B. Liederer

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Preclinical Pharmacokinetic/Pharmacodynamic Modeling and Simulation in the Pharmaceutical Industry: An IQ Consortium Survey Examining the Current Landscape

Arijit Chakravarty, Tycho Heimbach, Edgar Schuck, 2014, The AAPS Journal.

Disposition of GDC-0879, a B-RAF kinase inhibitor in preclinical species

Y. Ran, B. Liederer, E. Choo, 2009, Xenobiotica; the fate of foreign compounds in biological systems.

Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase.

D. Sampath, P. Dragovich, T. O'Brien, 2015, Toxicological sciences : an official journal of the Society of Toxicology.

Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Karl H. Clodfelter, P. Bauer, N. Kley, 2013, Bioorganic & medicinal chemistry letters.

Prediction of drug distribution in subcutaneous xenografts of human tumor cell lines and healthy tissues in mouse: application of the tissue composition-based model to antineoplastic drugs.

B. Liederer, S. Gould, C. Hop, 2015, Journal of pharmaceutical sciences.

Pharmacokinetic drivers of toxicity for basic molecules: strategy to lower pKa results in decreased tissue exposure and toxicity for a small molecule Met inhibitor.

Kevin A Ford, D. Sutherlin, M. Merchant, 2013, Toxicology and applied pharmacology.

Use of the Cassette-Dosing Approach to Assess Brain Penetration in Drug Discovery

Xingrong Liu, B. Liederer, C. Hop, 2012, Drug Metabolism and Disposition.

Use of Cassette Dosing to Enhance the Throughput of Rat Brain Microdialysis Studies

Xingrong Liu, B. Liederer, X. Ding, 2015, Drug Metabolism and Disposition.

Use of Cassette Dosing Approach to Assess Brain Penetration in Drug Discovery

B. Liederer, C. Hop, G. Deshmukh, 2012 .

Case Study: Moexipril Hydrochloride: A Prodrug of Moexiprilat

B. Liederer, 2007 .

Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.

Benjamin D. Sellers, K. Scearce-Levie, M. Volgraf, 2016, Journal of medicinal chemistry.

Comparison of in vitro-in vivo extrapolation of biliary clearance using an empirical scaling factor versus transport-based scaling factors in sandwich-cultured rat hepatocytes.

Xingrong Liu, B. Liederer, Susan D. Wong, 2013, Journal of pharmaceutical sciences.

Preclinical absorption, distribution, metabolism, excretion, and pharmacokinetic–pharmacodynamic modelling of N-(4-(3-((3S,4R)-1-ethyl-3-fluoropiperidine-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-4-yloxy)-3-fluorophenyl)-2-(4-fluorophenyl)-3-oxo-2,3-dihydropyridazine-4-carboxamide, a novel MET kinase inh

M. Merchant, Xingrong Liu, B. Liederer, 2011, Xenobiotica; the fate of foreign compounds in biological systems.

Cancer Therapy: Preclinical TargetingActivatedAktwithGDC-0068, aNovel SelectiveAkt Inhibitor That Is Efficacious in Multiple Tumor Models

Tyler T. Risom, M. Belvin, S. Gross, 2013 .

Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.

Jun Liang, J. Blake, B. Brandhuber, 2012, Journal of medicinal chemistry.

Evaluation of homogenization techniques for the preparation of mouse tissue samples to support drug discovery.

B. Liederer, Xiaorong Liang, S. Shahidi-Latham, 2011, Bioanalysis.

Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Brandon J. Bravo, Qiang Zhao, N. Skelton, 2013, Journal of medicinal chemistry.

Targeting the PI3K/Akt/mTOR-pathway with the pan-Akt inhibitor GDC-0068 in PIK3CA-mutant breast cancer brain metastases.

A. Giobbie-Hurder, S. Carter, H. Wakimoto, 2019, Neuro-oncology.

Preformulation study of epigallocatechin gallate, a promising antioxidant for topical skin cancer prevention.

B. Liederer, J. Blanchard, S. Proniuk, 2002, Journal of pharmaceutical sciences.

Supplementation of nicotinic acid with NAMPT inhibitors results in loss of in vivo efficacy in NAPRT1-deficient tumor models.

Leslie B. Lee, D. Sampath, P. Jackson, 2013, Neoplasia.

