EOS-984 / iTeos - LARVOL DELTA

iTeos Therapeutics Announces Its Intention to Wind Down Operations (GlobeNewswire) - "Following a thorough assessment of the Company’s development pipeline, business prospects, and financial position, the Company’s Board of Directors intends to wind down clinical and operational activities and focus on leveraging the Company’s cash balance to deliver near-term value to shareholders, including any proceeds from the potential sale of the Company’s intellectual property and assets such as EOS-984, EOS-215, and a preclinical obesity program targeting ENT1." "

Commercial • Oncology

Inhibition of ENT1 relieves intracellular adenosine-mediated T cell suppression in cancer. (PubMed, Nat Immunol) - "A combination of EOS301984 with anti-PD-1 led to synergistic control of tumor growth in a humanized mouse model of triple-negative breast cancer. ENT1 inhibition, therefore, augments anti-cancer immune responses through the restoration of pyrimidine nucleotide synthesis in T cells suppressed by adenosine."

Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • SLC29A1

iTeos Reports First Quarter 2025 Financial Results and Provides Business Updates (GlobeNewswire) - "Program Highlights:...APT-008: Completed enrollment of the second dose cohort of the EOS-984 + pembrolizumab combination portion and continued advancement in the combination dose escalation of the Phase 1 trial in advanced malignancies. Topline data assessing EOS-984 as a monotherapy and in combination with pembrolizumab in patients with advanced solid tumors anticipated in 2H25."

P1 data • Solid Tumor

iTeos Announces 2025 Strategic Priorities and Anticipated Milestones (GlobeNewswire) - "APT-008: Topline data assessing EOS-984 as a monotherapy and in combination with pembrolizumab in patients with advanced solid tumors anticipated in 2H25....TRM-010: Investigative New Drug (IND) application for EOS-215 anticipated in 1Q25."

IND • P1 data • Oncology • Solid Tumor

Intracellular adenosine drives profound lymphocyte suppression and can be reversed with EOS-984: A potent ENT1 antagonist (ESMO-IO 2024) - "EOS-984 blocked intracellular adenosine transport, rescuing proliferation and function of T cells stimulated in the presence of adenosine in vitro. In a humanized mouse model of anti-PD-1-resistant TNBC (MDA-MB-231), EOS-984 controlled tumor growth synergistically with nivolumab.Conclusions In conclusion, intracellular adenosine metabolism is a novel mechanism of T cell immunosuppression, amenable to ENT1 inhibition to enhance anti-cancer immune responses."

IO biomarker • Oncology • Pancreatic Cancer • Solid Tumor • Triple Negative Breast Cancer • CD8 • SLC29A1

iTeos Reports Third Quarter 2024 Financial Results and Provides Business Updates (GlobeNewswire) - "Program Highlights:...EOS-984:...(i) Completed enrollment of monotherapy dose escalation and initiated dosing of first cohort of EOS-984 + pembrolizumab combination portion in the Phase 1 APT-008 trial; (ii) Two poster presentations on preclinical and translational data highlighting the novel mechanism of action, monotherapy and combination activity combination activity with anti-PD-1 therapy, and the adenosine signature biomarker to be presented at the ESMO IO Congress 2024; (iii) Topline data from the Phase 1 APT-008 trial anticipated in 2025."

Clinical data • Enrollment status • P1 data • Preclinical • Solid Tumor

Adenosine drives profound lymphocyte immunosuppression via a previously underappreciated mechanism and can be reversed with EOS-984, a potent ENT1 antagonist (CRI-ENCI-AACR ICIC 2024) - "Finally, in a humanized mouse model of triple negative breast cancer resistant to anti-PD-1 blockade (MDA-MB-231), combination of EOS-984 with nivolumab synergistically led to control of tumor growth. Thus, ENT1 inhibition represents a novel approach to augment anti-cancer immune responses through restoring pyrimidine nucleotide synthesis in T cells suppressed by adenosine."

IO biomarker • Breast Cancer • Gastrointestinal Cancer • Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Solid Tumor • Triple Negative Breast Cancer • CD8 • SLC29A1

iTeos Reports Second Quarter 2024 Financial Results and Provides Business Updates (GlobeNewswire) - "Program Highlights:....(i) A2A-005: Data from the dose escalation portion of the Phase 2 trial with inupadenant and platinum-doublet chemotherapy in post-IO metastatic non-squamous NSCLC anticipated in late 2024; (ii) EOS-984:...Topline data from the Phase 1 trial anticipated in the second half of 2024."

P1 data • P2 data • Non Small Cell Lung Cancer

A First-in-Human Study of EOS301984 as Monotherapy or Combination Therapy in Adult Participants With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=84 | Recruiting | Sponsor: iTeos Therapeutics

Combination therapy • Metastases • Monotherapy • New P1 trial • Oncology • Solid Tumor

Discovery of EOS-984, a potent and selective ENT1 inhibitor (ACS-Fall 2024) - "ENT1 expression increases upon T cell activation, suggesting uptake of extracellular adenosine is a mechanism to limit T cell responses in high adenosine environments.EOS-984 is a first-in-class small molecule highly potent and selective inhibitor of ENT1, currently being evaluated in patients with advanced solid tumors. The medicinal chemistry efforts that lead to the discovery of EOS-984 will be detailed."

