On December 17, 2021 DisperSol Technologies LLC reported that it is has entered into a research collaboration with Ajax Therapeutics, Inc. to apply its KinetiSol technology to enhance the bioavailability of an Ajax drug candidate in development for the treatment of hematologic malignancies (Press release, Ajax Therapeutics, DEC 17, 2021, View Source [SID1234597435]).

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"Ajax is taking an innovative approach to developing a pipeline of selectively targeted small molecules and we look forward to applying our proprietary KinetiSol technology to help enhance the bioavailability of one of these promising drug candidates," said Dr. Edward Rudnic, CEO of DisperSol Technologies. "This collaboration is another example of our partnering strategy with our KinetiSol technology platform to help improve the bioavailability of next generation targeted therapies to provide new treatments for patients in need."

On December 17, 2021 Guardant Health, Inc. (Nasdaq: GH), a leading precision oncology company, reported that it has reached its target enrollment of 12,750 patients in ECLIPSE (Evaluation of ctDNA LUNAR Assay In an Average Patient Screening Encounter), a registrational study to evaluate the performance of its LUNAR-2 blood test to detect colorectal cancer (CRC) in average-risk adults (Press release, Guardant Health, DEC 17, 2021, View Source [SID1234597434]). Subject to positive study results, the number of patients currently enrolled in ECLIPSE is targeted to support a premarket approval (PMA) submission to the U.S. Food and Drug Administration in 2022.

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"Colorectal cancer screening rates have remained stubbornly low due to the nature of current screening methods. New modalities in colorectal cancer screening, such as a routine, accurate blood test like the one being studied in the ECLIPSE study, has the potential to increase screening rates dramatically," said AmirAli Talasaz, Guardant Health co-CEO. "Reaching this significant enrollment milestone highlights our ability to successfully run one of the largest cancer screening studies of its kind and gives us tremendous confidence in initiating large registrational studies in other cancer types, including the SHIELD screening study to detect lung cancer. It is also a testament not just to our team’s perseverance, but also to the commitment of our clinical researchers and the generosity of those enrolled in the study."

Today, it is estimated that 1 in 3 adults in the U.S. does not adhere to national CRC screening recommendations even though regular screening for colorectal cancer has been shown to improve survival rates.1,2 Increasing screening rates to 80% from current levels could reduce the number of people diagnosed with CRC by 22% by 2030.3 However, current screening methods are time consuming and, in the case of a colonoscopy, invasive. LUNAR-2 is intended to improve CRC screening rates by offering a simple blood test that overcomes barriers associated with current testing methods and facilitates access to screening tests to more individuals and communities where access may be limited.

"Given the importance of this study and the size of the cohort, we’re grateful Guardant Health has been able to enroll 12,750 study participants in just over two years during a global pandemic," said William M. Grady, M.D., Professor, Clinical Research Division, Fred Hutchinson Cancer Research Center. "We look forward to evaluating the data from the ECLIPSE study to increase our understanding of blood-based screening in patients at average risk for colorectal cancer."

ECLIPSE is a prospective, multi-site registrational study to evaluate the performance of the company’s LUNAR-2 blood test to detect colorectal cancer in individuals aged 45-84 in the U.S. who are at average risk for colorectal cancer, including those who have historically been underrepresented in clinical research and identify as Native American and Black or African American. More details about ECLIPSE can be found at NCT04136002.

On December 17, 2021 Iktos, a company specialized in Artificial Intelligence for new drug design, and The Drug Discovery Unit (DDU), School of Life Sciences, The University of Dundee, focused on the discovery of therapeutics for neglected diseases and the translation of novel biology through small molecule drug discovery, reported entering a collaboration to apply Iktos’s generative modelling artificial intelligence (AI) technology in one of DDU’s drug discovery programs (Press release, Iktos, DEC 17, 2021, View Source [SID1234597433]). Under the agreement, Iktos will apply its de novo ligand and structure-based generative modelling technologies, its AI-based retrosynthesis analysis and planning tool Spaya, and know-how complementing DDU’s drug discovery capabilities to expedite the identification of potential pre-clinical candidates and to identify additional novel chemical matter with suitable properties.

