Links to the following publications and presentations, which are located on outside websites, are provided for informational purposes only and do not constitute the opinions or views of vTv Therapeutics.
Azeliragon
Publications
- Burstein, A. H., Brantley, S. J., Dunn, I. , Altstiel, L. D. and Schmith, V. (2019), Assessment of Azeliragon QTc Liability Through Integrated, Model‐Based Concentration QTc Analysis. Clinical Pharmacology in Drug Development
- Burstein AH, Sabbagh M, Andrews R, Valcarce C, Dunn I, Altstiel L. Development of Azeliragon, an Oral Small Molecule Antagonist of the Receptor for Advanced Glycation Endproducts, for the Potential Slowing of Loss of Cognition in Mild Alzheimer’s Disease. J Prev Alz Dis 2018;5(2):149-154
- Sabbagh MN, Agro A, Bell J, Aisen PS, Schweizer E, Galasko D. PF-04494700, an oral inhibitor of receptor for advanced glycation end products (RAGE), in Alzeimer disease. Alzheimer Dis Assoc Disord 2011;25(3):206-212
- Galasko D, Bell J, Mancuso JY, Kupiec JW, Sabbagh MN, van Dyck C, Thomas RG, Aisen PS; Alzheimer’s Disease Cooperative Study. Clinical trial of an inhibitor of RAGE-Aβ interactions in Alzheimer disease. Neurology 2014; 82(17):1536-42
- Burstein AH, Grimes I, Galasko DR, Aisen PS, Sabbagh M, Mjalli AM. Effect of TTP488 in patients with mild to moderate Alzheimer disease. BMC Neurol 2014;14:12
- Chen Y., Akirav E, Chen W, Henegariu O, Moser B, Desai D, Shen J, Webster J, Andrews R, Mjalli A, Rothlein R, Schmidt AM, Clynes R, Herold K. RAGE Ligation Affects T Cell Activation and Controls T Cell Differentiation. J Immunol 2008; 181:4272-4278
Presentations and Posters
- Gooch A, Kirby L, Hendrix S, Nicodemus-Johnson J, Humphries L, Dunn I, Valcarce C, Burstein A. Safety and Efficacy Results from the Phase 2 Elevage Study of Azeliragon in Mild Alzheimer’s disease and type 2 diabetes. Presented at 2021 ADPD. March 10, 2021 – Virtual.
- Gooch A, Kirby L, Humphries L, Dunn I, Valcarce C, Burstein A. The Azeliragon Elevage Study: Study Update and Preliminary Data on Baseline Characteristics of Participants with Mild Alzheimer’s Disease and Type 2 Diabetes Randomized in Part 1. Presented at 2020 CTAD. November 4, 2020 – Virtual.
- Burstein A, Dunn I, Gooch A, Valcarce C. Effects of azeliragon on ADAS-cog and CDR domains and individual items in patients with mild Alzheimer’s disease and type 2 diabetes (T2D). Presented at the 2020 Alzheimer’s Association International Conference (AAIC). July 29, 2019 – Virtual
- Valcarce C, Dunn I, Burstein A. Linking Diabetes and Alzheimer’s Disease through RAGE. A Retrospective Analysis of Azeliragon Phase 2 and Phase 3 Studies. Presented at the 2019 Alzheimer’s Association International Conference (AAIC). July 17, 2019. Los Angeles, California
- Valcarce C, Dunn I, Soeder T, Burstein A. Inflammatory biomarkers, brain volumetric MRI, FDG-Pet results in patients with type 2 diabetes in azeliragon phase 3 trial in mild Alzheimer’s disease (AD). Presented at 14th International Conference on Alzheimer’s & Parkinson’s Diseases. March 30, 2019. Lisbon, Portugal
- Sabbagh M, Dunn I, Gooch A, Soeder T, Kieburtz K, Valcarce C, Altstiel L, Burstein A. Safety and efficacy results from the phase 3, multicenter, 18-month STEADFAST trial of azeliragon in participants with mild Alzheimer’s disease. Presented at 2018 CTAD. October 26, 2018. Barcelona, Spain
- Valcarce C, Dunn I, Soeder T, Burstein A. Is RAGE the missing link between diabetes and dementia? Results from a subgroup analysis of the STEADFAST trial. Presented at 2018 CTAD. October 24, 2018. Barcelona, Spain
