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

General Information of DME (ID: DE85D2P)

• DME Name: UDP-glucuronosyltransferase 1A9 (UGT1A9) DME Info
• Gene Name: UGT1A9

Molecule-Related Drug & Molecule List

38 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[1]
Ambrisentan	DMD1QXW	Pulmonary arterial hypertension	BB01.0	Approved	[2]
Canagliflozin	DMFRM1I	Non-insulin dependent diabetes	5A11	Approved	[3]
Dapagliflozin	DM28UJG	Non-insulin dependent diabetes	5A11	Approved	[4]
Darolutamide	DMV7YFT	Prostate cancer	2C82.0	Approved	[5]
Dexibuprofen	DMFYBD0	Ankylosing spondylitis	FA92.0	Approved	[6]
Diclofenac	DMPIHLS	Chronic renal failure	GB61.Z	Approved	[7]
Dihydroartemisinin	DMBXVMZ	Malaria	1F40-1F45	Approved	[8]
Empagliflozin	DMRF9YK	Type-1 diabetes	5A10	Approved	[9]
Entacapone	DMLBVKQ	Parkinson disease	8A00.0	Approved	[10]
Etodolac	DM6WJO9	Osteoarthritis	FA00-FA05	Approved	[6]
Fenofibrate	DMFKXDY	Coronary atherosclerosis		Approved	[11]
Flurbiprofen	DMGN4BY	Osteoarthritis	FA00-FA05	Approved	[6]
Fostamatinib	DM6AUHV	Immune thrombocytopenic purpura	3B64.13	Approved	[]
Gemfibrozil	DMD8Q3J	Hyperlipidaemia	5C80	Approved	[12]
Haloperidol	DM96SE0	Delirium		Approved	[6]
Ibuprofen	DM8VCBE	Dysmenorrhea	GA34.3	Approved	[6]
Indomethacin	DMSC4A7	Bursitis		Approved	[13]
Ketobemidone	DMM3L6Z	Pain	MG30-MG3Z	Approved	[6]
Labetalol	DMK8U72	Hypertension	BA00-BA04	Approved	[14]
Lumiracoxib	DM1S4AG	Chronic renal failure	GB61.Z	Approved	[6]
Mycophenolate mofetil	DMPQAGE	Hepatosplenic T-cell lymphoma		Approved	[15]
Mycophenolic acid	DMRBMAU	Crohn disease	DD70	Approved	[16]
Naproxen	DMZ5RGV	Bursitis		Approved	[17]
Nateglinide	DMLK2QH	Diabetic complication	5A2Y	Approved	[6]
PF-04449913	DMSB068	Chronic myelomonocytic leukaemia	2A40	Approved	[18]
PF-04971729	DM79VXT	Type-2 diabetes	5A11	Approved	[19]
Propofol	DMB4OLE	Anaesthesia	9A78.6	Approved	[6]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[20]
Retigabine	DMGNYIH	Behcet disease	4A62	Approved	[21]
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[22]
Sulfamethoxazole	DMB08GE	Acute otitis media	AB00	Approved	[6]
Tapentadol hydrochloride	DMXLSH3	Acute pain	MG31	Approved	[23]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[24]
Valdecoxib	DMAY7H4	Osteoarthritis	FA00-FA05	Approved	[6]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[6]
Vorinostat	DMWMPD4	Adult acute monocytic leukemia		Approved	[25]
Zileuton	DMVRIC2	Allergic asthma	CA23.0	Approved	[6]

10 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ataluren	DM4GXW3	Cystic fibrosis	CA25	Phase 3	[26]
Curcumin	DMQPH29	Solid tumour/cancer	2A00-2F9Z	Phase 3	[27]
Dabigatran etexilate	DMRDZ4X	Venous thromboembolism	BD72	Phase 3	[28]
GSK1265744	DMT8J0I	Human immunodeficiency virus infection	1C62	Phase 3	[29]
MURAGLITAZAR	DMG3NFZ	N. A.	N. A.	Phase 3	[30]
BCP-13498	DM2BO9W	N. A.	N. A.	Phase 2	[1]
LE-SN38	DMW50NF	Colorectal cancer	2B91.Z	Phase 2	[31]
Topiroxostat	DMA04DE	Gout	FA25	Phase 2	[32]
Vadimezan	DMK7CYX	Solid tumour/cancer	2A00-2F9Z	Phase 2	[33]
LM-94	DMW3QGJ	N. A.	N. A.	Phase 1/2	[34]

1 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
EUGENOL	DM7US1H	Discovery agent	N.A.	Patented	[27]

2 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Seratrodast	DMPNTDL	Allergic asthma	CA23.0	Discontinued in Phase 3	[6]
Gavestinel	DM8IL1U	Nerve injury	ND56.4	Discontinued in Phase 2	[6]

3 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Anthraflavic acid	DMN1YFU	N. A.	N. A.	Investigative	[27]
Chrysin	DM7V2LG	Discovery agent	N.A.	Investigative	[27]
phloretin	DMYA50U	Discovery agent	N.A.	Investigative	[27]

