Kinex receives FDA approval to begin Phase I study of KX2-391 Ointment for actinic keratosis

Kinex Pharmaceuticals announced the receipt of an allowance by the US FDA for the Company's KX2-391 Ointment for the commencement of a Phase I clinical study in actinic keratosis. This is the Company's third IND to be allowed by the US FDA in the past 12 months.

KX2-391 is a synthetic, orally active and highly selective inhibitor of Src tyrosine kinase signaling and tubulin polymerization. KX2-391 promotes the induction of p53, G2/M arrest of proliferating cell populations and subsequent apoptosis via the stimulation of Caspase-3 and PARP cleavage. Potent inhibition of the growth of human keratinocytes and several melanoma cell lines in vitro suggests the potential clinical activity for actinic keratosis and dermatologic malignancies. In addition, KX2-391 has also been observed to inhibit T cell migration and endothelial tubule formation in vitro, suggesting additional potential therapeutic benefits for skin conditions like psoriasis where pathology is supported by lymphocyte infiltration, inflammation, and/or angiogenesis.

"The encouraging pre-clinical data for KX2-391 Ointment has led us to progress into this clinical study. Actinic keratosis is a pre-malignant condition and fits nicely into our oncology portfolio," said Dr. Rudolf Kwan, Chief Medical Officer of Kinex Pharmaceuticals.

Kinex has licensed out the use of KX2-391 for dermatological indications in the Greater China Territory to a company specializing in pharmaceutical formulations, PharmaEssentia Corp. (Taipei, Taiwan). The scientific leader of this project at PharmaEssentia, Dr. Jer Hsu stated, "I would like to congratulate our team for the successful development of the KX2-391 ointment formulation in collaboration with our excellent collaborative partner, Kinex Pharmaceuticals. We are also leading the effort to advance this formulation for the clinical indication of psoriasis in Taiwan." Dr. KoChung Lin, CEO of PharmaEssentia said, "We are delighted to see the successful collaboration in the allowance for the KX2-391 IND for Actinic Keratosis by US FDA. We are also looking forward to applying for a Taiwan IND for KX2-391 ointment and launching our clinical development program for psoriasis in Taiwan. Our collaboration with Kinex has been rewarding and we will use our joint momentum to bring KX2-391 Ointment into the clinic in Asia, expeditiously."

KX2-391 is also being developed as an oral agent for oncology indications and has been tested in four clinical studies, thus far. In defining its pharmacological activity in tumor cells, both in vitro and in vivo, KX2-391 has been shown to have potent activity against a wide range of solid tumors as well as leukemia cell lines, including cell lines that are resistant to commonly used cancer drugs. Kinex has also partnered with Hanmi Pharmaceuticals (Seoul, Korea) to develop the oral formulation of KX2-391 for oncology indications in the Korea and greater China Territory. In partnership with Hanmi Pharmaceuticals, the safety, tolerability and pharmacokinetics of KX2-391 have been studied in more than 120 patients in both solid and liquid tumors. A study of KX2-391 in combination with paclitaxel is currently being conducted in South Korea and sponsored through the collaboration with Hanmi Pharmaceuticals.

Dr. Wing Kai Chan, Head of Clinical Operations for Asia Pacific for Kinex, said, "The ability to develop the new topical formulation of KX2-391 for hyper-proliferative skin diseases shows how Kinex is effectively building up its pipeline of drug candidates. I look forward to working with our partner PharmaEssentia to initiate the clinical trials of KX2-391 Ointment for psoriasis, and oral KX2-391 for leukemia and other oncology indications."