Single- and multiple-dose pharmacokinetics, potential for CYP3A inhibition, and food effect in patients with cancer and healthy subjects receiving ipatasertib

J. Tabernero, R. Meng, B. Liederer, 2021, Cancer Chemotherapy and Pharmacology.

Preclinical assessment of the ADME, efficacy and drug-drug interaction potential of a novel NAMPT inhibitor

D. Sampath, P. Dragovich, B. Liederer, 2019, Xenobiotica; the fate of foreign compounds in biological systems.

Cardiotoxicity Associated with Nicotinamide Phosphoribosyltransferase Inhibitors in Rodents and in Rat and Human-Derived Cells Lines

A. Bruening-Wright, D. Sampath, P. Dragovich, 2017, Cardiovascular Toxicology.

Translational and pharmacokinetic‐pharmacodynamic application for the clinical development of GDC‐0334, a novel TRPA1 inhibitor

Simon S. Gao, B. Liederer, P. Belloni, 2021, Clinical and translational science.

Targeting Activated Akt with GDC-0068, a Novel Selective Akt Inhibitor That Is Efficacious in Multiple Tumor Models

Tyler T. Risom, M. Belvin, S. Gross, 2013, Clinical Cancer Research.

Evaluation of Ipatasertib Interactions with Itraconazole and Coproporphyrin I and III in a Single Drug Interaction Study in Healthy Subjects

E. Cho, B. Liederer, R. Sane, 2021, The Journal of Pharmacology and Experimental Therapeutics.

Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.

G. L. Hamilton, Adam R. Johnson, C. Eigenbrot, 2019, Bioorganic & medicinal chemistry letters.

Pan-Cancer Metabolic Signature Predicts Co-Dependency on Glutaminase and De Novo Glutathione Synthesis Linked to a High-Mesenchymal Cell State.

Marie Evangelista, A. Daemen, W. Sandoval, 2018, Cell metabolism.

Topical formulation studies with DEET (N,N-diethyl-3-methylbenzamide) and cyclodextrins.

M. Kallen, B. Liederer, J. Blanchard, 2002, Journal of pharmaceutical sciences.

Enzymes involved in the bioconversion of ester-based prodrugs.

R. Borchardt, B. Liederer, 2006, Journal of pharmaceutical sciences.

Integrated Lead Optimization: Translational Models as We Advance Toward the Clinic

Bianca M. Liederer, Xingrong Liu, Simon Wong, 2017 .

RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases

Adam R. Johnson, M. van Lookeren Campagne, J. Webster, 2019, Cell Death & Differentiation.

Structure of human RIPK1 kinase domain in complex with GNE684

Adam R. Johnson, M. van Lookeren Campagne, J. Webster, 2019 .

Dependence of tumor cell lines and patient-derived tumors on the NAD salvage pathway renders them sensitive to NAMPT inhibition with GNE-618.

Leslie B. Lee, D. Sampath, P. Jackson, 2013, Neoplasia.

Abstract B154: A first-in-human trial of GDC-0068: A novel, oral, ATP-competitive Akt inhibitor, demonstrates robust suppression of the Akt pathway in surrogate and tumor tissues.

J. Tabernero, Kui Lin, Yibing Yan, 2011 .

GluN2A NMDA Receptor Enhancement Improves Brain Oscillations, Synchrony, and Cognitive Functions in Dravet Syndrome and Alzheimer’s Disease Models

Benjamin D. Sellers, J. Elstrott, K. Scearce-Levie, 2020, Cell reports.

Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors

R. Bourgon, K. Walter, T. Pham, 2013, Clinical Cancer Research.

Predictive Biomarkers and Personalized Medicine Loss of NAPRT 1 Expression by Tumor-Speci fi c Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors

R. Bourgon, H. Koeppen, P. Haverty, 2013 .

Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors.

Jun Liang, P. Trojer, R. Cummings, 2016, Bioorganic & medicinal chemistry letters.

From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.

Jun Liang, P. Trojer, Y. Ran, 2017, Bioorganic & medicinal chemistry letters.

Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.

Jun Liang, P. Trojer, R. Cummings, 2016, Bioorganic & medicinal chemistry letters.

Balancing Blood Sample Volume with 3Rs: Implementation and Best Practices for Small Molecule Toxicokinetic Assessments in Rats.

Brian Dean, Jacqueline Tarrant, B. Liederer, 2016, ILAR journal.

An alternative approach for quantitative bioanalysis using diluted blood to profile oral exposure of small molecule anticancer drugs in mice.

B. Liederer, L. Berezhkovskiy, Yuzhong Deng, 2013, Journal of Pharmacy and Science.

Evaluation of dried blood spot sampling following cassette dosing in drug discovery.

B. Liederer, Xiaorong Liang, L. Berezhkovskiy, 2011, Bioanalysis.

Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties.

Yang Xiao, Lei Zhang, Karl H. Clodfelter, 2013, Bioorganic & medicinal chemistry letters.

Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.

N. Skelton, D. Sampath, K. Bair, 2016, Journal of medicinal chemistry.

Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.

Karl H. Clodfelter, N. Skelton, D. Sampath, 2015, Bioorganic & medicinal chemistry letters.

Measuring NAD(+) levels in mouse blood and tissue samples via a surrogate matrix approach using LC-MS/MS.

P. Dragovich, B. Liederer, C. Hop, 2014, Bioanalysis.

Case Study: Olmesartan Medoxomil: A Prodrug of Olmesartan

B. Liederer, 2007 .

Preclinical Pharmacokinetic/Pharmacodynamic Modeling and Simulation in the Pharmaceutical Industry: An IQ Consortium Survey Examining the Current Landscape

Jerome T. Mettetal, J. Mettetal, T. Maurer, 2015, The AAPS Journal.

Identification of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Yang Xiao, Lei Zhang, Deepak Sampath, 2013, Bioorganic & medicinal chemistry letters.

Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.

Karl H. Clodfelter, P. Bauer, N. Kley, 2013, Journal of medicinal chemistry.

High-throughput liquid chromatography/mass spectrometry method for the quantitation of small molecules using accurate mass technologies in supporting discovery drug screening.

Xingrong Liu, B. Liederer, C. Hop, 2013, Rapid communications in mass spectrometry : RCM.

A TRPA1 inhibitor suppresses neurogenic inflammation and airway contraction for asthma treatment

Simon S. Gao, J. Elstrott, M. Volgraf, 2021, The Journal of experimental medicine.

Use of Subcutaneous and Intraperitoneal Administration Methods to Facilitate Cassette Dosing in Microdialysis Studies in Rats

Xingrong Liu, B. Liederer, M. Durk, 2018, Drug Metabolism and Disposition.

Preclinical QSP Modeling in the Pharmaceutical Industry: An IQ Consortium Survey Examining the Current Landscape

Fan Wu, Brian Topp, Bianca M. Liederer, 2018, CPT: pharmacometrics & systems pharmacology.

Significant differences in the disposition of cyclic prodrugs of opioid peptides in rats and guinea pigs following IV administration.

R. Borchardt, B. Liederer, H. Ouyang, 2005, Journal of pharmaceutical sciences.

GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved in Vivo Profile.

Benjamin D. Sellers, K. Scearce-Levie, M. Volgraf, 2017, ACS medicinal chemistry letters.

Translational pharmacokinetic-pharmacodynamic analysis in the pharmaceutical industry: an IQ Consortium PK-PD Discussion Group perspective.

Jerome T. Mettetal, J. Mettetal, Patrick E. Trapa, 2017, Drug discovery today.

An algorithm for evaluating potential tissue drug distribution in toxicology studies from readily available pharmacokinetic parameters.

Dolores Diaz, Brian Dean, Donna M Dambach, 2013, Journal of pharmaceutical sciences.

Correlation of tissue-plasma partition coefficients between normal tissues and subcutaneous xenografts of human tumor cell lines in mouse as a prediction tool of drug penetration in tumors.

B. Liederer, L. Salphati, C. Hop, 2013, Journal of pharmaceutical sciences.

Pan-Cancer Metabolic Signature Predicts Co-Dependency on Glutaminase and De Novo Glutathione Synthesis Linked to a High-Mesenchymal Cell State.

A. Daemen, W. Sandoval, G. Hatzivassiliou, 2018, Cell metabolism.

Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Brandon J. Bravo, Qiang Zhao, N. Skelton, 2013, Journal of medicinal chemistry.

Stability of oxymethyl-modified coumarinic acid cyclic prodrugs of diastereomeric opioid peptides in biological media from various animal species including human.

R. Borchardt, B. Liederer, 2005, Journal of pharmaceutical sciences.

The Absolute Bioavailability and Absorption, Metabolism, and Excretion of Ipatasertib, a Potent and Highly Selective Protein Kinase B (Akt) Inhibitor

B. Liederer, R. Sane, Shuguang Ma, 2023, Drug Metabolism and Disposition.

RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases

Adam R. Johnson, M. van Lookeren Campagne, J. Webster, 2019, Cell Death & Differentiation.

Effects of amino acid chirality and the chemical linker on the cell permeation characteristics of cyclic prodrugs of opioid peptides.

R. Borchardt, B. Liederer, T. Siahaan, 2006, Journal of medicinal chemistry.

Preclinical stereoselective disposition and toxicokinetics of two novel MET inhibitors

D. Sutherlin, Xingrong Liu, B. Liederer, 2012, Xenobiotica; the fate of foreign compounds in biological systems.