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XO/URAT1 Dual target inhibitors for HUA

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  • Project profile
    Project name: XO/URAT1 Dual target inhibitors for HUA
    Indications: Hyperuricemia (HUA)
    Research phase: Phase 1 is ongoing in China
    Cooperation demands: License-out or co-development
  • Highlights

    1. Dual inhibitor of XO / URAT1, Orally-active, the inhibitory activity of URAT1 is better than that of benzbromarone.

    (1) Xanthine Oxidase (XO) Inhibitor

    Xanthine oxidase (XO) is a critical enzyme in the metabolism of purines to uric acid. Effective urate lowering via xanthine oxidase inhibition therapy is associated with a high risk of gout flares at the start of therapy.

    (2) Urate transporter 1 (URAT1) Inhibitor

    Urate transporter 1 (URAT1) is a major protein involved in uric acid reabsorption (about 90%). URAT1 inhibitors are thought to be a highly effective and promising class of uricosuric agents for treating hyperuricemia.

    2. Good efficacy and safety in the preclinical study.

    (1) No toxicity was observed in the preclinical study.

    (2) Therapeutic effect in black-capped monkeys:

    The results of in vivo efficacy experiments showed that:
    a) Asset dose-dependently increases the amount of xanthine and hypoxanthine in blood, and inhibits XO activity.
    b) Asset dose-dependently promotes renal uric acid excretion and inhibits URAT1 activity.

  • Project Introduction

    1. Asset type: XO/URAT1 Dual target inhibitors

    2. Indication: Hyperuricemia (HUA)

    3. Modality: Small molecular

    4. Research phase: Phase 1 is ongoing in China

    5. Patent: granted in CN and the US (2036)

    6. Cooperation demands: License-out or co-development

    7. Research progress:

    (1) Phase 1 trial in China.
    (2) Patent has been granted in both CN and the US.
    (3) Inhibitory effect on uric acid was shown in black-capped monkeys.

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