Kinex Pharmaceuticals, LLC and Hanmi Pharmaceutical Co., Ltd. announced today the execution of a license agreement from Hanmi Pharmaceuticals granting Kinex Pharmaceuticals exclusive rights to their Orascovery technology (which includes a non-absorbed compound that facilitates the absorption of compounds that are usually not orally bioavailable or absorbed) and their current lead products including an oral formulation of paclitaxel, which is already in Phase II clinical trials in Korea, and an oral formulation of irinotecan, which has just completed Phase I clinical trials in Korea.

The Orascovery program is one of the key platforms developed by Hanmi Pharmaceuticals. HM30181A is a P-glycoprotein pump inhibitor, (known for its effect in pumping drugs back to the gastrointestinal tract and thereby reducing drug absorption) which inhibits the pumping action of this protein and therefore, serves as an oral absorption enhancer. This compound is very potent and is largely not absorbed and therefore, exerts its effect mainly in the gastrointestinal tract.

In preclinical studies, it has been shown that the administration of this absorption enhancer together with paclitaxel enhances the oral bioavailability of paclitaxel from 1% to >40%. For irinotecan and topotecan, the oral bioavailabilities were shown to be enhanced from 8% and 11% to >40% and >50%, respectively. The composition of matter of HM30181A is covered by issued patents.

The acquisition of an oral formulation of paclitaxel is important to both Kinex and Hanmi Pharmaceuticals as the taxanes have been shown to exhibit a strong synergistic effect with KX01, an orally bioavailable dual src kinase/pretubulin inhibitor that Kinex Pharmaceuticals and Hanmi Pharmaceuticals have been collaborating to develop since April 2011.

Under the terms of the agreement, Kinex Pharmaceuticals will acquire the rights to the development and commercialization of all products derived from the Orascovery program for all indications in the United States, European Union, Eastern Europe, Russia, South America, Australia, New Zealand, Taiwan and Hong Kong. Korea, Japan, Mainland China and India are not included in this agreement.

Kinex Pharmaceuticals will assume all development responsibility and associated costs in the licensed territories and will collaborate with Hanmi Pharmaceuticals during this process.

Kinex Pharmaceuticals will provide Hanmi Pharmaceuticals with an up-front payment and all other payments will be effective when the first product is approved by regulatory authorities or when Kinex Pharmaceuticals has achieved certain events that create shareholder value. There will also be royalty payments associated with product sales. A joint development team will be established to foster the collaboration.

Dr. Gwan Sun Lee, Chief Executive Officer of Hanmi Pharmaceuticals states: “This collaboration is an important strategic decision for Hanmi Pharmaceuticals as this will facilitate our company to further expand our product portfolio in the United States, European Union and other geographic areas. The choice of Kinex Pharmaceuticals, a good partner in the KX01 development, allows us to further strengthen our collaboration.”

Dr. Jeewoong Son, Chief Medical Officer and Senior Vice-President of Research and Development, states: “We were impressed by the experience of the management team of Kinex Pharmaceuticals. Our first collaboration on KX01 has been successful and our joint development team has functioned very well. We are excited to collaborate with the scientific team of Kinex Pharmaceutical and to explore the potential synergy between KX01 and the Orascovery program. This strategic move will create a lot of value for both companies.”

“We are delighted to be selected by Hanmi Pharmaceuticals to work with them on the Orascovery program. We are impressed by their strong commitment to research and development and their business growth strategy. This collaboration will also further strengthen our product pipeline and will provide the opportunity to explore the synergy between our lead compounds and an oral form of taxol, which may create substantial value for Kinex,” states President Emeritus of Kinex Pharmaceuticals, Dr. Allen Barnett, who was credited for his effort in the discovery and development of Claritin when he was working at the Schering-Plough Research Institute.

“We are impressed by the Orascovery program, in particular, the ability to enhance the oral bioavailability of paclitaxel and irinotecan to >40%. Together with their team, we are confident that our joint effort will explore the full potential of these important anti-cancer drugs given with the convenience of an oral route,” states Chief Medical Officer of Kinex Pharmaceuticals, Dr. Rudolf Kwan, who was previously Vice-President of Clinical Research, Schering-Plough Research Institute.

Dr. David Hangauer, Chief Scientific Officer, states: “The opportunity to collaborate with this well established research and development team is particularly important because of the strong synergy that has been demonstrated between KX01 and the taxanes; this may allow the development of an excellent combination therapy to help patients in the future.”

