TRV130
 | |
| Systematic (IUPAC) name | |
|---|---|
|
[(3-Methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine | |
| Clinical data | |
| Legal status |
|
| Routes of administration | IV |
| Identifiers | |
| ATC code | None |
| Chemical data | |
| Formula | C22H30N2O2S |
| Molar mass | 386.55 g·mol−1 |
TRV130 is an opioid drug that is under evaluation in human clinical trials for the treatment of acute severe pain. It is a functionally selective μ-opioid receptor agonist developed by Trevena Inc. TRV130 elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β-arrestin 2 recruitment and receptor internalization, it displays less adverse effects than morphine.[1][2][3]
References
- ↑ Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS (October 2013). "Structure-Activity Relationships and Discovery of a G Protein Biased μ Opioid Receptor Ligand, [(3-Methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the Treatment of Acute Severe Pain". J. Med. Chem. 56 (20): 8019–31. doi:10.1021/jm4010829. PMID 24063433.
- ↑ DeWire SM, Yamashita DS, Rominger DH, Liu G, Cowan CL, Graczyk TM, Chen XT, Pitis PM, Gotchev D, Yuan C, Koblish M, Lark MW, Violin JD (March 2013). "A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine". J. Pharmacol. Exp. Ther. 344 (3): 708–17. doi:10.1124/jpet.112.201616. PMID 23300227.
- ↑ Soergel DG, Subach RA, Sadler B, Connell J, Marion AS, Cowan C, Violin JD, Lark MW (October 2013). "First clinical experience with TRV130: Pharmacokinetics and pharmacodynamics in healthy volunteers". J Clin Pharmacol 54 (3): 351–7. doi:10.1002/jcph.207. PMID 24122908.
External links
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