Dawn Trueman

TL;DR: It is demonstrated that AZD2811 can be formulated in nanoparticles using ion pairing agents to give improved efficacy and tolerability in preclinical models with less frequent dosing and can increase the therapeutic index of molecularly targeted agents, including kinase inhibitors targeting cell cycle and oncogenic signal transduction pathways.

TL;DR: The biological characterization of AZD3514 is described, an orally bioavailable drug that inhibits androgen-dependent and -independent AR signaling and shows antitumor activity in the HID28 mouse model of CRPC in vivo.

TL;DR: Clinical candidate 6-(4-{4-[2-acetylpiperazin-1-yl)-3-(trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine (12), designated AZD3514, that is being evaluated in a Phase I clinical trial in patients with castrate-resistant prostate cancer.

TL;DR: Targeting Aurora B kinase with AZD2811 nanoparticles is a novel approach to deliver a cell-cycle inhibitor in AML, and have potential to improve on the clinical activity seen with cell- cycle agents in this disease.

TL;DR: The biological characterisation of AZD3514 is described, an oral drug that targets AR function, with a novel mechanism of action that can result in down-regulation of AR protein in vivo, and the ability to down-regulate AR under such conditions differentiates AZD 3514 from the AR antagonists bicalutamide and MDV3100.