PART I [Financial Statements (Unaudited)](index=5&type=section&id=Item%201.%20Financial%20Statements%20(Unaudited)) The unaudited financial statements show increased assets and equity from public offerings, continued net losses, and strong financing inflows supporting liquidity [Condensed Balance Sheets](index=5&type=section&id=Condensed%20Balance%20Sheets) The balance sheet reflects significant growth in total assets and stockholders' equity, primarily from capital raises, while liabilities decreased Condensed Balance Sheet Highlights (in thousands) | Account | Sep 30, 2021 (in thousands) | Dec 31, 2020 (in thousands) | Change (in thousands) | | :--- | :--- | :--- | :--- | | **Assets** | | | | | Cash and cash equivalents | $108,428 | $72,037 | +$36,391 | | Marketable securities (Short & Long-term) | $277,340 | $211,548 | +$65,792 | | **Total Assets** | **$399,444** | **$298,269** | **+$101,175** | | **Liabilities** | | | | | Contract liability (Current & Long-term) | $62,183 | $83,773 | -$21,590 | | **Total Liabilities** | **$81,815** | **$99,995** | **-$18,180** | | **Stockholders' Equity** | | | | | **Total Stockholders' Equity** | **$317,629** | **$198,274** | **+$119,355** | - The significant increase in stockholders' equity was primarily driven by capital raised from a follow-on public offering and an at-the-market (ATM) offering program during the first nine months of 2021[23](index=23&type=chunk) [Condensed Statements of Operations and Comprehensive Loss](index=6&type=section&id=Condensed%20Statements%20of%20Operations%20and%20Comprehensive%20Loss) The statement of operations shows increased collaboration revenue but also higher R&D and G&A expenses, leading to an increased net loss Statement of Operations Highlights (in thousands, except per share data) | Metric | Three Months Ended Sep 30, 2021 (in thousands) | Three Months Ended Sep 30, 2020 (in thousands) | Nine Months Ended Sep 30, 2021 (in thousands) | Nine Months Ended Sep 30, 2020 (in thousands) | | :--- | :--- | :--- | :--- | :--- | | Collaboration revenue | $8,976 | $8,967 | $24,979 | $8,967 | | Research and development | $15,503 | $10,025 | $42,048 | $27,647 | | General and administrative | $5,186 | $3,938 | $14,830 | $11,384 | | **Loss from operations** | **($11,713)** | **($4,996)** | **($31,899)** | **($30,064)** | | **Net loss** | **($11,582)** | **($4,926)** | **($31,550)** | **($29,360)** | | **Net loss per share** | **($0.31)** | **($0.17)** | **($0.92)** | **($1.26)** | - The year-over-year increase in R&D and G&A expenses reflects the company's growth and the advancement of its clinical programs[17](index=17&type=chunk) - The significant increase in collaboration revenue for the nine-month period is due to the timing of the GSK agreement, which became effective in July 2020[17](index=17&type=chunk)[93](index=93&type=chunk) [Condensed Statements of Cash Flows](index=9&type=section&id=Condensed%20Statements%20of%20Cash%20Flows) Cash flows highlight substantial financing inflows from equity offerings, offsetting cash used in operating and investing activities Cash Flow Summary for the Nine Months Ended September 30 (in thousands) | Cash Flow Activity | 2021 (in thousands) | 2020 (in thousands) | | :--- | :--- | :--- | | Net cash (used in) provided by operating activities | ($39,122) | $67,059 | | Net cash used in investing activities | ($69,253) | ($141,689) | | Net cash provided by financing activities | $144,766 | $121,801 | | **Net increase in cash, cash equivalents and restricted cash** | **$36,391** | **$47,171** | - Financing activities were the primary source of cash in the first nine months of 2021, with **$86.0 million** from a public offering and **$57.3 million** from an at-the-market program[26](index=26&type=chunk)[29](index=29&type=chunk)[30](index=30&type=chunk) - The cash provided by operations in 2020 was mainly due to the **$100 million** upfront payment from GSK[26](index=26&type=chunk)[94](index=94&type=chunk) [Notes to Condensed Financial Statements](index=10&type=section&id=Notes%20to%20Condensed%20Financial%20Statements%20(Unaudited)) Notes detail the company's liquidity position, revenue sources from the GSK collaboration, and allocation of transaction price - As of September 30, 2021, the company had cash, cash equivalents, and marketable securities