Table 1.

Motilin receptor agonists for treatment of disorders associated with delayed gastric emptying

Compound	Structure	Profile	Clinical data
Mitemcinal (GM-611)	Macrolide	Mimicked ability of motilin to cause short-lived contraction of rabbit duodenal muscle. Profiled in vivo using several different animal models (Takanashi and Cynshi, 2009).	Increased gastric emptying and symptomatic relief over 3 months in subset of patients with diabetic gastroparesis, a body mass index of <35 kg·m−2 and good glycaemic control (McCallum et al., 2007).
GSK962040	Small molecule	Translation of recombinant receptor data achieved using human and rabbit isolated stomach, demonstrating long-lasting facilitation of motor nerve activity (Sanger et al., 2009; Broad et al., 2012).	Increased gastric emptying maintained during 14 days repeat dosing in healthy volunteers (Dukes et al., 2009; 2010) and in patients with type I diabetes mellitus and gastroparesis (Hellström et al., 2011).
BMS-591348	Small molecule/peptide hybrid; structure shows example 11A from Li et al. (2004).	Characterized as an agonist using recombinant human receptors (measuring changes in intracellular calcium) and shown to have a favourable desensitization profile using a cell-based tachyphylaxis assay.	None available
RQ-00201894	Small molecule; structure not yet disclosed.	Active at human recombinant receptor and increased gastric emptying in dogs (Takahashi et al., 2010).	None available