Projected human oral bioavailability ~60% and half-life ~16h Target Inhibition and Efficacy RLY-2608 – First Mutant Selective Inhibitor to Enter the Clinic Limited potency against WT PI3Kα and other PI3K isoforms 30 Favorable Favorable Tolerability | --- | --- | |-----------------------------------------------------------|-------------------------------------------------------------------| | | | | Favorable Favorable Efficacy | | | Robust tumor regression at tolerable doses in mouse model | HCC1954 | | 2500 ...

ESMO Disclosure Call Materials September 2022 Confidential | © 2022 Relay Therapeutics 1 Disclaimer This presentation contains forward-looking statements and information about our current and future prospects and our operations and financial results, which are based on currently available information. All statements other than statements of historical facts contained in this presentation, including statements regarding our strategy, future financial condition, future operations, projected costs, prospects, ...

Pipeline and Programs - Relay Therapeutics' pipeline includes RLY-4008 (selective FGFR2 inhibitor) with encouraging efficacy in FGFR2-fusion+ cholangiocarcinoma (CCA) without prior FGFRi [59] - RLY-2608 (PI3KαPAN inhibitor) is in development, with initial clinical data expected in the first half of 2023 [53, 137] - The company is also developing a selective CDK2 inhibitor, with clinical start expected in Q4 2023 or Q1 2024 [53, 157] - An ERα degrader program is underway, with a development candidate nomination expected in 2023 [53, 166] RLY-4008 (Selective FGFR2 Inhibitor) - A pivotal study is aligned with the FDA for FGFR2-fusion+ cholangiocarcinoma (CCA) without prior FGFRi, with a target enrollment of 100 patients [59, 98] - Preliminary data as of April 19, 2022, showed promising radiographic tumor regression in FGFRi-naïve cholangiocarcinoma QD patients [60, 92] - The company has enrolled 115 patients across 39 sites and 11 countries over 19 months for RLY-4008 [101] Financial Status - As of the end of Q2 2022, Relay Therapeutics had $838 million in cash, cash equivalents, and investments [53] - The company's current cash position is expected to fund the current operating plan into 2025 [53, 180]

