- Study will evaluate the safety and efficacy of the combination of iTeos’ EOS100850 and Merck’s KEYTRUDA® (pembrolizumab)
Gosselies, Belgium and Cambridge, Mass. – Dec. 12, 2019 – iTeos Therapeutics SA, a privately-held biotechnology company developing novel cancer immunotherapies, announced today that it has entered into an agreement with a subsidiary of Merck, known as MSD outside the United States and Canada, to evaluate the safety and efficacy of EOS100850, iTeos’ investigational A2A receptor antagonist, in combination with KEYTRUDA® (pembrolizumab), Merck’s anti-PD-1 (programmed death receptor-1) therapy, in patients with solid tumors.
The Phase 1/2 trial will enroll patients with multiple solid tumors, with the initial goal of determining the safety and tolerability of the combination therapy. The trial is expected to begin enrollment in early 2020.
Joanne Jenkins Lager, M.D, Chief Medical Officer of iTeos Therapeutics, commented: “We believe that our differentiated, selective A2A receptor antagonist will be complementary to a range of immuno-oncology approaches and we are excited to initiate our first combination study of EOS100850 with KEYTRUDA®. Unlike other A2A antagonists, EOS100850 was purposely designed to have very high potency in the tumor micro-environment and unique selectivity for the A2A receptor. We look forward to evaluating how these two agents interact and complement each other as they have distinct mechanisms to overcome immunosuppression in the tumor microenvironment.”
iTeos’ lead therapeutic candidate, EOS100850, is a non-brain penetrant A2A receptor antagonist that retains high potency in the presence of elevated adenosine concentrations such as those measured in the tumor microenvironment. It is currently in a Phase 1/1b study as a monotherapy.
KEYTRUDA® is a registered trademark of Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc., Kenilworth, N.J., USA.
About the iTeos Adenosine A2A Receptor Antagonist (EOS100850)
The high level of adenosine in the microenvironment of many tumors plays a significant role in tumor immune evasion. The adenosine A2A receptor is the primary adenosine receptor expressed on immune cells. In the presence of adenosine, this receptor suppresses T cell activity. In preclinical studies, EOS100850, iTeos’ A2A receptor antagonist, restores T cell activity and promotes anti-tumor activity in preclinical models, as well as synergizing with several immune-checkpoint inhibitors and chemotherapy. Preliminary evidence of clinical activity has been described in kidney, lung and prostate cancer in clinical studies of A2A receptor antagonists and other agents targeting the adenosine axis. In contrast to other clinical-stage A2A receptor antagonists, EOS100850 retains high potency in the presence of elevated adenosine concentrations measured in the tumor microenvironment and is non-brain penetrant. EOS100850 has been extensively evaluated for safety, efficacy and oral bioavailability in numerous preclinical models.
For information on EOS100850 clinical trials, please visit www.clinicaltrials.gov.
For further information, please contact:
Michel Detheux, CEO
Amber Fennell, Catherine Day, Matthew Neal and Sukaina Virji
Consilium Strategic Communications
+44 203 709 5700
Stern Investor Relations, Inc.
+1 212 362 1200
– First patient enrolled in dose escalation portion of Phase 1/2 study of EOS-448, an antagonist anti-TIGIT antibody that enables antibody dependent cellular cytotoxicity (ADCC) – – ADCC-enabled TIGIT programs are progressing into pivotal trials – – Initial clinical data expected in 1H 2021 – Cambridge, MA and Gosselies, Belgium – February 27, 2020 – iTeos Therapeutics Inc., a privately-held clinical-stage biotechnology company developing innovative cancer immunotherapies, announced today that it has enrolled the first patient in its Phase 1/2 study with EOS884448 (EOS-448), the company’s investigational ADCC-enabled antagonist anti-TIGIT antibody drug candidate. Michel Detheux, PhD, President and Chief Executive Officer of iTeos, commented: “EOS-448 is an ADCC-enabled antagonist anti-TIGIT antibody that has been designed to maximize the therapeutic benefit of blocking TIGIT checkpoint inhibitors while engaging Fcγ receptors. The importance of TIGIT as a target for next-generation immunotherapy is becoming increasingly apparent in our field and, alongside our best-in-class adenosine A2A receptor antagonist EOS-850, iTeos now has two highly innovative immunotherapy programs in clinical development for patients suffering with advanced cancers.” Joanne Lager, M.D., Chief Medical Officer of iTeos, added, “ADCC-enabled antagonist anti-TIGIT programs are emerging as promising new immuno-oncology therapies. In preclinical studies, EOS-448 promotes anti-tumor immunity both alone and in combination with other oncology therapies. We believe it is well-positioned to provide important new therapeutic options for cancer patients. We look forward to evaluating EOS-448 in our now initiated Phase 1/2 trial and to reporting initial safety and efficacy results in the