13]
MR000042 Acemetacin Indomethacin Hydrolysis - Esterase Hydrolysis Acemetacin [14]
MR014202 AFP464 Aminoflavone Hydrolysis - Hydrolyzation AFP464 [15]
MR008909 Ampiroxicam Piroxicam Unclear - Unclear Ampiroxicam [2]
MR012559 Arecoline Arecaidine Unclear - Unclear Arecoline [16]
MR008908 Bacampicillin Ampicillin Hydrolysis - Hydrolysis Bacampicillin [17]
MR006035 Benazepril Benazeprilat Unclear - Unclear Benazepril [18]
MR014206 Bitolterol Colterol Hydrolysis - Hydrolyzation Bitolterol [19]
MR007567 Bopindolol 18-502 Hydrolysis - Hydrolyzation Bopindolol [11], [12]
MR008094 Carbenicillin Indanyl Sodium Carbenicillin Unclear - Unclear Carbenicillin Indanyl Sodium [3]
MR012052 Ceftobiprole medocaril BAL 9141 Unclear - Unclear Ceftobiprole medocaril [20]
MR003207 Ciclesonide Desisobutyrylciclesonide Hydrolysis - Hydrolysis Ciclesonide [21], [22], [23], [24]
MR006538 Clevidipine H-152/81 Unclear - Unclear Clevidipine [25], [26]
MR012327 CO-101 Gemcitabine Unclear - Unclear CO-101 [27]
MR009467 EMITEFUR 1-ethoxymethyl-5-fluorouracil Unclear - Unclear EMITEFUR [9]
MR009469 EMITEFUR 3-cyano-2,6-dihydropyrimidine (CNDP) Unclear - Unclear EMITEFUR [9]
MR000946 Eslicarbazepine acetate Eslicarbazepine Unclear - Unclear Eslicarbazepine acetate [28]
MR008462 ETIPREDNOL DICLOACETATE Carboxyl metabolite Unclear - Unclear ETIPREDNOL DICLOACETATE [7]
MR008464 ETIPREDNOL DICLOACETATE Hydroxyl metabolite Unclear - Unclear ETIPREDNOL DICLOACETATE [7]
MR012144 Irinotecan SN-38 Unclear - Unclear Etirinotecan pegol [29]
MR011479 FK-973 FR67042 Unclear - Unclear FK-973 [30]
MR011481 FK-973 FR66974 Unclear - Unclear FK-973 [30]
MR011483 FK-973 FR66980 Unclear - Unclear FK-973 [30]
MR011482 FR66974 FR900482 Unclear - Unclear FK-973 [30]
MR011480 FR67042 FR900482 Unclear - Unclear FK-973 [30]
MR010884 Fosinopril Fosinoprilat Unclear - Unclear Fosinopril [31]
MR005143 Hydroxyprogesterone caproate 17alpha- Hydroxyprogesterone Hydrolysis - Hydrolyzation Hydroxyprogesterone caproate [4], [5]
MR012962 Ibrutinib Desacryl-Ibrutinib Unclear - Unclear Ibrutinib [1]
MR009236 Ingrezza (+)-alpha-HTBZ Hydrolysis - Hydrolysis Ingrezza [32]
MR014199 KAR5585 KAR5417 Hydrolysis - Hydrolyzation KAR5585 [33]
MR011887 KRP-297 Metabolite M1 KRP-297 Metabolite M5,M9 Unclear - Unclear KRP-297 [34]
MR014195 Laninamivir octanoate Laninamivir Hydrolysis - Hydrolyzation Laninamivir octanoate [35]
MR008466 Managlinat dialanetil R-134450 Unclear - Unclear Managlinat dialanetil [8]
MR008715 Moexipril Moexiprilat Hydrolysis - Hydrolysis Moexipril [36]
MR007670 Nitazoxanide Nitazoxanide metabolite T Oxidation - Deacetylation Nitazoxanide [37]
MR001817 Olmesartan medoxomil Olmesartan Unclear - Unclear Olmesartan medoxomil [38], [39]
MR010892 Oseltamivir Oseltamivir carboxylate Unclear - Unclear Oseltamivir [40]
MR010893 Perindopril Perindoprilat Unclear - Unclear Perindopril [41]
MR008089 Pivampicillin Ampicillin Hydrolysis - Hydrolysis Pivampicillin [42]
MR009407 R7128 PSI-6130 Unclear - Unclear R7128 [43]
MR014046 Remdesivir Nucleoside Monophosphate GS-441524 Unclear Remdesivir [44]
MR008486 Remogliflozin etabonate Remogliflozin Unclear - Unclear Remogliflozin etabonate [6]
MR010973 Salsalate Salicylic acid Unclear - Unclear Salsalate [45]
MR011372 TAK-491 Azilsartan Unclear - Unclear TAK-491 [46]
MR013885 Tecarfarin ATI-5900 Unclear - Unclear Tecarfarin [47]
MR010909 Tecfidera Monomethyl fumarate Unclear - Unclear Tecfidera [48], [49]
MR004897 Testosterone undecanoate Testosterone Hydrolysis - Esterase hydrolyzation Testosterone undecanoate [50]
MR013003 TNP-470 TNP-470 Metabolite MIV Unclear - Unclear TNP-470 [10]
MR002436 Trandolapril Trandolaprilat Unclear - Unclear Trandolapril [51]
MR002485 Valbenazine [+]alpha-HTBZ Hydrolysis - Hydrolysis Valbenazine [32], [52]
MR007814 Valganciclovir Ganciclovir Hydrolysis - Hydrolysis Valganciclovir [53]
⏷ Show the Full List of 51 MR(s)
References
1 Extrahepatic metabolism of ibrutinib
2 Pharmacokinetic drug interactions between ampiroxicam and sulfaphenazole in rats
3 GI absorption of beta-lactam antibiotics I: kinetic assessment of competing absorption and degradation in GI tract
4 Transplacental transfer and metabolism of 17-alpha-hydroxyprogesterone caproate
5 The association among cytochrome P450 3A, progesterone receptor polymorphisms, plasma 17-alpha hydroxyprogesterone caproate concentrations, and spontaneous preterm birth. Am J Obstet Gynecol. 2017 Sep;217(3):369.e1-369.e9.
6 Assessment of the drug interaction risk for remogliflozin etabonate, a sodium-dependent glucose cotransporter-2 inhibitor: evidence from in vitro, human mass balance, and ketoconazole interaction studies
7 Identification of esterase involved in the metabolism of two corticosteroid soft drugs. Biochem Pharmacol. 2017 Mar 1;127:82-89.
8 Population pharmacokinetic model for a novel oral hypoglycemic formed in vivo: comparing the use of active metabolite data alone versus using data of upstream and downstream metabolites
9 Phase I assessment of the pharmacokinetics, metabolism, and safety of emitefur in patients with refractory solid tumors
10 Pharmacokinetics and metabolism of O-(chloroacetyl-carbamoyl) fumagillol (TNP-470, AGM-1470) in rhesus monkeys
11 Bopindolol: pharmacological basis and clinical implications
12 Bopindolol. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy
13 Anti-tumour activity of a first-in-class agent NUC-1031 in patients with advanced cancer: results of a phase I study
14 DrugBank(Pharmacology-Metabolism)Acemetacin
15 Validation and implementation of a liquid chromatography/tandem mass spectrometry assay to quantitate aminoflavone (NSC 686288) in human plasma
16 Genetic toxicology and toxicokinetics of arecoline and related areca nut compounds: an updated review
17 Comparative study of bacampicillin and ampicillin in the treatment of uncomplicated gonorrhoea
18 DrugBank(Pharmacology-Metabolism):Benazepril
19 Bitolterol mesylate: a beta-adrenergic agent. Chemistry, pharmacokinetics, pharmacodynamics, adverse effects and clinical efficacy in asthma
20 Pharmacokinetics and pharmacodynamics of ceftobiprole, an anti-MRSA cephalosporin with broad-spectrum activity
21 Ciclesonide Drugs. 2004;64(5):511-9; discussion 520-1. doi: 10.2165/00003495-200464050-00005.
22 Deposition and metabolism of inhaled ciclesonide in the human lung Eur Respir J. 2010 Nov;36(5):1113-9. doi: 10.1183/09031936.00172309.
23 LC-HRMS/MS study of the prodrug ciclesonide and its active metabolite desisobutyryl-ciclesonide in plasma after an inhalative administration to horses for doping control purposes. Drug Test Anal. 2022 Feb;14(2):252-261. doi: 10.1002/dta.3174.
24 Visualizing the spatial localization of ciclesonide and its metabolites in rat lungs after inhalation of 1-m aerosol of ciclesonide by desorption electrospray ionization-time of flight mass spectrometry imaging. Int J Pharm. 2021 Feb 15;595:120241. doi: 10.1016/j.ijpharm.2021.120241.