Oncology • Solid Tumor • SLC29A1

iTeos Reports First Quarter 2024 Financial Results and Provides Business Updates (GlobeNewswire) - "Inupadenant (EOS-850): insurmountable small molecule antagonist targeting adenosine A2A receptor in second-line NSCLC. A2A-005: Completed enrollment of Phase 2 A2A-005 dose escalation. Data from the dose escalation portion of the Phase 2 trial with inupadenant and platinum-doublet chemotherapy in post-IO metastatic non-squamous NSCLC anticipated in late 2024....R&D expenses were $34.5 million for the quarter ended March 31, 2024, as compared to $25.6 million for the same quarter of 2023. The increase compared to the comparative period was primarily due to increases in activities related to the belrestotug, inupadenant, and EOS-984 programs, and included the addition of new R&D employees hired to help advance these programs."

Commercial • P2 data • Lung Cancer • Lung Non-Squamous Non-Small Cell Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

iTeos Presents EOS-984 Preclinical Data Demonstrating Restoration of T Cell Activity from Adenosine Suppression at the American Association for Cancer Research Annual Meeting 2024 (GlobeNewswire) - "In preclinical studies, blockade of intracellular adenosine accumulation by EOS-984 enabled proliferation of memory T cells and TILs despite high adenosine concentrations, resulting in the restoration of T cell function and enhanced tumor cell killing. Furthermore, combination of EOS-984 with anti-PD-1 therapy synergistically led to the control of tumor growth in a humanized mouse model of triple negative breast cancer resistant to anti-PD-1 blockade. Due to its mechanism of action, EOS-984 holds potential as a combination partner beyond anti-PD-1 therapy, including other immuno-oncology agents, cell therapies, and bispecific T cell engagers....Topline data from the Phase 1 trial is anticipated in the second half of 2024."

P1 data • Preclinical • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

iTeos to Highlight Preclinical Data on First-In-Class EOS-984 Targeting ENT1 at the American Association for Cancer Research Annual Meeting 2024 (GlobeNewswire) - "iTeos Therapeutics...announced a poster presentation of preclinical data on EOS-984, a first-in-class small molecule antagonist targeting equilibrative nucleoside transporter 1 (ENT1), at the American Association for Cancer Research (AACR) Annual Meeting, being held April 5-10, 2024 in San Diego, California."

Preclinical • Oncology

iTeos Announces 2024 Strategic Priorities and Anticipated Milestones (GlobeNewswire) - "EOS-984: Preclinical mechanism of action data anticipated in the second quarter of 2024; Topline data from the Phase 1 dose escalation trial in advanced malignancies anticipated in the second half of 2024."

P1 data • Preclinical • Oncology

iTeos Reports Third Quarter 2023 Financial Results and Provides Business Updates (GlobeNewswire) - "Inupadenant (EOS-850): Continued progression of the two-part A2A-005 Phase 2 trial with inupadenant and platinum-doublet chemotherapy in post-IO metastatic non-squamous NSCLC. Topline data from Phase 2 A2A-005 are anticipated in late 2024. EOS-984: Completed enrollment of the first dose cohort and continued advancement in the dose escalation of the Phase 1 trial in advanced malignancies. Topline data from the Phase 1 trial are anticipated in late 2024....R&D expenses were $30.6 million for the quarter ended September 30, 2023, as compared to $23.9 million for the same quarter of 2022. The increases in each comparative period were primarily due to increases in activities related to the belrestotug, inupadenant, and EOS-984 programs."

Commercial • P1 data • P2 data • Lung Cancer • Lung Non-Squamous Non-Small Cell Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

iTeos Reports First Quarter 2023 Financial Results and Provides Business Updates (GlobeNewswire) - "The company completed Investigational New Drug / Clinical Trials Application-enabling activities, including toxicity studies, and anticipates initiating clinical studies for EOS-984 mid-year 2023."

New trial • Oncology • Solid Tumor

iTeos Reports Fourth Quarter and Full Year 2022 Financial Results and Provides Business Updates (GlobeNewswire) - "The company completed Investigational New Drug / Clinical Trials Application-enabling activities including toxicity studies and anticipates initiating clinical studies for EOS-984 in mid-2023."

IND • Oncology • Solid Tumor

iTeos Provides Business Updates and Clinical Development Plans for 2023 (GlobeNewswire) - "We expect to advance EOS-448, our anti-TIGIT, antibody, into Phase 3 in combination with GSK’s ant-PD-1, Jemperli (dostarlimab) and also continue to advance studies targeting the adenosine pathway through our inupadenant program. Additionally, EOS-984, a first-in-class therapy designed to inhibit a novel target in the adenosine pathway, is expected to enter the clinic in mid-2023..."

New P3 trial • New trial • Oncology