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Publications

Date Source Title
22nd Annual Scientific Meeting and Education Day of the Society for Neuro-oncology

The IDH1 mutant inhibitor AG-120 shows strong inhibition of 2-HG production in an orthotopic IDH1 mutant glioma model in vivo

22nd Annual Scientific Meeting and Education Day of the Society for Neuro-oncology

Combined use of the pan-IDH mutant inhibitor AG-881 with radiation therapy shows added benefit in an orthotopic IDH1 mutant glioma model in vivo

22nd Annual Scientific Meeting and Education Day of the Society for Neuro-oncology

AG-120, A First-in-Class Mutant IDH1 Inhibitor in Patients with Recurrent or Progressive IDH1 Mutant Glioma: Updated Results from the Phase 1 Non-Enhancing Glioma Population

AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics

AG-881, a brain penetrant, potent, pan-mutant IDH (mIDH) inhibitor for use in mIDH solid and hematologic malignancies

AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics

AG-120, a first-in-class mutant IDH1 inhibitor, promotes morphological changes and induces expression of liver-specific genes in IDH1 mutant cholangiocarcinoma

AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics

AG-120, a first-in-class mutant IDH1 inhibitor, promotes morphological changes and induces expression of liver-specific genes in IDH1 mutant cholangiocarcinoma

ACS Medicinal Chemistry Letters

Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2‑HG in Vivo

Nature

Metabolic control of TH17 and induced Treg cell balance by an epigenetic mechanism

Blood

AG-348 enhances pyruvate kinase activity in red blood cells from patients with PK deficiency

22nd EHA Congress

Effects of AG-348, a pyruvate kinase activator, in patients with pyruvate kinase deficiency: Updated results from the DRIVE PK study

22nd EHA Congress

Enasidenib in mutant-IDH2 Relapsed or Refractory Acute Myeloid Leukemia (R/R AML): Results of a Phase 1/2 study

Blood

Enasidenib induces acute myeloid leukemia cell differentiation to promote clinical response

2017 ASCO Annual Meeting

Enasidenib in mutant IDH2 R/R AML: results of Phase 1 dose escalation and expansion study

Blood

Enasidenib in mutant-IDH2 relapsed or refractory acute myeloid leukemia

2017 ASCO Annual Meeting

Differentiation Syndrome associated with enasidenib, a selective inhibitor of mutant IDH2

2017 ASCO Annual Meeting

Phase 1 study of AG-120, an IDH1 mutant enzyme inhibitor: results from the cholangiocarcinoma dose escalation and expansion cohorts

2017 ASCO Annual Meeting

Pharmacokinetic/pharmacodynamic (PK/PD) profile of AG-120 in patients with IDH1-mutant cholangiocarcinoma from a phase 1 study of advanced solid tumors

2017 ASCO Annual Meeting

ClarIDHy: a phase 3, multicenter, randomized, double-blind study of AG-120 vs placebo in patients with an advanced cholangiocarcinoma with an IDH1 mutation

Annual Review of Biochemistry

Isocitrate Dehydrogenase Mutation and (R)-2-Hydroxyglutarate: From Basic Discovery to Therapeutics Development

Keystone on Tumor Metabolism

Metabolic collateral vulnerabilities of MTAP-deleted cancers as therapeutic opportunities

Cancer Discovery

AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

58th ASH Annual Meeting

Determination of IDH1 Mutational Burden and Clearance via Next-Generation Sequencing in Patients With IDH1 Mutation-Positive Hematologic Malignancies Receiving AG-120, a First-in-Class Inhibitor of Mutant IDH1

58th ASH Annual Meeting

Characterization of metabolic response to AG-348, an allosteric activator of red cell pyruvate kinase, in healthy volunteers and pyruvate kinase deficiency patients

58th ASH Annual Meeting

Iron Overload Is Highly Prevalent in All Disease Severity States in Pyruvate Kinase Deficiency (PKD)

58th ASH Annual Meeting

Enasidenib (AG-221), a Potent Oral Inhibitor of Mutant Isocitrate Dehydrogenase 2 (IDH2) Enzyme, Induces Hematologic Responses in Patients with Myelodysplastic Syndromes (MDS)

58th ASH Annual Meeting

Effects of AG-348, a Pyruvate Kinase Activator, on Anemia and Hemolysis in Patients with Pyruvate Kinase (PK) Deficiency: Data from the DRIVE PK Study

58th ASH Annual Meeting

Safety, tolerability, pharmacokinetics, and pharmacodynamics of multiple doses of AG-519, an allosteric activator of pyruvate kinase-R in healthy subjects

58th ASH Annual Meeting

Population pharmacokinetics and pharmacodynamics of AG-519, a pyruvate kinase activator for the treatment of pyruvate kinase deficiency, in human healthy volunteers

