JNJ-61803534: A Comprehensive Report on an Investigational RORγt Inverse Agonist

I. Introduction to JNJ-61803534

A. Overview and Origin

JNJ-61803534 is an investigational small molecule, developed as an orally active RORγt (Retinoic Acid Receptor-Related Orphan Receptor gamma t) inverse agonist. Its primary therapeutic aim was the treatment of autoimmune and inflammatory diseases, with a particular focus on psoriasis.[1] The oral route of administration is a significant feature, potentially offering advantages over biologic treatments for similar conditions which often require parenteral administration.

The development of JNJ-61803534 was a collaborative effort. The primary entities involved were Phenex Pharmaceuticals AG, based in Heidelberg, Germany, and Janssen Research & Development, LLC, a subsidiary of Johnson & Johnson Innovative Medicine, headquartered in the USA.[6] This partnership structure is common in the pharmaceutical industry, leveraging the specialized discovery and medicinal chemistry expertise often found in smaller biotechnology firms like Phenex Pharmaceuticals with the extensive resources for preclinical testing, large-scale clinical trials, and regulatory navigation typically possessed by large pharmaceutical corporations like Janssen. The contributions from Phenex Pharmaceuticals appear significant in the early discovery and chemical optimization phases, while Janssen likely led the broader preclinical characterization and clinical development program.

B. Chemical Properties

JNJ-61803534 belongs to the chemical class of thiazole bisamide derivatives. This specific structural class was the result of targeted medicinal chemistry efforts aimed at overcoming limitations, particularly CYP450 autoinduction in rats, which had hampered the development of earlier-generation thiazole amide RORγt inverse agonists.[6]

Key chemical identifiers and properties include: