Prurisol™

Prurisol™ is Cellceutix’s anti-psoriasis drug candidate.  It is a small molecule (MW=344) that acts through immune modulation and PRINS reduction. Prurisol 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. Prurisol is synthesized through a five-step process using commercially available starting materials.  A patent application covering Prurisol was filed in January of 2012 and is pending.

Clinical Development
Cellceutix is developing Prurisol under FDA guidance that a 505(b)(2) designation is an appropriate development pathway. The initial clinical research will be a brief Bio-equivalence crossover study expected to last approximately 45 days with the primary endpoint of demonstration that Prurisol converts to abacavir in humans, as it has been shown to do in animal models. Upon successful completion of the crossover trial, the Company will initiate a larger Phase 2/3 clinical trial under a 505(b)(2) designation, which would permit Prurisol to move to advanced trials because the active moiety of Prurisol is that of a drug already approved by the FDA.

Cellceutix Completes Patient Enrollment in Clinical Trial of Prurisol

BEVERLY, MA–(Marketwired – Jun 2, 2014) – Cellceutix Corporation (OTCQB: CTIX) (the “Company”), a clinical stage biopharmaceutical company developing innovative therapies in oncology, dermatology, and antibiotic applications, reports today that patient enrollment has been completed in the Company’s Phase 1 crossover study of its anti-psoriasis drug candidate Prurisol. Cellceutix expects lab results, pharmacokinetic studies, and analysis to take approximately two months. If the data shows bioequivalence of Prurisol with Abacavir Sulfate, the Company will then schedule a meeting with the U.S. Food and Drug Administration regarding initiating a Phase 2/3 trial of Prurisol through the 505(b)(2) regulatory pathway.

Please visit http://clinicaltrials.gov/ct2/show/NCT02101216?term=prurisol&rank=1

Prurisol Labratory Summary

Prurisol is more effective than conventional therapies in human psoriatic tissue xenografts

» Prurisol (10 mg/kg PO twice/ day x 21 days)

» 84% reduction in lesion appearance

» 99% reduction in lesions based on histology

» 96% reduction in serum PRINS

» 87% reduction in serum IL-20

» No reoccurrence of lesions within 180 days

» Methotrexate (7.5 mg/kg IP once/ day x 5 days)

» 63% reduction in lesion appearance

» 76% reduction in lesions based on histology

» 48% reduction in serum PRINS

» 46% reduction in serum IL-20

» Lesions reoccurred in 61 days

Prurisol is a small molecule, acting on the principles of immune modulation 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

Prurisol was studied in mice that were irradiated with 350 Rads whole body to suppress graft rejection, and then engrafted with human psoriatic tissue by inserting human psoriatic tissue under the skin using a trocar. Groups of ten mice were treated with Prurisol orally for 21 days with either 10 mg/kg Prurisol once/ day or 10 mg/kg Prurisol twice/day, or with 7.5 mg/kg methotrexate IP once/day, or untreated mice 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, PRINS RNA in psoriatic lesions, and blood IL-20 levels. For these parameters, Prurisol was compared to controls and methotrexate.

In a second experiment, groups of 10 immunocompetent CD-1 mice were treated with one or two doses of 10 mg/kg Prurisol daily or 3 mg/kg efalizumab SC once per week for 3 weeks. CD4+ and CD8+ lymphocyte counts were also measured by flow cytometry and compared to efalizumab. Prurisol significantly reduced all psoriatic endpoints measured relative to controls


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

Prurisol 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, Prurisol can be given orally and is well-tolerated.

A variation of Prurisol in human xenograft model. The top row animals show a relatively clean coat with limited discernibility of psoriasis. The bottom row are the untreated control animals.

By SAR, the lead candidate Prurisol is selected. Prurisol in human xenograft model. The top row animals show a clean coat with no evidence of psoriasis, essentially showing that Prurisol cured the psoriasis in the mice. The bottom row shows the untreated control animals.





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