molecules of the month


topical (skin-restricted) ROR_ antagonist

efficacy in psoriasis model / minipig PK

from GSK-805 and met. stability reduction

Sci. Rep., Apr. 28, 2021

Eternity Bioscience, NJ / Shanghai Hengrui, CN

1 min read

The Eternity Bioscience/Shanghai Hengrui RORγ antagonist, SHR168442, is a skin-restricted, topical compound intended to treat psoriasis. As a master regulator of Th17 immune cells which are significantly involved in allergic diseases, both positive and negative oral modulators of RORγt had been hotly pursued, though many have ceased clinical development. SHR168442 was “optimized” to be rapidly cleared compared to its starting point, GSK-805. A skin-restricted compound may address the safety concerns of systemic exposure. Another topical RORγ antagonist, GSK2981278, had failed in Ph. I for psoriasis, but the target may not have been fully engaged. SHR168442 does not seem to have entered clinical development yet.

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