Naloxegol is a peripherally acting μ-opioid receptor antagonist (PAMORA) and a polyethylene glycol (PEG)-modified derivative of naloxol. It is designed to selectively antagonize peripheral μ-opioid receptors while having limited penetration across the blood-brain barrier.
Naloxegol is primarily used in pharmaceutical applications for the management of opioid-induced constipation (OIC) in adults receiving opioids for chronic non-cancer pain.
Naloxegol is a well-characterized gastrointestinal pharmaceutical API used in the development and manufacture of formulations intended to address opioid-induced constipation.
Important API quality attributes include identity, assay, related substances, water content, residual solvents, elemental impurities and other applicable pharmaceutical quality parameters.
CAS Number: 854601-70-0
Molecular Formula: C34H53NO11
Molecular Weight: 651.79 g/mol
Chemical Name: (5α,6α)-17-Allyl-6-(2,3,4,5-tetrahydro-6,8-dioxo-7H-4,5-epoxy-1H,3H-benzo[e]azepin-7-yl)-4,5-epoxy-3,6,9,12,15-pentaoxaoctadecan-1-ol
Drug Class: Peripherally Acting μ-Opioid Receptor Antagonist (PAMORA)
Therapeutic Class: Opioid Antagonist
Therapeutic Area: Gastroenterology / Pain Management
Molecule Type: Synthetic Small Molecule
Naloxegol is a peripherally acting μ-opioid receptor antagonist that blocks opioid activity at peripheral μ-opioid receptors in the gastrointestinal tract.
Its pharmacological activity includes:
Naloxegol is structurally related to naloxol and has been modified with a PEG moiety to reduce central nervous system penetration.
Naloxegol API is relevant to:
Naloxegol is specifically developed for the treatment of opioid-induced constipation in adults with chronic non-cancer pain.
Unlike centrally acting opioid antagonists, Naloxegol is designed to act predominantly at peripheral opioid receptors, particularly in the gastrointestinal tract. This allows it to counter opioid-induced gastrointestinal effects while maintaining the analgesic effect of opioid medicines.
Naloxegol is a synthetic PEGylated opioid antagonist. Its chemical structure contains multiple ether linkages and a hydroxyl group associated with the PEG chain.
The API's physical appearance, particle characteristics, polymorphic properties and other physical attributes should be controlled according to the applicable pharmaceutical specification.
A controlled Naloxegol API manufacturing process may involve:
Typical Naloxegol API testing may include:
Store Naloxegol API in a tightly closed container under controlled pharmaceutical storage conditions, protected from excessive moisture, heat and direct light.
Final storage conditions should be established according to validated stability data and the applicable API specification.
Naloxegol is relevant to research involving:
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |