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A potential first-in-class oral antibiotic with recent positive Ph. III data. The orally administered gepotidacin is a member of a novel class of type IIA topoisomerase inhibitors, also called novel bacterial topoisomerase inhibitors (NBTIs), for which the mode of action and binding mode with a topoisomerase was first disclosed in 2010 by GSK. NBTIs target…

Potential for an improved sGC stimulator for resistant hypertension. BAY 1165747 (BAY-747) is a new, structurally distinct, soluble guanylate cyclase (sGC) stimulator with potential in the treatment of resistant hypertension. Identified through ultrahigh-throughput screening, it features an imidazo[1,2-a]pyridine core, distinct from the previously described 2-(1-benzyl-1H-pyrazol-3-yl) pyrimidine sGC stimulators. The property-based design led to an improved…

An early heme-binding inhibitor of the once red-hot immunotherapy target, IDO1. Indoleamine 2,3-dioxygenase 1 (IDO1) is an extrahepatic tryptophan-metabolizing enzyme which is believed to contribute to the evasion of the immune system by tumors, making it an attractive target for cancer immunotherapy, especially in combination with immune checkpoint inhibitors like Merck’s pembrolizumab or BMS’s nivolumab.…

ACT-777991: next-generation CXCR3 antagonist in Phase I trials for Type 1 diabetes. ACT-777991, an oral and insurmountable CXCR3 antagonist discovered by Idorsia (formerly Actelion), is under investigation for the treatment of Type 1 Diabetes (T1D). Despite the complex history of CXCR3 antagonists, ACT-777991 has shown promise with demonstrated in vivo efficacy in T1D mouse models.…

A Ph. II liver-targeting HBV core protein modulator optimized for ADMET properties. Linvencorvir (RG7907), a novel HBV core protein allosteric modulator, offers a promising treatment option for chronic hepatitis B which affects 296 million people globally. It possesses an interesting glue-like mechanism that causes the HBV core protein to aggregate into incompetent capsids, reminiscent of…

Upcycling a γ-secretase inhibitor for a potentially first- & best-in-class treatment for aggressive desmoid tumors. Nirogacestat was recently granted FDA priority review for rare, aggressive, locally invasive, soft-tissue desmoid tumors (DTs). This reversible, non-competitive gamma secretase inhibitor (GSI) draws its anticancer activity from its ability to block Notch signaling, and is the lead drug from…