RLAY Relay Therapeutics Inc.

31.54
+0.29  (+1%)
Previous Close 31.25
Open 31.2
52 Week Low 25.72
52 Week High 64.37
Market Cap $3,340,169,392
Shares 105,902,644
Float 73,672,615
Enterprise Value $2,658,777,545
Volume 141,153
Av. Daily Volume 979,401
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Upcoming Catalysts

Drug Stage Catalyst Date
RLY-4008
Solid tumors
Phase 1
Phase 1
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Drug Pipeline

Drug Stage Notes
RLY-1971 and GDC-6036
Solid tumors
Phase 1
Phase 1
Phase 1b trial has been initiated.

Latest News

  1. Murcko brings over 30 years of chemistry development in biotech experience to the synthetic biology startup

    Today, Octant, a therapeutics company integrating novel high-throughput experimental technologies with computation to solve complex challenges in drug discovery, announced the appointment of Mark Murcko as Strategic Advisor and Board Member. Murcko brings over three decades of industry experience, having been at the center of many transformational biotech efforts, most recently as founding CSO and Board Member of Dewpoint Therapeutics. Murcko is working closely with the company to scale Octant to its next phase of growth and further develop its chemistry platform.

    This press release features multimedia. View the full release here: https://www.businesswire.com/news/home/20211014005238/en/

    Murcko brings over 30 years of chemistry development in biotech experience to the synthetic biology startup

    Today, Octant, a therapeutics company integrating novel high-throughput experimental technologies with computation to solve complex challenges in drug discovery, announced the appointment of Mark Murcko as Strategic Advisor and Board Member. Murcko brings over three decades of industry experience, having been at the center of many transformational biotech efforts, most recently as founding CSO and Board Member of Dewpoint Therapeutics. Murcko is working closely with the company to scale Octant to its next phase of growth and further develop its chemistry platform.

    This press release features multimedia. View the full release here: https://www.businesswire.com/news/home/20211014005238/en/

    Mark Murcko (Photo: Business Wire)

    Mark Murcko (Photo: Business Wire)

    "We have been working with Mark for over a year as a Board Member and are thrilled to share that he's now working with us day-to-day," said Sri Kosuri, CEO of Octant. "Mark's unique experience and expertise will help us scale Octant, not only in helping guide our research and development, but also as a drug discovery business. We're excited to have him working with us even more closely."

    Octant was founded with a vision to transform the treatment of complex diseases using high-throughput multiplexed biology and chemistry. Octant focuses on building molecules with complex target profiles that modulate multiple receptors, cellular pathways, and mutations. After opening its lab in 2019, Octant has built a team of top interdisciplinary talent, built a high-throughput chemistry and synthetic biology platform, expanded its computational platform, and has established multiple therapeutic programs, with multiple lead series showing efficacy in pre-clinical models.

    "It has been a pleasure serving on the Octant Board and seeing the progress the company has made in a short period of time," said Murcko. "I share Sri and Ramsey's vision and am excited to work with the founders in this expanded new role while we scale Octant from a startup to a drug company."

    Murcko is a Senior Lecturer at M.I.T. and co-founder and Board Member at Relay Therapeutics (NASDAQ:RLAY) and Board member and founding CSO at Dewpoint Therapeutics. Until November 2011, Mark was chief technology officer and chair of the scientific advisory board of Vertex Pharmaceuticals. Mark has contributed to nine approved medicines for glaucoma, HIV/AIDS, Hepatitis-C, and Cystic Fibrosis, as well as numerous additional first-in-class drug candidates for cancer, influenza, and inflammation/immunology.

    Mark also serves on Octant's SAB, where he joins other SAB members:

    • Charles Zuker - Professor of Biochemistry and Molecular Biophysics, and of Neuroscience, Columbia University Medical Center; Investigator, Howard Hughes Medical Institute; Cofounder, Aurora Biosciences, Kallyope, & Senomyx.
    • Debbie Marks - Associate Professor of Systems Biology, Harvard University; Assistant Professor, Harvard Medical School; Associate Member, Broad Institute.
    • Hosea Nelson - Professor of Chemistry, California Institute of Technology.
    • Vijay Pande – General Partner, Andreessen Horowitz; Former Henry Dreyfus Professor of Chemistry and Professor of Structural Biology and of Computer Science at Stanford University; Cofounder, Globavir BioSciences & Folding@home.

    About Octant Bio

    Octant is a therapeutics company building drugs to navigate the complexity of human diseases. Octant engineers drugs with novel mechanisms of actions guided by massive datasets in engineered human cells that unlock insights between genomes, biochemical function, and disease phenotypes. The Octant platform uses synthetic biology, high throughput multiplexed assays, synthetic chemistry, and computation to engineer and interrogate drugs, proteins, and signaling pathways at unprecedented scales. For more information visit www.octant.bio.

