Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTYMKBE)

• DTT Name: Gastric inhibitory polypeptide receptor (GIPR)
• Synonyms: Glucosedependent insulinotropic polypeptide receptor; GIPR
• Gene Name: GIPR
• DTT Type: Clinical trial target; [1]
• BioChemical Class: GPCR secretin
• UniProt ID: GIPR_HUMAN
• TTD ID: T41750
• Sequence:
  MTTSPILQLLLRLSLCGLLLQRAETGSKGQTAGELYQRWERYRRECQETLAAAEPPSGLA
  CNGSFDMYVCWDYAAPNATARASCPWYLPWHHHVAAGFVLRQCGSDGQWGLWRDHTQCEN
  PEKNEAFLDQRLILERLQVMYTVGYSLSLATLLLALLILSLFRRLHCTRNYIHINLFTSF
  MLRAAAILSRDRLLPRPGPYLGDQALALWNQALAACRTAQIVTQYCVGANYTWLLVEGVY
  LHSLLVLVGGSEEGHFRYYLLLGWGAPALFVIPWVIVRYLYENTQCWERNEVKAIWWIIR
  TPILMTILINFLIFIRILGILLSKLRTRQMRCRDYRLRLARSTLTLVPLLGVHEVVFAPV
  TEEQARGALRFAKLGFEIFLSSFQGFLVSVLYCFINKEVQSEIRRGWHHCRLRRSLGEEQ
  RQLPERAFRALPSGSGPGEVPTSRGLSSGTLPGPGNEASRELESYC
• Function: This is a receptor for GIP. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
• KEGG Pathway:
  cAMP signaling pathway (hsa04024)
  Neuroactive ligand-receptor interaction (hsa04080)
• Reactome Pathway:
  Glucagon-type ligand receptors (R-HSA-420092)
  G alpha (s) signalling events (R-HSA-418555)

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tirzepatide	DMQNMAT	Type 2 diabetes	5A11	Approved	[2]

8 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Retatrutide	DM8WU0Q	Obesity	5B81	Phase 3	[3]
AMG 133	DMSRCIS	Obesity	5B81	Phase 2	[4]
LY3437943	DMN37M6	Obesity	5B81	Phase 2	[5]
CT 868	DMI7XMU	Type 2 diabetes	5A11	Phase 1	[6]
CT-388	DMWHBE5	Obesity	5B81	Phase 1	[7]
LY3532226	DM9IZG3	Type 2 diabetes	5A11	Phase 1	[8]
LY3537021	DMJUXW7	Type 2 diabetes	5A11	Phase 1	[9]
SAR438335	DM7QO05	Type-2 diabetes	5A11	Phase 1	[1]

2 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
RG7685	DMPQC18	Type-2 diabetes	5A11	Discontinued in Phase 2	[10]
RG7697	DMI1XQ9	Type-2 diabetes	5A11	Discontinued in Phase 2	[11]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Type 2 diabetes	5A11	Liver tissue	6.53E-02	-0.19	-1.27

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] Dual GIP and GLP-1 Receptor Agonist Tirzepatide Improves Beta-cell Function and Insulin Sensitivity in Type 2 Diabetes. J Clin Endocrinol Metab. 2021 Jan 23;106(2):388-396.
• [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] An update on peptide-based therapies for type 2 diabetes and obesity. Peptides. 2023 Mar;161:170939.
• [5] 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.
• [6] Clinical pipeline report, company report or official report of Carmot Therapeutics.
• [7] Emerging glucagon-like peptide 1 receptor agonists for the treatment of obesity. Expert Opin Emerg Drugs. 2021 Sep;26(3):231-243.
• [8] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
• [9] ClinicalTrials.gov (NCT04586907) A Single- and Multiple-Ascending Dose Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of LY3537021 in Healthy Participants and Patients With Type 2 Diabetes Mellitus. U.S.National Institutes of Health.
• [10] Company report (Roche pipeline: October 16, 2012)
• [11] Company report (Roche pipeline: 16 October 2014)