IDEAYA Biosciences Announces First-Patient-In for Phase 1/2 Combination Trial of IDE397, A Potential First-in-Class MAT2A Inhibitor, and Trodelvy® in MTAP-Deletion Non-Small Cell Lung Cancer

Rhea-AI Summary

IDEAYA Biosciences (NASDAQ:IDYA) has announced the enrollment of its first non-small cell lung cancer (NSCLC) patient in the Phase 1/2 combination trial of IDE397 and Trodelvy®. The trial, conducted in collaboration with Gilead, evaluates this novel combination in patients with MTAP-deletion solid tumors.

Following encouraging preliminary data in bladder cancer, the trial has expanded into NSCLC, where MTAP-deletion occurs in up to 20% of cases. IDE397 is being developed as a potential first-in-class MAT2A inhibitor, while Trodelvy® is an established Trop2-directed antibody-drug conjugate. Under the collaboration agreement, IDEAYA maintains study sponsorship while Gilead provides Trodelvy supply, with both companies retaining commercial rights to their respective compounds.

Positive

• Expansion of clinical trial into NSCLC represents significant market opportunity with MTAP-deletion present in up to 20% of cases
• Encouraging preliminary data from bladder cancer cohort supports expansion strategy
• Strategic collaboration with Gilead enhances development capabilities while maintaining commercial rights

Negative

• IDE397 and its combination with Trodelvy remain unapproved by regulatory agencies
• Safety and efficacy of the combination therapy has not yet been established
• Targeting a competitive space with no currently approved targeted therapies for MTAP-deletion

SOUTH SAN FRANCISCO, Calif., Sept. 4, 2025 /PRNewswire/ -- IDEAYA Biosciences, Inc. (Nasdaq: IDYA), a leading precision medicine oncology company, today announced they have enrolled their first patient with non-small cell lung cancer (NSCLC) in the ongoing Phase 1/2 combination trial of IDE397, a potential first-in-class, small molecule adenosyltransferase 2a (MAT2a) inhibitor, and Trodelvy^® (sacituzumab govitecan-hziy), a Trop2-directed antibody-drug conjugate (ADC), in patients with methylthioadenosine phosphorylase (MTAP)-deletion solid tumors. IDEAYA is conducting the trial pursuant to a clinical study collaboration and supply agreement with Gilead, where the initial focus was in MTAP-deletion urothelial cancer (UC). In April 2025, the companies announced expansion of the combination trial into MTAP-deletion NSCLC.

"We are encouraged by the preliminary expansion data from our Phase 1/2 combination trial with IDE397 and Trodelvy in MTAP-deleted bladder cancer and excited to have dosed the first patient in the non-small cell lung cancer cohort. This marks an important step in our broader clinical strategy to evaluate the combination across multiple solid tumors with MTAP-deletion," said Darrin Beaupre, Chief Medical Officer, IDEAYA Biosciences. 

"MTAP-deletion is found in up to 20% of non-small cell lung cancer and remains an area with no approved targeted therapies. We're pleased to expand our collaboration with IDEAYA and explore the potential of this novel combination in a patient population with limited treatment options," said Bilal Piperdi, MD, Vice President, Clinical Development Oncology at Gilead Sciences. 

Pursuant to the clinical study collaboration and supply agreement, IDEAYA and Gilead retain the commercial rights to their respective compounds, including with respect to use as a monotherapy or combination agent. IDEAYA is the study sponsor, and Gilead will provide the supply of Trodelvy to IDEAYA.

Trodelvy is currently approved in more than 50 countries for second-line or later metastatic triple-negative breast cancer (TNBC) patients and in more than 40 countries for certain patients with pre-treated HR+/HER2- metastatic breast cancer.

The use of Trodelvy in MTAP-deletion NSCLC and UC is investigational, and the safety and efficacy of this use have not been established. IDE397 monotherapy or in combination with Trodelvy has not been approved by any regulatory agency and the efficacy and safety of this combination has not been established.

Trodelvy and Gilead are trademarks of Gilead Sciences, Inc., or its related companies.

About IDEAYA Biosciences
IDEAYA is a precision medicine oncology company committed to the discovery, development, and commercialization of transformative therapies for cancer. Our approach integrates expertise in small-molecule drug discovery, structural biology and bioinformatics with robust internal capabilities in identifying and validating translational biomarkers to develop tailored, potentially first-in-class targeted therapies aligned to the genetic drivers of disease. We have built a deep pipeline of product candidates focused on synthetic lethality and antibody-drug conjugates, or ADCs, for molecularly defined solid tumor indications. Our mission is to bring forth the next wave of precision oncology therapies that are more selective, more effective, and deeply personalized with the goal of altering the course of disease and improving clinical outcomes for patients with cancer.

Forward-Looking Statements
This press release contains forward-looking statements, including, but not limited to, statements related to the potential therapeutic benefits of IDE397and Trodelvy combination. Such forward-looking statements involve substantial risks and uncertainties that could cause IDEAYA's preclinical and clinical development programs, future results, performance or achievements to differ significantly from those expressed or implied by the forward-looking statements. Such risks and uncertainties include, among others, the uncertainties inherent in the drug development process, including IDEAYA's programs' early stage of development, the process of designing and conducting preclinical and clinical trials, the regulatory approval processes, the timing of regulatory filings, the challenges associated with manufacturing drug products, IDEAYA's ability to successfully establish, protect and defend its intellectual property, and other matters that could affect the sufficiency of existing cash to fund operations. IDEAYA undertakes no obligation to update or revise any forward-looking statements. For a further description of the risks and uncertainties that could cause actual results to differ from those expressed in these forward-looking statements, as well as risks relating to the business of IDEAYA in general, see IDEAYA's Annual Report on Form 10-K dated February 18, 2025 and any current and periodic reports filed with the U.S. Securities and Exchange Commission.

Investor and Media Contact
IDEAYA Biosciences
Joshua Bleharski, Ph.D.
Chief Financial Officer
investor@ideayabio.com

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SOURCE IDEAYA Biosciences, Inc.

FAQ

What is the significance of IDEAYA's Phase 1/2 trial expansion for IDE397 and Trodelvy in NSCLC?

The expansion represents an important opportunity to address MTAP-deletion NSCLC, which affects up to 20% of cases and currently has no approved targeted therapies.

How does the collaboration between IDEAYA Biosciences and Gilead work for the IDE397 trial?

IDEAYA is the study sponsor and maintains commercial rights to IDE397, while Gilead provides Trodelvy supply and retains its commercial rights. Both companies collaborate on the clinical development.

What is the current regulatory status of IDE397 and its combination with Trodelvy?

The combination therapy is still investigational and has not been approved by any regulatory agency. Safety and efficacy have not yet been established.

What are the current approved indications for Trodelvy?

Trodelvy is approved in over 50 countries for second-line metastatic triple-negative breast cancer and in over 40 countries for certain pre-treated HR+/HER2- metastatic breast cancer patients.

What type of cancer patients are being targeted in IDEAYA's IDE397 combination trial?

The trial targets patients with MTAP-deletion solid tumors, specifically focusing on non-small cell lung cancer (NSCLC) and urothelial cancer (UC) patients.