Kelatorphan

Summary

Kelatorphan is a research compound and mixed inhibitor of enkephalin-degrading enzymes, including neprilysin (NEP) and aminopeptidase N (APN). By blocking the breakdown of endogenous enkephalins, it potentiates endogenous opioid activity without directly activating opioid receptors. It has been studied primarily in preclinical models for analgesia and as a tool compound to investigate the endogenous opioid system. It has not advanced to approved clinical use.

Mechanism of Action

Inhibits neutral endopeptidase (NEP, enkephalinase, neprilysin) and aminopeptidase N (APN), thereby preventing the enzymatic degradation of endogenous enkephalins and other opioid peptides, leading to enhanced and prolonged opioid receptor activation.

Routes of Administration

Goals & Uses

• Reducing tolerance to exogenous opioidsResearchLow
• Pharmacological tool for opioid system researchResearchModerate
• Analgesia via endogenous opioid potentiationPain ManagementLow

Contraindications

• Human clinical use (unapproved compound)RegulatoryHigh

Adverse Effects

• Local Injection Site ReactionsDermatologicalUnknown
• Opioid-like side effects (potential)Central Nervous SystemUnknown

Drug Interactions

• Neprilysin inhibitors (e.g., sacubitril)Moderate
• Opioid analgesics (e.g., morphine)Moderate

Population Constraints

• Human subjects (general population)Regulatory/SafetyAbsolute

Regulatory Status

• European UnionUnapprovedNot approved or authorized by the EMA; used only in preclinical research.
• United StatesUnapprovedResearch compound only; no IND or NDA on record for clinical development.
• United KingdomUnapprovedNo MHRA approval; research use only.

Kelatorphan has not been approved by any regulatory authority (FDA, EMA, or MHRA). It remains a research/investigational tool compound used primarily in preclinical pharmacological studies.

Evidence & Sources

No sources recorded yet.