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The DDU was established in 2006 to respond to a lack of drug targets identified for neglected tropical diseases being translated into therapeutics for diseases impacting the poorest people in the world. The DDU translates basic science into lead compounds to validate putative drug targets, to use as tools to investigate disease pathways and, when appropriate, advance to pre-clinical drug candidates for multiple diseases, e.g. TB and cancer.

Iktos’s AI technology, based on deep generative models, helps to bring new insights and directions into the drug discovery process based on a comprehensive data-driven chemical structure generation technology. This technology automatically designs virtual novel molecules with all of the characteristics of a successful drug molecule. This approach, validated through Iktos’s other collaborations, is a novel solution to one of the key challenges in drug design: rapid identification of molecules that simultaneously satisfy multiple parameters, such as potency, selectivity, safety, and project-specific properties. This approach uniquely enables the exploration of chemical space and produces innovative molecule designs with greater freedom to operate.

Iktos has recently diversified its R&D efforts into the development of an AI technology for retrosynthesis. Identifying and selecting synthetic pathways is one of the most challenging and time-consuming tasks in synthetic and medicinal chemistry. Iktos has developed AI based retrosynthesis analysis and planning tool Spaya by harnessing the power of data-driven retrosynthesis algorithm for systematic exploration and prioritisation of synthetic routes for a desired compound in minutes.

Professor Paul Wyatt, Head of the DDU said, "We are thrilled to be working with Iktos to drive our projects towards drug candidates. Iktos AI platform combined with our own in-house computational and medicinal chemistry design teams provide a powerful combination for innovative new drug design."

"We are thrilled and proud to join forces with DDU with the aim to help in the discovery of therapeutics for neglected diseases and the translation of novel biology through small molecule drug discovery," commented Yann Gaston-Mathé, President and CEO of Iktos. "Pleased to have earned DDU’s trust, we are confident that together with DDU and their established R&D partners, we will be able to identify promising novel chemical matter and solve complex multiparametric optimisation problems. The feedback from DDU’s research team will be highly valuable as we improve our product offerings. Our strategy has always been to tackle challenging problems alongside our collaborators where we can demonstrate value generation for new and on-going drug discovery projects."

On December 17, 2021, Oncternal Therapeutics, Inc. ("Oncternal") reported that it entered into an Open Market Sale AgreementSM (the "Sale Agreement") with Jefferies LLC (the "Agent"), pursuant to which Oncternal may offer and sell shares of Oncternal’s common stock having an aggregate offering price of up to $50,000,000 from time to time, in "at the market" offerings through the Agent (Filing, 8-K, Oncternal Therapeutics, DEC 17, 2021, View Source [SID1234597410]). Sales of the shares of common stock, if any, will be made at prevailing market prices at the time of sale, or as otherwise agreed with the Agent. The Agent will receive a commission from Oncternal of 3.0% of the gross proceeds of any shares of common stock sold under the Sale Agreement.

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Oncternal is not obligated to sell, and the Agent is not obligated to buy or sell, any shares of common stock under the Sale Agreement. No assurance can be given that Oncternal will sell any shares of common stock under the Sale Agreement, or, if it does, as to the price or amount of shares of common stock that it sells or the dates when such sales will take place.

In the Sale Agreement, Oncternal agreed to indemnify the Agent against certain liabilities, including under the Securities Act of 1933, as amended, or to contribute payments that the Agent may be required to make because of such liabilities.

The shares of common stock sold pursuant to the Sale Agreement will be offered pursuant to a shelf registration statement on Form S-3 (File No. 333-254985), which became effective on April 15, 2021. Oncternal filed a prospectus supplement with the U.S. Securities and Exchange Commission on December 17, 2021 in connection with the offer and sale of shares of Oncternal’s common stock pursuant to the Sale Agreement.

A copy of the Sale Agreement is attached as Exhibit 1.1 hereto and is incorporated herein by reference. The foregoing description of the Sale Agreement does not purport to be complete and is qualified in its entirety by reference to the full text of the Sale Agreement.

A copy of the opinion of Latham & Watkins LLP relating to the validity of the shares of common stock that may be sold pursuant to the Sale Agreement is filed herewith as Exhibit 5.1.

On December 17, 2021 Genoscience Pharma, a clinical stage biotechnology company developing unique lysosomotropic drug candidates for the treatment of cancer, auto-immune and infectious diseases through autophagy modulation, reported the licensing of its PPT-1 inhibitor, GNS561, in cholangiocarcinoma indication, to GENFIT (Nasdaq and Euronext: GNFT), a late-stage biopharmaceutical company dedicated to improving the lives of patients with metabolic and chronic liver diseases (Press release, GenoScience, DEC 17, 2021, View Source [SID1234597409]). GENFIT will develop and commercialize investigational treatment with GNS561 in cholangiocarcinoma, in the United States, Canada and Europe, including the United Kingdom and Switzerland.

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Under the agreement, GENFIT is committed to taking a €3 million ($3.4M) equity stake in Genoscience Pharma through the subscription of new ordinary shares. GENFIT will also contribute clinical and regulatory milestone payments and tiered royalties (financial terms not disclosed). The first payable milestone is contingent on positive results from the phase 2 clinical trial in cholangiocarcinoma, which is expected to start in the first half of 2022.

GNS561 is a novel clinical-stage autophagy/PPT1 inhibitor developed by Genoscience Pharma in cholangiocarcinoma indication, which is an orphan disease. The inhibitor has completed preclinical studies and a phase 1b trial confirming the rationale for targeting cholangiocarcinoma, a rare liver malignancy with high mortality and with limited treatment options.

"This is a great step for the development of GNS561 as a new potential treatment option in liver cancer, as it offers an innovative mechanism of action for patients with high unmet needs," said Philippe Halfon, CEO of Genoscience Pharma. "We believe that GENFIT is a highly qualified partner for the development of GNS561 in cholangiocarcinoma and we will provide GENFIT with our expertise in oncology to support their development plan. On our side, we will pursue the development of GNS561 in other oncology indications as well as research in other therapeutic areas."

"This decision fully aligns with our strategic roadmap by broadening our asset portfolio within our cholestatic disease franchise, through the addition of an innovative drug candidate with the potential to address considerable unmet needs for patients," said Pascal Prigent, CEO of GENFIT. "The scientific rationale, together with preclinical and clinical evidence, supports further development of the asset, and our plan is to start the phase 2 program in the first half of 2022. We believe that GNS561’s mechanism of action is very promising. Given the current landscape, standard of care and lack of marketed options, and based on KOL opinions, we will interact with regulatory agencies to investigate accelerated paths to approval, post phase 2."

About cholangiocarcinoma
Cholangiocarcinoma is a type of cancer that forms in the slender tubes (bile ducts) that carry the digestive fluid bile. Cholangiocarcinoma occurs mostly in people over the age of 50. Cholangiocarcinoma is divided into intrahepatic and extrahepatic types based on where the disease occurs in the bile ducts. Cholangiocarcinoma is often diagnosed when it is advanced, making successful treatment difficult to achieve. Several risk factors of chronic inflammatory damage and increased cellular turnover have been established, such as primary sclerosing cholangitis, a cholestatic liver disease, liver flukes, biliary tract cysts, hepatolithiasis and toxins. Treatment options for cholangiocarcinoma are limited and associated with high rates of tumor recurrence and short survival times.

About GNS561
GNS561 is a PPT-1 (Palmitoyl Protein Thioesterase-1) inhibitor that blocks autophagy. Autophagy is activated in tumor cells in response to certain conditions, due to tumor cell growth in advanced cancers. One of the key organelles implicated in the autophagy process is the lysosome. By entering the lysosome and binding to its target, GNS561 has an important inhibiting activity on late-stage autophagy, which leads to tumor cell death. GNS561 is an investigational compound and has not been registered by any regulatory authority.