molecules of the month


oral ROR_t inverse agonist

Ph. I in HV up to 200 mg w/ PD, discontinued

from HTS + opt.

Scientific Reports, May 26, 2021

Janssen R&D, La Jolla, CA

2 mins read

The Janssen RORgt inhibitor, JNJ-61803534, is an oral clinical candidate that was well-tolerated in humans up to 200 mg and demonstrated PD. Unfortunately, development was terminated due to findings in a rabbit embryo-fetal study where fetal development was impacted by JNJ-61803534 treatment. The JNJ team shares a lot of useful human data in the paper, including human PK (half-life of 164-170 h!) and PD. The variability in the human PD data is a good reminder that clinical data is often a lot noisier than preclinical data. When drug toxicity is a potential concern, the variability in PK and PD in humans makes it more difficult to find an optimal dose in practice than it might sound on paper. JNJ-61803534 was well…

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