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  2. CAMBRIDGE, Mass., Oct. 12, 2021 (GLOBE NEWSWIRE) -- Relay Therapeutics, Inc. (NASDAQ:RLAY), a clinical-stage precision medicine company transforming the drug discovery process by combining leading-edge computational and experimental technologies, announced today the pricing of an underwritten public offering of 13,207,547 shares of its common stock at a public offering price of $26.50 per share. Relay Therapeutics also granted the underwriters a 30-day option to purchase up to an additional 1,981,132 shares of its common stock. The gross proceeds from the offering, before deducting underwriting discounts and commissions and offering expenses, are expected to be approximately $350 million, excluding any exercise of the underwriters' option…

    CAMBRIDGE, Mass., Oct. 12, 2021 (GLOBE NEWSWIRE) -- Relay Therapeutics, Inc. (NASDAQ:RLAY), a clinical-stage precision medicine company transforming the drug discovery process by combining leading-edge computational and experimental technologies, announced today the pricing of an underwritten public offering of 13,207,547 shares of its common stock at a public offering price of $26.50 per share. Relay Therapeutics also granted the underwriters a 30-day option to purchase up to an additional 1,981,132 shares of its common stock. The gross proceeds from the offering, before deducting underwriting discounts and commissions and offering expenses, are expected to be approximately $350 million, excluding any exercise of the underwriters' option to purchase additional shares. All of the shares in the offering are to be sold by Relay Therapeutics.

    Goldman Sachs & Co. LLC, J.P. Morgan, Cowen and Guggenheim Securities are acting as joint book-running managers for the offering. The offering is expected to close on or about October 15, 2021, subject to customary closing conditions.

    The shares of common stock are being offered by Relay Therapeutics pursuant to an effective shelf registration statement that was previously filed with the U.S. Securities and Exchange Commission (SEC). A preliminary prospectus supplement and accompanying prospectus relating to and describing the terms of the offering was filed with the SEC on October 12, 2021. The final prospectus supplement and accompanying prospectus relating to the offering will be filed with the SEC and may be obtained, when available, from Goldman Sachs & Co. LLC, by mail at 200 West Street, New York, NY 10282, Attention: Prospectus Department, by telephone at (866) 471-2526, or by email at prospectus-ny@ny.email.gs.com; J.P. Morgan Securities LLC, c/o Broadridge Financial Solutions, 1155 Long Island Avenue, Edgewood, NY 11717, by telephone at 866-803-9204 or by email at prospectus-eq_fi@jpmorganchase.com; Cowen and Company, LLC, Attn: Prospectus Department, c/o Broadridge Financial Solutions, 1155 Long Island Avenue, Edgewood, NY 11717, Attn: Prospectus Department, by email at PostSaleManualRequests@broadridge.com, or by telephone at (833) 297-2926; Guggenheim Securities, LLC, Attn: Equity Syndicate Department, 330 Madison Avenue, 8th Floor, New York, NY 10017, by telephone at (212) 518-9544, or by email at GSEquityProspectusDelivery@guggenheimpartners.com; or by accessing the SEC's website at www.sec.gov.

    This press release shall not constitute an offer to sell or the solicitation of an offer to buy these securities, nor shall there be any sale of these securities in any state or jurisdiction in which such offer, solicitation or sale would be unlawful prior to registration or qualification under the securities laws of any such state or jurisdiction.

    About Relay Therapeutics

    Relay Therapeutics (NASDAQ:RLAY) is a clinical-stage precision medicines company transforming the drug discovery process by combining leading-edge computational and experimental technologies with the goal of bringing life-changing therapies to patients. Relay Therapeutics is the first of a new breed of biotech created at the intersection of disparate technologies. Relay Therapeutics' Dynamo™ platform integrates an array of leading-edge computational and experimental approaches designed to drug protein targets that have previously been intractable. Relay Therapeutics' initial focus is on enhancing small molecule therapeutic discovery in targeted oncology and genetic disease.

    Cautionary Note Regarding Forward-Looking Statements

    This press release contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995, as amended, including, without limitation, statements regarding the closing of Relay's anticipated public offering. The words "may," "will," "could," "would," "should," "expect," "plan," "anticipate," "intend," "believe," "estimate," "predict," "project," "potential," "continue," "target" and similar expressions are intended to identify forward-looking statements, although not all forward-looking statements contain these identifying words.