- Burstein A, Dunn I, Altstiel L. Analysis of treatment emergent adverse event incidences in phase 2 study of azeliragon reveal potential attenuation of psychiatric system organ class (SOC) adverse events and expected drug effects in gastrointestinal SOC. Presented at 2017 CTAD. November 2, 2017. Boston, MA
- Burstein A, Lamson M, Sale M, Brantley S, Gooch A, Dunn I, Altstiel L. Effect of CYP2C8 and CYP3A4 inhibition and CYP induction on the pharmacokinetics of azeliragon. Presented at 2017 CTAD. November 2, 2017. Boston, MA
- Burstein A, Gooch A, Brantley S, Lamson M, Dunn I, Altstiel L. Effect of mild or moderate hepatic impairment on the clearance of azeliragon. Presented at 2017 CTAD. November 2, 2017. Boston, MA
- Burstein A, Dunn I, Soeder T, Sabbagh M, Altstiel L. Azeliragon Phase 2b Survival Analysis Supports Beneficial Effects on Delaying Time to Cognitive Deterioration in Patients with Mild Alzheimer’s Disease. Presented at 2016 Alzheimer’s Association International Conference (AAIC). July 27, 2016. Toronto, Canada
- Sabbagh MN, Burstein A, Dunn I, Valcarce C, Rose EA, Doody R, Sano M, Schneider LS, Galasko DR. “TTP488: From futile to fast track” AAIC 2015
- Burstein A, Galasko D, Aisen P, Thomas R, Grimes I, Clark DJ, Mjalli A, Orlande C. Evaluation of the relationship between TTP488 plasma concentrations and changes in ADAS-cog relative to placebo. Alzheimer’s & Dementia 2013;9(4, Supplement): 279-280
- Kostura MJ, Kindy MS, Burstein A, Valcarce C, Polisetti D, Andrews R, Mjalli AM. Efficacy of RAGE antagonists in murine model of Alzheimer’s disease. Alzheimer’s & Dementia 2014;10(4, Supplement): 638-639.
TTP399
Publications
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- Vella A, Freeman J, Dunn I, Keller K, Buse J, Valcarce C. Targeting hepatic glucokinase to treat diabetes with TTP399, a hepatoselective glucokinase activator. Science Translational Medicine 16 Jan 2019
Presentations and Posters
- Freeman J, Dunn I, Valcarce C. Mechanism matters: preliminary evidence that activation of glucokinase by TTP399 does not increase plasma or urine ketones in type 1 diabetes. Presented at the 56th EASD Conference – Virtual, September 22, 2020.
- Valcarce C, Freeman J, Dunn I, Dvergsten C, Klein KR, Buse J. The Simplici-T1 trial: Activation of glucokinase by TTP399 improves glycemic control in patients with T1DM. Presented at the 56th EASD Conference – Virtual, September 22, 2020.
- Buse J, Klein K, Freeman J, Dunn I, Valcarce C. The Simplici-T1 Trial: Glucokinase Activator TTP399 Improves Glycemic Control in Patients with Type 1 Diabetes. Presented at the American Diabetes Association’s 80th Scientific Sessions – Virtual, June 13, 2020
- Valcarce C, Klein K, Freeman J, Dunn I, Buse B. The Simplici-T1 Trial: Relationship between Glycemic Control and Insulin Dose. Presented at the American Diabetes Association’s 80th Scientific Sessions – Virtual, June 13, 2020
- Valcarce C, Freeman J, Dunn I, Dvergsten C, Soeder T and Buse J. Results from the sentinel and learning phase of the Simplici-T1 study, the first clinical trial to test activation of glucokinase as an adjunctive treatment for type 1 diabetes. Presented at the 55th EASD conference, September 18, 2019, Barcelona, Spain
- Buse J, Valcarce C, Freeman J, Dunn I, Dvergsten C, Kirkman S, Alexander k, Jamie D and Bergamo K. Simplici-T1: First Clinical Trial to Test Activation of Glucokinase as an Adjunctive Treatment for Type 1 Diabetes; Presented at the American Diabetes Association 78th Scientific Sessions, June 25, 2018, Orlando, Florida
- Valcarce C, Grimes I, and Freeman J. TTP399, a Novel, Liver Selective Glucokinase Activator: Results from a 10 Day Pilot Study in Patients with Type 2 Diabetes Mellitus (T2DM) Naïve to Drug; Presented at the American Diabetes Association 76th Scientific Sessions, June 12, 2016, New Orleans, Louisiana