[PART I. FINANCIAL INFORMATION](index=7&type=section&id=PART%20I.%20FINANCIAL%20INFORMATION) [Item 1. Financial Statements (Unaudited)](index=7&type=section&id=Item%201.%20Financial%20Statements%20(Unaudited)) Net loss decreased to $138.8 million in H1 2022 due to the absence of a 2021 in-process R&D expense [Condensed Consolidated Balance Sheets](index=7&type=section&id=Condensed%20Consolidated%20Balance%20Sheets) Total assets decreased to $889.4 million as of June 30, 2022, primarily due to a reduction in cash and cash equivalents Condensed Consolidated Balance Sheet Highlights (in thousands) | Account | June 30, 2022 | December 31, 2021 | | :--- | :--- | :--- | | Cash and cash equivalents | $107,736 | $280,119 | | Investments | $730,254 | $677,954 | | **Total Assets** | **$889,421** | **$1,008,443** | | Total current liabilities | $43,902 | $24,321 | | **Total Liabilities** | **$109,784** | **$110,635** | | **Total Stockholders' Equity** | **$779,637** | **$897,808** | [Condensed Consolidated Statements of Operations and Comprehensive Loss](index=8&type=section&id=Condensed%20Consolidated%20Statements%20of%20Operations%20and%20Comprehensive%20Loss) Net loss significantly decreased in Q2 2022 to $76.8 million, primarily due to the non-recurrence of 2021 one-time expenses Statement of Operations Summary (in thousands, except per share data) | Metric | Q2 2022 | Q2 2021 | H1 2022 | H1 2021 | | :--- | :--- | :--- | :--- | :--- | | Total revenue | $365 | $844 | $784 | $1,796 | | Research and development expenses | $60,511 | $45,147 | $112,178 | $75,769 | | In-process R&D expenses | $0 | $123,000 | $0 | $123,000 | | General and administrative expenses | $17,465 | $14,422 | $33,533 | $27,156 | | **Net loss** | **$(76,788)** | **$(193,399)** | **$(138,834)** | **$(235,582)** | | Net loss per share, basic and diluted | $(0.71) | $(2.10) | $(1.28) | $(2.58) | [Condensed Consolidated Statements of Cash Flows](index=10&type=section&id=Condensed%20Consolidated%20Statements%20of%20Cash%20Flows) Net cash used in operating activities was $106.3 million in H1 2022, a significant shift from cash provided in 2021 Cash Flow Summary (in thousands) | Activity | Six Months Ended June 30, 2022 | Six Months Ended June 30, 2021 | | :--- | :--- | :--- | | Net cash (used in) provided by operating activities | $(106,266) | $18,500 | | Net cash used in investing activities | $(68,996) | $(207,553) | | Net cash provided by financing activities | $2,879 | $3,176 | | **Net decrease in cash, cash equivalents and restricted cash** | **$(172,383)** | **$(185,877)** | - The significant decrease in cash from operating activities in H1 2022 compared to H1 2021 is largely due to a **$74.8 million** positive change in accounts receivable in 2021 that did not recur, related to payments from the Genentech collaboration[31](index=31&type=chunk) [Item 2. Management's Discussion and Analysis of Financial Condition and Results of Operations](index=17&type=section&id=Item%202.%20Management's%20Discussion%20and%20Analysis%20of%20Financial%20Condition%20and%20Results%20of%20Operations) Management discusses the clinical pipeline, increased R&D expenses, and cash reserves sufficient to fund operations into at least 2025 - The company is advancing its pipeline, with RLY-4008 moving towards a potential accelerated approval path in CCA, RLY-2608 in a first-in-human trial, and RLY-1971 being developed in collaboration with Genentech[77](index=77&type=chunk) R&D and G&A Expense Comparison (in millions) | Expense Category | H1 2022 | H1 2021 | Change | | :--- | :--- | :--- | :--- | | Research & Development | $112.2 | $75.8 | +$36.4 | | General & Administrative | $33.5 | $27.2 | +$6.3 | - The company believes its cash, cash equivalents, and investments of **$838.0 million** as of June 30, 2022, will be sufficient to fund operating expenses and capital expenditure requirements into at least 2025[90](index=90&type=chunk)[134](index=134&type=chunk) - The decrease in net loss for H1 2022 compared to H1 2021 was primarily due to the non-recurrence of a **$123.0 million** in-process R&D expense and an **$11.9 million** loss on consolidation of a VIE, both related to the acquisition of ZebiAI in Q2 2021[115](index=115&type=chunk)[118](index=118&type=chunk)[119](index=119&type=chunk) [Item 3. Quantitative and Qualitative Disclosures About Market Risk](index=27&type=section&id=Item%203.%20Quantitative%20and%20Qualitative%20Disclosures%20About%20Market%20Risk) The company faces minimal market risk from interest rate changes on investments and negligible foreign currency exchange risk due to U.S.-centric operations - The primary market risk is interest rate sensitivity on the company's investment portfolio; a hypothetical 100 basis point adverse movement is not expected to materially impact results[144](index=144&type=chunk) - Foreign currency exchange risk is not considered material as operations are mainly in the U.S. and expenses are denominated in U.S. dollars[146](index=146&type=chunk) [Item 4. Controls and Procedures](index=27&type=section&id=Item%204.%20Controls%20and%20Procedures) Management concluded that disclosure controls and procedures were effective as of June 30, 2022, with no material changes to internal controls - The CEO and CFO concluded that as of June 30, 2022, the company's disclosure controls and procedures were effective[149](index=149&type=chunk) - No material changes to the internal control over financial reporting occurred during the fiscal quarter ended June 30, 2022[150](index=150&type=chunk) [PART II. OTHER INFORMATION](index=29&type=section&id=PART%20II.%20OTHER%20INFORMATION) [Item 1. Legal Proceedings](index=29&type=section&id=Item%201.%20Legal%20Proceedings) As of June 30, 2022, the company was not party to any legal proceedings expected to have a material adverse effect on its business - The company is not currently involved in any litigation or legal proceedings expected to have a material adverse effect on its business[153](index=153&type=chunk) [Item 1A. Risk Factors](index=29&type=section&id=Item%201A.%20Risk%20Factors) The company outlines extensive risks including clinical development, third-party reliance, funding needs, competition, and intellectual property protection [Risks Related to Product Candidates](index=29&type=section&id=Risks%20Related%20to%20Our%20Product%20Candidates) Risks include the company's lack of completed clinical trials, unpredictability of early-stage data, and intense competition in product development - The company has never successfully completed any clinical trials and may be unable to do so for its product candidates (RLY-1971, RLY-4008, RLY-2608)[155](index=155&type=chunk) - Positive data from preclinical or early clinical studies are not necessarily predictive of the results of later clinical trials[167](index=167&type=chunk) - The company faces substantial competition, which may result in others developing or commercializing products more successfully[194](index=194&type=chunk) [Risks Related to Reliance on Third Parties](index=37&type=section&id=Risks%20Related%20to%20Our%20Reliance%20on%20Third%20Parties) The company heavily relies on third parties for its Dynamo™ platform, clinical trials (CROs), and manufacturing (CMOs), posing significant operational risks - The company's collaboration with D. E. Shaw Research, utilizing the proprietary Anton 2 supercomputer, is critical to its Dynamo platform, and termination could materially harm the business[204](index=204&type=chunk)[207](index=207&type=chunk) - The company relies on third parties (CROs) to conduct all its clinical trials and is dependent on them for execution and regulatory compliance[212](index=212&type=chunk) - The company contracts with third-party manufacturers (CMOs) for all its product candidates and does not own any manufacturing facilities, creating risks in supply, quality, and cost[222](index=222&type=chunk) [Risks Related to Financial Position and Capital](index=43&type=section&id=Risks%20Related%20to%20Our%20Financial%20Position%20and%20Ability%20to%20Raise%20Additional%20Capital) The company has a limited operating history, significant accumulated losses, and will require substantial additional funding to continue development programs - The company has a limited operating history, has incurred significant operating losses since inception, and anticipates continued losses, with an accumulated deficit of **$906.9 million** as of June 30, 2022[242](index=242&type=chunk) - The company will need to raise substantial additional funding, and failure to do so may force delays or elimination of product development programs[250](index=250&type=chunk) [Risks Related to Intellectual Property](index=48&type=section&id=Risks%20Related%20to%20Our%20Intellectual%20Property) Success depends on patent protection and trade secrets, facing uncertainties in biotech IP, complex collaboration terms, and potential infringement claims - The company's ability to protect its proprietary technology and obtain patent protection is crucial, but the patent position of biotech companies is highly uncertain and involves complex legal questions[265](index=265&type=chunk)[271](index=271&type=chunk) - Much of the company's R&D is performed under the DESRES Agreement, which involves joint ownership of work product and complex IP rights that could lead to disputes[268](index=268&type=chunk)[270](index=270&type=chunk) - The company may face legal proceedings from third parties alleging infringement of their IP rights, which could be uncertain, expensive, and have a material adverse effect on the business[286](index=286&type=chunk) [Item 2. Unregistered Sales of Equity Securities and Use of Proceeds](index=73&type=section&id=Item%202.%20Unregistered%20Sales%20of%20Equity%20Securities%20and%20Use%20of%20Proceeds) There were no unregistered sales of equity securities during the reporting period - None[394](index=394&type=chunk) [Item 5. Other Information](index=73&type=section&id=Item%205.%20Other%20Information) The board of directors decided to hold an annual advisory vote on executive compensation based on stockholder preference - The company will hold an annual advisory 'say-on-pay' vote for executive compensation, based on stockholder preference[395](index=395&type=chunk) [Item 6. Exhibits](index=74&type=section&id=Item%206.%20Exhibits) This section lists the exhibits filed with the Form 10-Q, including corporate governance documents and required certifications - The exhibits filed include corporate governance documents and required certifications under the Sarbanes-Oxley Act[397](index=397&type=chunk)