    Any forward-looking statements in this press release, such as the intended offering terms, are based on management's current expectations and beliefs and are subject to a number of risks, uncertainties and important factors that may cause actual events or results to differ materially from those expressed or implied by any forward-looking statements contained in this press release, including, without limitation, uncertainties related to market conditions and the completion of the public offering on the anticipated terms or at all. These and other risks and uncertainties are described in greater detail in the section entitled "Risk Factors" in Relay's most recent annual report on Form 10-K and quarterly report on Form 10-Q filed with the SEC, as well as discussions of potential risks, uncertainties, and other important factors in Relay's other filings with the SEC, including those contained or incorporated by reference in the preliminary prospectus supplement and accompanying prospectus related to the public offering filed with the SEC. Any forward-looking statements contained in this press release represent Relay's views only as of the date hereof and should not be relied upon as representing its views as of any subsequent date. Relay explicitly disclaims any obligation to update any forward-looking statements, except as required by law.

    Contact:

    Pete Rahmer

    Senior Vice President, Corporate Affairs and Investor Relations

    617-322-0715

    prahmer@relaytx.com

    Media:

    Dan Budwick

    1AB

    973-271-6085

    dan@1abmedia.com



    Primary Logo

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  3. CAMBRIDGE, Mass., Oct. 11, 2021 (GLOBE NEWSWIRE) -- Relay Therapeutics, Inc. (NASDAQ:RLAY), a clinical-stage precision medicine company transforming the drug discovery process by combining leading-edge computational and experimental technologies, announced today that it has commenced an underwritten public offering of $350 million of shares of its common stock. Relay Therapeutics also intends to grant the underwriters a 30-day option to purchase up to an additional fifteen percent (15%) of the shares of common stock offered in the public offering. All of the shares in the proposed offering are to be sold by Relay Therapeutics.

    Goldman Sachs & Co. LLC, J.P. Morgan, Cowen and Guggenheim Securities are acting as joint book-running managers for…

    CAMBRIDGE, Mass., Oct. 11, 2021 (GLOBE NEWSWIRE) -- Relay Therapeutics, Inc. (NASDAQ:RLAY), a clinical-stage precision medicine company transforming the drug discovery process by combining leading-edge computational and experimental technologies, announced today that it has commenced an underwritten public offering of $350 million of shares of its common stock. Relay Therapeutics also intends to grant the underwriters a 30-day option to purchase up to an additional fifteen percent (15%) of the shares of common stock offered in the public offering. All of the shares in the proposed offering are to be sold by Relay Therapeutics.

    Goldman Sachs & Co. LLC, J.P. Morgan, Cowen and Guggenheim Securities are acting as joint book-running managers for the proposed offering. The offering is subject to market and other conditions, and there can be no assurance as to whether or when the offering may be completed, or as to the actual size or terms of the offering.

    The shares of common stock are being offered by Relay Therapeutics pursuant to an effective shelf registration statement that was previously filed with the U.S. Securities and Exchange Commission (SEC). A preliminary prospectus supplement and accompanying prospectus relating to and describing the terms of the offering will be filed with the SEC and may be obtained, when available, from: Goldman Sachs & Co. LLC, by mail at 200 West Street, New York, NY 10282, Attention: Prospectus Department, by telephone at (866) 471-2526, or by email at prospectus-ny@ny.email.gs.com; J.P. Morgan Securities LLC, c/o Broadridge Financial Solutions, 1155 Long Island Avenue, Edgewood, NY 11717, by telephone at 866-803-9204 or by email at prospectus-eq_fi@jpmorganchase.com; Cowen and Company, LLC, Attn: Prospectus Department, c/o Broadridge Financial Solutions, 1155 Long Island Avenue, Edgewood, NY 11717, Attn: Prospectus Department, by email at PostSaleManualRequests@broadridge.com, or by telephone at (833) 297-2926; Guggenheim Securities, LLC, Attn: Equity Syndicate Department, 330 Madison Avenue, 8th Floor, New York, NY 10017, by telephone at (212) 518-9544, or by email at GSEquityProspectusDelivery@guggenheimpartners.com; or by accessing the SEC's website at www.sec.gov.

    This press release shall not constitute an offer to sell or the solicitation of an offer to buy these securities, nor shall there be any sale of these securities in any state or jurisdiction in which such offer, solicitation or sale would be unlawful prior to registration or qualification under the securities laws of any such state or jurisdiction.

    About Relay Therapeutics

    Relay Therapeutics (NASDAQ:RLAY) is a clinical-stage precision medicines company transforming the drug discovery process by combining leading-edge computational and experimental technologies with the goal of bringing life-changing therapies to patients. Relay Therapeutics is the first of a new breed of biotech created at the intersection of disparate technologies. Relay Therapeutics' Dynamo™ platform integrates an array of leading-edge computational and experimental approaches designed to drug protein targets that have previously been intractable. Relay Therapeutics' initial focus is on enhancing small molecule therapeutic discovery in targeted oncology and genetic disease.