25 Pharmacodynamic, pharmacokinetic and clinical effects of clevidipine, an ultrashort-acting calcium antagonist for rapid blood pressure control
26 Human cytochrome p450 induction and inhibition potential of clevidipine and its primary metabolite h152/81. Drug Metab Dispos. 2006 May;34(5):734-7.
27 Phase I study of oral CP-4126, a gemcitabine derivative, in patients with advanced solid tumors
28 Pharmacokinetics and drug interactions of eslicarbazepine acetate Epilepsia. 2012 Jun;53(6):935-46. doi: 10.1111/j.1528-1167.2012.03519.x.
29 Integrated population pharmacokinetics of etirinotecan pegol and its four metabolites in cancer patients with solid tumors
30 A new antitumor antibiotic, FK973: its metabolism in the blood and the antitumor effects of its metabolites on experimental models
31 Simultaneous quantification of fosinopril and its active metabolite fosinoprilat in rat plasma by UFLC-MS/MS: Application of formic acid in the stabilization of an ester-containing drug
32 Pharmacologic Characterization of Valbenazine (NBI-98854) and Its Metabolites J Pharmacol Exp Ther. 2017 Jun;361(3):454-461. doi: 10.1124/jpet.116.239160.
33 Tryptophan hydroxylase 1 Inhibition Impacts Pulmonary Vascular Remodeling in Two Rat Models of Pulmonary Hypertension
34 Absorption, metabolism, and excretion of [14C]MK-0767 (2-methoxy-5-(2,4-dioxo-5-thiazolidinyl)-N-[[4-(trifluoromethyl)phenyl] methyl]benzamide) in humans
35 Laninamivir octanoate: a new long-acting neuraminidase inhibitor for the treatment of influenza
36 Moexipril. A review of its use in the management of essential hypertension
37 Metabolism of nitazoxanide in rats, pigs, and chickens: Application of liquid chromatography coupled to hybrid linear ion trap/Orbitrap mass spectrometer
38 The new oral angiotensin II antagonist olmesartan medoxomil: a concise overview J Hum Hypertens. 2002 May;16 Suppl 2:S13-6. doi: 10.1038/sj.jhh.1001391.
39 Nanoemulsion strategy for olmesartan medoxomil improves oral absorption and extended antihypertensive activity in hypertensive rats Colloids Surf B Biointerfaces. 2014 Mar 1;115:286-94. doi: 10.1016/j.colsurfb.2013.12.016.
40 Pharmacokinetics of oseltamivir phosphate and oseltamivir carboxylate in non-pregnant and pregnant rhesus monkeys
41 Clinical review of perindopril in the treatment of hypertension
42 Absorption of ester prodrugs in Caco-2 and rat intestine models
43 Selected replicon variants with low-level in vitro resistance to the hepatitis C virus NS5B polymerase inhibitor PSI-6130 lack cross-resistance with R1479
44 Population pharmacokinetic modeling of GS-441524, the active metabolite of remdesivir, in Japanese COVID-19 patients with renal dysfunction
45 AMPK: mediating the metabolic effects of salicylate-based drugs?
46 Development, validation and application of the liquid chromatography tandem mass spectrometry method for simultaneous quantification of azilsartan medoxomil (TAK-491), azilsartan (TAK-536), and its 2 metabolites in human plasma
47 Effect of tecarfarin, a novel vitamin K epoxide reductase inhibitor, on coagulation in beagle dogs
48 Dimethyl fumarate alleviates the nitroglycerin (NTG)-induced migraine in mice
49 Dimethyl fumarate: A review of preclinical efficacy in models of neurodegenerative diseases
50 Importance of measuring testosterone in enzyme-inhibited plasma for oral testosterone undecanoate androgen replacement therapy clinical trials
51 Trandolapril: a clinical profile Am J Hypertens. 1995 Oct;8(10 Pt 2):68S-70S. doi: 10.1016/0895-7061(95)00192-1.
52 Pharmacokinetic and Pharmacologic Characterization of the Dihydrotetrabenazine Isomers of Deutetrabenazine and Valbenazine. Clin Pharmacol Drug Dev. 2023 Apr;12(4):447-456. doi: 10.1002/cpdd.1205.
53 Pharmacokinetic profile of ganciclovir after its oral administration and from its prodrug, valganciclovir, in solid organ transplant recipients

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