Drug intelligence / Profile preview

PAP-1

Development stage
Phase 1
Modality
Small Molecules
Administration
Oral, Intraperitoneal, Topical
01

Overview

PAP-1 is a **potent and selective small molecule inhibitor** of the voltage-gated potassium channel **Kv1.3**, with an EC50 of 2 nM. Kv1.3 channels are highly expressed on **effector memory T (TEM) cells**. By selectively blocking Kv1.3, PAP-1 suppresses the proliferation and function of TEM cells, resulting in anti-inflammatory effects. PAP-1 is highly selective over other Kv channels and has been shown to be effective in various preclinical models of inflammatory diseases, including allergic contact dermatitis and psoriasis. Studies demonstrate efficacy via oral, intraperitoneal, and topical administration, with good absorption and minimal toxicity reported in animal studies. PAP-1 is currently not approved for human use and is primarily used as a research tool for studying T cell-mediated immune responses[1][2][3][5][7].

Other names
5-(4-Phenoxybutoxy)psoralen
02

Targets

KCNA3 (Potassium voltage-gated channel subfamily A member 3)

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