Mitemcinal
Mitemcinal (aka GM-611 or 3'-N-dimethyl-11-deoxy-3'-N-isopropyl-12-O-methyl-11-oxo-8,9-didehydroerythromycin is a motilin agonist derived from the macrolide antibiotic, erythromycin. It was discovered in the labs of Chugai Pharma.
Mitemcinal is orally administered and it is believed to have strong prokinetic[1] characteristics (similar to parent molecule,) but lack antibiotic properties[2] (unlike erythromycin.)
Presently, erythromycin is commonly used off-label for gastric motility indications such as Gastroparesis. If Mitemcinal can be shown to be as effective a prokinetic agent, it would represent a significant advance in the GI field as treatment with this drug would not carry the risk of unintentional selection of antibiotic-resistant bacteria. This concept greatly intrigued Chugai, and the company pursued it as an ideal candidate for a long-term prokinetic agent to treat lower gastrointestinal deficiencies including Gastroparesis[3].
Unfortunately, the FDA were unconvinced that the Phase II trials successfully demonstrated an increase in gastric emptying among the population of diabetic gastroparesis patients above placebo[4]. Thus, although Chugai was able to demonstrate the required safety of the compound, development of this drug has stalled due to a lack of convincing efficacy data.
Notes
- ^ "A group of chemically unrelated drugs that relieve symptoms of reflux by speeding the clearance of acid from the oesophagus and stomach; also known as prokinetic agents"
- ^ Karamanolis G, Tack J (2006). "Promotility medications—now and in the future". Dig Dis. 24 (3–4): 297–307. doi:10.1159/000092883. PMID 16849857.
- ^ Ozaki K, Yogo K, Sudo H; et al. (2007). "Effects of mitemcinal (GM-611), an acid-resistant nonpeptide motilin receptor agonist, on the gastrointestinal contractile activity in conscious dogs". Pharmacology. 79 (4): 223–35. doi:10.1159/000101537. PMID 17426410.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: multiple names: authors list (link) - ^ McCallum RW, Cynshi O (2007). "Clinical trial: effect of mitemcinal (a motilin agonist) on gastric emptying in patients with gastroparesis - a randomized, multicentre, placebo-controlled study". Aliment Pharmacol Ther. 26 (8): 1121–30. doi:10.1111/j.1365-2036.2007.03461.x. PMID 17894654.
{{cite journal}}: Unknown parameter|month=ignored (help)