A comparative analysis found that non-diabetic patients with obesity on tirzepatide had a 64% lower risk of developing new-onset gastroparesis compared to those on semaglutide
It is well established that following a first stimulation, GPCRs that undergo desensitization display reduced responsiveness to a second stimulation with an agonist
Lin D, Wang M, Chen Y, Gong J, Chen L, Shi X, et al
Oral administration of PF-06882961 shows evidence of glucose-lowering in healthy human study participants PF-06882961 was selected as a candidate for clinical studies based on its in vitro and in vivo pharmacologic and disposition profile, including potent agonism of the GLP-1R, preclinical disposition attributes (e.g., low metabolic CL int in human hepatocytes), good safety margins versus the hERG channel (IC 50 = 4.3 M, Table S4) and broad panel screening (Table S8), and selectivity versus related class B GPCRs (Table S9)