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Broad-spectrum ALDH inhibitor for Melanoma Treatment

ID# 2019-4899
Reduction in Tumor Volume

Technology Summary

The aldehyde dehydrogenases (ALDH) overexpression by cancers is associated with a poor prognosis in many cancer types. The invention describes a novel broad-spectrum ALDH inhibitor, KS100. Broad-spectrum ALDH inhibition might be more efficacious for melanoma compared to isoform-specific inhibition. Enzymatic IC50s of KS100 were 207, 1,410 and 240 nM towards ALDH1A1, 2 and 3A1, respectively. The systemic toxicity of KS100 was mitigated by development of a nanoliposomal formulation, NanoKS100. NanoKS100 had a loading efficiency of ~69% and was stable long-term at 4°C. NanoKS100 was 5-fold more selective for killing melanoma cells compared to normal human fibroblasts. NanoKS100 administered intravenously was effective at inhibiting xenografted melanoma tumor growth by ~65% without organ related toxicities in melanoma mouse models.

Application & Market Utility

KS100 acts as a broad-spectrum ALDH inhibitor, and with minimal toxicity when encapsulated in liposome. 20 mg/kg/day i.v. led to a 65% reduction in UACC 903 and 1205 Lu xenograft volume. The compound could potentially be combined with other therapies in treatment of melanoma.

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