OncoArendi Therapeutics Announces Selection of Its Second Clinical Development Candidate: OATD-02 Fo

OncoArendi Therapeutics SA announced that it has selected OATD‑02 as its clinical development candidate for cancer immunotherapy. Submission of the Company's second Investigational New Drug ("IND") application is expected by the third quarter of 2018.

OATD-02 is a highly potent and selective small molecule inhibitor of two arginase isoforms (Arg-1 and Arg-2) in both biochemical and cell-based-assays. OATD-02 is the second arginase inhibitor to enter development.

OATD-02 has been shown to be effective in vivo in three different mouse models of cancer (colorectal, lung and melanoma) and demonstrated superior antitumor efficacy in combinations with the PD-L1 checkpoint inhibitor and with gemcitabine; resulting in a controlled tumor growth, and, in some cases in a full regression.

Pilot studies  also suggested a therapeutic potential of OATD-02 in glioblastoma multiforme (GBM), the most malignant brain tumor with no effective treatment.

"We believe that small molecule drugs preventing cancer cells from escaping from the immune surveillance have great potential in combination therapies and to be transformational medicines in the treatment of many types of cancer. The increasing number of clinical trials with multiple IDO inhibitors and various check-point inhibitor combinations additionally validate this approach. At OncoArendi, we are dedicated to research and development of the first-in-class or best-in-class small molecule-based therapies that in combination with other modalities, could significantly improve the treatment of unmet medical needs in many solid and hematopoietic cancers " said Marcin Szumowski, PhD, CEO of OncoArendi Therapeutics. "We are particularly excited about the potential of arginase as an additional new target in cancer immunotherapy and the potential of OATD-02 to become the best-in-class arginase inhibitor on the market. This compound demonstrated a potent extracellular and cellular activity while its pharmacological profile makes it suitable for oral dosing."

Formal pre-clinical development of OATD-02 will be initiated next month with GLP toxicology studies expected in Q4 of this year and first in human studies anticipated in the third quarter of 2018. OncoArendi Therapeutics’ arginase inhibitors, including OATD-02, are protected by two pending patents covering two structurally different groups of compounds.

About Arginase Science
Arginase has been recently validated as a promising target in immuno-oncology. Arginase is an enzyme that catalyzes the final step in the urea cycle, during which the body disposes of harmful ammonia. However, in cancer, arginase through its capacity to decrease arginine levels, blocks the natural antitumor immunity by suppressing activation and proliferation of T cells. Even a moderate decrease of arginine levels is immunosuppressive. T-cells deprived of arginine do not die – they retain the ability to expand when arginine is replenished. Since the majority of human cancers exhibit a highly increased arginase activity and decreased plasma arginine levels, arginase inhibitors are expected to exhibit a wide clinical utility, in particular in combinations with other therapeutic modalities, such as checkpoints inhibitors and immunogenic therapies.
With a decade-long expertise in the type of chemistry required to synthesize and optimize arginase inhibitors, promising initial data and a strong development team, OncoArendi has laid out a clear strategy to bring to the clinic the best in class arginase inhibitor.

About OncoArendi Therapeutics
OncoArendi Therapeutics SA is an innovative biopharmaceutical company based in Poland, focused exclusively on discovery and development of small molecules to treat patients with unmet medical needs in cancer and respiratory diseases. It currently employs 70 people, the majority of whom hold PhD degrees in biology and chemistry and has raised over 35 million USD to support the progression of four distinct new chemical entities at various stages of development to Phase II clinical trials.

OncoArendi has been developing arginase inhibitors for the past three years and has selected OATD-02 out of the in-house library of over 200 compounds obtained through rational drug design. OncoArendi continues to develop inhibitors against other undisclosed targets in cancer metabolism.

OncoArendi also has broad interest and commitment to chitinase science with three distinct small molecule drug discovery programs directed against different chitinase family targets. Its first clinical candidate OATD-01 is positioned to enter first-in-human Phase I clinical trial this fall. Potential therapeutic applications for compounds resulting from this R&D Chitinase Platform include treatment of numerous diseases such as asthma, idiopathic pulmonary fibrosis (IPF), chronic obstructive pulmonary disease (COPD) and sarcoidosis, as well as fibrotic diseases of other organs and some types of cancer.