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Uremic pruritus

The Global Burden of Disease Study suggested that there are 700 million cases of chronic kidney disease (CKD) worldwide. 50% of patients with CKD, and 90% of dialysis patients have uremic pruritus, a condition that have negative physiological, psychological, and social impacts on the patients. The condition severely interferes with patients’ sleeping patterns that devastates patient’s quality of life. Common forms of itch relief methods such as the use of anti-itch creams, antihistamines, corticosteroids, and gabapentin, are at times ineffective. Other kappa agonists given systemically may cause CNS-related side effects. Therefore, uremic pruritis (UP) is a condition that needs to be addressed urgently.

How LT5001 could help?

The API of LT5001, dinalbuphine sebacate (DNS), contains nalbuphine, a kappa agonist and mu antagonist that was used to treat pruritus. LT5001 is formulated as a topical ointment for easy to use and convenient application to the affected area. The systemic exposure is low or non-existent through the transdermal route, providing a peace of mind for compromised patients by sparing them from nephrotoxicity risks and CNS-related side effects. The formulation also allows the dosing regimen to be easily adjusted based on patients’ conditions.

Abnormal endogenous opioid ligand activity at μ and k opioid receptors has been proposed as the mechanism in uremic pruritus. As a topical ointment formulation, LT5001 (as a k agonist/ μ antagonist) is thought to have the potential to modulate peripheral opioid receptors present on sensory nerves and immune cells.


Development progress

The Phase 1b study in Taiwan has been completed and demonstrated that there are no safety concerns in patients treated with LT5001.