Enlicitide (Lipfendra)
The first oral PCSK9 inhibitor. A macrocyclic peptide tablet that lowered LDL cholesterol by 56–59% versus placebo in Phase 3.
The success of GLP-1 medicines and the rise of macrocyclic peptides are reshaping what peptide therapeutics can do, and what it takes to develop them.
GLP-1 (glucagon-like peptide-1) is a natural incretin hormone. Engineered analogues such as semaglutide and the dual GIP/GLP-1 agonist tirzepatide have delivered strong glycaemic control and weight loss once associated mainly with bariatric surgery.
How GLP-1 works
Stimulates insulin release when blood glucose is high.
Suppresses glucagon, so the liver releases less glucose.
Delays gastric emptying for a steadier glucose profile.
Acts on the brain to increase fullness and reduce intake.
Incretin science has moved from single to multi-receptor peptides, and several of these molecules are in our API pipeline.
Also moving fast
Linear peptides have dominated the market, but cyclising a peptide locks it into its active shape. That makes macrocycles one of the fastest-moving areas of drug discovery, with approved examples from cyclosporine A and octreotide to zilucoplan. In 2026 the field reached a milestone: the first oral macrocyclic peptides, from Merck and Johnson & Johnson, won FDA approval.
What cyclisation brings
Fewer free ends for proteases to attack.
Higher affinity and selectivity for the target.
Improved passage across membranes, including for oral dosing.
Access to protein–protein interfaces and intracellular proteins.
Ring chemistries we make
Two once-daily peptide tablets show that macrocycles can reach targets once open only to injectable antibodies.
The first oral PCSK9 inhibitor. A macrocyclic peptide tablet that lowered LDL cholesterol by 56–59% versus placebo in Phase 3.
The first oral peptide that blocks the IL-23 receptor, for moderate-to-severe plaque psoriasis. Discovered with Protagonist Therapeutics.
Longer analogues and macrocycles raise the bar at every step. Here is how we meet it.
AI-designed libraries and phage display screening to find linear and cyclic binders.
Explore → 02SynthesisLong analogues, lipidation and macrocyclisation, well beyond standard SPPS.
Explore → 03Lead optimisationSAR, stapling and half-life extension to balance potency with drug-like properties.
Explore → 04DevelopmentLC-MS, high-resolution MS and scalable routes designed in from the start.
Explore → 05GMPMulti-kilogram GMP supply at Unit 7, Visakhapatnam.
Explore →From GLP-1 analogues to macrocycles, we support you from first binder to GMP manufacturing.