General Information of DME (ID: DMEN065)
DME Name	Cytochrome P450 3A (CYP3A), .
Gene Name	CYP3A
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:        13 Drugs
Idelalisib	Drug Info	Approved	Chronic lymphocytic leukaemia	ICD11: 2A82	[1], [2]
Scopolamine	Drug Info	Approved	Nausea	ICD11: MD90	[3]
Dabigatran	Drug Info	Approved	Cerebral stroke	ICD11: 8B11	[4]
Osimertinib	Drug Info	Approved	Lung cancer	ICD11: 2C25	[5]
Captopril	Drug Info	Approved	Essential hypertension	ICD11: BA00	[6]
Maraviroc	Drug Info	Approved	Human immunodeficiency virus infection	ICD11: 1C60-1C62	[7]
Moxidectin	Drug Info	Approved	Onchocerciasis	ICD11: 1F6A	[8]
Phenmetrazine	Drug Info	Approved	Obesity	ICD11: 5B80-5B81	[9]
Trametinib	Drug Info	Approved	Melanoma	ICD11: 2C30	[10]
Relugolix	Drug Info	Approved	Prostate cancer	ICD11: 2C82	[11]
Ripretinib	Drug Info	Approved	Gastrointestinal stromal tumour	ICD11: 2B5B	[12]
Ceritinib	Drug Info	Approved	Lung cancer	ICD11: 2C25	[13], [14]
Ibutilide	Drug Info	Approved	Atrial fibrillation	ICD11: BC81	[15]
Drugs in Phase 4 Clinical Trial			Click to Show/Hide the Full List of Drugs:          1 Drugs
Grazoprevir	Drug Info	Phase 4	Viral hepatitis	ICD11: 1E51	[16]
Drugs in Phase 3 Clinical Trial			Click to Show/Hide the Full List of Drugs:        10 Drugs
Almonertinib	Drug Info	Phase 3	Lung cancer	ICD11: 2C25	[17]
Sotorasib	Drug Info	Phase 3	Lung cancer	ICD11: 2C25	[6]
Tasquinimod	Drug Info	Phase 3	Prostate cancer	ICD11: 2C82	[18]
FRC-8653	Drug Info	Phase 3	Essential hypertension	ICD11: BA00	[19]
Lanabecestat	Drug Info	Phase 3	Alzheimer disease	ICD11: 8A20	[20]
VX-787	Drug Info	Phase 3	Influenza A virus infection	ICD11: 1E30-1E32	[21]
BI 201335	Drug Info	Phase 3	Hepatitis C virus infection	ICD11: 1E50-1E51	[22]
Elagolix	Drug Info	Phase 3	Uterine leiomyoma	ICD11: 2E86	[23]
Mobocertinib	Drug Info	Phase 3	Lung cancer	ICD11: 2C25	[24]
sparsentan	Drug Info	Phase 3	Focal segmental glomerulosclerosis	ICD11: MF8Y	[25]
Drugs in Phase 2 Clinical Trial			Click to Show/Hide the Full List of Drugs:          8 Drugs
AMG 853	Drug Info	Phase 2	Asthma	ICD11: CA23	[26]
CP-122721	Drug Info	Phase 2	Depression	ICD11: 6A71	[27], [28]
Dextofisopam	Drug Info	Phase 2	Irritable bowel syndrome	ICD11: DD91	[29]
GTS-21	Drug Info	Phase 2	Schizophrenia	ICD11: 6A20	[30]
L-694,458	Drug Info	Phase 2	Cystic fibrosis	ICD11: CA25	[31]
MEDETOMIDINE	Drug Info	Phase 2	Pain	ICD11: MG30-MG3Z	[32]
BMS 791325	Drug Info	Phase 2	Hepatitis C virus infection	ICD11: 1E50-1E51	[33]
PF-04937319	Drug Info	Phase 2	Type-2 diabetes	ICD11: 5A11	[34]
Drugs in Phase 1 Clinical Trial			Click to Show/Hide the Full List of Drugs:          3 Drugs
X-396	Drug Info	Phase 1/2	Advanced solid tumour	ICD11: 2A00-2F9Z	[35]
PF9601N	Drug Info	Phase 1	Parkinsonism	ICD11: 8A00	[36]
CC-122	Drug Info	Phase 1	Chronic lymphocytic leukaemia	ICD11: 2A82	[37]

Full List of Metabolic Reactions (MR) Catalyzed by This DME
