Compound monographs — page 2
The Institute publishes a monograph for each of the 51 compounds in its assessment set. Each is one document in eight numbered parts with a per-indication evidence extract for every indication assessed.
Monographs
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Ipamorelin activates the ghrelin receptor on pituitary somatotrophs, producing growth-hormone release through a pathway distinct from and complementary to GHRH receptor signalling. Its defining pharmacological characteristic…
Low20 Feb 2026 -
Kisspeptin acts on KISS1 receptors on hypothalamic gonadotropin-releasing hormone neurons to stimulate GnRH secretion, and thereby luteinising hormone and follicle-stimulating hormone release. Because it acts upstream of GnRH it…
Low11 Jun 2025 -
KPV inhibits NF-κB activation and reduces pro-inflammatory cytokine production in epithelial and immune cells. Reported uptake through the intestinal peptide transporter PepT1 provides a plausible route for local action in…
Very low01 Mar 2024 -
Larazotide antagonises zonulin-mediated tight-junction disassembly, reducing paracellular permeability in intestinal epithelium. The therapeutic hypothesis in coeliac disease was that limiting gluten-peptide translocation across…
Moderate07 May 2026 -
Receptor pharmacology is that of the selective GLP-1 class. The pharmacokinetic engineering differs: self-association into heptamers at the subcutaneous depot slows absorption, and albumin binding through the palmitoyl chain…
High27 Aug 2024 -
A short-acting prandial GLP-1 receptor agonist. Its dominant pharmacodynamic effect is marked slowing of gastric emptying, which produces substantial postprandial glucose reduction with comparatively modest effects on fasting…
Moderate12 Apr 2025 -
LL-37 permeabilises bacterial membranes through an amphipathic helical mechanism and separately acts as a chemoattractant and immunomodulator through formyl peptide receptor 2. It also promotes angiogenesis and wound…
Low27 Apr 2026 -
GLP-1 receptor agonism supplies appetite suppression; GIP receptor antagonism is proposed to act on adipose tissue and central pathways in a manner that also reduces adiposity. The antibody scaffold gives a very long half-life…
Low19 May 2025 -
Mazdutide reproduces the natural dual activity of oxyntomodulin with a pharmacokinetic profile suitable for weekly dosing. The glucagon arm contributes energy expenditure and hepatic lipid mobilisation; the GLP-1 arm supplies…
Moderate22 Jun 2026 -
Melanotan-II is a potent non-selective melanocortin receptor agonist. MC1R agonism stimulates eumelanin synthesis in melanocytes, producing pigmentation without ultraviolet exposure. MC4R agonism concurrently suppresses appetite…
Very low02 Dec 2024 -
CEI-MN-043Mitochondrial and metabolic cofactorsUnapproved, research supply4 assessed outcomesversion 1.0
MOTS-c is described as a mitochondrial-encoded regulator of metabolic homeostasis that acts through the folate one-carbon cycle to raise 5-aminoimidazole-4-carboxamide ribonucleotide and thereby activate AMP-activated protein…
Very low20 Aug 2025 -
CEI-MN-045Mitochondrial and metabolic cofactorsUnapproved, research supply4 assessed outcomesversion 2.1
NAD+ is the central redox coenzyme of intermediary metabolism and the substrate of the sirtuin and poly-ADP-ribose polymerase enzyme families. Tissue NAD+ declines with age in several species, which is the basis of interest in…
Very low23 Aug 2026 -
Orforglipron activates the GLP-1 receptor from a non-peptide scaffold, producing the insulinotropic, glucagonostatic and central appetite effects of the class from an orally bioavailable molecule that does not require an…
Moderate30 Apr 2026 -
Amylin receptor agonism at the area postrema promoting meal-related satiation, with a formulation and half-life supporting weekly dosing. The therapeutic hypothesis is tolerability advantage rather than efficacy advantage.
Low20 Apr 2025 -
Pramlintide reproduces the postprandial actions of endogenous amylin, which is deficient in insulin-deficient diabetes: it slows gastric emptying, suppresses inappropriate postprandial glucagon secretion, and promotes satiation…
Moderate15 Jul 2026 -
Bremelanotide activates central melanocortin-4 receptors, acting on hypothalamic and limbic circuits regulating sexual desire. Unlike phosphodiesterase-5 inhibitors it does not act on the peripheral vasculature. Its…
Moderate15 Aug 2024 -
Retatrutide adds glucagon receptor agonism to the dual incretin mechanism. Glucagon receptor activation increases hepatic fatty-acid oxidation and resting energy expenditure and reduces hepatic steatosis, and in the reported…
Moderate19 May 2023 -
Selank is reported to produce anxiolysis without sedation or dependence, attributed to modulation of GABAergic transmission and to inhibition of enkephalin degradation. It also carries the immunomodulatory activity of the tuftsin…
Low09 Feb 2026 -
Semaglutide is a full agonist at the glucagon-like peptide-1 receptor, a class B G protein-coupled receptor signalling principally through Gαs and adenylyl cyclase. In pancreatic beta cells the resulting rise in cyclic AMP…
High16 Aug 2024 -
Receptor pharmacology is identical to subcutaneous semaglutide. The distinguishing pharmacology is absorption: SNAC buffers the gastric microenvironment, inhibits local pepsin activity and transiently increases permeability…
High28 Jun 2024
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