Search Results - "Dodd, Stephanie"
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Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1
Published in Journal of medicinal chemistry (27-09-2018)“…Chronic myelogenous leukemia (CML) arises from the constitutive activity of the BCR-ABL1 oncoprotein. Tyrosine kinase inhibitors (TKIs) that target the…”
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The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1
Published in Nature (London) (30-03-2017)“…The selective allosteric ABL1 inhibitor ABL001 (asciminib) represents a new inhibitory mechanism for BCR–ABL1-driven malignancies, and its efficacy and…”
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Use of Physiologically Based Pharmacokinetic (PBPK) Modeling for Predicting Drug-Food Interactions: an Industry Perspective
Published in The AAPS journal (27-09-2020)“…The effect of food on pharmacokinetic properties of drugs is a commonly observed occurrence affecting about 40% of orally administered drugs. Within the…”
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Understanding Mechanisms of Food Effect and Developing Reliable PBPK Models Using a Middle-out Approach
Published in The AAPS journal (04-01-2021)“…Over the last 10 years, 40% of approved oral drugs exhibited a significant effect of food on their pharmacokinetics (PK) and currently the only method to…”
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Co-crystal formation based on structural matching
Published in European journal of pharmaceutical sciences (10-06-2016)“…A co-crystal is defined as a single crystalline structure composed of two or more components with no proton transfer which are solid at room temperature. Our…”
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Pharmacokinetics of asciminib in the presence of CYP3A or P‐gp inhibitors, CYP3A inducers, and acid‐reducing agents
Published in Clinical and translational science (01-07-2022)“…Asciminib is a first‐in‐class inhibitor of BCR::ABL1, specifically targeting the ABL myristoyl pocket. Asciminib is a substrate of CYP3A4 and P‐glycoprotein…”
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Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist
Published in ACS medicinal chemistry letters (10-06-2010)“…The blockade of aberrant hedgehog (Hh) signaling has shown promise for therapeutic intervention in cancer. A cell-based phenotypic high-throughput screen was…”
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Prediction of ARA/PPI Drug-Drug Interactions at the Drug Discovery and Development Interface
Published in Journal of pharmaceutical sciences (01-01-2019)“…Advances in understanding of human disease have prompted the U.S. Food and Drug Administration to classify certain molecules as "break-through therapies,"…”
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Automated Supersaturation Stability Assay to Differentiate Poorly Soluble Compounds in Drug Discovery
Published in Journal of pharmaceutical sciences (01-01-2018)“…Increasingly, in vitro assays evaluate a compound's tendency to maintain supersaturation toward improving oral absorption. Throughput remains a challenge and…”
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Streamlining Food Effect Assessment — Are Repeated Food Effect Studies Needed? An IQ Analysis
Published in The AAPS journal (15-06-2023)“…Current regulatory guidelines on drug-food interactions recommend an early assessment of food effect to inform clinical dosing instructions, as well as a…”
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Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor
Published in ACS medicinal chemistry letters (12-10-2017)“…Inhibition of mutant IDH1 is being evaluated clinically as a promising treatment option for various cancers with hotspot mutation at Arg132. Having identified…”
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Pharmacokinetics of Asciminib When Taken With Imatinib or With Food
Published in Clinical pharmacology in drug development (01-02-2022)“…Asciminib, a first‐in‐class, Specifically Targeting the Abelson kinase Myristoyl Pocket (STAMP) inhibitor with the potential to overcome resistance to…”
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The development of self-emulsifying oil-in-water emulsion adjuvant and an evaluation of the impact of droplet size on performance
Published in Journal of pharmaceutical sciences (01-04-2015)“…Microfluidization is an established technique for preparing emulsion adjuvant formulations for use in vaccines. Although this technique reproducibly yields…”
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Correction to: Use of Physiologically Based Pharmacokinetic (PBPK) Modeling for Predicting Drug-Food Interactions: an Industry Perspective
Published in The AAPS journal (26-11-2020)“…An Erratum to this paper has been published: https://doi.org/10.1208/s12248-020-00535-z…”
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The allosteric inhibitor ABL001 enables dual targeting of BCRABL1
Published in Nature (London) (30-03-2017)Get full text
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Optimization of 3‑Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors
Published in ACS medicinal chemistry letters (12-07-2018)“…Mutant isocitrate dehydrogenase 1 (IDH1) is an attractive therapeutic target for the treatment of various cancers such as AML, glioma, and glioblastoma. We…”
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Abstract A144: Inhibition of 2-HG production in IDH mutant xenograft models
Published in Molecular cancer therapeutics (01-11-2013)“…Abstract Isocitrate dehydrogenase 1 and 2 (IDH1/2) oxidize isocitrateto α-ketoglutarate (α-KG), a cofactor needed for the function of over 100 enzymes1…”
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ABL001, a Potent Allosteric Inhibitor of BCR-ABL, Prevents Emergence of Resistant Disease When Administered in Combination with Nilotinib in an in Vivo Murine Model of Chronic Myeloid Leukemia
Published in Blood (06-12-2014)“…Background: Chronic myelogenous leukemia (CML) and a subset of acute lymphoblastic leukemia (ALL) are caused by the t(9;22)(q34;q11.2) chromosome…”
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COUNTERION QUANTIFICATION FOR DISCOVERY CHEMISTRY AND PRE-FORMULATION SALT SCREENING
Published in Journal of liquid chromatography & related technologies (01-05-2012)“…A fast method was developed to determine the amount of anions and cations present in discovery samples using a reagent free ion chromatography system. The…”
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The influence of selected factors on the knowledge, perceptions, and academic practices of faculty of schools of public health in China about the increasing sex ratio as a priority social issue: Implications for professional education
Published 01-01-1996“…Faculty of schools of public health are in a position to teach students, conduct research on priority social issues, and collaborate with official and…”
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