of **$385.8 million** and believes these funds are sufficient to support planned operations for at least the next 12 months[32](index=32&type=chunk) - The company's revenue is derived entirely from its collaboration agreement with GlaxoSmithKline (GSK) for its MAT2A, Pol Theta, and WRN synthetic lethality programs[93](index=93&type=chunk)[109](index=109&type=chunk) - The agreement, effective July 2020, included a **$100 million** upfront payment[94](index=94&type=chunk) Collaboration Revenue by Program (in thousands) | Program | Three Months Ended Sep 30, 2021 (in thousands) | Nine Months Ended Sep 30, 2021 (in thousands) | | :--- | :--- | :--- | | MAT2A | $2,802 | $6,032 | | Pol Theta | $4,679 | $13,288 | | WRN | $1,495 | $5,659 | | **Total** | **$8,976** | **$24,979** | - As of September 30, 2021, the company had **$65.2 million** in transaction price allocated to remaining performance obligations under the GSK agreement, including R&D services and material rights for the MAT2A, Pol Theta, and WRN programs[118](index=118&type=chunk) - The company has a clinical trial collaboration with Pfizer to evaluate darovasertib in combination with Pfizer's binimetinib (MEK inhibitor) and crizotinib (cMET inhibitor)[107](index=107&type=chunk) - Pfizer supplies these compounds at no cost[107](index=107&type=chunk) [Management's Discussion and Analysis of Financial Condition and Results of Operations](index=27&type=section&id=Item%202.%20Management%27s%20Discussion%20and%20Analysis%20of%20Financial%20Condition%20and%20Results%20of%20Operations) Management discusses pipeline advancements, increased R&D and G&A expenses, and a strong liquidity position bolstered by recent equity financing [Business Overview and Pipeline Update](index=27&type=section&id=Business%20Overview%20and%20Pipeline%20Update) This section details progress in clinical trials for IDE397 and darovasertib, preclinical pipeline advancements, and COVID-19 impact - **IDE397 (MAT2A Inhibitor):** The company is actively enrolling patients in the fifth dose escalation cohort of its Phase 1 trial for solid tumors with MTAP deletions[122](index=122&type=chunk) - The drug has been generally well-tolerated, and preliminary clinical activity, including tumor shrinkage, has been observed[126](index=126&type=chunk)[127](index=127&type=chunk) - The company targets cohort expansion in H1 2022 and submission of an option data package to GSK in H1 2022, which could trigger a **$50 million** payment[134](index=134&type=chunk) - **Darovasertib (PKC Inhibitor):** The company is evaluating darovasertib in a Phase 1/2 trial for tumors with GNAQ/GNA11 mutations, including metastatic uveal melanoma (MUM)[172](index=172&type=chunk) - Clinical development includes monotherapy and combinations with Pfizer's binimetinib and crizotinib[174](index=174&type=chunk) - A clinical data update is targeted for Q4 2021, with plans to seek FDA guidance on a potential registration-enabling trial in H1 2022[176](index=176&type=chunk)[201](index=201&type=chunk) - **Preclinical Pipeline:** The company is advancing several preclinical synthetic lethality programs[144](index=144&type=chunk) - **PARG:** A potential development candidate has been selected, with IND-enabling studies planned[149](index=149&type=chunk) - **Pol Theta (with GSK):** A development candidate is planned for selection in December 2021[154](index=154&type=chunk) - **Werner Helicase (WRN) (with GSK):** The program has demonstrated in vivo efficacy and PD response[159](index=159&type=chunk) - **COVID-19 Impact:** The company continues to monitor the pandemic's impact on its clinical trials[209](index=209&type=chunk) - While logistical constraints exist, the pandemic has not materially affected the company's supply chain or development schedule to date[213](index=213&type=chunk) [Results of Operations](index=40&type=section&id=Results%20of%20Operations) Results show increased collaboration revenue, significant rises in R&D and G&A expenses, and a slight increase in net loss Comparison of Nine Months Ended September 30 (in thousands) | Metric | 2021 (in thousands) | 2020 (in thousands) | Change (in thousands) | % Change | | :--- | :--- | :--- | :--- | :--- | | Collaboration revenue | $24,979 | $8,967 | +$16,012 | +179% | | Research and development | $42,048 | $27,647 | +$14,401 | +52% | | General and administrative | $14,830 | $11,384 | +$3,446 | +30% | | **Net loss** | **($31,550)** | **($29,360)** | **($2,190)** | **(7%)** | - The **52% increase** in R&D expenses for the nine months ended Sep 30, 2021, compared to the same period in 2020, was primarily driven by higher payroll costs from increased headcount, increased fees to CROs/CMOs for advancing lead candidates, and higher clinical trial costs for IDE397 and darovasertib[247](index=247&type=chunk) - The **30% increase** in G&A expenses was mainly due to higher stock-based compensation, increased payroll expenses from headcount growth, and higher facility and software costs[249](index=249&type=chunk) [Liquidity and Capital Resources](index=42&type=section&id=Liquidity%20and%20Capital%20Resources) The company maintains a strong liquidity position with substantial cash and marketable securities, bolstered by recent public and ATM offerings - As of September 30, 2021, the company had **$385.8 million** in cash, cash equivalents, and marketable securities[226](index=226&type=chunk)[251](index=251&type=chunk) - The company raised net proceeds of **$86.0 million** from a follow-on public offering in July 2021 and **$57.3 million** from its at-the-market (ATM) facility during the first nine months of 2021[29](index=29&type=chunk)[30](index=30&type=chunk)[219](index=219&type=chunk) - Management believes that existing cash, cash equivalents, and marketable securities are sufficient to fund planned operations for at least 12 months from the financial statement issuance date[226](index=226&type=chunk) [Quantitative and Qualitative Disclosures About Market Risk](index=46&type=section&id=Item%203.%20Quantitative%20and%20Qualitative%20Disclosures%20About%20Market%20Risk) The company's primary market risk is interest rate sensitivity on its cash and investments, which is not expected to be material due to their short-term nature - The company's main market risk is potential loss from adverse changes in interest rates affecting its **$385.5 million** in cash equivalents and marketable securities[272](index=272&type=chunk) - Due to the short-term and low-risk nature of the investment portfolio (money market funds, U.S. government securities, commercial paper, corporate bonds), a **10% change** in interest rates is not expected to materially impact the fair value of these financial instruments[272](index=272&type=chunk) [Controls and Procedures](index=46&type=section&id=Item%204.%20Controls%20and%20Procedures) Management concluded that disclosure controls and procedures were effective, with no material changes to internal control over financial reporting - Management concluded that the company's disclosure controls and procedures were effective as of September 30, 2021[275](index=275&type=chunk) - There were no changes in internal control over financial reporting during the quarter that have materially affected, or are reasonably likely to materially affect, such controls[276](index=276&type=chunk) PART II—OTHER INFORMATION [Legal Proceedings](index=47&type=section&id=Item%201.%20Legal%20Proceedings) The company is not currently involved in any legal proceedings deemed to have a material adverse effect on its business - As of the filing date, the company is not involved in any material legal proceedings[278](index=278&type=chunk) [Risk Factors](index=47&type=section&id=Item%201A.%20Risk%20Factors) Key risks include early-stage development, dependence on product candidate success, reliance on collaborations, need for financing, and competition - **Financial and Operational Risks:** The company is an early-stage entity with a limited operating history, no approved products, and has incurred significant losses since inception, which are expected to continue[281](index=281&type=chunk)[282](index=282&type=chunk) - It will require substantial additional financing to achieve its goals[287](index=287&type=chunk) - **Development and Regulatory Risks:** The business is highly dependent on the successful development and regulatory approval of its product candidates, a lengthy and uncertain process[281](index=281&type=chunk) - The company has never completed a clinical trial and has limited experience with regulatory submissions[306](index=306&type=chunk)[316](index=316&type=chunk) - **Collaboration