    Cautionary Note Regarding Forward-Looking Statements

    This press release contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995, as amended, including, without limitation, statements regarding Relay's anticipated public offering. The words "may," "will," "could," "would," "should," "expect," "plan," "anticipate," "intend," "believe," "estimate," "predict," "project," "potential," "continue," "target" and similar expressions are intended to identify forward-looking statements, although not all forward-looking statements contain these identifying words.

    Any forward-looking statements in this press release, such as the intended offering terms, are based on management's current expectations and beliefs and are subject to a number of risks, uncertainties and important factors that may cause actual events or results to differ materially from those expressed or implied by any forward-looking statements contained in this press release, including, without limitation, uncertainties related to market conditions and the completion of the public offering on the anticipated terms or at all. These and other risks and uncertainties are described in greater detail in the section entitled "Risk Factors" in Relay's most recent annual report on Form 10-K and quarterly report on Form 10-Q filed with the SEC, as well as discussions of potential risks, uncertainties, and other important factors in Relay's other filings with the SEC, including those contained or incorporated by reference in the preliminary prospectus supplement and accompanying prospectus related to the proposed public offering to be filed with the SEC. Any forward-looking statements contained in this press release represent Relay's views only as of the date hereof and should not be relied upon as representing its views as of any subsequent date. Relay explicitly disclaims any obligation to update any forward-looking statements, except as required by law.

    Contact:

    Pete Rahmer

    Senior Vice President, Corporate Affairs and Investor Relations

    617-322-0715

    prahmer@relaytx.com

    Media:

    Dan Budwick

    1AB

    973-271-6085

    dan@1abmedia.com



    Primary Logo

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  4. Interim data suggest that RLY-4008 is a highly selective FGFR2 inhibitor that has not shown to be limited by off-target toxicities of hyperphosphatemia (FGFR1) and diarrhea (FGFR4)

    RLY-4008 demonstrated tumor shrinkage in all six pan-FGFR treatment-naïve FGFR2 fusion positive cholangiocarcinoma patients with three achieving confirmed partial responses

    Interim data support potential clinical benefits of optimized inhibition of FGFR2 regardless of alteration (fusions, mutations, and amplifications), line of treatment or tumor type

    Relay Therapeutics anticipates selecting a once daily recommended Phase 2 dose and initiating expansion cohorts prior to the end of 2021

    Relay Therapeutics to host a conference call today at 12:30 pm E.T.

    CAMBRIDGE…

    Interim data suggest that RLY-4008 is a highly selective FGFR2 inhibitor that has not shown to be limited by off-target toxicities of hyperphosphatemia (FGFR1) and diarrhea (FGFR4)

    RLY-4008 demonstrated tumor shrinkage in all six pan-FGFR treatment-naïve FGFR2 fusion positive cholangiocarcinoma patients with three achieving confirmed partial responses

    Interim data support potential clinical benefits of optimized inhibition of FGFR2 regardless of alteration (fusions, mutations, and amplifications), line of treatment or tumor type

    Relay Therapeutics anticipates selecting a once daily recommended Phase 2 dose and initiating expansion cohorts prior to the end of 2021

    Relay Therapeutics to host a conference call today at 12:30 pm E.T.

    CAMBRIDGE, Mass., Oct. 08, 2021 (GLOBE NEWSWIRE) -- Relay Therapeutics, Inc. (NASDAQ:RLAY), a clinical-stage precision medicine company transforming the drug discovery process by combining leading-edge computational and experimental technologies, today announced interim clinical data for RLY-4008, a highly selective irreversible and oral small molecule inhibitor of FGFR2, in a first-in-human trial in patients with FGFR2-altered cholangiocarcinoma and multiple other solid tumors. The data are being presented today at the virtual AACR-NCI-EORTC Molecular Targets Conference and suggest that RLY-4008 is the first investigational therapy designed to selectively bind to FGFR2 to avoid off‐isoform toxicities for the treatment of patients with FGFR2-altered tumors.

    As will be presented at the conference, study investigators reported robust inhibition of FGFR2 in the first 49 subjects that was not shown to be limited by off-target toxicities, including hyperphosphatemia and diarrhea, in the interim clinical data. The initial toxicity data suggest that certain dose levels administered can achieve >85% continuous inhibition of FGFR2. At those levels, acute toxicities that would limit dose intensity have generally not been observed to date. The interim clinical data included results from FGFR2-altered solid tumors, with approximately 80% of all patients treated achieving reductions in tumor size at the cut-off date of September 9, 2021. In pan-FGFRi treatment-naïve cholangiocarcinoma patients, RLY-4008 demonstrated tumor shrinkage in all six pan-FGFR treatment-naïve FGFR2 fusion positive cholangiocarcinoma patients, with three achieving confirmed partial responses. Three of these six patients remain on study and a fourth patient went on to surgery with curative intent. Relay Therapeutics anticipates selecting a once daily recommended Phase 2 dose and initiating expansion cohorts prior to the end of 2021.