MR ID Reactant Product MR Type Source Drug REF MR013857 Almonertinib Almonertinib Metabolite HS-10296-M2 Unclear - Unclear Almonertinib [38] MR011355 AMG 853 AMG 853 Metabolite M2 Unclear - Unclear AMG 853 [26] MR011356 AMG 853 AMG 853 Metabolite M3 Unclear - Unclear AMG 853 [26] MR008538 BMS 791325 BMS-794712 Oxidation - N-demethylation BMS 791325 [33] MR007423 CP-122721 CP-677623 Unclear - Unclear CP-122721 [27], [28] MR007418 CP-125611 Quinone Unclear - Unclear CP-122721 [27], [28] MR007421 CP-125611 CP-919230 Oxidation - N-dealkylation CP-122721 [27], [28] MR012618 Dextofisopam Dextofisopam Metabolite M1 Unclear - Unclear Dextofisopam [29] MR012621 Dextofisopam Metabolite M3 Dextofisopam Metabolite M5 Unclear - Unclear Dextofisopam [29] MR010556 Divalproex sodium 5-OH-VPA Unclear - Unclear Divalproex sodium [39] MR010557 Divalproex sodium 3-OH-VPA Unclear - Unclear Divalproex sodium [39] MR010558 Divalproex sodium 4-OH-VPA Unclear - Unclear Divalproex sodium [39] MR010560 Divalproex sodium (3Z)-2-propylpent-3-enoic acid Unclear - Unclear Divalproex sodium [39] MR001000 Exemestane 6-hydroxymethylandrosta-1,4,6-triene-3,17-dione Oxidation - Deamination Exemestane [40] MR003633 FRC-8653 FRC-8653 Metabolite M1 Oxidation - Dehydrogenation FRC-8653 [19] MR007240 Grazoprevir Unclear Unclear - Unclear Grazoprevir [16] MR005814 GTS-21 2-OH-GTS-21 Oxidation - O-demethylation GTS-21 [30] MR005812 GTS-21 4-OH-GTS-21 Oxidation - O-demethylation GTS-21 [30] MR005131 Cortisone 6-beta-hydrocortisol Oxidation - 6-beta-hydroxylation Hydrocortisone [41] MR001427 Lapatinib ditosylate Lapatinib ditosylate metabolite M1 Oxidation - Debenzylation Lapatinib ditosylate [42], [43], [42] MR001418 Lapatinib ditosylate metabolite M1 Reactive Quinoneimine metabolite Unclear - Unclear Lapatinib ditosylate [42], [43], [42] MR012670 LY-333531 N-desmethyl ruboxistaurin Oxidation - N-demethylation LY-333531 [44], [45], [46] MR010859 Maraviroc Maraviroc Metabolite H2 Unclear - Unclear Maraviroc [47] MR010861 Maraviroc Maraviroc Metabolite H7,H8H10,H11 Oxidation - Mono-oxidation Maraviroc [47] MR010863 Maraviroc Maraviroc Metabolite H12,H13 Oxidation - Mono-oxidation Maraviroc [47] MR010865 Maraviroc Maraviroc Metabolite H6 Unclear - Unclear Maraviroc [47] MR010864 Maraviroc Metabolite H12,H13 Maraviroc Metabolite H3,H4,H5,H9 Oxidation - Mono-oxidation Maraviroc [47] MR010860 Maraviroc Metabolite H2 Maraviroc Metabolite H1 Unclear - Unclear Maraviroc [47] MR010862 Maraviroc Metabolite H7,H8H10,H11 Maraviroc Metabolite H3,H4,H5,H9 Oxidation - Mono-oxidation Maraviroc [47] MR012640 Medetomidine Hydroxymedetomidine Unclear - Unclear Medetomidine [32] MR004785 Mirtazapine Mirtazapine-N-oxide Oxidation - N-oxidation Mirtazapine [48] MR004786 Mirtazapine N-desmethylmirtazapine Oxidation - N-demethylation Mirtazapine [49] MR001860 Ospemifene 4'-hydroxylation Ospermifene Unclear - Unclear Ospemifene [50] MR012218 PD-153035 PD-153035 M1 Oxidation - N-oxidation PD-153035 [51] MR012219 PD-153035 PD-153035 M2 Oxidation - 7-O-desmethylation PD-153035 [51] MR012220 PD-153035 PD-153035 M3 Oxidation - O-demethylation PD-153035 [51] MR008674 Ripretinib DP-5439 Unclear - Unclear Ripretinib [52] MR011489 S-297995 Nor-naldemedine Oxidation - N-dealkylation S-297995 [53] MR013824 Scopolamine L-(-)-Norscopolamine Unclear - Unclear Scopolamine [3] MR011629 VX-787 VX-787 glucuronide metabolite Conjugation - Glucuronidation VX-787 [54] ⏷ Show the Full List of 40 MR(s)