- Valcarce C. The Importance of Tissue Selectivity and Preservation of the Physiological Regulation when Targeting Key Metabolic Regulators as Glucokinase; Presented at the Keystone Symposia on New Therapeutics for Diabetes and Obesity, April 19, 2016, La Jolla, California
- Valcarce C. TTP399, A Liver Selective Glucokinase Activator Increases Efficacy of Currently Marketed Therapies for Type 2 Diabetes; Presented at the 75th Annual Scientific Session of the American Diabetes Association, June 3, 2015, Boston Massachusetts
- Valcarce C. TTP399, a Liver-Selective Glucose Kinase Activator (GKA), Lowers Glucose and Does NOT Increase Lipids in Subjects with Type 2 Diabetes Mellitus (T2DM); (Abstract #122-OR). Presented at the 74th Annual Scientific Session of the American Diabetes Association, June 13, 2014, San Francisco California
- Valcarce C. TTP399, A Liver Selective Glucokinase Activator (GKA) that Preserves the Physiological Regulation of Glucokinase (GK) by GK Regulatory Protein (GKRP)
TTP273
Publications
Presentations and Posters
- Valcarce C., Dunn I., Freeman J. Effects of the Oral, Small Molecule GLP-1R Agonist, TTP273, on Patients with Stage 2 Hypertension: Results from a Post-Hoc Analysis of the Phase 2 LOGRA Study; American Diabetes Association 79th Scientific Sessions in San Francisco, CA, June 7-11, 2019
- Freeman J., Dunn I., Valcarce C. Beyond Topline Results for the Oral (Non-Peptide) GLP-1R Agonist TTP273 in Type 2 Diabetes: How much and When?; 53rd Annual Meeting of the European Association for the Study of Diabetes (EASD) held in Lisbon, Portugal, September 11–15, 2017
- Freeman J., Soeder T., Dunn I., Valcarce C. Is Less More? Learning to Dose the Oral, Nonpeptide GLP-1R Agonist, TTP273 in Type 2 Diabetics; Presented at the American Diabetes Association 77th Scientific Sessions in San Diego, CA, June 9-13, 2017
- Freeman J., Dvergsten C., Dunn I., Valcarce C. TTP273, Oral (Nonpeptide) GLP-1R Agonist: Improved Glycemic Control without Nausea and Vomiting in Phase 2; Presented at the American Diabetes Association 77th Scientific Sessions in San Diego, CA, June 9-13, 2017
- Freeman J, Agolory J, and Valcarce C. Preclinical Findings with Oral GLP-1 Receptor Agonist TTP273 Reinforce Importance of Neuro-Enteroendocrine Signaling; Presented at the American Diabetes Association 76th Scientific Sessions, June 12, 2016, New Orleans, Louisiana
- Freeman J, Gustafson S, Dunn I, Burstein A, and Valcarce C. Oral Small Molecule GLP-1 Receptor (GLP-1R) Agonists for Type 2 Diabetes (T2DM) with Negligible Nausea and Vomiting; Presented at the Keystone Symposia on New Therapeutics for Diabetes and Obesity, April 18, 2016, La Jolla, California – View Presentation Slides
- Freeman J, Weaver S, Davis S, Rao M, Quada J, Santhosh K, Yokum S, Polisetti D, Andrews R, Tabrizifard S, Sturchler E, McDonald P, Agolory J, Gustafson S and Valcarce C. TTP273: Oral, G protein Pathway Selective Clinical-Stage GLP-1 Receptor (GLP-1R) Agonist; poster presented at the Keystone Symposia on G-Protein Coupled Receptors: Structure, Signaling and Drug Discovery, held in Keystone, Colorado. February 22, 2016
- Gustavson, S.TTP273, an Orally-Available Glucagon-like Peptide-1 (GLP-1) Agonist, Notably Reduces Glycemia in Subjects with Type 2 Diabetes Mellitus (T2DM); (Abstract # 155-OR) Presented at the 74th Annual Scientific Session of the American Diabetes Association, June 13, 2014, San Francisco, California
- Gustavson, S.TTP054, a Novel, Orally-Available Glucagon-like Peptide-1 (GLP-1) Agonist, Lowers HbA1c in Subjects with Type 2 Diabetes Mellitus (T2DM); (Abstract # 156-OR) Presented at the 74th Annual Scientific Session of the American Diabetes Association, June 13, 2014, San Francisco, California