GLP-1 receptor as a
Trojan horse into the bloodstream.
The GLP-1 receptor is expressed on intestinal cells and triggers a well-characterized transcytosis pathway — the cell internalizes the bound molecule and releases it on the basolateral side, directly into systemic circulation. Semaglutide (Ozempic) exploits a crude version of this. The 22Rx discovery is the small molecule anchor compounds that bind the GLP-1R extracellular domain and carry arbitrary therapeutic payloads — peptides, proteins, nucleic acids, biologics — through the same door.
Every needle.
Now a pill.
| Injectable Drug | Indication | Current Revenue | 22Rx Version |
|---|---|---|---|
| Semaglutide (Ozempic) | T2 Diabetes / Obesity | $21B/yr | Oral GLP-1 conjugate |
| Adalimumab (Humira) | Rheumatoid Arthritis / IBD | $14B/yr | Oral TNF-α inhibitor |
| Pembrolizumab (Keytruda) | Pan-cancer immunotherapy | $25B/yr | Oral PD-1 blocker |
| Epoetin (Procrit) | Anemia (CKD / chemo) | $5B/yr | Oral EPO mimetic conjugate |
| Any injectable (platform claim) | Any indication | $350B combined | Oral via GLP-1R ECD anchor |
Not a formulation trick.
A receptor-mediated biology.
Oral bioavailability failures happen for two reasons: the molecule is destroyed in the GI tract, or it cannot cross the intestinal epithelium. The GLP-1R anchor compounds solve both. The small molecule anchor is stable orally. The receptor-mediated transcytosis pathway actively transports the conjugate across the epithelium — delivering intact payload into systemic circulation. This is not passive absorption. It is active cellular transport.