Synonyms: CT-327 | CT327 | K-252a-PEG2K | Pegylated K-252 | SNA-120 | SNA120
Compound class:
Synthetic organic
Comment: Pegcantratinib (CT-327/SNA-120) is a clinical stage agent that inhibits the intracellular kinase domain of tropomyosin-related receptor kinase A (TrkA; NTRK1). TrkA is the high affinity receptor for nerve growth factor (NGF), and is a key target in pruritus, within the NGF-TrkA-TRPV1 pathway. As a TrkA inhibitor pegcantratinib is being evaluated as a potential topical treatment for inflammatory skin conditions. Chemically it is a 2kDa PEG derivative of K-252a that was originally developed by Sienna Biopharmaceuticals. PEG conjugation facilitates the delivery of high levels of the active ingredient to skin cells, and avoids the systemic side effects associated with an orally delivered version of the drug.
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References |
1. Roblin D, Yosipovitch G, Boyce B, Robinson J, Sandy J, Mainero V, Wickramasinghe R, Anand U, Anand P. (2015)
Topical TrkA Kinase Inhibitor CT327 is an Effective, Novel Therapy for the Treatment of Pruritus due to Psoriasis: Results from Experimental Studies, and Efficacy and Safety of CT327 in a Phase 2b Clinical Trial in Patients with Psoriasis. Acta Derm Venereol, 95 (5): 542-8. [PMID:25594427] |