2016 SNO Annual Meeting

AG-120, a first-in-class mutant IDH1 inhibitor inpatients with recurrent or progressive IDH1mutant glioma: results from the phase 1 glioma expansion cohorts

2016 CTOS Annual Meeting

A phase 1 study of AG-120, an IDH1 mutant enzyme inhibitor: results from the chondrosarcoma dose escalation and expansion cohorts

Cell Reports

Differential Aspartate Usage Identifies a Subset of Cancer Cells Particularly Dependent on OGDH

Journal of Inherited Metabolic Disease

A small molecule inhibitor of mutant IDH2 rescues cardiomyopathy in a D-2-hydroxyglutaric aciduria type II mouse model

21st EHA Congress

Preclinical pharmacokinetics and pharmacodynamics of AG-519, an allosteric pyruvate kinase activator

21st EHA Congress

Effects of AG-348, a pyruvate kinase activator, on anemia and hemolysis in patients with pyruvate kinase deficiency: early data from the DRIVE-PK study

21st EHA Congress

The pyruvate kinase activator AG-348 improves murine β-thalassemic anemia and corrects ineffective erythropoiesis

21st EHA Congress

A phase 1, single and multiple ascending dose study of safety, tolerability, pharmacokinetics and pharmacodynamics of AG-519, an allosteric activator of pyruvate kinase-R in healthy subjects

21st EHA Congress

AG-519 is a potent activator of mutant pyruvate kinase associated with hemolytic anemia

Cell Reports

MTAP Deletions in Cancer Create Vulnerability to Targeting of the MAT2A/PRMT5/RIOK1 Axis

Annals of Oncology

IDH mutations in cancer and progress toward development of targeted therapeutics

Immunity Journal

Network Integration of Parallel Metabolic and Transcriptional Data Reveals Metabolic Modules that Regulate Macrophage Polarization

PNAS Journal

Mutant IDH is sufficient to initiate enchondromatosis in mice

Blood Journal

IDH2 mutation-induced histone and DNA hypermethylation is progressively reversed by small-molecule inhibition

PLOS One

Mesenchymal Phenotype Predisposes Lung Cancer Cells to Impaired Proliferation and Redox Stress in Response to Glutaminase Inhibition

Blood

AG-221, a Small Molecule Mutant IDH2 Inhibitor, Remodels the Epigenetic State of IDH2-Mutant Cells and Induces Alterations in Self-Renewal/Differentiation in IDH2-Mutant AML Model in Vivo

Chemistry & Biology

Action at a Distance: Allostery and the Development of Drugs to Target Cancer Cell Metabolism

Nature

Mutant IDH inhibits HNF-4α to block hepatocyte differentiation and promote biliary cancer

The Journal of Biological Chemistry

Biochemical, Cellular and Biophysical Characterization of a Potent Inhibitor of Mutant Isocitrate Dehydrogenase IDH1

Science Magazine

Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation

Science Magazine

An Inhibitor of Mutant IDH1 Delays Growth and Promotes Differentiation of Glioma Cells

Chemistry & Biology

Small Molecule Activation of PKM2 in Cancer Cells Induces Serine Auxotrophy.

Genes & Development

D-2-hydroxyglutarate produced by mutant IDH1 perturbs collagen maturation and basement membrane function.

Nature

IDH1(R132H) mutation increases murine haematopoietic progenitors and alters epigenetics.

Science Magazine

Understanding the Warburg effect: the metabolic requirements of cell proliferation.

Cancer Cell

Metabolic reprogramming: a cancer hallmark even warburg did not anticipate.

Nature

Transformation by the (R)-enantiomer of 2-hydroxyglutarate linked to EGLN activation.

The Oncologist

Cancer-associated isocitrate dehydrogenase mutations.

Biochemistry

Full-length human glutaminase in complex with an allosteric inhibitor.

Nature

Functional genomics reveal that the serine synthesis pathway is essential in breast cancer.

Cancer Cell

Leukemic IDH1 and IDH2 Mutations Result in a Hypermethylation Phenotype, Disrupt TET2 Function, and Impair Hematopoietic Differentiation.

Trends in Molecular Medicine

IDH mutations in glioma and acute myeloid leukemia

Cancer Cell

The Common Feature of Leukemia-Associated IDH1 and IDH2 Mutations Is a Neomorphic Enzyme Activity Converting a-Ketoglutarate to 2-Hydroxyglutarate

Journal of Experimental Medicine

Cancer-associated metabolite 2-hydroxyglutarate accumulates in acute myelogenous leukemia with isocitrate dehydrogenase 1 and 2 mutations

Nature

Cancer-associated IDH1 mutations produce 2-hydroxyglutarate(2HG)