Bevurogant (BI 730357) is a retinoid-related orphan receptor-gamma t (RORγt) antagonist[1]. Retinoic acid-related orphan receptors (RORs, including RORα, RORβ, and RORγ) act as transcription factors upon binding with their ligands. RORγt, a subtype of RORγ, promotes Th17 cell responses through transcription of IL-17A, IL-17F, IL-22, and IL-23R[2]. Bevurogant is used in research on chronic inflammatory diseases such as psoriasis[3].
References:
[1] Choi H J, Madari S, Huang F. Utilising Endogenous Biomarkers in Drug Development to Streamline the Assessment of Drug–Drug Interactions Mediated by Renal Transporters: A Pharmaceutical Industry Perspective[J]. Clinical Pharmacokinetics, 2024: 1-15.
[2] Carmona-Rocha E, Rusiñol L, Puig L. New and emerging oral/topical small-molecule treatments for psoriasis[J]. Pharmaceutics, 2024, 16(2): 239.
[3] Ooi Q X, Kristoffersson A, Korell J, et al. Bounded integer model‐based analysis of psoriasis area and severity index in patients with moderate‐to‐severe plaque psoriasis receiving BI 730357[J]. CPT: Pharmacometrics & Systems Pharmacology, 2023, 12(6): 758-769.
Bevurogant（BI 730357）是一种类视黄醇相关孤儿受体-γt（RORγt）拮抗剂[1]。视黄酸相关孤儿受体（ROR，包括 RORα、RORβ 和 RORγ）在与其配体结合后充当转录因子，RORγT是RORγ的一种亚型，可通过 IL-17A、IL-17F、IL-22和IL-23R的转录促进辅助性T细胞17（Th17）反应[2]。Bevurogant可用于慢性炎症性疾病的研究，例如银屑病[3]。