CellCeutix pharmaceutical company

• KM-133 (10 mg/kg PO twice/ day x 14 days)
• 84% reduction in lesion appearance
• 99% reduction in lesions based on histology
• 96% reduction in serum PRINS
• 87% reduction in serum IL-20
• 8-fold increase in 12-R lipoxygenase activity compared to methotrexate
• No reoccurrence of lesions within 180 days
• Methotrexate (7.5 mg/kg PO once/ day x 14 days)
• 63% reduction in lesion appearance
• 86% reduction in lesions based on histology
• 48% reduction in serum PRINS
• 46% reduction in serum IL-20
• Lesions reoccurred in 61 days

 

KM-133 is a small molecule, acting on the principles of immune stimulation and PRINS reduction , that has been found to be effective against psoriasis in animal models, both in induced psoriasis as well as a xenograft model with human psoriatic tissue.
Details
KM-133 was studied in mice that were irradiated with 120 Rads whole body to suppress graft rejection, and then engrafted with human psoriatic tissue.  Groups of ten mice were treated orally for 14 days with either 10 mg/kg KM-133 once/day, 10 mg/kg KM-133 twice/day, 7.5 mg/kg methotrexate once/day or acted as controls.  The mice were followed for 180 days.  Endpoints were skin appearance, based on a score of 0 for normal appearance to 10 for severe lesion, histological observations, also based on a score of 0 for normal appearance to 10 for severe lesion, and blood levels of PRINS, IL-20 and 12-R lipoxygenase activity. For these parameters, KM-133 was compared to controls and methotrexate.  CD4+ and CD8+ lymphocyte counts were also measured and compared to efalizumab.
KM-133 significantly reduced all psoriatic endpoints measured relative to controls (p<0.01).  The higher dose of KM-133 reduced psoriatic endpoints more than methotrexate (p<0.01).

 

In addition, psoriasis did not recur during the study period with the higher dose of KM-133 whereas with methotrexate, psoriasis recurred after an average of 61 days. 
Treatment with KM-133 caused less reduction in CD4+ lymphocyte counts than did efalizumab.  Weight loss in the treated animals was within acceptable limits. 

KM-133 given at 10 mg/kg twice/day was shown to be more effective than methotrexate in reducing psoriatic skin lesions in a human xenograft model. In addition, KM-133 can be given orally and is well-tolerated.