While peptides are currently the dominant approach to GLP-1 agonism, Ambrosia Biosciences is pursuing a small-molecule approach.
Ambrosia Biosciences has completed a Series B round with $100 million in proceeds, which the Colorado biotech will use to unlock what it characterizes as the next stage of obesity treatments: small-molecule GLP-1 pills.
The oversubscribed round will help bankroll a Phase 1 study of Ambrosia’s lead asset and advance its broader small-molecule pipeline, including candidates that target other key cardiometabolic pathways such as GIP and amylin, according to a company release on Tuesday.
The raise was co-led by Blue Owl Healthcare Opportunities, Redmile and Deep Track Capital, all new investors. Other funders included BVF Partners, Boulder Ventures, Samsara BioCapital and Janus Henderson Investors.
Peptides currently dominate the GLP-1 game. Novo Nordisk’s semaglutide—marketed as Ozempic for type 2 diabetes and Wegovy for weight loss—is a peptide analog of the GLP-1 hormone. The same is true of Eli Lilly’s tirzepatide, branded as Mounjaro for diabetes and Zepbound for obesity, though these drugs also act on the GIP receptor. Compared to peptides, which have low metabolic stability, small molecules generally make for better oral drugs and are easier to manufacture.
In late December 2025, the FDA approved a pill version of Novo’s Wegovy, bringing peptide GLP-1s to the oral arena. Notably, Eli Lilly’s weight loss pill orforglipron, which is currently under review with a decision expected in the coming days, is a small molecule.
Ambrosia looks to follow in orforglipron’s footsteps—but also to surpass it. “As the field moves beyond first-generation molecules, we see a meaningful opportunity for differentiated small molecule modulators that are designed with combinability in mind,” CEO Nick Traggis said in a statement on Tuesday.
Ambrosia’s approach looks at the structural biology of the target receptor and leverages an AI-driven molecule design engine to generate differentiated assets. Produced using this platform, the biotech’s lead asset is a GLP-1 drug with an “emphasis on lower effective human dosing, superior 24-hour target coverage, and improved combinability,” according to its website.
Ambrosia is hardly the only company pushing the GLP-1 game beyond peptides. Structure Therapeutics, for instance, is working on aleniglipron, which is likewise a small-molecule.
Earlier this month, the biotech released mid-stage data for the asset, touting a 16.3% placebo-adjusted mean weight reduction at 44 weeks, an effect BMO Capital Markets analysts said in a March 16 note was “highly competitive and better than orforglipron and the Wegovy pill.” Structure plans to launch a late-stage program for aleniglipron later this year.
