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news.Kinex Pharmaceuticals announced today that the first actinic keratosis patient has been dosed with KX2-391 ointment in Austin, Texas.
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KX2-391 (KX01), a dual Src/pre-tubulin inhibitor, is a small molecule drug that has excellent skin penetration when formulated as a topical ointment.
The pre-tubulin activity causes hyperproliferating cells to undergo apoptosis due to a disruption of the tubulin dynamics needed for these cells to pass through mitosis. Actinic Keratosis (AK) is a very common skin disease that appears as rough, dry, scaly patches or growths that form on the skin when the skin is badly damaged by ultraviolet rays from the sun or through indoor tanning.
Ultraviolet rays can cause damage to DNA and RNA leading to keratinocyte mutations and uncontrolled growth. Reduction of the tumor suppressor p53 level has also been implicated in the unchecked proliferation of dysplastic keratinocytes.
KX2-391 also potently increases p53 levels during unchecked proliferation thereby potentially addressing the dysregulation of p53 in AK.
Dr. Rudolf Kwan, Chief Medical Officer of Kinex Pharmaceuticals commented "Actinic Keratosis is a common dermatological problem with long term overexposure to the sun’s ultraviolet light. If left untreated, AK can progress to squamous cell carcinoma, a type of skin cancer. Once a patient is afflicted with AK lesions, they tend to continue getting new AK lesions for life. We are hopeful to offer a new treatment option for these patients."
"The mechanisms of action, and physical properties of KX2-391, are opening the door for a range of therapeutic applications, both as a topical formulation for skin diseases and as an oral formulation for oncology diseases. I am very pleased to see yet another compound emanating from our platform technologies expand its potential clinical utility," remarked David Hangauer, Kinex’s Chief Scientific Officer.
Flint Besecker, Chief Operating Officer at Kinex added "This ointment evolved out of our joint collaboration with our Taiwan partner, PharmEssentia. It demonstrates the shareholder impact our partnership capital can provide as we work creatively throughout the year on projects under the leadership of our Global Joint Scientific Committee. KX2-391 has developed into a drug candidate with multiple applications including an ointment for psoriasis by our partner PharmEssentia, an oral formulation for oncology applications, and now an ointment application for actinic keratosis. This is yet another important expansion of our clinical portfolio in the US and abroad."