    "RLY-4008 clinical data exemplifies the power of the Relay Therapeutics Dynamo™ platform and approach to discovering innovative medicines," said Don Bergstrom, M.D., Ph.D., executive vice president of R&D at Relay Therapeutics. "Not only has the platform succeeded in creating a selective and purpose-built investigational therapy, but the initial clinical evidence of RLY-4008 has also shown the potential to positively impact the course of disease for patients with FGFR2 altered cancers. We continue to evaluate the once daily dose schedule to determine which dose to take forward into expansion cohorts before year-end. Using the same approach, we are building a deep portfolio of precision medicine programs that have the potential to impact patients with the hard-to-treat diseases. Thank you to the patients, investigators and clinical trial teams who have put their faith in our investigational therapy."

    RLY-4008 First-in-Human Trial Interim Results

    RLY-4008 is currently being evaluated in an ongoing dose-escalation first-in-human trial in patients with FGFR2 altered tumors regardless of prior FGFRi treatment. The study is designed to determine the maximum tolerated dose and recommended Phase 2 dosing as well as assess initial safety and tolerability. Approximately 125 patients are planned to enroll in the study, which is being conducted in two parts, a dose escalation (part 1) and a dose expansion (part 2). As of the cut-off date of September 9, 2021, 48 of the 49 patients enrolled had a primary FGFR2-alteration, of which a majority were FGFR2-fusion cholangiocarcinoma. Most patients had high disease burden with multiple prior treatments including pan-FGFR inhibitors, and several had FGFR2 resistance mutations detected by ctDNA at baseline. Patients were treated at nine different once daily (QD) or twice daily (BID) dose levels, ranging from 20 mg QD to 70 mg QD and 20 mg BID to 100 mg BID. As of the cut-off date, duration of treatment ranged from 4 to 45 weeks.

    Initial Safety Analysis

    RLY-4008 has generally been well tolerated in the 49 patients treated as of September 9, 2021. With regard to dosing, the QD schedule has been prioritized due to its preferable tolerability (only one dose limiting toxicity (DLT) observed across all dose levels) and high target coverage (lowest dose, 20 mg, exceeding 85% receptor occupancy). Within the BID dosing schedule there were five DLTs observed, and receptor occupancy ranged from 90% to 98% across the BID doses.

    Across all QD doses only 16% of patients, all Grade 1 or 2, experienced hyperphosphatemia, a toxicity that has been shown to limit dose intensity for pan-FGFR inhibitors in other studies. These data indicate that RLY-4008 had little or no FGFR1 inhibition at the examined dose levels. Additionally, little or no diarrhea was observed with RLY-4008 treatment suggesting minimal or no FGFR4 inhibition in treated patients to date across dose levels. Together, the interim data suggest that RLY-4008 is a highly selective FGFR2 inhibitor in humans.

    Most treatment emergent adverse events were low-grade adverse events and manageable. There have been no Grade 4 or 5 adverse events. Given that retinal toxicity has been observed with FGFRi treatment, the trial is designed to assess retinopathy and retinal pigment epithelial dystrophy (RPED) adverse events, which have been observed in seven patients (14%), three of which occurred in the QD regimen. All seven of these events were Grade 1-2, which were self-limiting or resolved upon treatment interruption.

    To date, a maximum tolerated dose has not been reached and QD dose exploration is ongoing to determine the recommended Phase 2 dose (RP2D).

    Initial Efficacy Analysis

    The interim clinical data indicate that RLY-4008 has the potential to provide tumor reduction across a number of FGFR2 alterations and lines of treatment. Key interim data include:

    • Promising early activity in FGFRi naïve cholangiocarcinoma FGFR2 fusion patients, with confirmed RECISTv1.1 partial responses observed in 3/6 patients with deep tumor regressions (-56% to -83%), and 3/6 patients continuing on treatment and a fourth who went on to surgery with curative intent.
    • Radiographic tumor shrinkage and complete clearance of circulating tumor DNA (ctDNA) in 70% of patients with acquired resistance mutations (N=10), including molecular brake (N550) and gatekeeper (V565) mutations, suggesting the potential for RLY-4008 to treat or prevent on-target acquired resistance.
    • Early signs of activity observed outside of FGFR2-fusion positive cholangiocarcinoma, including tumor reduction in 6 out of 8 evaluable patients with activating mutations (1 confirmed PR, 1 unconfirmed PR, and 4 SD (based on RECISTv1.1 criteria)) and 3 out of 3 patients with amplifications (all SD).
    • Approximately 80% of all patients treated achieved radiographic tumor regressions; this was observed across all dose levels, tumor types and FGFR2 alterations, and in patients with prior FGFR inhibitor treatment.