Risks:** The company's collaboration with GSK is critical[281](index=281&type=chunk) - Potential revenue is significantly dependent on GSK exercising its option for the MAT2A program and continuing development of other partnered programs[299](index=299&type=chunk) - Termination or non-exercise by GSK would materially harm the business[299](index=299&type=chunk) - **Pandemic Risk:** The COVID-19 pandemic may materially and adversely affect business operations, including the pace of enrollment in and conduct of current or future clinical trials[284](index=284&type=chunk)[389](index=389&type=chunk) [Other Part II Information](index=106&type=section&id=Other%20Part%20II%20Information) This section confirms no unregistered equity sales, notes non-applicable disclosures, and lists filed exhibits including certifications - Item 2: There were no unregistered sales of equity securities during the quarter[550](index=550&type=chunk) - Items 3, 4, and 5 (Defaults Upon Senior Securities, Mine Safety Disclosures, Other Information) were not applicable[553](index=553&type=chunk)[554](index=554&type=chunk)[555](index=555&type=chunk) - Item 6 lists the exhibits filed with the Form 10-Q, including amendments to agreements and required CEO/CFO certifications[557](index=557&type=chunk)

UNITED STATES SECURITIES AND EXCHANGE COMMISSION Washington, D.C. 20549 FORM 10-Q (Mark One) ☒ QUARTERLY REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES AND EXCHANGE ACT OF 1934 For the quarterly period ended June 30, 2021 OR ☐ TRANSITION REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES AND EXCHANGE ACT OF 1934 For the transition period from to Commission File Number: 001-38915 IDEAYA Biosciences, Inc. (Exact name of registrant as specified in its charter) Delaware 47-4268251 (State or othe ...

[Forward-Looking Statements](index=2&type=section&id=FORWARD-LOOKING%20STATEMENTS) This section outlines forward-looking statements concerning future operations, financial results, and product development, subject to inherent risks and uncertainties - Forward-looking statements cover future operations, financial results, product development, and business strategy, subject to known and unknown risks and uncertainties where actual results may differ materially[5](index=5&type=chunk) - Key areas include progress and costs of product candidates like **IDE397** and **darovasertib**, clinical and regulatory plans, COVID-19 impact, potential collaboration payments, and future financial performance[7](index=7&type=chunk)[10](index=10&type=chunk) [PART I—FINANCIAL INFORMATION](index=5&type=section&id=PART%20I%E2%80%94FINANCIAL%20INFORMATION) This section provides the unaudited financial statements, management's discussion and analysis, market risk disclosures, and internal controls [Financial Statements (Unaudited)](index=5&type=section&id=Item%201.%20Financial%20Statements%20(Unaudited)) This section presents the unaudited condensed financial statements for Q1 2021, including balance sheets, operations, equity, and cash flows, with explanatory notes [Condensed Balance Sheets](index=5&type=section&id=Condensed%20Balance%20Sheets) This subsection provides a snapshot of the company's financial position, detailing assets, liabilities, and equity as of March 31, 2021 Condensed Balance Sheet Highlights (in thousands) | Account | March 31, 2021 | December 31, 2020 | | :--- | :--- | :--- | | Cash and cash equivalents | $136,752 | $72,037 | | Marketable securities (Short & Long-term) | $173,649 | $211,548 | | **Total Assets** | **$326,097** | **$298,269** | | Contract liability (Current & Long-term) | $77,571 | $83,773 | | **Total Liabilities** | **$92,971** | **$99,995** | | **Total Stockholders' Equity** | **$233,126** | **$198,274** | [Condensed Statements of Operations and Comprehensive Loss](index=6&type=section&id=Condensed%20Statements%20of%20Operations%20and%20Comprehensive%20Loss) This subsection details the company's financial performance, including revenue, expenses, and net loss for the reported periods Statement of Operations Highlights (in thousands, except per share data) | Metric | Three Months Ended Mar 31, 2021 | Three Months Ended Mar 31, 2020 | | :--- | :--- | :--- | | Collaboration revenue | $7,247 | $0 | | Research and development | $11,566 | $9,026 | | General and administrative | $4,816 | $3,452 | | **Loss from operations** | **($9,135)** | **($12,478)** | | **Net loss** | **($9,021)** | **($12,043)** | | **Net loss per common share, basic and diluted** | **($0.28)** | **($0.59)** | [Condensed Statements of Cash Flows](index=8&type=section&id=Condensed%20Statements%20of%20Cash%20Flows) This subsection outlines the cash inflows and outflows from operating, investing, and financing activities for the reported periods Cash Flow Highlights (in thousands) | Activity | Three Months Ended Mar 31, 2021 | Three Months Ended Mar 31, 2020 | | :--- | :--- | :--- | | Net cash used in operating activities | ($13,724) | ($9,545) | | Net cash provided by investing activities | $36,435 | $10,906 | | Net cash provided by financing activities | $42,004 | $34 | - Financing activities in Q1 2021 were primarily driven by **$41.9 million** in net proceeds from the at-the-market (ATM) offering program[24](index=24&type=chunk) [Notes to Condensed Financial Statements (Unaudited)](index=9&type=section&id=Notes%20to%20Condensed%20Financial%20Statements%20(Unaudited)) This subsection provides detailed explanations and additional information supporting the condensed financial statements - The company, a synthetic lethality precision medicine oncology firm, has incurred significant losses since inception, with an accumulated deficit of **$136.0 million** as of March 31, 2021[26](index=26&type=chunk)[29](index=29&type=chunk) - The company raised **$41.9 million** in net proceeds from its ATM offering program in Q1 2021, with an additional **$14.6 million** gross proceeds raised from April 1 to May 9, 2021[27](index=27&type=chunk)[28](index=28&type=chunk) - Management believes **$310.4 million** in cash, cash equivalents, and marketable securities as of March 31, 2021, are sufficient to fund planned operations for at least the next 12 months[30](index=30&type=chunk) - A significant Collaboration, Option and License Agreement was signed with **GlaxoSmithKline (GSK)** in June 2020 for **MAT2A**, **Pol Theta**, and **WRN** programs, including a **$100.0 million** upfront payment in July 2020[90](index=90&type=chunk)[91](index=91&type=chunk) - For the GSK collaboration, six performance obligations were identified, recognizing **$7.2 million** in collaboration revenue in Q1 2021, disaggregated by program: **MAT2A ($1.5M)**, **Pol Theta ($3.5M)**, and **WRN ($2.2M)**[108](index=108&type=chunk)[110](index=110&type=chunk) [Management's Discussion and Analysis of Financial Condition and Results of Operations](index=25&type=section&id=Item%202.%20Management's%20Discussion%20and%20Analysis%20of%20Financial%20Condition%20and%20Results%20of%20Operations) Management discusses financial condition, operational results, and progress of key clinical programs, including **IDE397** and **darovasertib**, alongside liquidity and COVID-19 impact [Pipeline Overview](index=25&type=section&id=Pipeline%20Overview) This subsection details the progress and status of the company's key clinical and preclinical drug development programs - **IDE397 (MAT2A Inhibitor):** A Phase 1 clinical trial for solid tumors with MTAP deletions has initiated, with first patient dosed and cohort enrollment complete; preliminary PD data expected in H2 2021[122](index=122&type=chunk)[125](index=125&type=chunk)[126](index=126&type=chunk) - **PARG Inhibitor:** This preclinical program targets tumors with homologous recombination deficiencies (HRD), aiming to identify a development candidate in 2021[134](index=134&type=chunk)[142](index=142&type=chunk) - **Pol Theta (POLQ) Inhibitor:** In collaboration with **GSK**, this program targets tumors with BRCA or other HRD mutations, with a development candidate selection targeted for 2021[143](index=143&type=chunk)[148](index=148&type=chunk) - **Darovasertib (IDE196 - PKC Inhibitor):** Patient enrollment continues for combination therapy arms with **binimetinib** and **crizotinib** for metastatic uveal melanoma (MUM), with a clinical data update and FDA guidance for a potential registrational study anticipated in H2 2021[166](index=166&type=chunk)[193](index=193&type=chunk) - Preliminary data for the **darovasertib/crizotinib** combination in MUM showed tumor reduction in **2 of 2** evaluable patients, including one unconfirmed