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VITAE PHARMACEUTICALS, INC filed this Form S-1 on 08/12/2014
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ABCG1 Gene Induction
(Hairless Mouse Skin, n=4)

  SREBP1c Gene Induction
(Hairless Mouse Skin, n=4)


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Figure 21: VTP-38543 induced genes critical for lipid transport and lipid synthesis in skin.

        VTP-38543 was also tested in primary cultures of human epidermal keratinocytes for induction of these same lipid metabolism and transport markers. As shown in Figure 22 below, VTP-38543 induced the expression of both ABCG1 and SREBP1c in a concentration-dependent manner in primary human cells.

ABCG1 Gene Induction
(Human Epidermal Keratinocytes)

  SREBP1c Gene Induction
(Human Epidermal Keratinocytes)


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Figure 22: In primary cultures of human epidermal keratinocytes, VTP-38543 significantly increased expression of ABCG1 and SREBP1c after 24 hours.

        LXR activation has been shown to reduce inflammation in multiple human cell types including macrophages. IL-6 is a key cytokine involved in skin inflammation and is expressed in human macrophages. Consistent with its anti-inflammatory effect in the mouse dermatitis model, as shown in Figure 23 below, VTP-38543 was able to reduce IL-6 expression in human THP-1 macrophages in a concentration dependent manner.

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