Publications & Presentations - Nimbus Therapeutics

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Phase 1/2 Trial of the HPK1 Inhibitor NDI-101150 as Monotherapy and in Combination with Pembrolizumab: Clinical Update

Discovery of NDI-101150, a highly potent and selective HPK1 inhibitor for the treatment of cancer, through structure-based drug design

NDI-101150 is a Potent and Highly Selective HPK1 Inhibitor that Both Synergizes with and Differentiates from anti-PD1 Immune Checkpoint Blockade

Preliminary Monotherapy and Pharmacokinetic Results from an Ongoing Phase 1a Dose Escalation Study of NDI-101150, a Highly Selective Oral Hematopoietic Progenitor Kinase 1 (HPK1) Inhibitor

NDI-101150 is a Potent and Highly Selective Hematopoietic Progenitor Kinase 1 (HPK1) Inhibitor that Promotes a Robust and Broad Anti-Tumor Immune Response

AACR-NCI-EORTC 2023

Hematopoietic Progenitor Kinase 1 (HPK1) Inhibition Enhances Antibody Secretion, Pro-inflammatory Cytokine Production and Proliferation of Primary Human B Cells

Characterization of pharmacokinetics, pharmacodynamics, tolerability and clinical activity in Phase 1 studies of the novel allosteric tyrosine kinase 2 (TYK2) inhibitor NDI-034858

Discovery of NTX-801, a Cbl-b inhibitor with anti-tumor activity in syngeneic models

Analysis of histologic, molecular and clinical improvement in moderate-to-severe psoriasis: Results from a Phase 1b trial of the novel allosteric TYK2 inhibitor NDI-034858

A Highly Selective and Potent HPK1 Inhibitor Induces Robust Tumor Growth Inhibition as a Single Agent and in Combination with anti-PD1 in Multiple Syngeneic Tumor Models

A Highly Selective and Potent HPK1 Inhibitor Enhances Immune Cell Activation and Induces Robust Tumor Growth Inhibition in a Syngeneic Tumor Model

EORTC-NCI-AACR Symposium 2020

A Highly Selective and Potent HPK1 Inhibitor Enhances Immune Cell Activation and Induces Robust Tumor Growth Inhibition in a Syngeneic Tumor Model

AACR Virtual Annual Meeting II, 2020

A Highly Selective and Potent HPK1 Inhibitor Enhances Immune Cell Activation and Induces Robust Tumor Growth Inhibition in a Syngeneic Tumor Model

2018 International Congress on Spondyloarthritides

TYK2 promotes IL-23 induced type 3 immunity and disease progression in SpA

The AASLD Liver Meeting 2017

Plasma Metabolites for de Novo Lipogenesis and Pharmacodynamic Activity of Acetyl-CoA Carboxylase Inhibitor GS-0976

Keystone Immuno-Metabolism Conference 2017

Selective Acetyl-CoA Carboxylase Inhibitor ND-646 Suppresses Th17- and Promotes Treg-mediated Immune Response in vitro and in vivo

NDI-010976, A Potent, Liver-Directed, Oral Inhibitor of Acetyl-CoA Carboxylase for Non-Alcoholic Steatohepatitis: A Phase 1 Single Ascending Dose Study in Healthy Volunteers

NDI-010976, A Potent, Liver-Directed, Oral Inhibitor of Acetyl CoA Carboxylase for Non-Alcoholic Steatohepatitis: Pharmacodynamic Effects on Hepatic De Novo Lipogenesis in Obese but Otherwise Healthy Adult Male Volunteers

Combination Therapy with a Liver Selective Acetyl CoA Carboxylase Inhibitor ND-654 and Sorafenib Improves Efficacy in the Treatment of Cirrhotic Rats with Hepatocellular Carcinoma

Modulation of Lipid Metabolism Through Inhibition of Acetyl-CoA Carboxylase with ND-646 Leads to Potent Inhibition of Breast Cancer Cell Growth in vitro and in vivo

Potent and Selective Tyk2 Inhibitor is Highly Efficacious in Rodent Models of Inflammatory Bowel Disease and Psoriasis

Anti-leukemic Activity of the TYK2 Selective Inhibitor NDI-031301 in T-cell Acute Lymphoblastic Leukemia

Keystone Symposium 2015

ND-630, a Potent and Liver-Directed Acetyl-CoA Carboxylase Inhibitor, Reduces Hepatic Steatosis and Improves Dyslipidemia in Diet-Induced Obese and Diabetic Rat Models of Non-Alcoholic Fatty Liver Disease

Liver Selective Acetyl-CoA Carboxylase Inhibition by ND-654 Improves Survival in Cirrhotic Rats with Hepatocellular Carcinoma

Liver-directed allosteric inhibitors of acetyl-CoA carboxylase favorably impact pathophysiology in the progression from NAFLD to NASH and Hepatocellular Carcinoma, including hepatic steatosis, inflammation, and fibrosis