References

• [1] Polymorphic expression of UGT1A9 is associated with variable acetaminophen glucuronidation in neonates: a population pharmacokinetic and pharmacogenetic study. Clin Pharmacokinet. 2018 Oct;57(10):1325-1336.
• [2] Clinical pharmacokinetics and drug-drug interactions of endothelin receptor antagonists in pulmonary arterial hypertension. J Clin Pharmacol. 2012 Dec;52(12):1784-805.
• [3] Effects of rifampin, cyclosporine A, and probenecid on the pharmacokinetic profile of canagliflozin, a sodium glucose co-transporter 2 inhibitor, in healthy participants. Int J Clin Pharmacol Ther. 2015 Feb;53(2):115-28.
• [4] Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27.
• [5] Drug-drug interaction potential of darolutamide: in vitro and clinical studies. Eur J Drug Metab Pharmacokinet. 2019 Dec;44(6):747-759.
• [6] 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.
• [7] Glucuronidation of nonsteroidal anti-inflammatory drugs: identifying the enzymes responsible in human liver microsomes. Drug Metab Dispos. 2005 Jul;33(7):1027-35.
• [8] Eurartesim - European Medicines Agency
• [9] Empagliflozin (Jardiance): a novel SGLT2 inhibitor for the treatment of type-2 diabetes. P T. 2015 Jun;40(6):364-8.
• [10] Kinetic characterization of the 1A subfamily of recombinant human UDP-glucuronosyltransferases. Drug Metab Dispos. 2005 Jul;33(7):1017-26.
• [11] Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8.
• [12] The UDP-glucuronosyltransferase 2B7 isozyme is responsible for gemfibrozil glucuronidation in the human liver. Drug Metab Dispos. 2007 Nov;35(11):2040-4.
• [13] Contribution of UDP-glucuronosyltransferases 1A9 and 2B7 to the glucuronidation of indomethacin in the human liver. Eur J Clin Pharmacol. 2007 Mar;63(3):289-96.
• [14] Regulation of UDP-glucuronosyltransferase (UGT) 1A1 by progesterone and its impact on labetalol elimination. Xenobiotica. 2008 Jan;38(1):62-75.
• [15] The evolution of population pharmacokinetic models to describe the enterohepatic recycling of mycophenolic acid in solid organ transplantation and autoimmune disease. Clin Pharmacokinet. 2011 Jan;50(1):1-24.
• [16] Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. Drug Metab Dispos. 2011 Mar;39(3):448-55.
• [17] S-Naproxen and desmethylnaproxen glucuronidation by human liver microsomes and recombinant human UDP-glucuronosyltransferases (UGT): role of UGT2B7 in the elimination of naproxen. Br J Clin Pharmacol. 2005 Oct;60(4):423-33.
• [18] Metabolism, excretion and pharmacokinetics of [14C]glasdegib (PF-04449913) in healthy volunteers following oral administration. Xenobiotica. 2017 Dec;47(12):1064-1076.
• [19] The effect of renal impairment on the pharmacokinetics and pharmacodynamics of ertugliflozin in subjects with type 2 diabetes mellitus. J Clin Pharmacol. 2017 Nov;57(11):1432-1443.
• [20] FDA Label of Regorafenib. The 2020 official website of the U.S. Food and Drug Administration.
• [21] Retigabine N-glucuronidation and its potential role in enterohepatic circulation. Drug Metab Dispos. 1999 May;27(5):605-12.
• [22] Pharmacokinetic interaction involving sorafenib and the calcium-channel blocker felodipine in a patient with hepatocellular carcinoma. Invest New Drugs. 2011 Dec;29(6):1511-4.
• [23] Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett. 2008 Jan;2(1):67-75.
• [24] The UDP-glucuronosyltransferase 1A9 enzyme is a peroxisome proliferator-activated receptor alpha and gamma target gene. J Biol Chem. 2003 Apr 18;278(16):13975-83.
• [25] Age-dependent hepatic UDP-glucuronosyltransferase gene expression and activity in children. Front Pharmacol. 2016 Nov 16;7:437.
• [26] Ataluren pharmacokinetics in healthy Japanese and Caucasian subjects. Clin Pharmacol Drug Dev. 2019 Feb;8(2):172-178.
• [27] Differential and special properties of the major human UGT1-encoded gastrointestinal UDP-glucuronosyltransferases enhance potential to control chemical uptake. J Biol Chem. 2004 Jan 9;279(2):1429-41.
• [28] Dabigatran acylglucuronide, the major human metabolite of dabigatran: in vitro formation, stability, and pharmacological activity. Drug Metab Dispos. 2010 Sep;38(9):1567-75.
• [29] Disposition and metabolism of cabotegravir: a comparison of biotransformation and excretion between different species and routes of administration in humans. Xenobiotica. 2016;46(2):147-62.
• [30] Involvement of multiple cytochrome P450 and UDP-glucuronosyltransferase enzymes in the in vitro metabolism of muraglitazar. Drug Metab Dispos. 2007 Jan;35(1):139-49.
• [31] Correlation between plasma concentration ratios of SN-38 glucuronide and SN-38 and neutropenia induction in patients with colorectal cancer and wild-type UGT1A1 gene. Oncol Lett. 2012 Mar;3(3):694-698.
• [32] Characterization of N-glucuronidation of 4-(5-pyridin-4-yl-1H-[1,2,4]triazol-3-yl) pyridine-2-carbonitrile (FYX-051): a new xanthine oxidoreductase inhibitor. Drug Metab Dispos. 2007 Dec;35(12):2143-8.
• [33] Predicting pharmacokinetics and drug interactions in patients from in vitro and in vivo models: the experience with 5,6-dimethylxanthenone-4-acetic acid (DMXAA), an anti-cancer drug eliminated mainly by conjugation. Drug Metab Rev. 2002 Nov;34(4):751-90.
• [34] The "albumin effect" and drug glucuronidation: bovine serum albumin and fatty acid-free human serum albumin enhance the glucuronidation of UDP-glucuronosyltransferase (UGT) 1A9 substrates but not UGT1A1 and UGT1A6 activities. Drug Metab Dispos. 2008 Jun;36(6):1056-62.