    Consistent with the preclinical profile, these early clinical data support Relay Therapeutics' belief that RLY-4008 has broad therapeutic potential across FGFR2 alterations and tumor types.

    Relay Therapeutics anticipates selecting an RP2D and initiating expansion cohorts before the end of 2021. Relay Therapeutics also expects to give a data update from this ongoing first-in-human study in 2022.

    Conference Call Information

    Relay Therapeutics will host a live webcast and conference call today beginning at 12:30 pm E.T. to discuss the results. To access the live call, please dial (833) 540-1168 (domestic) or (929) 517-0359 (international) and refer to conference ID 4657916. A webcast of the conference call will be available under "News and Presentations" in the Media & Investors section of Relay Therapeutics' website at http://ir.relaytx.com. The archived webcast will be available on Relay Therapeutics' website approximately two hours after the conference call and will be available for 30 days following the call.

    The data presentation from the AACR-NCI-EORTC Molecular Targets Conference is also available on the Relay Therapeutics website under "Publications/Presentations" near the bottom of https://relaytx.com/pipeline/.

    About RLY-4008

    RLY-4008 is a potent, selective and oral small molecule inhibitor of FGFR2, a receptor tyrosine kinase that is frequently altered in certain cancers. FGFR2 is one of four members of the FGFR family, a set of closely related proteins with highly similar protein sequences and properties. Preclinically, RLY-4008 demonstrated FGFR2-dependent killing in cancer cell lines and induced regression in in vivo models, while minimal inhibition of other targets was observed, including other members of the FGFR family. In addition, RLY-4008 demonstrates strong activity against known clinical on-target resistance mutations in cellular and in vivo preclinical models. RLY-4008 is currently being evaluated in a first-in-human clinical trial designed to evaluate the safety and tolerability of RLY-4008 in patients with advanced or metastatic FGFR2-altered solid tumors. To learn more about the first-in-human clinical trial of RLY-4008, please visit here.

    About Relay Therapeutics

    Relay Therapeutics (NASDAQ:RLAY) is a clinical-stage precision medicines company transforming the drug discovery process by combining leading-edge computational and experimental technologies with the goal of bringing life-changing therapies to patients. Relay Therapeutics is the first of a new breed of biotech created at the intersection of disparate technologies. Relay Therapeutics' Dynamo™ platform integrates an array of leading-edge computational and experimental approaches designed to drug protein targets that have previously been intractable. Relay Therapeutics' initial focus is on enhancing small molecule therapeutic discovery in targeted oncology and genetic disease. For more information, please visit www.relaytx.com or follow us on Twitter.

    Cautionary Note Regarding Forward-Looking Statements

    This press release contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995, as amended, including, without limitation, implied and express statements regarding: Relay Therapeutics' strategy, business plans and focus; the progress and timing of updates on the clinical development of the programs across Relay Therapeutics' portfolio, including the timing of selecting a recommended Phase 2 dose, initiating expansion cohorts of its first-in-human clinical trial of RLY-4008 and a data update of RLY-4008; and potential therapeutic effects and clinical benefits of RLY-4008, including its potential efficacy and tolerability, and whether preliminary results from the first-in-human clinical trial of RLY-4008 will be predictive of the final results of the trial or any future clinical trials of RLY-4008. The words "may," "might," "will," "could," "would," "should," "expect," "plan," "anticipate," "intend," "believe," "expect," "estimate," "seek," "predict," "future," "project," "potential," "continue," "target" and similar words or expressions are intended to identify forward-looking statements, although not all forward-looking statements contain these identifying words.

    Any forward-looking statements in this press release are based on management's current expectations and beliefs and are subject to a number of risks, uncertainties and important factors that may cause actual events or results to differ materially from those expressed or implied by any forward-looking statements contained in this press release, including, without limitation, risks associated with: the impact of COVID-19 on countries or regions in which Relay Therapeutics has operations or does business, as well as on the timing and anticipated results of its clinical trials, strategy and future operations; the delay of any current or planned clinical trials or the development of Relay Therapeutics' drug candidates; the risk that the results of its clinical trials may not be predictive of future results in connection with future clinical trials; Relay Therapeutics' ability to successfully demonstrate the safety and efficacy of its drug candidates; the timing and outcome of Relay Therapeutics' planned interactions with regulatory authorities; and obtaining, maintaining and protecting its intellectual property. These and other risks and uncertainties are described in greater detail in the section entitled "Risk Factors" in Relay Therapeutics' Quarterly Report on Form 10-Q for the quarter ended June 30, 2021, as well as any subsequent filings with the Securities and Exchange Commission. In addition, any forward-looking statements represent Relay Therapeutics' views only as of today and should not be relied upon as representing its views as of any subsequent date. Relay Therapeutics explicitly disclaims any obligation to update any forward-looking statements. No representations or warranties (expressed or implied) are made about the accuracy of any such forward-looking statements.

