 | |
| Clinical data | |
|---|---|
| Routes of administration | Oral |
| ATC code |
|
| Pharmacokinetic data | |
| Eliminationhalf-life | ~4.5 hours |
| Identifiers | |
| |
| CAS Number | |
| PubChemCID | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| Chemical and physical data | |
| Formula | C24H27FN2O |
| Molar mass | 378.491 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
Cebranopadol (developmental codeTRN-228 and formerlyGRT-6005) is ananalgesic of the benzenoid class which is currently under development for the treatment ofpain.[1] It is currently under development by Tris Pharma,[2][3] was originally discovered and developed byGrünenthal, and was formerly developed by Park Therapeutics andDepomed.[1][4][5][6] As of August 2025, the drug has reachedphase 3clinical trials.[1] Cebranopadol either has been encountered or could be encountered as an opioiddesigner drug.[7]
Cebranopadol is unique in itsmechanism of action via acting as afull agonist of theμ-opioid receptor (Ki = 0.7 nM; EC50 = 1.2 nM; IA = 104%) andnociceptin receptor (or NOP receptor) (Ki = 0.9 nM;EC50 = 13.0 nM;IATooltip intrinsic activity = 89%). It has lower affinity for theδ-opioid receptor (Ki = 18 nM; EC50 = 110 nM; IA = 105%), and is apartial agonist of theκ-opioid receptor (Ki = 2.6 nM; EC50 = 17 nM; IA = 67%).[4] TheEC50 values of 0.5–5.6 μg/kg when introduced intravenously and 25.1 μg/kg after oral administration.[8]
Cebranopadol showsantinociceptive andantihypertensive effects in a variety of differentanimal models of pain.[4] It has also been found to be more effective in models of chronicneuropathic pain than acutenociceptive pain compared to selective μ-opioid receptor agonists.[4] Relative to morphine,tolerance to the analgesic effects of cebranopadol has been found to be delayed (26 days versus 11 days for complete tolerance).[4] In addition, unlike morphine, cebranopadol has not been found to affectmotor coordination or reducerespiration in animals at doses in or over the dosage range for analgesia.[4] As such, it might have improved and prolongedefficacy and greatertolerability in comparison to existing opioid analgesics.[4]
As an agonist of the κ-opioid receptor, cebranopadol may have the capacity to producepsychotomimetic effects,dysphoria, and otheradverse reactions at sufficiently high doses, a property which could potentially limit its practical clinical dosage range, but would likely reduce the occurrence of patients taking more than their prescribed dose.[9]
{{cite press release}}:|last= has generic name (help)