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Verastem Oncology Announces Late Breaking and Regular Abstracts Accepted for Presentation at the AACR Annual Meeting 2026

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Preclinical research with VS-7375 in combination with PRMT5 inhibitors demonstrated strong durable tumor regressions in KRAS G12D pancreatic cancer models

In preclinical pancreatic, lung, and colorectal cancer models, VS-7375 (dual ON/OFF inhibitor) showed deeper and more sustained tumor regression compared to ON-only G12D or pan-RAS inhibitors

BOSTON--(BUSINESS WIRE)-- Verastem Oncology (Nasdaq: VSTM), a biopharmaceutical company committed to advancing new medicines for patients with RAS/MAPK pathway-driven cancers, today announced multiple abstracts have been accepted for presentation at the American Association for Cancer Research (AACR) Annual Meeting to be held April 17-22, 2026, in San Diego, CA.

“Preclinical data accepted for presentation at the AACR Special Conference in Cancer Research: RAS Oncogenesis and Therapeutics and the AACR Annual Meeting highlight our highly differentiated investigational asset VS-7375, an oral, KRAS G12D (ON/OFF) inhibitor in clinical development for pancreatic, lung, colorectal and other cancers harboring a G12D mutation, the most prevalent KRAS mutation in human cancers,” said Jonathan Pachter, Ph.D., chief scientific officer at Verastem Oncology. “While most agents targeting KRAS G12D-driven cancers bind preferentially only to the “ON” (active) or “OFF” (inactive) state of KRAS, VS-7375 engages both active and inactive states with extremely high affinity and long residence time, which corresponds to superior efficacy across pre-clinical models of G12D mutated cancers.”

Late-Breaking Abstracts

Late-breaking abstracts will be available on the AACR Annual Meeting website on April 17, 2026, 12 p.m. PT.

Session: Late-Breaking Research: Experimental and Molecular Therapeutics 2
Abstract #: LB183 / 5
Title: Strong durable tumor regressions with the KRAS G12D ON/OFF inhibitor VS-7375 in combination with PRMT5 inhibition in MTAP-deleted/KRAS G12D-mutant pancreatic cancer
Date and Time: April 20, 2026, 2 p.m. - 5 p.m. PT

Session: Late-Breaking Research: Experimental and Molecular Therapeutics 2
Abstract #: LB197 / 19
Title: VS-7375, a non-covalent dual ON/OFF KRAS G12D inhibitor, displays superior activity to ON-only KRAS G12D inhibitors in preclinical models of pancreatic cancer
Date and Time: April 20, 2026, 2 p.m. - 5 p.m. PT

Regular Abstracts

The accepted abstracts are available on the AACR Annual Meeting website: AACR Annual Meeting 2026

Session: Novel Antitumor Agents 3
Abstract & Poster Details: Abstract/Poster #7100, Poster Section #13, Poster Board #20
Title: VS-7375: An oral, selective KRAS G12D dual ON/OFF inhibitor with potent anti-tumor activity as a single agent and in combination with other agents
Date and Time: April 22, 2026, 9 a.m. - 12 p.m. PT

In the KP4 KRAS G12D pancreatic cancer model, VS-7375 (50 mg/kg twice daily), zoldonrasib (100 mg/kg once daily) and daraxonrasib (25 mg/kg once daily), produced similar initial tumor regression through day nine. By approximately day 20, however, zoldonrasib and daraxonrasib lost anti-tumor activity with tumor outgrowth, (mean tumor volume >850 mm by day 30) whereas VS-7375 maintained sustained tumor regression (mean tumor volume ~80 mm by day 30), consistent with pharmacodynamic analyses showing durable pathway inhibition only with VS-7375. VS-7375 also showed deeper tumor regression compared to these RAS ON-only inhibitors in KRAS G12D-mutated lung and colorectal xenograft models.

Session: Therapies Targeting Metastasis
Abstract & Poster Details: Abstract/Poster #2232, Poster Section #32, Poster Board #7
Title: Investigating the combined inhibition of RAF, MEK, and FAK in melanoma molecular subtypes
Date and Time: April 20, 2026, 9 a.m. - 12 p.m. PT

In mutant BRAF-driven models, the combination of the FAK inhibitor VS-4718 and the RAF/MEK clamp avutometinib, with or without the mutant BRAF inhibitor encorafenib, significantly delayed tumor onset, induced regression of established tumors and brain metastases, and prolonged overall survival.

AACR Special Conference in Cancer Research: RAS Oncogenesis and Therapeutics

At the AACR Special Conference in Cancer Research: RAS Oncogenesis and Therapeutics held March 5-8, 2026, Dr. Jonathan Pachter, delivered a plenary oral presentation titled, “Anti-tumor efficacy of the selective oral KRAS G12D dual ON/OFF inhibitor VS-7375 as a single agent and in combination with targeted agents.” This presentation can be found on the Company’s website on the Resources page.

