For pharmaceutical companies, patent agents, attorneys, and inventors, cracking this patent wall could unlock generic entry or spark new IP
The critical design decisions included: GIP backbone selection : Starting from GIP rather than GLP-1, as GIP naturally has weak cross-reactivity with GLP-1R, providing a scaffold for optimization Aib2 substitution : Replacing Ala2 with alpha-aminoisobutyric acid for DPP-4 resistance (identical strategy to semaglutide) C-terminal extension : Adding a GGPSSGAPPPS (Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser) 11-residue C-terminal extension that enhances GLP-1R binding C-20 fatty diacid acylation : Attaching an eicosanedioic acid (C-20 diacid) at Lys20 via a Glu-2xOEG linker for albumin binding The resulting molecule exhibits approximately 5:1 selectivity for GIPR over GLP-1R it is a full GIPR agonist and a partial GLP-1R agonist, yet clinically achieves superior outcomes to selective full GLP-1R agonists [7]
It is not licensed as a lipid-lowering medication, and patients requiring pharmacological cholesterol management should continue statins as recommended by NICE guidance, even whilst taking Saxenda for weight loss
The pharmacodynamic profile is significantly improved when these phytochemicals are added to nanoformulations because these formulations improve solubility, extend systemic circulation, and enable selective uptake by ovarian tissues [256]
Many common neuropathological factors are linked with progressive AD
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