General Information of DTT (ID: TT9O6WS)

DTT Name Glucagon receptor (GCGR) DTT Info
Gene Name GCGR

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Discontinued Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Investigative Drug(s)
2 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dasiglucagon DM74SVE Hypoglycemia 5A41 Approved [1]
Glucagon recombinant DMFLUTR Hypoglycemia 5A41 Approved [2]
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16 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Retatrutide DM8WU0Q Obesity 5B81 Phase 3 [3]
Efinopegdutide DMAN2V2 Non-alcoholic steatohepatitis DB92.1 Phase 2 [4]
LGD-6972 DMPL9KG Type-2 diabetes 5A11 Phase 2 [5]
LY-2409021 DMZOIP4 Type-2 diabetes 5A11 Phase 2 [6]
LY2944876 DML6XWR Diabetic complication 5A2Y Phase 2 [7]
LY3437943 DMN37M6 Obesity 5B81 Phase 2 [8]
MK-8521 DMVNAYE Type-2 diabetes 5A11 Phase 2 [9]
PF-06291874 DMN94QM Type-2 diabetes 5A11 Phase 2 [10]
REMD 477 DM13OVF Type-1 diabetes 5A10 Phase 2 [11]
TT-401 DMRQ0SA Type-2 diabetes 5A11 Phase 2 [9]
DD01 DM0JKZ6 Obesity 5B81 Phase 1 [12]
LY3305677 DMJMLLW Type 2 diabetes 5A11 Phase 1 [13]
Pemvidutide DMVOG8A Obesity 5B81 Phase 1 [14]
REGN1193 DMYBELW Type-2 diabetes 5A11 Phase 1 [15]
SAR425899 DM53IPE Diabetic complication 5A2Y Phase 1 [16]
ZP2929 DMRVDUM Type-1 diabetes 5A10 Phase 1 [17]
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⏷ Show the Full List of 16 Clinical Trial Drug(s)
33 Patented Agent(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
3-substituted-2-furancarboxylic acid hydrazide derivative 1 DMKEOH8 N. A. N. A. Patented [18]
3-substituted-2-furancarboxylic acid hydrazide derivative 5 DMLK29E N. A. N. A. Patented [18]
Aromatic ring compound 1 DMJX6DV N. A. N. A. Patented [18]
Aromatic ring compound 2 DMMAS3G N. A. N. A. Patented [18]
Aromatic ring compound 3 DM43APD N. A. N. A. Patented [18]
Aromatic ring compound 4 DMXGLST N. A. N. A. Patented [18]
Biphenyl carboxamidopropanoic acid derivative 1 DM6803W N. A. N. A. Patented [18]
Biphenyl carboxamidopropanoic acid derivative 2 DMQF2XN N. A. N. A. Patented [18]
Biphenyl carboxamidopropanoic acid derivative 3 DMLOVMP N. A. N. A. Patented [18]
Biphenyl carboxamidopropanoic acid derivative 4 DM715E8 N. A. N. A. Patented [18]
Heterocycle-containing compound 1 DM8PHBG N. A. N. A. Patented [18]
Heterocycle-containing compound 2 DM2KVMT N. A. N. A. Patented [18]
Heterocycle-containing compound 3 DMHMTF7 N. A. N. A. Patented [18]
Heterocycle-containing compound 4 DM6IRJL N. A. N. A. Patented [18]
Heterocycle-containing compound 5 DM6EY5Z N. A. N. A. Patented [18]
Picolinamido propanoic acid derivative 1 DMUP4DX N. A. N. A. Patented [18]
Picolinamido propanoic acid derivative 2 DMR74ET N. A. N. A. Patented [18]
Picolinamido propanoic acid derivative 3 DMP1RV5 N. A. N. A. Patented [18]
PMID25828189-Compound-19 DMEC1TR N. A. N. A. Patented [18]
PMID25828189-Compound-21 DM7D0CT N. A. N. A. Patented [18]
PMID25828189-Compound-22 DMC2O0Q N. A. N. A. Patented [18]
Pyrrolidine derivative 6 DMJ3ZP2 N. A. N. A. Patented [18]
Pyrrolidine derivative 7 DMIOJD6 N. A. N. A. Patented [18]
Pyrrolidine derivative 8 DMWPXJ5 N. A. N. A. Patented [18]
Quinolinyl compound 1 DMENZPR N. A. N. A. Patented [18]
Quinolinyl compound 2 DMGLK92 N. A. N. A. Patented [18]
Spiroimidazolone derivative 1 DMCPVRU N. A. N. A. Patented [18]
Spiroimidazolone derivative 2 DM3EAHB N. A. N. A. Patented [18]
Spiroimidazolone derivative 3 DM02J8N N. A. N. A. Patented [18]
Spiroimidazolone derivative 4 DMXIHPT N. A. N. A. Patented [18]
Spiroimidazolone derivative 5 DM5A62X N. A. N. A. Patented [18]
Spiroimidazolone derivative 6 DMJN5CI N. A. N. A. Patented [18]
Spiroimidazolone derivative 7 DM5A4TP N. A. N. A. Patented [18]
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⏷ Show the Full List of 33 Patented Agent(s)
5 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
BAY-27-9955 DMGDSCK Type-2 diabetes 5A11 Discontinued in Phase 1 [19]
BAY-73-7977 DMKJ3IA Diabetic complication 5A2Y Discontinued in Phase 1 [20]
NN-2501 DM95NDT Type-2 diabetes 5A11 Discontinued in Phase 1 [21]
DIO-901 DMAK3V7 Type-1 diabetes 5A10 Terminated [22]
NNC-252504 DM0BYU2 Type-2 diabetes 5A11 Terminated [23]
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13 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
BI-32169 DMN052T Discovery agent N.A. Investigative [24]
Des-His1[Glu9]glucagon-NH2 DMGTAZ4 Discovery agent N.A. Investigative [25]
DSR-17759 DM4EKHR Non-insulin dependent diabetes 5A11 Investigative [26]
