Arginase 1 (ARG1) and in recent years Arginase 2 (ARG2), have been described as attractive therapeutic targets in immuno-oncology giving rise to interest in drugs designed to address both novel targets. In this paper, Molecure discloses the structure, medicinal chemistry, broad characterization, and human PK predictions of OATD-02 – the first-in-class, orally bioavailable inhibitor which uniquely targets both intracellular ARG1 and ARG2. Additionally, the long drug-target residence time, moderate volume of distribution, and low clearance of OATD-02 may provide a novel drug against arginase-associated tumor immunosuppression and ARG2-dependent tumor cell growth which is currently being investigated in clinical trials.

Tuberous Sclerosis (TSC) leads to neoplasms in multiple organ systems including the lung (Lymphangioleiomyomatosis) and kidney (Angiomyolipomas). Current therapies are tumoristatic with mortality remaining at 4–14%. Our group utilized the tyrosine kinase inhibitor, Imatinib, which inhibits the PDGF pathway, as a novel agent in the treatment of TSC. Imatinib reduced tumor...

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