Difelikefalin is a selective kappa-opioid receptor (KOR) agonist and pharmaceutical active ingredient developed for the management of moderate-to-severe pruritus (itching) associated with certain chronic conditions.
Difelikefalin is a synthetic peripherally acting peptide designed to selectively activate kappa-opioid receptors. Unlike traditional centrally acting opioid agonists, its pharmacological activity is primarily directed toward peripheral KOR pathways.
Difelikefalin is identified by CAS No. 1025796-47-9. Its molecular formula is C36H53N7O6 and its molecular weight is approximately 679.86 g/mol.
Difelikefalin selectively activates kappa-opioid receptors, which are involved in the modulation of itch and sensory signaling. Activation of these receptors can reduce pruritic signaling and provide relief from itching.
Difelikefalin is a selective kappa-opioid receptor agonist. It binds to KORs expressed in peripheral tissues and sensory pathways involved in itch transmission.
Activation of these receptors modulates neuronal signaling associated with pruritus, thereby reducing the perception and intensity of itching.
Difelikefalin is used in pharmaceutical products for the treatment of:
Approved indications and formulations may vary by country and regulatory jurisdiction.
Difelikefalin is relevant to pharmaceutical manufacturers and formulation-development organizations working on antipruritic therapies, nephrology-related treatments and peripheral opioid receptor agonist products.
Because Difelikefalin is a peptide API, appropriate controls for identity, purity, peptide-related impurities, water content and solid-state characteristics are important during pharmaceutical development and manufacturing.
Difelikefalin API quality evaluation may include:
Testing should be performed using validated analytical methods appropriate for the API and intended formulation.
Difelikefalin intended for pharmaceutical manufacturing should comply with applicable GMP, quality-control and regulatory requirements. The final specification should correspond to the manufacturer's approved specification and intended market.
A batch-specific Certificate of Analysis (CoA) should provide relevant analytical results and acceptance criteria.
Difelikefalin should be stored in suitable, tightly closed packaging under the manufacturer's recommended storage conditions. Appropriate temperature and moisture controls should be maintained according to the approved material specification.
Difelikefalin is relevant to pharmaceutical companies and formulation-development organizations working with pruritus-management and chronic kidney disease-associated therapeutic products.
For commercial pharmaceutical applications, customers should verify the API form, grade, assay, peptide purity, impurity profile, specification, regulatory documentation and batch-specific CoA before use.
Consistent Difelikefalin quality is important for reliable pharmaceutical formulation and manufacturing. Appropriate control of identity, peptide purity, assay and related substances supports reproducible product quality.
Quality documentation may include a Certificate of Analysis, specification sheet, safety documentation and applicable regulatory information.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | NLT 98.0% by HPLC |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 10 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | ≤ 0.5% |
| Water Content | NMT 0.5% |
| Melting Point | 150°C – 154°C |