lessthanhalf
GLP-1 Specialist
Study published in nature yesterday: https://www.nature.com/articles/s41586-026-10427-5
They have taken a small molecule PPARα/γ/δ agonist, lanifibranor that is in clinical phase 3 trials for the treatment of metabolic dysfunction-associated steatohepatitis, and stuck it to a GLP-1 - GIP agonist peptide, causing substantially more weight loss than the GLP-1 - GIP peptide alone, and because the laniibranor is stuck to the peptide, it is preferentially taken up by cells that have GLP-1 receptors, allowing it to work at doses 1/6000th of the doses used in the phase 3 trials of the drug alone. Which is useful as the molecule alone has side effects. And allows specific precise targeting of the molecule to GLP-1 or GIP expressing cells.
In mice it looks like nearly twice the weight loss of something similar to tirzepatide, or nearly 40% weight loss, the fact that lanifibranor is already in phase 3 might speed things up a bit. Not quite ready for human trials, as they do not feel totally confident they fully understand the effects of PPARα/γ/δ agonism, though the drug is in phase 3 trials?
Not going to happen for quite a while, given what stage the research is at, but I would not be surprised if the basic concept is not repeated with various other small molecules attached to glp-1 peptides in future.
They have taken a small molecule PPARα/γ/δ agonist, lanifibranor that is in clinical phase 3 trials for the treatment of metabolic dysfunction-associated steatohepatitis, and stuck it to a GLP-1 - GIP agonist peptide, causing substantially more weight loss than the GLP-1 - GIP peptide alone, and because the laniibranor is stuck to the peptide, it is preferentially taken up by cells that have GLP-1 receptors, allowing it to work at doses 1/6000th of the doses used in the phase 3 trials of the drug alone. Which is useful as the molecule alone has side effects. And allows specific precise targeting of the molecule to GLP-1 or GIP expressing cells.
In mice it looks like nearly twice the weight loss of something similar to tirzepatide, or nearly 40% weight loss, the fact that lanifibranor is already in phase 3 might speed things up a bit. Not quite ready for human trials, as they do not feel totally confident they fully understand the effects of PPARα/γ/δ agonism, though the drug is in phase 3 trials?
Not going to happen for quite a while, given what stage the research is at, but I would not be surprised if the basic concept is not repeated with various other small molecules attached to glp-1 peptides in future.