first half of 2021.” About the EOS-448 Phase 1/2 Trial This Phase 1/2 study of EOS-448 is an open-label, dose-escalation study to assess the safety, pharmacokinetic, pharmacodynamic and preliminary clinical activity of EOS-448 in participants with advanced cancers. Participants’ tumors will be sampled before treatment and during treatment, to identify and confirm biomarkers to be used in further clinical development. Following dose escalation and determination of the recommended Phase 2 dose, the study design allows for the seamless expansion of patient cohorts to evaluate the anti-tumor activity of EOS-448 in specific tumor types. The trial will be conducted at multiple clinical sites in Europe and is expected to enroll approximately 30 patients with advanced cancer in the dose escalation portion. About TIGIT and EOS-448 TIGIT is an immune checkpoint inhibitor, which interacts with CD155 expressed on antigen-presenting cells or tumor cells to down-regulate T cell and Natural Killer (NK) cell functions. EOS-448 is a novel fully human IgG1 mAb against the TIGIT receptor to treat a wide range of tumor types expressing ligands of TIGIT and/or being infiltrated by TIGIT expressing immune cells. EOS-448 was designed to encompass multiple mechanisms to activate anti-tumor immunity, not only by restoring T cell effector functions, but also by depleting immunosuppressive Tregs or inducing direct cytotoxicity of TIGIT-expressing tumor cells and creating local inflammation by engaging Fcγ receptors on effector cells. During preclinical development, EOS-448 demonstrated potent competition with TIGIT-ligand binding as well as in vitro and ex-vivo ability to restore T cell function in human samples. EOS-448 has also confirmed preferred direct cytotoxicity on regulatory T cells when tested in human cancer samples and demonstrated a clean toxicity profile. EOS-448 has also demonstrated potent anti-tumor efficacy in a humanized mouse tumor model. For further information, please contact: Michel Detheux, CEO iTeos Therapeutics SA email@example.com Amber Fennell, Paul Kidwell, Matthew Neal and Sukaina Virji Consilium Strategic Communications +44 203 709 5700 firstname.lastname@example.org Sarah McCabe and Zofia Mita Stern Investor Relations, Inc. + 1 212 362 1200 iTeos@sternir.com
– EOS-448 is being investigated in a Phase 1/2a clinical trial in advanced solid tumors and the dose escalation portion of the trial was initiated in February 2020 – – EOS-448 has shown potent antitumor activity and a favourable tolerability profile in preclinical studies – Cambridge, MA and Gosselies, Belgium – June 22, 2020. iTeos Therapeutics, a clinical-stage biopharmaceutical company pioneering the discovery and development of a new generation of highly differentiated immuno-oncology therapeutics for patients, is presenting preclinical data for its investigational FcγR-engaging anti-TIGIT antibody, EOS-448, in a virtual poster presentation at the American Association of Cancer Research II (AACR II) Virtual Annual Meeting 2020, taking place June 22-24th. EOS-448 has demonstrated strong functional activity and a clean safety profile in its preclinical studies. iTeos enrolled the first patient in the dose escalation portion of its Phase 1/2a study with EOS-448 in February, 2020. “We are excited to have started the Phase 1 portion of our first-in-human studies with our FcγR-engaging anti-TIGIT antibody, EOS-448, which has demonstrated strong antitumor activity both as single agent and in combination as well as a clean tolerability profile in preclinical studies,” said Michel Detheux, Chief Executive Officer of iTeos Therapeutics. “We believe EOS-448 has significant potential to be beneficial to cancer patients in the clinic, on the basis of its potent activity in restoring antitumor immunity in preclinical studies, supported by its multiple mechanisms of action, as well as by the latest clinical data reported for compounds of the same class.” Summary of the Data to be Presented EOS-448, a novel FcγR-engaging anti-TIGIT antibody, is shown to be highly potent and demonstrates strong anti-tumor activity and a clean safety profile in the preclinical setting. In addition to its ability to reverse immunosuppression of NK and effector T cells, EOS-448 is an IgG1 antibody, and has been able to induce potent and preferential cytotoxicity directed against Tregs as compared to CD4 and CD8 effector cells. Characterization of cell populations show that tumor-infiltrating Tregs exhibit differentially high levels of TIGIT, making these cells preferentially susceptible to ADCC. Furthermore, among tumor-infiltrating lymphocytes, or TILs, CD4 and CD8 T cells expressing high levels of TIGIT typically display an exhausted profile. In preclinical tumor models of pre-established tumors, EOS-448 demonstrated strong tumor growth delay activity as a single agent and when combined with anti-PD-1 antibody, further increased the antitumor activity and resulted in complete responses in seven out of eight mice. The observed antitumor activity correlated with an increase of