1 minute read
Aug. 21, 2024
Molecule One-Pager: KT-474 (SAR444656)
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Small-molecule drug candidates are increasingly falling “ beyond the rule of 5 ,” making oral administration more challenging. Optimizing a drug’s solid form can improve its solubility and bioavailability when further molecular modifications are prohibitive. This minireview covers solid form strategies for increasing the solubility and oral [...]
Understanding how a small molecule ligand binds to its target is valuable in drug discovery, because it enables more efficient optimization through structure-based design, better mechanistic understanding of molecular pharmacology, and greater confidence in the therapeutic hypothesis from both safety and efficacy perspectives. Recently, Drug Hunter highlighted methods for target identification when the target is unknown.
Arvinas’ ARV-471 is an orally bioavailable CRBN-based ER PROTAC degrader for treating patients with ER+/HER2-breast cancer and the first PROTAC to enter Ph. III clinical trials. This molecule one-pager serves as a reference guide, offering an overview of the scientific significance of Arvinas’ ARV-471 program. It includes links to key presentations, publications, patents, preclinical and clinical PK data summaries, and more.
This article explains what LogD is, why LogD (or LogP) is important in drug discovery, rookie mistakes in drug discovery that come from overlooking LogD or LogP, and contains a LogD reference poster that shows the estimated amount of potency attributable to lipophilicity considerations alone. By Dennis Hu Jump to Cheat Sheet Lipophilicity is [...]
Nurix’s NX-2127 is an orally bioavailable BTK degrader that exhibits in vivo degradation across species and has advanced into first-in-human clinical trials for relapsed/refractory B-cell malignancies. This molecule one-pager serves as a reference guide, offering an overview of the scientific significance of Nurix's NX-2127 program. It includes links to key presentations, publications, patents, preclinical and clinical PK data summaries, and more.
