Erasca Announces Presentation of Preclinical Data on ERAS-801, a CNS-Penetrant EGFR Inhibitor with Broad Activity against Oncogenic EGFR Alterations, at AACR Conference on Brain Cancer
Erasca, Inc. (Nasdaq: ERAS) presented promising preclinical data for ERAS-801, a new EGFR inhibitor with significantly enhanced CNS penetration, at the AACR Conference. ERAS-801 shows a CNS penetration rate four times higher than existing EGFR inhibitors, demonstrating potent efficacy in over 90% of tested EGFR-mutant glioblastoma models. The company plans to submit an IND for refractory glioblastoma in Q1 2022. These advancements highlight ERAS-801's potential to improve outcomes for patients suffering from this aggressive cancer type.
- ERAS-801 exhibits CNS penetrance four times higher than approved EGFR inhibitors.
- Demonstrated efficacy in over 90% of glioblastoma patient-derived models.
- IND filing for refractory glioblastoma planned for Q1 2022.
- None.
ERAS-801's CNS penetration: four times higher than approved EGFR inhibitors
Comprehensive inhibition against oncogenic EGFR vIII and wildtype alterations
Improved outcomes in over
IND submission in refractory glioblastoma planned for Q1 2022
SAN DIEGO, Oct. 25, 2021 (GLOBE NEWSWIRE) -- Erasca, Inc. (Nasdaq: ERAS), a clinical-stage precision oncology company singularly focused on discovering, developing, and commercializing therapies for patients with RAS/MAPK pathway-driven cancers, today announced the presentation of preclinical data for ERAS-801, a small molecule epidermal growth factor receptor (EGFR) inhibitor specifically designed to have high central nervous system (CNS) penetration for the treatment of glioblastoma multiforme (GBM), at the American Association for Cancer Research (AACR) Special Virtual Conference on Brain Cancer.
“While mutations in EGFR are common oncogenic drivers in glioblastoma, approved EGFR inhibitors lack both sufficient CNS penetration for primary brain tumors and clinical activity against oncogenic EGFR alterations that are prevalent in GBM,” said Jonathan E. Lim, M.D., Erasca’s chairman, CEO, and co-founder. “ERAS-801 is an EGFR inhibitor with four times the CNS penetrance of approved EGFR inhibitors, resulting in robust CNS enrichment while limiting systemic exposure. In more than 30 GBM patient-derived preclinical models, ERAS-801 demonstrated potent activity across mutant and wildtype oncogenic EGFR alterations, and we are highly encouraged by the extensive therapeutic potential of ERAS-801 for patients with this aggressive malignancy.”
David A. Nathanson, Ph.D., Associate Professor of Molecular and Medical Pharmacology at the University of California, Los Angeles (UCLA), added, “About
About ERAS-801
ERAS-801 is a highly potent, selective, and reversible small molecule EGFR inhibitor with significantly enhanced CNS penetration. ERAS-801 has a 3.7:1 brain-to-plasma ratio and a Kp,uu (partition coefficient that measures unbound drug concentration) that is up to four times higher than approved EGFR inhibitors, indicating a higher concentration of unbound drug in the brain compared to the blood. Utilizing fluorodeoxyglucose-positron emission tomography (FDG-PET), a pharmacodynamic marker of metabolically active tumors, the Nathanson lab evaluated inhibition of tumor metabolism in over 30 patient-derived preclinical glioblastoma models following treatment with different FDA-approved EGFR inhibitors. At clinically relevant exposures, ERAS-801 demonstrated a survival benefit in over
About Erasca
At Erasca, our name is our mission: To erase cancer. We are a clinical-stage precision oncology company singularly focused on discovering, developing, and commercializing therapies for patients with RAS/MAPK pathway-driven cancers. Our company was co-founded by leading pioneers in precision oncology and RAS targeting to create novel therapies and combination regimens designed to comprehensively shut down the RAS/MAPK pathway for the treatment of cancer. We have assembled what we believe to be the deepest RAS/MAPK pathway-focused pipeline in the industry. We believe our team’s capabilities and experience, further guided by our scientific advisory board which includes the world’s leading experts in the RAS/MAPK pathway, uniquely position us to achieve our bold mission of erasing cancer.
Cautionary Note Regarding Forward-Looking Statements
Erasca cautions you that statements contained in this press release regarding matters that are not historical facts are forward-looking statements. The forward-looking statements are based on our current beliefs and expectations and include, but are not limited to: our expectations regarding the potential therapeutic benefits of our product candidates and the potential patient populations for our product candidates, including ERAS-801; and the planned advancement of our development pipeline, including the development plan and planned IND filing date for ERAS-801. Actual results may differ from those set forth in this press release due to the risks and uncertainties inherent in our business, including, without limitation: our approach to the discovery and development of product candidates based on our singular focus on shutting down the RAS/MAPK pathway, a novel and unproven approach; delays in our preclinical and clinical development programs; our dependence on third parties to conduct manufacturing, research, and preclinical and clinical testing; unexpected adverse side effects or inadequate efficacy of our product candidates that may limit their development, regulatory approval, and/or commercialization, or may result in recalls or product liability claims; unfavorable results from preclinical studies or clinical trials; results from preclinical studies or early clinical trials not necessarily being predictive of future results; regulatory developments in the United States and foreign countries; our ability to obtain and maintain intellectual property protection for our product candidates and maintain our rights under intellectual property licenses; our ability to fund our operating plans with our current cash, cash equivalents, and investments; our ability to maintain undisrupted business operations due to the COVID-19 pandemic; and other risks described in our prior filings with the Securities and Exchange Commission (SEC), including under the heading “Risk Factors” in our most recent quarterly report on Form 10-Q and any subsequent filings with the SEC. You are cautioned not to place undue reliance on these forward-looking statements, which speak only as of the date hereof, and we undertake no obligation to update such statements to reflect events that occur or circumstances that exist after the date hereof. All forward-looking statements are qualified in their entirety by this cautionary statement, which is made under the safe harbor provisions of the Private Securities Litigation Reform Act of 1995.
Contact:
Joyce Allaire
LifeSci Advisors, LLC
jallaire@lifesciadvisors.com
FAQ
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