References
1	Clinical drug interaction profile of idelalisib in healthy subjects
2	Identification of Novel Pathways in Idelalisib Metabolism and Bioactivation
3	Pharmacokinetics and pharmacodynamics in clinical use of scopolamine
4	The Potentially Significant Role of CYP3A-Mediated Oxidative Metabolism of Dabigatran Etexilate and Its Intermediate Metabolites in Drug-Drug Interaction Assessments Using Microdose Dabigatran Etexilate
5	Metabolism and pharmacokinetic study of deuterated osimertinib
6	Absorption, metabolism and excretion of [(14)C]-sotorasib in healthy male subjects: characterization of metabolites and a minor albumin-sotorasib conjugate
7	Pharmacokinetics and safety of maraviroc in neonates
8	Moxidectin and the avermectins: Consanguinity but not identity
9	DrugBank(Pharmacology-Metabolism):Phenmetrazine
10	Pharmacokinetic Interaction Between the MEK1/MEK2 Inhibitor Trametinib and Oral Contraceptives Containing Norethindrone and Ethinyl Estradiol in Female Patients With Solid Tumors
11	An Efficient UPLC-MS/MS Method Established to Detect Relugolix Concentration in Rat Plasma
12	The Pharmacokinetic Effect of Itraconazole and Voriconazole on Ripretinib in Beagle Dogs by UPLC-MS/MS Technique
13	Effect of ceritinib on the pharmacokinetics of coadministered CYP3A and 2C9 substrates: a phase I, multicenter, drug-drug interaction study in patients with ALK?+?advanced tumors
14	Drug interactions between ALK inhibitors and warfarin with concurrent use of bucolome: a case report
15	Progesterone Metabolites Inhibit the Human Ether-a-go-go-Related Gene and Predict QT Interval Length
16	FDA:Grazoprevir
17	Itraconazole and rifampicin, as CYP3A modulators but not P-gp modulators, affect the pharmacokinetics of almonertinib and active metabolite HAS-719 in healthy volunteers
18	Anti-cancer potency of tasquinimod is enhanced via albumin-binding facilitating increased uptake in the tumor microenvironment
19	Metabolism and metabolic inhibition of cilnidipine in human liver microsomes. Acta Pharmacol Sin. 2003 Mar;24(3):263-8.
20	Clinically Negligible Pharmacokinetic and Pharmacodynamic Interactions Between Lanabecestat and Dabigatran Etexilate, a Prototypical P-gp Substrate
21	Single- and multiple-dose pharmacokinetics and safety of pimodivir, a novel, non-nucleoside polymerase basic protein 2 subunit inhibitor of the influenza A virus polymerase complex, and interaction with oseltamivir: a Phase 1 open-label study in healthy volunteers
22	Effect of itraconazole on the pharmacokinetics of faldaprevir in healthy subjects
23	Quantitative Assessment of Elagolix Enzyme-Transporter Interplay and Drug-Drug Interactions Using Physiologically Based Pharmacokinetic Modeling
24	DrugBank(Pharmacology-Metabolism):Mobocertinib
25	Effect of Multiple Doses of Sparsentan on the Single-Dose Pharmacokinetics of Dapagliflozin: An Open-Label Drug-Drug Interaction Study in Healthy Adults
26	Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors
27	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.