IFNγ-secreting CD4 and CD8 T cells and preferential Treg depletion within the tumor microenvironment. When the same anti-TIGIT clone was built on an antibody isotype with low FcγR binding capabilities and tested in the same model, or when our anti-TIGIT EOS-448 was dosed in FcγR knockout mice, antitumor activity was lost demonstrating the key role of FcγR engagement for the therapeutic activity of anti-TIGIT therapies. When tested in NHP, EOS-448 demonstrated a dose-proportional increase in exposure with a classical human IgG1 profile. The increase in exposure correlated with increased target engagement. We observed full occupancy of the TIGIT receptor which was maintained for at least 1 week at the highest tested dose. EOS-448 was shown to have a favorable tolerability profile in these preclinical toxicology studies, and the NOAEL was the highest tested dose of 10mg/kg. The abstract and video presentation details are as follows: Title: Preparation of a clinical trial with a-TIGIT antagonist antibody EOS-448, which demonstrates potent preclinical activity and safe toxicology profile Session: Immune Checkpoints 4 Abstract #: 3720 Poster #: 3161 Authors: Thi Lien-Anh Nguyen, et al. The abstract was posted online at 12:01 a.m. EDT on Friday, May 15 on the AACR conference website. The e-poster website will be launched today, June 22, the first day of the AACR Virtual Annual Meeting II. All e-posters will be made available for browsing on this date. EOS-448 Clinical Development (ClinicalTrials.gov Trial Identifier: NCT04335253) This Phase 1/2a study of EOS-448 is an open-label, dose-escalation study to assess the safety, pharmacokinetic, pharmacodynamic and preliminary clinical activity of EOS-448 in participants with advanced cancers. Participants’ tumors will be sampled before treatment and during treatment, to identify and confirm biomarkers to be used in further clinical development. Following dose escalation and determination of the recommended Phase 2 dose, the study design allows for the seamless expansion of patient cohorts to evaluate the anti-tumor activity of EOS-448 in specific tumor types. The trial will be conducted at multiple clinical sites in Europe and is expected to enroll approximately 30 patients with advanced cancer represented in the dose escalation portion. About iTeos Therapeutics iTeos Therapeutics is a clinical-stage biopharmaceutical company pioneering the discovery and development of a new generation of highly differentiated immuno-oncology therapeutics for patients. iTeos Therapeutics leverages its deep understanding of the tumor microenvironment and immunosuppressive pathways to design novel product candidates with an aim to improve the clinical benefit of oncology therapies. The innovative pipeline includes two clinical-stage programs targeting novel, validated immuno-oncology pathways designed to build on prior learnings in the field to have differentiated pharmacological and clinical profiles. The most advanced product candidate, EOS-850, is designed as a highly selective small molecule antagonist of the adenosine A2a receptor, in the adenosine triphosphate adenosine pathway, a key driver of immunosuppression in the tumor microenvironment across a broad range of tumors. EOS-850 is being investigated in an open-label Phase 1/2a clinical trial in adult patients with advanced solid tumors and encouraging preliminary single-agent activity were observed in the dose escalation portion of the trial. The lead antibody product candidate, EOS-448, is an antagonist of TIGIT, or T-cell immunoreceptor with Ig and ITIM domains, a checkpoint that has a role in both inhibitory and stimulatory pathways in the immune system. EOS-448 was also designed to engage the Fc gamma receptor, or FcγR, to promote antibody-dependent cellular cytotoxicity, or ADCC, activity, including the elimination of tumor-infiltrating regulatory T cells, or Tregs. An open-label Phase 1/2a clinical trial of EOS-448 was recently initiated in adult patients with advanced solid tumors. In April 2020, the Company closed a $125 million Series B-2 financing from leading biotech investors including RA Capital, Boxer Capital, MPM Capital, Janus Henderson Advisors, RTW Investments, Invus, HBM Partners, Fund+, Vives II, SRIW and SFPI. iTeos Therapeutics is headquartered in Cambridge, MA with a research center in Gosselies, Belgium. For further information, please contact: Michel Detheux, CEO iTeos Therapeutics Inc email@example.com Amber Fennell, Paul Kidwell Consilium Strategic Communications +44 203 709 5700 firstname.lastname@example.org Sarah McCabe, Zofia Mita Stern Investor Relations, Inc. + 1 212 362 1200 iTeos@sternir.com
