| Hazard Information | Back Directory | [Uses]
OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study[1]. | [in vivo]
OATD-02 (10 mg/kg, oral gavage) generates a strong and a long pharmacodynamic effect in vivo, and has oral bioavailability of 13%, 30%, and 61% from mouse through rat to dog, respectively[1].
OATD-02 (5 mg/kg, oral gavage) increases fourfold of the L-arginine concentration in plasma sustained even 1 week after end of a treatment[1].
OATD-02 (twice per day at 50 mg/kg, oral gavage) inhibits the tumor growth in B16F10 orthotopic xenograft tumor model[1]. | Animal Model: | B16F10 orthotopic xenograft tumor model[1] | | Dosage: | Twice per day at 50 mg/kg for 15days | | Administration: | Oral gavage | | Result: | Inhibited tumor growth (TGI 46%). |
| [References]
[1] Borek B, et al. Arginase 1/2 Inhibitor OATD-02: From Discovery to First-in-man Setup in Cancer Immunotherapy. Mol Cancer Ther. 2023;22(7):807-817. DOI:10.1158/1535-7163.MCT-22-0721 |
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