αvβ6-Integrin, the biological target of 68Ga-Trivehexin, is a heterodimeric transmembrane cell adhesion receptor whose primary natural ligand is latency associated peptide (LAP)[2] in its complex with transforming growth factor beta 1 (TGF-β1).

[13] As the likely most important activator of TGF-β1,[4] αvβ6-integrin is often found overexpressed in tumors[14] and fibrosis,[15] which is why 68Ga-Trivehexin PET imaging is primarily relevant in this medical context.

The chelator comprised in Trivehexin is a triazacycloalkane with 3 phosphinic acid substituents, with the basic structure 1,4,7-triazacyclononane-1,4,7-triphosphinate[16] (frequently abbreviated TRAP).

The peptides are attached to the chelator core via the terminal amine group of the side chains of N-methyl lysine.

Then, Trivehexin (5–10 nmol) is added to the buffered 68Ga-containing solution, and the mixture is briefly heated to 50–100 °C (usually 2–3 min) to finalize the complexation reaction.

Most clinics use PET/CT or even PET/MRI systems that acquire morphological and functional images in a single workflow and thus, provide more detailed and useful medical information to the physician.

[26][27] The tracer then distributes with the blood flow and moves into tissues by diffusion, where it specifically binds to its target αvβ6-integrin, while an excess is excreted via the kidneys and the urine.

Consistent with the "tracer principle", the amount of pharmacologically active compound injected to a patient in the course of such an examination is extremely low.

No adverse or clinically detectable pharmacologic effects were observed following intravenous administration of 68Ga-Trivehexin when administered to cancer patients, and there were no significant changes in vital signs, laboratory study results, or electrocardiograms.

[27] In a study involving healthy volunteers, researchers again reported no adverse or clinically detectable pharmacologic effects and no significant changes in vital signs.