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

General Information of Drug (ID: DM32NWD)

• Drug Name: LIK-066 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Heart failure	BD10-BD13	Phase 2	[1]
Type-2 diabetes	5A11	Phase 2	[2]

• Cross-matching ID:
  PubChem CID: 52913524
  CAS Number: CAS 1291094-73-9
  TTD Drug ID: DM32NWD
  VARIDT Drug ID: DR01082

Molecule-Related Drug Atlas

Drug(s) Targeting Sodium/glucose cotransporter 2 (SGLT2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dapagliflozin	DM28UJG	Non-insulin dependent diabetes	5A11	Approved	[4]
Empagliflozin	DMRF9YK	Type-1 diabetes	5A10	Approved	[4]
Canagliflozin	DMFRM1I	Non-insulin dependent diabetes	5A11	Approved	[5]
PF-04971729	DM79VXT	Type-2 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]
AVE-2268	DMA42BV	Diabetic complication	5A2Y	Phase 2	[11]
YM-543	DMRZBPI	Type-2 diabetes	5A11	Phase 2	[12]

Drug(s) Targeting Sodium/glucose cotransporter 1 (SGLT1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sotagliflozin	DMMLXA9	Heart failure	BD10-BD13	Approved	[7]
YG1699	DM1NR1J	Type-1 diabetes	5A10	Phase 2	[13]
1614235 + 2330672	DMD751X	Type-2 diabetes	5A11	Phase 1	[3]
GSK1614235	DM7I1AQ	Type-2 diabetes	5A11	Phase 1	[14]
LX2761	DM8ZS7T	Type 2 diabetes	5A11	Phase 1	[15]
T-1095	DMGFS51	Diabetic complication	5A2Y	Discontinued in Phase 2	[16]
KURAIDIN	DMLDUJ1	Discovery agent	N.A.	Investigative	[17]
KURARINONE	DMH0G8W	Discovery agent	N.A.	Investigative	[17]
10-methoxy-N(1)-methylburnamine-17-O-veratrate	DMJW25X	Discovery agent	N.A.	Investigative	[18]
Alstiphyllanine F	DMKRAEW	Discovery agent	N.A.	Investigative	[18]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Sodium/glucose cotransporter 1 (SGLT1)	TT2UE56	SC5A1_HUMAN	Inhibitor	[3]
Sodium/glucose cotransporter 2 (SGLT2)	TTLWPVF	SC5A2_HUMAN	Inhibitor	[1]

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] ClinicalTrials.gov (NCT01824264) Dose-finding Study of LIK066 Compared With Placebo or Sitagliptin to Evaluate Change in HbA1c in Patients With Diabetes. U.S. National Institutes of Health.
• [3] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 915).
• [4] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [5] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [6] 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.
• [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] Effects of AVE2268, a substituted glycopyranoside, on urinary glucose excretion and blood glucose in mice and rats. Arzneimittelforschung. 2008;58(11):574-80.
• [12] Pharmacological Characterization of YM543, a Newly Synthesized, Orally Active SGLT2 Selective Inhibitor. Endocr Res. 2013 Aug;38(3):168-183.
• [13] ClinicalTrials.gov (NCT04956263) A Comparison of Postprandial Glucose After a Mixed Meal Tolerance Test, and the Metabolic Effects of Insulin Withdrawal in a Crossover Study of the Dual Systemic SGLT1 and SGLT2 Inhibitor YG1699, and the Selective SGLT2 Inhibitor Dapagliflozin in Subjects With Type 1 Diabetes. U.S.National Institutes of Health.
• [14] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [15] Clinical pipeline report, company report or official report of Lexicon Pharmaceuticals.
• [16] T-1095, an inhibitor of renal Na+-glucose cotransporters, may provide a novel approach to treating diabetes. Diabetes. 1999 Sep;48(9):1794-800.
• [17] Na+-glucose cotransporter (SGLT) inhibitory flavonoids from the roots of Sophora flavescens. Bioorg Med Chem. 2007 May 15;15(10):3445-9.
• [18] Alstiphyllanines E-H, picraline and ajmaline-type alkaloids from Alstonia macrophylla inhibiting sodium glucose cotransporter. Bioorg Med Chem. 2010 Mar 15;18(6):2152-2158.