General Information of Drug (ID: DM79VXT)

Drug Name
PF-04971729 Drug Info
Synonyms
Ertugliflozin; 1210344-57-2; PF04971729; UNII-6C282481IP; PF 04971729; CHEMBL1770248; 6C282481IP; AK174928; 1,6-Anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-5-C-(hydroxymethyl)-beta-L-idopyranose; Steglatro; (1S,2S,3S,4R,5S)-5-(4-chloro-3-(4-ethoxybenzyl)phenyl)-1-(hydroxymethyl)-6,8-dioxabicyclo[321]octane-2,3,4-triol; (1S,2S,3S,4R,5S)-5-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-1-(hydroxymethyl)-6,8-dioxabicyclo[321]octane-2,3,4-triol; Ertugliflozin [USAN:INN]; C22H25ClO7; PF-4971729; SGLT2 inhibitor (oral, type 2 diabetes), Pfizer; Sodium glucose cotransporter-2 inhibitor (oral, type 2 diabetes), Pfizer; Ertugliflozin/PF-04971729
Indication
Disease Entry ICD 11 Status REF
Type-2 diabetes 5A11 Approved [1]
Cross-matching ID
PubChem CID
44814423
CAS Number
CAS 1210344-57-2
TTD Drug ID
DM79VXT
INTEDE Drug ID
DR0604
ACDINA Drug ID
D00240

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dapagliflozin DM28UJG Non-insulin dependent diabetes 5A11 Approved [5]
Empagliflozin DMRF9YK Type-1 diabetes 5A10 Approved [5]
Canagliflozin DMFRM1I Non-insulin dependent diabetes 5A11 Approved [6]
Sotagliflozin DMMLXA9 Heart failure BD10-BD13 Approved [7]
Dapagliflozin Propanediol; Saxagliptin Hydrochloride DM34TXO Type-2 diabetes 5A11 Approved [8]
ASP1941 DMGQ1TV Liver disease DB90-BD99 Phase 3 [9]
Remogliflozin etabonate DMW4YK1 Type-1/2 diabetes 5A10-5A11 Phase 2 [10]
LIK-066 DM32NWD Heart failure BD10-BD13 Phase 2 [11]
AVE-2268 DMA42BV Diabetic complication 5A2Y Phase 2 [12]
YM-543 DMRZBPI Type-2 diabetes 5A11 Phase 2 [13]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [14]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [15]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [16]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [17]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [18]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [16]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [19]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [20]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [21]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [22]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [23]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [24]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [25]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [16]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [26]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [16]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [16]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [27]
Nateglinide DMLK2QH Diabetic complication 5A2Y Approved [16]
Haloperidol DM96SE0 Delirium Approved [16]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [28]
Dapagliflozin DM28UJG Non-insulin dependent diabetes 5A11 Approved [29]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [30]
Canagliflozin DMFRM1I Non-insulin dependent diabetes 5A11 Approved [29]
Bexagliflozin DMK56G0 Type 2 diabetes 5A11 Approved [31]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [32]
Urethane DM7NSI0 N. A. N. A. Phase 4 [33]
Remogliflozin etabonate DMW4YK1 Type-1/2 diabetes 5A10-5A11 Phase 2 [29]
Benzo(a)pyrene DMN7J43 N. A. N. A. Phase 1 [34]
T-1095 DMGFS51 Diabetic complication 5A2Y Discontinued in Phase 2 [29]
⏷ 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
Sodium/glucose cotransporter 2 (SGLT2) TTLWPVF SC5A2_HUMAN Modulator [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
UDP-glucuronosyltransferase 2B7 (UGT2B7) DEB3CV1 UD2B7_HUMAN Substrate [3]
UDP-glucuronosyltransferase 1A9 (UGT1A9) DE85D2P UD19_HUMAN Substrate [3]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Sodium/glucose cotransporter 2 (SLC5A2) OT93UUDI SC5A2_HUMAN Gene/Protein Processing [4]

References

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2 Dose-ranging efficacy and safety study of ertugliflozin, a sodium-glucose co-transporter 2 inhibitor, in patients with type 2 diabetes on a background of metformin.Diabetes Obes Metab.2015 Jun;17(6):591-8.
3 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.
4 Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. J Med Chem. 2011 Apr 28;54(8):2952-60. doi: 10.1021/jm200049r. Epub 2011 Mar 30.
5 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
6 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
7 LX4211, a dual SGLT1/SGLT2 inhibitor, improved glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial. Clin Pharmacol Ther. 2012 Aug;92(2):158-69.
8 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
9 Ipragliflozin: A novel sodium-glucose cotransporter 2 inhibitor developed in Japan.World J Diabetes.2015 Feb 15;6(1):136-44.
10 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
11 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
12 Effects of AVE2268, a substituted glycopyranoside, on urinary glucose excretion and blood glucose in mice and rats. Arzneimittelforschung. 2008;58(11):574-80.
13 Pharmacological Characterization of YM543, a Newly Synthesized, Orally Active SGLT2 Selective Inhibitor. Endocr Res. 2013 Aug;38(3):168-183.
14 Metabolism and transport of tamoxifen in relation to its effectiveness: new perspectives on an ongoing controversy. Future Oncol. 2014 Jan;10(1):107-22.
15 Determination of UDP-glucuronosyltransferase UGT2B7 activity in human liver microsomes by ultra-performance liquid chromatography with MS detection. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Jul 1;870(1):84-90.
16 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.
17 Pharmacokinetic and pharmacodynamic interaction of lorazepam and valproic acid in relation to UGT2B7 genetic polymorphism in healthy subjects. Clin Pharmacol Ther. 2008 Apr;83(4):595-600.
18 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
19 Pitavastatin: a review in hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168.
20 Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9.
21 Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet. 2005;44(5):467-94.
22 Pharmacogenomics of statins: understanding susceptibility to adverse effects. Pharmgenomics Pers Med. 2016 Oct 3;9:97-106.
23 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.
24 Glucuronidation of nonsteroidal anti-inflammatory drugs: identifying the enzymes responsible in human liver microsomes. Drug Metab Dispos. 2005 Jul;33(7):1027-35.
25 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.
26 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.
27 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.
28 Cannabidiol induces antioxidant pathways in keratinocytes by targeting BACH1. Redox Biol. 2020 Jan;28:101321. doi: 10.1016/j.redox.2019.101321. Epub 2019 Sep 5.
29 Discovery of novel N--D-xylosylindole derivatives as sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the management of hyperglycemia in diabetes. J Med Chem. 2011 Jan 13;54(1):166-78. doi: 10.1021/jm101072y. Epub 2010 Dec 3.
30 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
31 EGT1442, a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA(1c) levels in db/db mice and prolongs the survival of stroke-prone rats. Pharmacol Res. 2011 Apr;63(4):284-93. doi: 10.1016/j.phrs.2011.01.001. Epub 2011 Jan 5.
32 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
33 Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.
34 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.