Cebranopadol
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| Clinical data | |
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| Routes of administration | Oral |
| ATC code |
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| Pharmacokinetic data | |
| Elimination half-life | ~4.5 hours |
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Cebranopadol (developmental code GRT-6005) is an
phase III clinical trials
.
Cebranopadol is unique in its
full agonist of the μ-opioid receptor (Ki = 0.7 nM; EC50 = 1.2 nM; IA = 104%), and δ-opioid receptor (Ki = 18 nM; EC50 = 110 nM; IA = 105%), and as a partial agonist of the nociceptin receptor (Ki = 0.9 nM; EC50 = 13.0 nM; IA = 89%) and κ-opioid receptor (Ki = 2.6 nM; EC50 = 17 nM; IA = 67%).[1] The EC50 values of 0.5–5.6 µg/kg when introduced intravenously and 25.1 µg/kg after oral administration.[4]
Cebranopadol shows highly potent and effective
nociceptive pain compared to selective μ-opioid receptor agonists.[1] Relative to morphine, tolerance to the analgesic effects of cebranopadol has been found to be delayed (26 days versus 11 days for complete tolerance).[1] In addition, unlike morphine, cebranopadol has not been found to affect motor coordination or reduce respiration in animals at doses in or over the dosage range for analgesia.[1] As such, it may have improved and prolonged efficaciousness and greater tolerability in comparison to currently available opioid analgesics.[1]
As an agonist of the κ-opioid receptor, cebranopadol may have the capacity to produce
adverse 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.[5]