Pan-RAS molecular glue ERAS-0015 and pan-KRAS inhibitor ERAS-4001 are potent, oral inhibitors with potential best-in-class profiles in RASm solid tumors
Pipeline prioritization and workforce restructuring sharpens focus on programs targeting the highest unmet needs and with highest probability of success
Priced concurrent $160 million equity offering
Erasca to host conference call and webcast Friday, May 17, 2024 at 8:30 am ET
SAN DIEGO, May 16, 2024 (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 it has entered into exclusive license agreements for two preclinical RAS programs—a potential best-in-class pan-RAS molecular glue (ERAS-0015) and a potential first-in-class pan-KRAS inhibitor (ERAS-4001)—and provided a pipeline update. ERAS-0015 and ERAS-4001 are highly potent, orally bioavailable molecules with complementary RAS inhibitory mechanisms that have the potential to address unmet needs in nearly 2.7 million patients who are diagnosed annually globally with RAS-mutant (RASm) tumors, of which over 2.2 million patients are diagnosed with KRAS-mutant (KRASm) tumors.
As separately announced, Erasca has priced an equity offering of $160 million with a high quality group of new and existing healthcare-focused investors.
"We're thrilled to add ERAS-0015 and ERAS-4001 to our pipeline. Successful in-licensing of this RAS-targeting franchise with such broad potential to address unmet needs in patients helps advance our mission to erase cancer and is consistent with our focus on eradicating RAS/MAPK pathway-driven tumors," said Jonathan E. Lim, M.D., Erasca's chairman, CEO, and co-founder. "Based on the compelling preclinical data generated to date, we believe both molecules have the potential to demonstrate best-in-class (BIC) profiles within their respective categories of RAS inhibition. Over the long term, we have a unique opportunity to combine these two BIC molecules with distinct and complementary RAS inhibitory mechanisms to 'clamp' RAS and shut down MAPK signaling for the benefit of patients with these common RAS mutations."
Dr. Lim continued, "With the in-licensing of these RAS-targeting programs, we have made the difficult but necessary decision to deprioritize or externalize resourcing of our pipeline (ERAS-007, ERAS-801, and ERAS-4). This change has unfortunately impacted certain team members. We believe that further focusing our resources will allow us to advance the programs with the highest probability of success and largest potential for patient impact. This is undoubtedly a challenging time for our highly talented employees, particularly those affected by these changes. On behalf of Erasca, I would like to extend our heartfelt gratitude to all of our employees for their tremendous contributions and dedication to Erasca."
In-Licensed Programs: ERAS-0015 and ERAS-4001
In controlled preclinical studies using another pan-RAS molecular glue currently in clinical development, ERAS-0015 demonstrated 5- to 10-fold greater in vitro and in vivo potency and favorable absorption, distribution, metabolism, and excretion (ADME) properties and pharmacokinetic (PK) properties in multiple animal species. Under the terms of the ERAS-0015 license agreement, in exchange for an exclusive license to develop and commercialize ERAS-0015 in the Erasca territory (worldwide, excluding mainland China, Hong Kong, and Macau), Erasca will pay the licensor, Joyo Pharmatech Co., Ltd. (Joyo), a one-time upfront cash payment of $12.5 million, up to $176.5 million in cash upon the achievement of certain development, regulatory, and commercialization milestones, and a low- to mid-single digit percentage royalty. At Erasca's election, prior to the dosing of the first patient in a Phase 2 clinical trial by either Erasca or Joyo or the filing of a New Drug Application (NDA) (or foreign equivalent) by either Erasca or Joyo, Erasca can convert its territory to worldwide by making a one-time payment.
ERAS-4001 is a potent and selective inhibitor of KRAS that has the potential to provide an improved therapeutic window relative to RAS inhibitors and prevent KRAS wildtype-mediated resistance relative to mutant-selective approaches. Under the terms of the ERAS-4001 license agreement, in exchange for an exclusive worldwide license to develop and commercialize ERAS-4001, Erasca will pay the licensor, Medshine Discovery, Inc. (Medshine), a one-time upfront cash payment of $10.0 million, up to $160.0 million in cash upon the achievement of certain development, regulatory, and commercialization milestones, and a low-single digit percentage royalty.
Concurrent Pipeline Prioritization and Workforce Restructuring
In consideration of these in-licensing transactions, Erasca will implement the following pipeline and personnel changes to focus Erasca's resources on opportunities targeting the highest unmet needs and having the highest probability of success for patients:
HERKULES-3: ERAS-007 + EC in EC-naïve patients with BRAFm CRC: Deprioritized as clinical efficacy data (data to be presented at ASCO 2024) do not support continued evaluation
THUNDERBBOLT-1: ERAS-801 in recurrent glioblastoma: Due to the desire to focus internal resources on developing naporafenib and the RAS-targeting franchise, Erasca is exploring further advancement of ERAS-801 via select investigator-sponsored trial(s)
ERAS-4 pan-KRAS program: In conjunction with the in-licensing of ERAS-0015 and ERAS-4001, Erasca will discontinue its internal pan-KRAS program; provided that certain of the existing ERAS-4 molecules are included in the Medshine agreement as potential backup compounds for ERAS-4001
Workforce restructuring: Erasca will reduce its workforce by approximately 18%, primarily affecting employees working in drug discovery functions and on deprioritized programs. Erasca is deeply committed to easing this transition for its impacted colleagues and will offer comprehensive severance packages and career transition services
Key Upcoming Milestones
Erasca is providing the following guidance with respect to anticipated key milestones and clinical trial readouts:
Naporafenib (pan-RAF inhibitor)
SEACRAFT-1: Phase 1b trial for naporafenib plus trametinib in patients with RAS Q61X solid tumors
Initial Phase 1b combination signal-seeking efficacy data in relevant tumor types expected in Q4 2024
SEACRAFT-2: Randomized pivotal Phase 3 trial for naporafenib plus trametinib in patients with NRAS-mutant (NRASm) melanoma
Phase 3 pivotal trial initiation expected in Q2 2024
Phase 3 Stage 1 randomized dose optimization data expected in 2025
ERAS-0015 (pan-RAS molecular glue)
AURORAS-1: Phase 1 trial for ERAS-0015 in patients with RASm solid tumors
IND filing expected in H1 2025
Initial Phase 1 monotherapy data in relevant tumor types expected in 2026
ERAS-4001 (pan-KRAS inhibitor)
BOREALIS-1: Phase 1 trial for ERAS-4001 in patients with KRASm solid tumors
IND filing expected in Q1 2025
Initial Phase 1 monotherapy data in relevant tumor types expected in 2026
Conference Call and Webcast Information
Erasca will hold a conference call and webcast Friday, May 17, 2024 at 8:30 am ET. The webcast link for the conference call is The dial-in number is 1-877-451-6152 (U.S./Canada) or 1-201-389-0879 (international). The conference ID for all callers is 13746639. The live webcast and replay may be accessed by visiting Erasca's website at Erasca.com/events.