Kappa-opioid antagonist
Kappa-opioid receptor antagonist
- Reduces dynorphin-driven dysphoria and stress-related anti-reward drive
- May reduce stress-induced drug relapse vulnerability
- κ-blockade may contribute to its anti-craving and antidepressant-like effects
- κ antagonism explored for MDD/anhedonia (aticaprant Phase 3 negative)
Drugs with this mechanism (8)
- 7-OH-mitragynine — Kratom's potent mu-opioid metabolite; carries most of the opioid effect and most of the dependence risk.
- Buprenorphine buccal film — Buccal buprenorphine film for continuous chronic pain; not an addiction-treatment product.
- Buprenorphine SC (weekly/monthly) — Extended-release injectable buprenorphine for opioid use disorder; flexible depot intervals.
- Buprenorphine — Partial mu agonist with a ceiling effect; a mainstay of opioid use disorder.
- Buprenorphine patch — Transdermal buprenorphine for continuous chronic pain; not for acute or as-needed use.
- Naltrexone — Opioid antagonist for alcohol and opioid use disorder; monthly injectable option.
- Buprenorphine ER injection — Monthly subcutaneous buprenorphine depot for moderate-to-severe opioid use disorder.
- Naltrexone ER injection — Extended-release injectable naltrexone for alcohol and opioid use disorders.
Self-check
- What drives the dysphoria targeted by kappa antagonism?
Dynorphin-driven anti-reward signaling. - What was the Phase 3 result for aticaprant in the MDD/anhedonia program described?
Negative.
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