- Proceeds support advancing clinical development of next-generation cancer immunotherapies targeting A2A adenosine receptor and anti-TIGIT immune checkpoint - - Oversubscribed round co-led by new investors RA Capital Management and Boxer Capital - - New investors Janus Henderson Investors, RTW Investments and Invus also participated along with previous Series B investors including MPM Capital and HBM Partners - Cambridge, MA and Gosselies, Belgium – April 1, 2020 – iTeos Therapeutics Inc., a privately-held clinical-stage biotechnology company developing innovative cancer immunotherapies, announced today the closing of an oversubscribed Series B2 financing, which raised a total of $125 million. The Series B2 financing round was co-led by RA Capital Management and Boxer Capital, and included new investors Janus Henderson Investors, RTW Investments and Invus along with existing investors MPM Capital, HBM Partners, 6 Dimensions Capital, Curative Ventures, Fund+, VIVES Louvain Technology Fund, SRIW, and SFPI. Proceeds from the financing will support the Company's continued growth and advance the clinical development of its two lead product candidates, EOS-850, a best-in-class adenosine A2A receptor antagonist and EOS-448, an ADCC-enabled anti-TIGIT antibody. EOS-850 is currently being evaluated in a Phase 1/2 clinical trial both as a single agent and in combination in several solid tumor indications. The Company plans to initiate dosing for the combination cohorts for this trial in the second quarter of 2020. The Company also recently initiated the Phase 1 portion of a Phase 1/2 clinical study of EOS-448, currently being evaluated in patients with solid tumors and hematological malignancies. Proceeds from this financing will also support the advancement of additional first-in-class preclinical programs targeting the adenosine pathway and Tregs. "We are very pleased to have the strong support of this leading class of investors who share our excitement for the highly innovative oncology therapies we have developed at iTeos,” said Michel Detheux, PhD, President and Chief Executive Officer at iTeos. “We look forward to accelerating and expanding our clinical development efforts to identify the most promising indications and combinations for people suffering with cancer. This financing maximizes our ability to execute our development plans alone or in partnership.” "iTeos’ pipeline of best-in-class agents has the potential to usher in a new wave of immuno-oncology therapeutics and the Company is well-positioned to make a significant, positive impact in the treatment of patients with a wide variety of cancer types,” commented Derek DiRocco, Principal, RA Capital Management. “We are thrilled to collaborate with this experienced group of high-quality investors and partner with the iTeos management team as they continue to innovate and progress these exciting programs through clinical development.” “The iTeos team has done a remarkable job developing a pipeline of differentiated, potentially best-in-class cancer therapies,” said Aaron Davis, Co-Founder and Chief Executive Officer, Boxer Capital of the Tavistock Group. “We are pleased to be joining them as they continue to execute and implement their vision for transforming the cancer treatment landscape.” Derek DiRocco and Aaron Davis will join the iTeos Board as Non-Executive Directors. About iTeos Therapeutics iTeos Therapeutics is a privately-held, clinical-stage biopharmaceutical company dedicated to transforming the lives of people living with cancer by designing and developing next generation immunotherapies targeting two key resistance pathways to checkpoint therapy: the adenosine pathway and regulatory T cells (Tregs). The Company’s lead program, EOS-850, is a best-in-class adenosine A2A receptor antagonist currently in a Phase 1/2 study. Its second program, a fully human ADCC-enabling anti-TIGIT antibody (EOS-448), entered the clinic in February 2020. iTeos Therapeutics is headquartered in Cambridge, MA with a world-class research center in Gosselies, Belgium. For more information, please visit www.iteostherapeutics.com. About RA Capital Management RA Capital Management is a multi-stage investment manager dedicated to evidence-based investing in public and private healthcare and life science companies that are developing drugs, medical devices, and diagnostics. The flexibility of its strategy allows RA Capital to provide seed funding to startups and to lead private, IPO, and follow-on financings for its portfolio companies, both facilitating the crossover process and allowing management teams to drive value creation with fewer capital concerns from inception through commercialization. For more information, please visit https://www.racap.com. About Boxer Capital, LLC Boxer Capital, LLC is a private biotechnology investment fund based in San Diego, California that invents and invests in drug development across multiple therapeutic indications. Founded by the life sciences team at Tavistock Group in 2005, Boxer Capital maintains a concentrated portfolio of public and private companies. For more information, please visit www.boxercap.com. For further information, please contact: Michel Detheux, CEO iTeos Therapeutics SA email@example.com Amber Fennell, Paul Kidwell, Matthew Neal and Sukaina Virji Consilium Strategic Communications +44 203 709 5700 firstname.lastname@example.org Sarah McCabe and Zofia Mita Stern Investor Relations, Inc. + 1 212 362 1200 iTeos@sternir.com