desmetramadol

Desmetramadol is an investigational opioid analgesic and the main active metabolite of tramadol. It is a small molecule that acts as a potent G-protein biased agonist at the human µ-opioid receptor (MOR), providing analgesia comparable to morphine and oxycodone but with reduced risk of opioid-induced respiratory depression due to minimal β-arrestin2 recruitment. Unlike tramadol, desmetramadol does not require metabolic activation by CYP2D6 and thus avoids interindividual variability in efficacy related to CYP2D6 polymorphisms. It also inhibits norepinephrine reuptake, contributing to its analgesic effects. Desmetramadol is being developed primarily for the treatment of moderate to severe pain and has reached phase II clinical trials as an oral solution under the brand name Omnitram[1][3][4][5][7].

Brand names

Omnitram

Other names

O-demethyl-tramadolracemic O-desmethyltramadolM1 (as tramadol metabolite)