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

General Information of DME (ID: DEB30C5)

• DME Name: Carboxylesterase 1 (CES1) DME Info
• Gene Name: CES1

Molecule-Related Drug & Molecule List

9 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Candesartan	DMRK8OT	Chronic heart failure	BD1Z	Approved	[1]
Dexmethylphenidate	DMUQE2A	Attention deficit hyperactivity disorder	6A05.Z	Approved	[2]
Enalapril	DMNFUZR	Congestive heart failure	BD10	Approved	[3]
Fenofibrate	DMFKXDY	Coronary atherosclerosis		Approved	[]
Irinotecan	DMP6SC2	Adenocarcinoma	2D40	Approved	[4]
Methylphenidate	DM7SJD6	Attention deficit hyperactivity disorder	6A05.Z	Approved	[5]
PSI-7977	DMLSUWZ	HCV 1-6 infection	1E51	Approved	[6]
Rufinamide	DMWE60C	Epilepsy	8A60-8A68	Approved	[7]
Salbutamol	DMN9CWF	Acute asthma	CA23	Approved	[8]

5 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dabigatran etexilate	DMRDZ4X	Venous thromboembolism	BD72	Phase 3	[9]
MK-4827	DMLYGH4	Ovarian cancer	2C73	Phase 3	[10]
Pradaxa	DM2ZYX9	Stroke	8B20	Phase 3	[11]
TA-6366	DMR32KN	N. A.	N. A.	Phase 3	[12]
E6005	DM1S489	Atopic dermatitis	EA80	Phase 2	[13]

1 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Nitrophenyl acetate	DMHSD8A	N. A.	N. A.	Investigative	[14]

References

• [1] Different hydrolases involved in bioactivation of prodrug-type angiotensin receptor blockers: carboxymethylenebutenolidase and carboxylesterase 1. Drug Metab Dispos. 2013 Nov;41(11):1888-95.
• [2] Dexmethylphenidate hydrochloride in the treatment of attention deficit hyperactivity disorder. Neuropsychiatr Dis Treat. 2006 Dec;2(4):467-73.
• [3] Absorption and cleavage of enalapril, a carboxyl ester prodrug, in the rat intestine: in vitro, in situ intestinal perfusion and portal vein cannulation models. Biopharm Drug Dispos. 2015 Sep;36(6):385-397.
• [4] Irinotecan and its active metabolite, SN-38: review of bioanalytical methods and recent update from clinical pharmacology perspectives. Biomed Chromatogr. 2010 Jan;24(1):104-23.
• [5] Methylphenidate is stereoselectively hydrolyzed by human carboxylesterase CES1A1. J Pharmacol Exp Ther. 2004 Aug;310(2):469-76.
• [6] Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977. J Biol Chem. 2010 Nov 5;285(45):34337-47.
• [7] Investigation of the metabolism of rufinamide and its interaction with valproate. Drug Metab Lett. 2011 Dec;5(4):280-9.
• [8] Effect of carboxylesterase 1 c.428G>A single nucleotide variation on the pharmacokinetics of quinapril and enalapril. Br J Clin Pharmacol. 2015 Nov;80(5):1131-8.
• [9] Pharmacogenomics of novel direct oral anticoagulants: newly identified genes and genetic variants. J Pers Med. 2019 Jan 17;9(1). pii: E7.
• [10] Summary of FDA-approved anticancer cytotoxic drugs at May 2019.
• [11] Conventional liquid chromatography/triple quadrupole mass spectrometry based metabolite identification and semi-quantitative estimation approach in the investigation of in vitro dabigatran etexilate metabolism. Anal Bioanal Chem. 2013 Feb;405(5):1695-704.
• [12] Inhibition of human liver carboxylesterase (hCE1) by organophosphate ester flame retardants and plasticizers: implications for pharmacotherapy. Toxicol Sci. 2019 Jul 3. pii: kfz149.
• [13] Safety and efficacy of topical E6005, a phosphodiesterase 4 inhibitor, in Japanese adult patients with atopic dermatitis: results of a randomized, vehicle-controlled, multicenter clinical trial. J Dermatol. 2014 Jul;41(7):577-85.
• [14] Characterization of pyrethroid hydrolysis by the human liver carboxylesterases hCE-1 and hCE-2. Arch Biochem Biophys. 2006 Jan 1;445(1):115-23.