Company Overview - Relay Therapeutics is a patient-driven, growth-oriented biotech company focused on validated targets and therapeutic areas [7, 8, 9] - The company utilizes the Dynamo™ Platform, integrating experimentation and computation to improve drug discovery efficiency [15, 14] - Relay Therapeutics has 3 clinical assets: RLY-2608 (PI3KαPAN), RLY-4008 (FGFR2), and RLY-1971 (SHP2), with more programs in the pipeline [33, 10] RLY-4008 (FGFR2 Inhibitor) - RLY-4008 is a highly selective and irreversible FGFR2 inhibitor [80] - Early clinical data shows tumor regressions across several tumor and alteration types, with 3 out of 6 FGFR-inhibitor naïve cholangiocarcinoma patients exhibiting confirmed partial responses (PRs) [58] - In FGFR inhibitor-naïve FGFR2-fusion+ cholangiocarcinoma, 3 out of 6 patients exhibited a confirmed PR [92] RLY-2608 (PI3KαPAN Inhibitor) - The PI3Kα opportunity represents a large market in precision oncology, with approximately 156,000 US patients with solid tumors [108] - RLY-2608 has shown mutant and isoform biochemical selectivity [120] - Preclinical studies show in vivo tumor regressions across both H1047R and E545K mutation hotspots [123] Pipeline and Future Expectations - Initial clinical data update for RLY-2608 is expected in the first half of 2023 [51] - A GDC-6036 (KRAS G12C) combo trial with RLY-1971 (SHP2) was initiated in July 2021 [51] - Relay Therapeutics reported $898 million in cash, cash equivalents, and investments as of the end of Q1 2022 [51]