    Contact:

    Pete Rahmer

    Senior Vice President, Corporate Affairs and Investor Relations

    617-322-0715

    prahmer@relaytx.com

    Media:

    Dan Budwick

    1AB

    973-271-6085

    dan@1abmedia.com



    Primary Logo

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  5. RLY-2608 preferentially binds mutant PI3Kα at a novel allosteric site discovered by the Dynamo™ platform

    Preclinically, achieved tumor regressions in vivo with significantly reduced impact on glucose metabolism compared to active site inhibitors

    RLY-2608's pan-mutant inhibition has the potential to address over 100,000 patients per year in the U.S.

    CAMBRIDGE, Mass., Oct. 07, 2021 (GLOBE NEWSWIRE) -- Relay Therapeutics, Inc. (NASDAQ:RLAY), a clinical-stage precision medicine company transforming the drug discovery process by combining leading-edge computational and experimental technologies, today shared preclinical data at the virtual AACR-NCI-EORTC Molecular Targets Conference for RLY-2608, the first allosteric, pan-mutant (H1047X, E542X…

    RLY-2608 preferentially binds mutant PI3Kα at a novel allosteric site discovered by the Dynamo™ platform

    Preclinically, achieved tumor regressions in vivo with significantly reduced impact on glucose metabolism compared to active site inhibitors

    RLY-2608's pan-mutant inhibition has the potential to address over 100,000 patients per year in the U.S.

    CAMBRIDGE, Mass., Oct. 07, 2021 (GLOBE NEWSWIRE) -- Relay Therapeutics, Inc. (NASDAQ:RLAY), a clinical-stage precision medicine company transforming the drug discovery process by combining leading-edge computational and experimental technologies, today shared preclinical data at the virtual AACR-NCI-EORTC Molecular Targets Conference for RLY-2608, the first allosteric, pan-mutant (H1047X, E542X and E545X) and isoform-selective PI3Kα inhibitor.

    The data presented at the conference show that in preclinical models, RLY-2608 preferentially binds mutant PI3Kα at a novel allosteric site discovered by the Dynamo™ platform. Scientists at Relay Therapeutics solved the full-length structure of PI3Kα, performed long time-scale molecular dynamic simulations to elucidate differences in motion between wild-type (WT) and mutant PI3Kα, and leveraged these insights to enable the design of RLY-2608. In biochemical and cellular assays, RLY-2608 inhibited the three major classes of PI3Kα oncogenic mutations (H1047X, E542X and E545X) while sparing WT PI3Kα. The data further suggest that RLY-2608 is also highly selective against other PI3K family members and exquisitely selective across the kinome. The data suggest that projected clinically relevant doses of RLY-2608 achieved tumor regression in PIK3CA mutant in vivo xenograft models representing H1047R and E545K mutations with significantly reduced impact on glucose metabolism compared to non-mutant selective active site inhibitors. In higher species, dosing of RLY-2608 resulted in exposures exceeding 90% inhibition of mutant PI3Kα in cells without resulting in elevated glucose levels or histopathological changes associated with dysregulation of glucose metabolism that are seen with non-mutant selective inhibitors.

    These results support advancement of RLY-2608 into clinical development as a differentiated mechanism of mutant PI3Kα inhibition with the first-in-human study anticipated to start in the first half of 2022. RLY-2608 is the lead program of multiple preclinical efforts at Relay Therapeutics to discover and develop mutant selective inhibitors of PI3Kα.

    RLY-2608 has the potential to address over 100,000 patients per year in the United States, one of the largest patient populations for a precision oncology medicine. Selectivity for all three mutation hot spots (H1047X, E542X and E545X) has the potential to effectively double the addressable patient population compared to selectivity for only H1047X.

    "The data shared today provide another proof point that we're developing what we believe to be the first known pan-mutant selective allosteric inhibitor of PI3Kα," said Don Bergstrom, M.D., Ph.D., executive vice president of R&D at Relay Therapeutics. "We believe RLY-2608 has the potential to address a significant unmet medical need in a large population and have validated our approach for developing mutant selective inhibitors of PI3Kα. RLY-2608 is only the start of our PI3Kα efforts, and by leveraging our Dynamo™ platform, we plan to build a franchise around this target for the long-term."

    Conference Call Information

    Relay Therapeutics will host a live webcast and conference call tomorrow, October 8, beginning at 12:30 pm E.T. to discuss the results of this presentation and the RLY-4008 presentation tomorrow. To access the live call, please dial (833) 540-1168 (domestic) or (929) 517-0359 (international) and refer to conference ID 4657916. A webcast of the conference call will be available under "News and Presentations" in the Media & Investors section of Relay Therapeutics' website at http://ir.relaytx.com. The archived webcast will be available on Relay Therapeutics' website approximately two hours after the conference call and will be available for 30 days following the call.