partial response with a **54%** tumor reduction[181](index=181&type=chunk) [Results of Operations](index=37&type=section&id=Results%20of%20Operations) This subsection analyzes the company's financial performance, comparing key revenue and expense metrics across periods Comparison of Three Months Ended March 31, 2021 and 2020 (in thousands) | Metric | Q1 2021 | Q1 2020 | Change | % Change | | :--- | :--- | :--- | :--- | :--- | | Collaboration Revenue | $7,247 | $0 | $7,247 | 100% | | Research & Development | $11,566 | $9,026 | $2,540 | 28% | | General & Administrative | $4,816 | $3,452 | $1,364 | 40% | | **Net Loss** | **($9,021)** | **($12,043)** | **$3,022** | **25%** | - The YoY increase in R&D expenses was primarily due to a **$1.3 million** increase in payroll and stock-based compensation from higher headcount and a **$1.0 million** increase in external costs for the **IDE397** Phase 1 trial[236](index=236&type=chunk) - The YoY increase in G&A expenses was mainly driven by a **$1.0 million** increase in payroll and stock-based compensation due to increased headcount supporting growth as a public company[237](index=237&type=chunk) [Liquidity and Capital Resources](index=40&type=section&id=Liquidity%20and%20Capital%20Resources) This subsection assesses the company's ability to meet its short-term and long-term financial obligations and fund operations - As of March 31, 2021, the company held **$310.4 million** in cash, cash equivalents, and marketable securities[239](index=239&type=chunk) - Management believes existing cash, cash equivalents, and marketable securities will be sufficient to fund planned operations into **2025**[240](index=240&type=chunk) [Quantitative and Qualitative Disclosures About Market Risk](index=43&type=section&id=Item%203.%20Quantitative%20and%20Qualitative%20Disclosures%20About%20Market%20Risk) This section addresses the company's market risk exposure, primarily interest rate risk on investments, deemed immaterial due to their short-term, low-risk nature - The company's primary market risk is interest rate sensitivity on its **$310.1 million** of cash equivalents and marketable securities, with a 10% interest rate change not expected to have a material effect due to short-term, low-risk investments[258](index=258&type=chunk) [Controls and Procedures](index=43&type=section&id=Item%204.%20Controls%20and%20Procedures) Management concluded that disclosure controls and procedures were effective as of March 31, 2021, with no material changes to internal control over financial reporting - The CEO and CFO concluded that the company's disclosure controls and procedures were effective at a reasonable assurance level as of quarter-end[261](index=261&type=chunk) - No material changes to the company's internal control over financial reporting occurred during the quarter[262](index=262&type=chunk) [PART II—OTHER INFORMATION](index=44&type=section&id=PART%20II%E2%80%94OTHER%20INFORMATION) This section covers legal proceedings, key risk factors, unregistered equity sales, and a list of filed exhibits [Legal Proceedings](index=44&type=section&id=Item%201.%20Legal%20Proceedings) The company is not currently involved in any legal proceedings expected to have a material adverse effect on its business - The company is not currently a party to any legal proceedings deemed to have a material adverse effect on the business[264](index=264&type=chunk) [Risk Factors](index=44&type=section&id=Item%201A.%20Risk%20Factors) This section details significant investment risks, including early-stage operations, historical losses, product development dependency, collaboration reliance, and COVID-19 impact - The company is an early-stage biopharmaceutical firm with limited operating history, significant losses since inception, and no approved products, making future viability assessment difficult[267](index=267&type=chunk)[268](index=268&type=chunk) - Business highly depends on successful development of product candidates and companion diagnostics, a lengthy, expensive, and uncertain process[267](index=267&type=chunk)[301](index=301&type=chunk) - Significant reliance on the **GSK** collaboration means potential revenue reduction if **GSK** does not exercise its **MAT2A** option or terminates other programs[267](index=267&type=chunk)[284](index=284&type=chunk) - Risks include patient enrollment in rare disease clinical trials, competition from larger companies, and reliance on third parties for manufacturing[267](index=267&type=chunk)[319](index=319&type=chunk)[354](index=354&type=chunk)[388](index=388&type=chunk) - The **COVID-19** pandemic poses a risk that could materially and adversely affect business operations, including clinical trial enrollment and conduct[269](index=269&type=chunk)[374](index=374&type=chunk) [Unregistered Sales of Equity Securities and Use of Proceeds](index=103&type=section&id=Item%202.