DwLIP-GCGRrx DMW9GT7 Diabetic complication 5A2Y Investigative [27]
glucagon-(1-6) DMVWDHM Discovery agent N.A. Investigative [28]
hGCGR antagonist DMOIPYD Discovery agent N.A. Investigative [29]
L-168049 DM3UGMD Diabetic complication 5A2Y Investigative [26]
MAR-531 DMKT21X Hypoglycemia 5A41 Investigative [26]
NNC 92-1687 DMPQ1HL Discovery agent N.A. Investigative [30]
[des-His1,Tyr5,Glu9,D-Ala10]glucagon-NH2 DM1EPZB Discovery agent N.A. Investigative [31]
[des-His1,Tyr5,Glu9,D-Phe10]glucagon-NH2 DM06Q2V Discovery agent N.A. Investigative [31]
[des-His1,Tyr5,Glu9,D-Tyr10]glucagon-NH2 DMFLVED Discovery agent N.A. Investigative [31]
[des-His1,Tyr5,Glu9]glucagon-NH2 DM93I0B Discovery agent N.A. Investigative [31]
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⏷ Show the Full List of 13 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
2 Glucagon receptor expression and glucagon stimulation of ghrelin secretion in rat stomach. Biochem Biophys Res Commun. 2007 Jun 15;357(4):865-70.
3 Is retatrutide (LY3437943), a GLP-1, GIP, and glucagon receptor agonist a step forward in the treatment of diabetes and obesity? Expert Opin Investig Drugs. 2023 May;32(5):355-359.
4 Emerging glucagon-like peptide 1 receptor agonists for the treatment of obesity. Expert Opin Emerg Drugs. 2021 Sep;26(3):231-243.
5 Addressing Unmet Medical Needs in Type 2 Diabetes: A Narrative Review of Drugs under Development. Curr Diabetes Rev. 2015 March; 11(1): 17-31.
6 Short-term administration of the glucagon receptor antagonist LY2409021 lowers blood glucose in healthy people and in those with type 2 diabetes. Diabetes Obes Metab. 2015 Apr;17(4):414-22.
7 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
8 LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept. Cell Metab. 2022 Sep 6;34(9):1234-1247.e9.
9 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
10 Clinical pipeline report, company report or official report of pfizer.
11 Effect of a glucagon receptor antibody (REMD-477) in type 1 diabetes: A randomized controlled trial. Diabetes Obes Metab. 2018 May;20(5):1302-1305.
12 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
13 IBI362?(LY3305677), a weekly-dose GLP-1 and glucagon receptor dual agonist, in Chinese adults with overweight or obesity: A randomised, placebo-controlled, multiple ascending dose phase 1b study. EClinicalMedicine. 2021 Aug 13;39:101088.
14 Effects of ALT-801, a GLP-1 and glucagon receptor dual agonist, in a translational mouse model of non-alcoholic steatohepatitis. Sci Rep. 2022 Apr 23;12(1):6666.
15 A first-in-human pharmacodynamic and pharmacokinetic study of a fully human anti-glucagon receptor monoclonal antibody in normal healthy volunteers. Diabetes Obes Metab. 2018 Feb;20(2):283-291.
16 Company report (Sanofi) (drug: LIXisenatide)
17 Company report (Zealandpharma)
18 Small molecule glucagon receptor antagonists: a patent review (2011 - 2014).Expert Opin Ther Pat. 2015 Jul;25(7):819-30.
19 Effects of a novel glucagon receptor antagonist (Bay 27-9955) on glucagon-stimulated glucose production in humans. Diabetologia. 2001 Nov;44(11):2018-24.
20 WO patent application no. 2012,0351,39, Prodrugs comprising an exendin linker conjugate.
21 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018428)
22 Effects of low-dose and high-dose glucagon on glucose production and gluconeogenesis in humans. Metabolism. 2000 Jan;49(1):39-46.
23 A novel glucagon receptor antagonist, NNC 25-0926, blunts hepatic glucose production in the conscious dog. J Pharmacol Exp Ther. 2007 May;321(2):743-52.
24 BI-32169, a bicyclic 19-peptide with strong glucagon receptor antagonist activity from Streptomyces sp. J Nat Prod. 2004 Sep;67(9):1528-31.
25 Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1401-5.
26 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: 251).
27 Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2009).
28 Glucagon1-6 binds to the glucagon receptor and activates hepatic adenylate cyclase. J Biol Chem. 1979 Jan 25;254(2):268-9.
29 A novel glucagon receptor antagonist inhibits glucagon-mediated biological effects. Diabetes. 2004 Dec;53(12):3267-73.
30 Discovery and structure-activity relationship of the first non-peptide competitive human glucagon receptor antagonists. J Med Chem. 1998 Dec 17;41(26):5150-7.
31 Topographical amino acid substitution in position 10 of glucagon leads to antagonists/partial agonists with greater binding differences. J Med Chem. 1996 Jun 21;39(13):2449-55.