Mr. Chuck Lannon, Vice-Chairman of the Board, states: “Hanmi is a great partner to Kinex Pharmaceuticals and we have enjoyed our working relationship tremendously. The fact that our partner is providing us more of a success-based agreement is a reflection of their confidence in the Kinex team and also their goodwill to help Kinex to develop into a successful pharmaceutical company.”

Kinex Pharmaceuticals has announced that its oncology drug, KX2-391, has entered a clinical trial entitled “A Phase Ib Rising Multiple-Dose Clinical Study to Evaluate Safety, Tolerability, and Activity of Oral Monotherapy with KX2-391 in Elderly Subjects with Acute Myeloid Leukemia (AML) Who Are Refractory to or Have Declined Standard Induction Therapy”. This compound is a dual Src kinase/tubulin polymerization inhibitor that has previously been evaluated in a Phase 1 study.

The study commenced in July 2011 at Roswell Park Cancer Institute (RPCI) in Buffalo, New York and Thomas Jefferson University in Philadelphia, Pennsylvania and is currently recruiting patients.

This study has been designed to determine the Recommended Phase 2 Dose of KX2-391 when administered once-daily. The trial will evaluate safety, tolerability and pharmacokinetics. An exploratory biomarker for target inhibition will also be evaluated.

For more information on this study, visit www.clinicaltrials.gov

Kinex Pharmaceuticals presented an abstract at the Annual Meeting of the American Association for the Study of Liver Diseases (AASLD), which was held on November 4-8, 2011 in San Francisco, CA.

The poster entitled “KX01, a dual-mechanism Src/pretubulin inhibitor, is synergistic with sorafenib but not with doxorubicin against liver cancer cells” was authored by Drs. Yahao Bu, Robert Gish, Jane Fang, Johnson Lau and David Hangauer and was presented during the Experimental Hepatocarcinogenesis session.

Kinex Pharmaceuticals investigators included Drs. Lau, Hangauer and Bu who serve as CEO, CSO and Senior Scientist at the Company.

The paper focused on research performed at Kinex that demonstrated that the expression of both Src kinase, and its activated form, were increased in patients with liver cancer. KX01 (KX2-391) exhibits potent anti-proliferative activity against multiple liver cancer cell lines with GI50 in the range of 20-80nM. At 5 times the GI50 concentration, both HuH7 and HepG2 cells showed significant tubulin disassembly/disarray following 5 hours of KX01 exposure, as determined by immunofluoresence staining. DNA content analysis showed KX01 was potent in inducing G2/M arrest. In addition, there was an increase in the number of cells showing apoptosis as reflected by DNA fragmentation and caspase activation.

The effect of a combination of KX01 and Sorafenib or Doxorubicin, drugs currently used to treat liver cancer, was evaluated by determination of the combination index. When the combination of KX01 and Sorafenib was tested, the combination showed weak synergy, or an additive effect, in multiple liver cancer cell lines. In contrast, when KX01 is used in combination with Doxorubicin, significant antagonism was demonstrated. KX01 is not subject to p-glycoprotein efflux as it shows equal potency against MDR cells compared to their parental non-MDR counterparts. KX01 also exhibited potent anti-angiogenesis and vasculature disrupting activities in an in vitro tube formation assay. Unlike vinca alkaloid tubulin polymerization inhibitors, such as vincristine, KX01 did not inhibit PC12 neurite outgrowth even at 200nM, consistent with the lack of neurotoxicity observed in animals and patients. A Phase 1 clinical trial demonstrated that KX01 is well-tolerated in patients with advanced malignancies and has an MTD of 40mg when administered twice-daily, on a continuous basis. These data provide a rationale for testing KX01 as a single agent or in combination with Sorafenib (but not Doxorubicin) in patients with liver cancer.

Kinex Pharmaceuticals has closed a $5M round of equity financing. The funds were raised from accredited investors and will be used to advance the Company’s clinical development programs.

“Kinex management has demonstrated to its investor base that it has successfully deployed capital to advance its clinical programs and to build value in its pipeline of novel compounds”, said Charles E. Lannon, Vice-Chairman of the Board of Directors and Managing Partner of Pharminex LLC, a major Kinex investor. Read more>

Kinex Pharmaceuticals, LLC announced today that Dr. Allen Barnett has elected to step down from the Board of Directors upon his appointment as President Emeritus focusing his effort on Research and Development. After an extensive search, the Board has appointed Mr. Flint Besecker to the Board of Directors to fill the Board seat vacated by Dr. Barnett. Read more>