Stephanie Kay Dodd

TL;DR: Describing ABL001 (asciminib), a potent and selective allosteric ABL1 inhibitor that is undergoing clinical development testing in patients with CML and Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukaemia, shows similar cellular potencies but distinct patterns of resistance mutations.

TL;DR: Structural-activity relationship studies led to the discovery of a potent and specific Smoothened antagonist N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-2-methyl-4'-(trifluoromethoxy)biphenyl- 3-carboxamide (5m, NVP-LDE225), which is currently in clinical development.

TL;DR: The discovery of asciminib (ABL001), the first allosteric BCR-ABL1 inhibitor to reach the clinic, and structure-based optimization for potency, physicochemical, pharmacokinetic, and drug-like properties, culminated in ascinib, which is currently undergoing clinical studies in CML patients.

TL;DR: Optimization efforts are reported on toward the identification of clinical candidate IDH305, a potent and selective mutant IDH1 inhibitor that has demonstrated brain exposure in rodents and has progressed into human clinical trials for the treatment of cancers with IDH 1 mutation.

TL;DR: This study developed a novel and simple low shear process to prepare stable reproducible emulsions without the use of any proprietary equipment that prepared a novel 20-nm-sized emulsion that was stable, reproducible, and showed adjuvant effects.