28	Metabolism, pharmacokinetics, and excretion of the substance P receptor antagonist CP-122,721 in humans: structural characterization of the novel major circulating metabolite 5-trifluoromethoxy salicylic acid by high-performance liquid chromatography-tandem mass spectrometry and NMR spectroscopy
29	In vitro prediction and in vivo verification of enantioselective human tofisopam metabolite profiles
30	Metabolism and disposition of GTS-21, a novel drug for Alzheimer's disease. Xenobiotica. 1999 Jul;29(7):747-62.
31	Orally active inhibitors of human leukocyte elastase. II. Disposition of L-694,458 in rats and rhesus monkeys
32	Metabolic stability and determination of cytochrome P450 isoenzymes' contribution to the metabolism of medetomidine in dog liver microsomes. Biomed Chromatogr. 2010 Aug;24(8):868-77.
33	Effect of CYP3A5*3 genetic variant on the metabolism of direct-acting antivirals in vitro: a different effect on asunaprevir versus daclatasvir and beclabuvir J Hum Genet. 2020 Jan;65(2):143-153. doi: 10.1038/s10038-019-0685-2.
34	Metabolites in safety testing assessment in early clinical development: a case study with a glucokinase activator
35	Mass balance, metabolic disposition, and pharmacokinetics of [(14)C]ensartinib, a novel potent anaplastic lymphoma kinase (ALK) inhibitor, in healthy subjects following oral administration
36	CYP-dependent metabolism of PF9601N, a new monoamine oxidase-B inhibitor, by C57BL/6 mouse and human liver microsomes
37	Drug-Drug Interaction Study to Assess the Effect of Cytochrome P450 Inhibition and Induction on the Pharmacokinetics of the Novel Cereblon Modulator Avadomide (CC-122) in Healthy Adult Subjects
38	Absorption, metabolism, excretion, and safety of [(14)C]almonertinib in healthy Chinese subjects
39	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.
40	In vitro metabolism of exemestane by hepatic cytochrome P450s: impact of nonsynonymous polymorphisms on formation of the active metabolite 17beta-dihydroexemestane. Pharmacol Res Perspect. 2017 Apr 27;5(3):e00314.
41	Cortisol metabolism in vitro--III. Inhibition of microsomal 6 beta-hydroxylase and cytosolic 4-ene-reductase. J Steroid Biochem Mol Biol. 1993 Dec;46(6):827-32.
42	Detoxication versus Bioactivation Pathways of Lapatinib In Vitro: UGT1A1 Catalyzes the Hepatic Glucuronidation of Debenzylated Lapatinib Drug Metab Dispos. 2021 Mar;49(3):233-244. doi: 10.1124/dmd.120.000236.
43	Case Study 11: Considerations for Enzyme Mapping Experiments-Interaction Between the Aldehyde Oxidase Inhibitor Hydralazine and Glutathione. Methods Mol Biol. 2021;2342:809-823. doi: 10.1007/978-1-0716-1554-6_30.
44	The interactions of a selective protein kinase C beta inhibitor with the human cytochromes P450. Drug Metab Dispos. 2002 Sep;30(9):957-61.
45	Effects of chronic renal failure on the pharmacokinetics of ruboxistaurin and its active metabolite 338522
46	Disposition of [14C]ruboxistaurin in humans
47	Assessment of the absorption, metabolism and absolute bioavailability of maraviroc in healthy male subjects
48	FDA label:Mirtazapine
49	Clinical pharmacokinetics of mirtazapine
50	Ospemifene metabolism in humans in vitro and in vivo: metabolite identification, quantitation, and CYP assignment of major hydroxylations. Drug Metabol Drug Interact. 2013;28(3):153-61.
51	Metabolism of epidermal growth factor receptor targeting probe [11C]PD153035: impact on biodistribution and tumor uptake in rats
52	Effects of CYP3A Inhibition, CYP3A Induction, and Gastric Acid Reduction on the Pharmacokinetics of Ripretinib, a Switch Control KIT Tyrosine Kinase Inhibitor
53	Absorption, distribution, metabolism, and excretion of radiolabeled naldemedine in healthy subjects
54	#N/A

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