UNITED STATES SECURITIES AND EXCHANGE COMMISSION WASHINGTON, DC 20549 FORM 10-Q (Mark One) ☒ QUARTERLY REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES EXCHANGE ACT OF 1934 For the quarterly period ended March 31, 2022 OR ☐ TRANSITION REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES EXCHANGE ACT OF 1934 For the transition period from to Commission File Number: 001-39385 RELAY THERAPEUTICS, INC. (Exact Name of Registrant as Specified in its Charter) (State or other jurisdiction of incorporati ...

UNITED STATES SECURITIES AND EXCHANGE COMMISSION Washington, D.C. 20549 FORM 10-K (Mark One) ☒ ANNUAL REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES EXCHANGE ACT OF 1934 For the fiscal year ended December 31, 2021 OR ☐ TRANSITION REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES EXCHANGE ACT OF 1934 FOR THE TRANSITION PERIOD FROM TO Commission File Number: 001-39385 RELAY THERAPEUTICS, INC. (Exact name of Registrant as specified in its Charter) Delaware 47-3923475 (State or other jurisdicti ...

Company Presentation February 2022 Confidential | © 2022 Relay Therapeutics 1 Disclaimer This presentation contains forward-looking statements and information about our current and future prospects and our operations and financial results, which are based on currently available information. All statements other than statements of historical facts contained in this presentation, including statements regarding our strategy, future financial condition, future operations, projected costs, prospects, plans, obje ...

January 2022 RELAY® THERAPE U TI C S 40th Annual J.P. Morgan Healthcare Conference Company Presentation Confidential | © 2022 Relay Therapeutics 1 Disclaimer This presentation contains forward-looking statements and information about our current and future prospects and our operations and financial results, which are based on currently available information. All statements other than statements of historical facts contained in this presentation, including statements regarding our strategy, future financial ...

UNITED STATES SECURITIES AND EXCHANGE COMMISSION WASHINGTON, DC 20549 FORM 10-Q (Mark One) ☒ QUARTERLY REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES EXCHANGE ACT OF 1934 For the quarterly period ended September 30, 2021 OR ☐ TRANSITION REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES EXCHANGE ACT OF 1934 For the transition period from to Commission File Number: 001-39385 RELAY THERAPEUTICS, INC. (Exact Name of Registrant as Specified in its Charter) (State or other jurisdiction of incorpo ...