About VS-7375, an Oral KRAS G12D (ON/OFF) Inhibitor

VS-7375 is a potential best-in-class, potent, and selective oral KRAS G12D dual ON/OFF inhibitor. VS-7375 is the lead program from the Verastem Oncology discovery and development collaboration with GenFleet Therapeutics. Verastem initiated VS-7375-101, an international Phase 1/2 clinical trial, in June of 2025 in the U.S., that is evaluating the safety and efficacy of VS-7375 in patients with advanced KRAS G12D mutant solid tumors. In July 2025, U.S. Food and Drug Administration (FDA) granted Fast Track Designation (FTD) to VS-7375 for the first-line treatment of patients with KRAS G12D-mutated locally advanced or metastatic adenocarcinoma of the pancreas (PDAC) and for the treatment of patients with KRAS G12D-mutated locally advanced or metastatic PDAC who have received at least one prior line of standard systemic therapy.

About the GenFleet Therapeutics Collaboration

The collaboration with GenFleet Therapeutics aims to advance three oncology discovery programs related to RAS/MAPK pathway-driven cancers. The collaboration provides Verastem with an exclusive option to obtain a license for each of the three compounds in the collaboration after the successful completion of pre-determined milestones in a Phase 1 trial. Verastem selected VS-7375 (also known as GFH375), an oral KRAS G12D (ON/OFF) inhibitor, as its lead program in December 2023 and the license for VS-7375 that was exercised in January 2025 is the first one from this collaboration. The licenses would give Verastem development and commercialization rights outside the GenFleet markets of mainland China, Hong Kong, Macau, and Taiwan.

About Verastem Oncology

Verastem Oncology (Nasdaq: VSTM) is a biopharmaceutical company committed to developing and commercializing new medicines to improve the lives of patients diagnosed with RAS/MAPK pathway-driven cancers. Verastem markets AVMAPKI™ FAKZYNJA™ CO-PACK in the U.S. Our pipeline is focused on novel small molecule drugs that inhibit critical signaling pathways in cancer that promote cancer cell survival and tumor growth, including RAF/MEK inhibition, FAK inhibition, and KRAS G12D inhibition. For more information, please visit www.verastem.com and follow us on LinkedIn.

Forward-Looking Statements

This press release includes forward-looking statements. These forward-looking statements generally can be identified by the use of words such as “anticipate,” “expect,” “plan,” “could,” “may,” “believe,” “estimate,” “forecast,” “goal,” “project,” and other words of similar meaning. Such forward-looking statements address various matters about, among other things, Verastem Oncology’s programs and product candidates, strategy, future plans and prospects, including statements related to the potential for and timing of commercialization of product candidates, the expected outcome and benefits of the Company’s collaboration with GenFleet Therapeutics (Shanghai), Inc., the timing of commencing and completing trials and compiling data, the expected timing of the presentation of data by the Company and the potential clinical value of various of the Company’s clinical trials. Each forward-looking statement contained in this press release is subject to risks and uncertainties that could cause actual results to differ materially from those expressed or implied by such statement. Applicable risks and uncertainties include, among others: the uncertainties inherent in research and development, such as the possibility of negative or unexpected results of clinical trials; that we may not see a return on investment on the payments we have and may continue to make pursuant to the collaboration and option agreement with GenFleet, or that GenFleet may fail to fully perform under the agreement; that we may not be successful in our continued commercialization of AVMAPKI FAKZYNJA CO-PACK; that the development and commercialization of our product candidates may take longer or cost more than planned, including as a result of conducting additional studies or our decisions regarding execution of such commercialization; that data may not be available when expected; risks associated with preliminary and interim data, which may not be representative of more mature data; risks associated with the recent changes in administration policy or actions that may create regulatory uncertainty that may adversely affect our business; risks associated with the current administration’s reductions to the FDA’s workforce and any subsequent reductions that may lead to disruptions and delays in the FDA’s review and oversight of our product candidates and impact the FDA’s ability to provide timely feedback on our development programs; that our product candidates may not receive regulatory approval, become commercially successful products, or result in new treatment options being offered to patients; and the risks identified under the heading "Risk Factors" as detailed in the Company’s Annual Report on Form 10-K for the year ended December 31, 2025, as filed with the Securities and Exchange Commission (SEC) on March 4, 2026, as well as the other information we file with the SEC, are possibly realized. We caution investors not to place considerable reliance on the forward-looking statements contained in this press release. You are encouraged to read our filings with the SEC, available at www.sec.gov, for a discussion of these and other risks and uncertainties. The forward-looking statements in this press release speak only as of the date of this press release, and we undertake no obligation to update or revise any of these statements. Our business is subject to substantial risks and uncertainties, including those referenced above. Investors, potential investors, and others should give careful consideration to these risks and uncertainties.

For Investor and Media Inquiries:

Julissa Viana

Vice President, Corporate Communications,

Investor Relations & Patient Advocacy

investors@verastem.com or

media@verastem.com

Source: Verastem Oncology

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