Liver-Directed Allosteric Inhibitors of Acetyl-CoA Carboxylase Reduce Hepatic Steatosis and Improve Dyslipidemia in Diet-Induced Obese Rat Models and Reduce Inflammation and Fibrosis in a Cirrhotic Rat Model

Identification of Highly Potent and Selective Tyk2 Inhibitors for the Treatment of Autoimmune Diseases Through Structure-Based Drug Design

Potent and Selective Tyk2 Inhibitors Block Th1- and Th17- Mediated Immune Responses and Reduce Disease Progression in Rodent Models of Delayed-Type Hypersensitivity and Psoriasis

Liver Selective Acetyl-CoA Carboxylase Inhibition by ND-654 Decreases Hepatocellular Carcinoma Development in Cirrhotic Rats

Acetyl-CoA Carboxylase Inhibition by ND646 reduces fatty acid synthesis and inhibits cell proliferation in human non-small cell lung cancer cells

Acetyl-CoA Carboxylase Inhibition by ND-630 Inhibits Fatty Acid Synthesis, Stimulates Fatty Acid Oxidation, Reduces Body Weight, Improves Insulin Sensitivity, and Modulates Dyslipidemia in Rats

Liver Selective Acetyl-CoA Carboxylase Inhibition by ND-654 and Related Analogs Inhibits Hepatic Fatty Acid Synthesis, Stimulates Hepatic Fatty Acid Oxidation, Reduces Hepatic Steatosis, and Modulates Dyslipidemia in Diet-Induced Obese Rats

Acetyl-CoA Carboxylase Inhibition by ND-630 Inhibits Fatty Acid Synthesis and Stimulates Fatty Acid Oxidation in Cultured Cells and in Experimental Animals

Synergistic Blockade of ABC DLBCL Proliferation with a Selective Inhibitor of IRAK4 in Combination with Inhibition of the B-Cell Receptor Signaling Network

Identification of Highly Potent and Selective Interleukin-1 Receptor-Associated Kinase 4 Inhibitors for the Treatment of Rheumatic Diseases

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Publications

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July 10, 2023 | Journal of Medicinal Chemistry

Discovery of a potent and selective tyrosine kinase 2 inhibitor: TAK-279

AUGUST 26, 2022 | FRONTIERS IN IMMUNOLOGY

Targeting the Cbl-b-Notch1 axis as a novel immunotherapeutic strategy to boost CD8+ T-cell responses

JULY, 13, 2022 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Potent and selective TYK2-JH1 inhibitors highly efficacious in rodent model of psoriasis

May 6, 2021 | Expert Opinion on Therapeutic Patents

Inhibitors of immuno-oncology target HPK1 - a patent review (2016 to 2020)

June 1, 2020 | Diabetes, Obesity and Metabolism

Preclinical evaluation of tyrosine kinase 2 inhibitors for human beta‐cell protection in type 1 diabetes

March 9, 2020 | The Journal of Clinical Investigation

TYK2 inhibition reduces type 3 immunity and modifies disease progression in murine spondyloarthritis

April 3, 2019 | Nature

An allosteric mechanism for potent inhibition of human ATP-citrate lyase

October 02, 2018 | Cell Reports

The kinase activity of hematopoietic progenitor kinase 1 is essential for the regulation of T cell function

September 20, 2018 | Metabolism

Inhibition of Acetyl-CoA Carboxylase by Phosphorylation or the Inhibitor ND-654 Suppresses Lipogenesis and Hepatocellular Carcinoma

July 5, 2017 | HEPATOLOGY

Acetyl-Coenzyme A Carboxylase Inhibition Reduces De Novo Lipogenesis in Overweight Male Subjects: A Randomized, Double-Blind, Crossover Study

March 14, 2017 | British Journal of Haemotology

Anti-leukaemic activity of the TYK2 selective inhibitor NDI-031301 in T-cell acute lymphoblastic leukaemia

November 2, 2016 | Current Opinion in Structural Biology

Accelerating drug discovery through tight integration of expert molecular design and predictive scoring

September 19, 2016 | Nature Medicine

Inhibition of acetyl-CoA carboxylase suppresses fatty acid synthesis and tumor growth of non-small cell lung cancer in preclinical models

March 14, 2016 | PNAS

Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats

November 30, 2015 | Exp Med

Selective interleukin-1 receptor–associated kinase 4 inhibitors for the treatment of autoimmune disorders and lymphoid malignancy

January 27, 2015 | J Am Chem Soc

Accurate and Reliable Prediction of Relative Ligand Binding Potency in Prospective Drug Discovery by Way of a Modern Free-Energy Calculation Protocol and Force Field

December 5, 2014 | J Exp Med

Recent advances in the discovery of small molecule inhibitors of Interleukin 1 Receptor-Associated Kinase 4 (IRAK4) as a therapeutic target for inflammation and oncology disorders

May 15, 2009 | Journal of Immunology

Hematopoietic progenitor kinase 1 is a negative regulator of dendritic cell activation

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