Single agonists of the glucagon-like peptide-1 receptor (GLP-1R) have been a success in the treatment of obesity, but monomeric dual or triple agonists have demonstrated improved efficacy on energy intake, appetite or metabolic function.
Oxyntomodulin (OXM) is a peptide hormone released by intestinal L cells after food intake. It acts as a dual agonist of glucagon-like peptide 1 (GLP-1) and glucagon receptors, regulating appetite, energy expenditure and glucose metabolism. However, its short plasma half-life limits its therapeutic potential.
Eli Lilly & Co. has divulged relaxin receptor 1 (RXFP1; LGR7) agonists reported to be useful for the treatment of diabetes, stroke, atherosclerosis, pulmonary hypertension, chronic obstructive pulmonary disease, hypercholesterolemia, chronic kidney disease and diabetes nephropathy, among others.
Adipose tissue is essential for energy balance, but its dysfunction due to excessive lipid accumulation contributes to metabolic disorders such as insulin resistance, dyslipidemia and type 2 diabetes. Thus, regulating adipogenesis represents a promising strategy for combating obesity-related complications.
Neurocrine Biosciences Inc. has divulged cyclic peptides acting as corticotropin-releasing factor 1 and 2 (CRF1 and CRF2) antagonists reported to be useful for the treatment of congenital adrenal hyperplasia, cancer, osteoporosis, myopathy, hyperglycemia, Cushing syndrome, peptic ulcers and hypertension, among others.
Guangdong Zhongsheng Ruichuang Pharmaceutical Co. Ltd. has described glucagon-like peptide 1 receptor (GLP-1R) agonists reported to be useful for the treatment of type 2 diabetes, obesity, atherosclerosis, nonalcoholic or metabolic dysfunction-associated steatohepatitis (NASH/MASH), hyperglycemia, cerebral infarction, hypertension and Parkinson’s disease.
Metabolic dysfunction-associated steatohepatitis (MASH) is a progressive liver disease that has limited available therapies. Shanghai Minwei Biotechnology Co. Ltd. has developed and presented data for MWN-105, a GLP-1/GIP/FGF21 triple agonist aimed at controlling metabolic dysfunction and fibrosis during MASH.
Insparin is a protein isolated from human adenovirus Ad36 that induces cellular glucose uptake without impacting safety. A preclinical study of insparin looked at its potential antidiabetic effects compared to those of pioglitazone.
Glucagon-like peptide 1 receptor (GLP-1R) agonism is a validated approach for treating obesity. ECC-4703 is a small molecule and liver-targeting compound developed by Eccogene Co. Ltd. It is an agonist of thyroid hormone receptor β (THR-β) and its metabolic impact on preclinical models of obesity in combination with semaglutide was investigated.
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