Loxicodegol was developed by Nektar Therapeutics as an opioid analgesic with low abuse potential for the treatment of chronic pain . The lack of abuse potential is believed to be... The lack of abuse potential is believed to be due to the drug's slow rate of entry into brain, a unique characteristic compared to others in the opioid class.
- Mechanism
- Curator reviewed · 1 reference
Loxicodegol is a full agonist at the μ-opioid receptor. It also displays selectivity towards this subtype with an affinity of 237 nM compared to 4150 nM and >100000 nM for the δ- and κ-opioid receptors. The μ-opioid receptor is activated with an EC₅₀ of 12.5 μM. Activation of this receptor produces an inhibitory effect on neurotransmission through Gi/Go coupling. Opioid medications like Loxicodegol inhibit voltage gated Ca²⁺ channel opening presynaptically on C fibres and activate inward-rectifying K⁺ channels post-synaptically on 2nd order neurons, leading to hyperpolarization. Together, these prevent the nociceptive signal from traveling up the spinal cord to the brain. In the brain, opioids work through a mechanism of inhibition of inhibition to allow regulatory neurons to suppress nociception.
- Primary indication
- Loxicodegol was developed as an opioid analgesic with low abuse potential for use in treating chronic pain.Curator reviewed
- Formula / weight
- C31H49NO10 · 595.73 g/mol (avg)
- Also known as
- Loxicodegol
- Code names
- NKTR-181
Resolves to
RQHILGKAOIGUHU-XPLSERNMSA-NSMILES[H][C@@]12OC3=C(OC)C=CC4=C3[C@@]11CCN(C)[C@]([H])(C4)[C@]1(O)CC[C@]2([H])OCCOCCOCCOCCOCCOCCOCWhat you can answer from here — as of June 15, 2026
Which drugs share a target with Oxycodegol, and which of those have an active Phase 3 trial?
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