    The data presentation from the AACR-NCI-EORTC Molecular Targets Conference is also available on the Relay Therapeutics website under "Publications/Presentations" near the bottom of https://relaytx.com/pipeline/.

    About RLY-2608

    RLY-2608 is the lead program of multiple preclinical efforts to discover and develop mutant selective inhibitors of PI3Kα. PI3Kα is the most frequently mutated kinase in all cancers, with oncogenic mutations detected in about 13% of patients with solid tumors. Traditionally, the development of PI3Kα inhibitors has focused on the active, or orthosteric, site. The therapeutic index of orthosteric inhibitors is limited by the lack of clinically meaningful selectivity for mutant versus WT PI3Kα and off-isoform activity. Toxicity related to inhibition of WT PI3Kα and other PI3K isoforms results in sub-optimal inhibition of mutant PI3Kα with reductions in dose intensity and frequent discontinuation. The Dynamo™ platform enabled the discovery of RLY-2608, the first known allosteric, pan-mutant (H1047X, E542X and E545X), and isoform-selective PI3Kα inhibitor designed to overcome these limitations. Relay Therapeutics solved the full-length cryo-EM structure of PI3Kα, performed computational long time-scale molecular dynamic simulations to elucidate conformational differences between WT and mutant PI3Kα, and leveraged these insights to support the design of RLY-2608. RLY-2608 is on path to initiate a first-in-human clinical trial in the first half of 2022, subject to submission of an investigational new drug application and acceptance by the FDA.

    About Relay Therapeutics

    Relay Therapeutics (NASDAQ:RLAY) is a clinical-stage precision medicines company transforming the drug discovery process by combining leading-edge computational and experimental technologies with the goal of bringing life-changing therapies to patients. Relay Therapeutics is the first of a new breed of biotech created at the intersection of disparate technologies. Relay Therapeutics' Dynamo™ platform integrates an array of leading-edge computational and experimental approaches designed to drug protein targets that have previously been intractable. Relay Therapeutics' initial focus is on enhancing small molecule therapeutic discovery in targeted oncology and genetic disease. For more information, please visit www.relaytx.com or follow us on Twitter.

    Cautionary Note Regarding Forward-Looking Statements

    This press release contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995, as amended, including, without limitation, implied and express statements regarding: Relay Therapeutics' strategy, business plans and focus; the progress and timing of updates on the clinical development of the programs across Relay Therapeutics' portfolio, including the timing of initiation of a first-in-human clinical trial of RLY-2608; potential therapeutic effects and anticipated clinical benefits of RLY-2608; Relay Therapeutics' plans to build a franchise around PI3Kα; the potential target patient population of RLY-2608; and whether preclinical results of RLY-2608 will be predictive of future clinical trials of RLY-2608. The words "may," "might," "will," "could," "would," "should," "expect," "plan," "anticipate," "intend," "believe," "expect," "estimate," "seek," "predict," "future," "project," "potential," "continue," "target" and similar words or expressions are intended to identify forward-looking statements, although not all forward-looking statements contain these identifying words.

    Any forward-looking statements in this press release are based on management's current expectations and beliefs and are subject to a number of risks, uncertainties and important factors that may cause actual events or results to differ materially from those expressed or implied by any forward-looking statements contained in this press release, including, without limitation, risks associated with: the impact of COVID-19 on countries or regions in which Relay Therapeutics has operations or does business, as well as on the timing and anticipated results of its clinical trials, strategy and future operations; the delay of any current or planned clinical trials or the development of Relay Therapeutics' drug candidates; the risk that the results of its clinical trials may not be predictive of future results in connection with future clinical trials; Relay Therapeutics' ability to successfully demonstrate the safety and efficacy of its drug candidates; the timing and outcome of Relay Therapeutics' planned interactions with regulatory authorities; and obtaining, maintaining and protecting its intellectual property. These and other risks and uncertainties are described in greater detail in the section entitled "Risk Factors" in Relay Therapeutics' Quarterly Report on Form 10-Q for the quarter ended June 30, 2021, as well as any subsequent filings with the Securities and Exchange Commission. In addition, any forward-looking statements represent Relay Therapeutics' views only as of today and should not be relied upon as representing its views as of any subsequent date. Relay Therapeutics explicitly disclaims any obligation to update any forward-looking statements. No representations or warranties (expressed or implied) are made about the accuracy of any such forward-looking statements.

    Contact:

    Pete Rahmer

    Senior Vice President, Corporate Affairs and Investor Relations

    617-322-0715

    prahmer@relaytx.com

    Media:

    Dan Budwick

    1AB

    973-271-6085

    dan@1abmedia.com



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