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pegcantratinib
- Development stage
- Phase 2
- Lead developer
- Sienna Biopharmaceuticals
- Modality
- Small Molecules
- Administration
- Topical
01
Overview
Pegcantratinib is a synthetic, PEGylated small molecule inhibitor of the intracellular kinase domain of tropomyosin-related receptor kinase A (TrkA; NTRK1), the high-affinity receptor for nerve growth factor (NGF). By antagonizing TrkA, pegcantratinib disrupts NGF-TrkA signaling implicated in pruritus and inflammatory skin conditions. It is formulated as a topical agent to maximize local delivery and minimize systemic exposure. Originally developed by Cephalon and later by Sienna Biopharmaceuticals, pegcantratinib has been investigated primarily for pruritus associated with psoriasis, atopic dermatitis, plaque psoriasis, neuropathic pain, and cutaneous cylindroma tumors[1][3][6][7]. Clinical trials have shown it to be well tolerated but efficacy results have been mixed; development has since been discontinued for all indications[6][7].
- Other names
- pegcantratinib
02
Targets
NTRK3 (Tropomyosin receptor kinase C)NTRK2 (Tropomyosin-related kinase receptor type B)NTRK1 (Tropomyosin-related receptor kinase A)
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