Table 1.

A summary of GIPR antagonists with compound classifications, structures, stage of development and supporting references where available. Amino acid sequences are provided for peptide-based antagonists using single-letter abbreviations. ‘Pal’ indicates a C-16 palmitic acid attachment, ‘γE-C16’ indicates a palmitic acid attached via gamma-glutamic acid, ‘Aib’ indicates inclusion of the unnatural amino acid, 2-aminoisobutyric acid. ‘mGIPAb’ is a murine monoclonal antibody while ‘hGIPR’ is human based. Cases in which structures are not available are denoted ‘N/A’.

Compound name	Compound classification	Structure	Stage of development	Company/institution	Reference
SKL-1459	Small molecule	N/A	Preclinical	Sanwa Kagaku Kenkyusho Co.	Nakamura et al. (2012, 2018)
GIP(3–42)	Peptide	EGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ	Preclinical	University of Copenhagen	Deacon et al. (2006), Hansen et al. (2016)
GIP(3–30)NH2	Peptide	EGTFISDYSIAMDKIHQQDFVNWLLAQK-NH2	Preclinical with acute study in humans	University of Copenhagen	Deacon et al. (2006), Hansen et al. (2016), Sparre-Ulrich et al. (2017), Gasbjerg et al. (2018)
GIP(7–30)	Peptide	EGTFISDYSIAMDKIHQQDFVNWLLAQK	Preclinical	Boston University	Tseng et al. (1999)
GIP(4–42)	Peptide	GTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ	Preclinical	Ulster University	Kerr et al. (2011)
GIP(5–42)	Peptide	TFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ	Preclinical	Ulster University	Kerr et al. (2011)
GIP(6–42)	Peptide	FISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ	Preclinical	Ulster University	Kerr et al. (2011)
GIP(7–42)	Peptide	ISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ	Preclinical	Ulster University	Kerr et al. 2011
GIP(8–42)	Peptide	SDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ	Preclinical	Ulster University	Kerr et al. (2011)
(Pro3)GIP	Peptide	YAPGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ	Preclinical	Ulster University	Gault et al. (2002)
(Ala3)GIP	Peptide	YAAGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ	Preclinical	Ulster University	Gault et al. (2007a,b, c)
(Phe3)GIP	Peptide	YAFGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ	Preclinical	Ulster University	Gault et al. (2007a,b, c)
(Tyr3)GIP	Peptide	YAYGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ	Preclinical	Ulster University	Gault et al. (2007a, b, c )
(Hyp3)GIP	Peptide	YAOGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ	Preclinical	Ulster University	O’Harte et al. (2006)
(Hyp3)GIP(K16Pal)	Peptide	YAOGTFISDYSIAMDK-[Pal]-IHQQDFVNWLLAQKGKKNDWKHNITQ	Preclinical	Ulster University	O’Harte et al. (2006)
GIP(3–30)-Cex-K40Pal	Peptide	EGTFISDYSIAMDKIHQQDFVNWLLAQKPSSGAPPPSK[Pal]	Preclinical	Ulster University	Pathak et al. (2015a)
GIP(6–30)-Cex-K40Pal	Peptide	EGTFISDYSIAMDKIHQQDFVNWLLAQKPSSGAPPPSK[Pal]	Preclinical	Ulster University	Pathak et al. (2015b)
Pro3GIP(3–30)-Cex-K40Pal	Peptide	PGTFISDYSIAMDKIHQQDFVNWLLAQKPSSGAPPPSK[Pal]	Preclinical	Ulster University	Pathak et al. (2015a)
[Nα-Ac,L14,R18,E21] hGIP(5–31)-K11(γE-C16)	Peptide	TFISDYK-[γE-C16]-IALDKIRQQEFVNWLLAQKG	Preclinical	Novo Nordisk	Yang et al. (2022)
NαAc,K10[γEγE-C16], Arg18,hGIP(5–42)	Peptide	TFISDKSIALDK-[γE-C16]-IRQQEFVNWLLAQKGKKNDWKHNITQ	Preclinical	Novo Nordisk	Yang et al. (2022)
GIPg013	Monoclonal antibody	N/A	Preclinical	MedImmune / AstraZeneca	Ravn et al. (2013)
GIPmAb	Monoclonal antibody	N/A	Preclinical	Case Western Reserve University	Boylan et al. (2015)
hGIPR-Ab	Monoclonal antibody	N/A	Preclinical	Amgen	Killion et al. (2018)
mGIPR-Ab/P1	Peptide-Monoclonal antibody conjugate	[mGIPAb]-GGGGG-H-Aib-EGTFTSDVSSYLE-Aib-QAAKEFIAWLVKGGG	Preclinical	Amgen	Lu et al. (2021)
hGIPR-Ab/P1	Peptide-Monoclonal antibody conjugate	[hGIPAb]-GGGGG-H-Aib-EGTFTSDVSSYLE-Aib-QAAKEFIAWLVKGGG	Preclinical	Amgen	Lu et al. (2021)
AMG133	Peptide-Monoclonal antibody conjugate	N/A	Phase 2 to be completed 2025	Amgen	Clinical Trial Identifier: NCT05669599