molecules of the month

“Compound 10”

gut-restricted, selective COX-2 inhibitor

in vivo showed no inhibition of gut COX-2

from modification of etoricoxib

Journal of Medicinal Chemistry

Janssen, Spring House, US

Chemical structure of compound 10 Janssen gut-restricted COX-2 inhibitor
1 min read

The Janssen gut-restricted COX-2 inhibitor, compound 10, is a tool compound used to test the hypothesis that gut-restricted COX-2 inhibition would be beneficial for cancer without the cardiovascular risk of systemic COX-2 inhibition. Unfortunately, IVIVC of several compounds demonstrated that in vivo efficacy was not driven by gut COX-2 inhibition, but by residual systemic activity. Reviewer Mike Koehler found this story particularly interesting this month. Though it was not a positive result, this is a great case study for getting decision-making biological data quickly using medicinal chemistry.

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