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PAP-1 is a small molecule Kv1.3 blocker that was developed through classical medicinal chemistry from the medicinal plant Ruta graveolens (= the common rue or the herb of grace). Instigated by anecdotal reports from Chile and Austria in 1987 that tea prepared from Ruta graveolens supposedly have beneficial effects in patients with multiple sclerosis, a group of scientists at the University of Kiel in Germany started extracting Ruta and screening the extracts for potassium channel blockers. The investigators identified 5-methoxypsoralen (5-MOP) as the active principle of the plant and demonstrated in off-label single-case studies that 5-MOP improves visual field defects in multiple sclerosis patients. However, since 5-MOP was not suitable for the long-term treatment of MS because of its phototoxicity (= interaction with DNA under UVA irradiation), we designed derivatives of 5-MOP that are not phototoxic and considerably more potent and selective.

The most potent and drug-like of these novel derivatives is PAP-1, which inhibits Kv1.3 with an EC50 of 2 nM and displays an excellent selectivity over other potassium channels.

October 2016
October 2016 Press Release on KPI Therapeutics Presenting Positive Data at Skin Disease Conference
June 2016
June 2016 Press Release About Promising Results of Dalazatide in Lupus Study
June 2016 Fact Sheet: What Is Lupus?
January 2016
January 2016 Press Release on KPI Biotech Showcase
January 2016 Board Member George Miljanich passes
December 2015
December 2015 AIRMID Makes Board Changes
November 2015
November 2015 New Lupus Treatment Being Tested for Younger Patients