%20Unregistered%20Sales%20of%20Equity%20Securities%20and%20Use%20of%20Proceeds) This section confirms no unregistered sales of equity securities occurred during the reported period - No unregistered sales of equity securities occurred in the reported period[533](index=533&type=chunk) [Exhibits](index=104&type=section&id=Item%206.%20Exhibits) This section lists exhibits filed with Form 10-Q, including CEO/CFO certifications and an amendment to the Pfizer collaboration agreement - Key exhibits filed include **CEO** and **CFO** certifications and Amendment No. 2 to the Clinical Trial Collaboration and Supply Agreement with **Pfizer Inc.**, dated April 8, 2021[540](index=540&type=chunk)

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, 2020 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 001-38915 IDEAYA Biosciences, Inc. (Exact name of Registrant as specified in its Charter) (State or other jurisdiction of incorporation o ...

UNITED STATES SECURITIES AND EXCHANGE COMMISSION Washington, D.C. 20549 FORM 10-Q (Mark One) ☒ QUARTERLY REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES AND EXCHANGE ACT OF 1934 For the quarterly period ended September 30, 2020 OR ☐ TRANSITION REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES AND EXCHANGE ACT OF 1934 For the transition period from to Commission File Number: 001-38915 IDEAYA Biosciences, Inc. (Exact name of registrant as specified in its charter) Delaware 47-4268251 (State or ...

UNITED STATES SECURITIES AND EXCHANGE COMMISSION Washington, D.C. 20549 (Mark One) ☒ QUARTERLY REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES AND EXCHANGE ACT OF 1934 For the quarterly period ended June 30, 2020 OR ☐ TRANSITION REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES AND EXCHANGE ACT OF 1934 For the transition period from to Commission File Number: 001-38915 IDEAYA Biosciences, Inc. (Exact name of registrant as specified in its charter) Delaware 47-4268251 (State or other jurisdic ...

UNITED STATES SECURITIES AND EXCHANGE COMMISSION Washington, D.C. 20549 (Mark One) ☒ QUARTERLY REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES AND EXCHANGE ACT OF 1934 For the quarterly period ended March 31, 2020 OR ☐ TRANSITION REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES AND EXCHANGE ACT OF 1934 For the transition period from to Commission File Number: 001-38915 IDEAYA Biosciences, Inc. (Exact name of registrant as specified in its charter) Delaware 47-4268251 (State or other jurisdi ...

Product Development and Clinical Trials - The lead product candidate, IDE196, is a PKC inhibitor targeting genetically-defined cancers with GNAQ or GNA11 mutations, currently in a Phase 1/2 clinical trial[15]. - As of March 15, 2020, a total of 53 patients have been enrolled in the IDE196 monotherapy arm for metastatic uveal melanoma, with 49 patients specifically having GNAQ or GNA11 mutations[26]. - The Phase 2 monotherapy dose for IDE196 has been set at 400 mg BID, which has shown a 44% increase in average steady state exposure and a 40% increase in trough concentration compared to the 300 mg BID dose[26]. - The company plans to submit an IND for the MAT2A program targeting solid tumors with MTAP deletions in Q4 2020, representing a significant advancement in their synthetic lethality pipeline[16]. - The synthetic lethality program targeting Pol-theta for tumors with homologous recombination deficiency is expected to designate a development candidate in the second half of 2020[32]. - The company is collaborating with Pfizer to evaluate the safety and efficacy of IDE196 in combination with binimetinib in patients with tumors harboring GNAQ or GNA11 mutations, targeting to initiate this trial in mid-2020[15]. - The ongoing Phase 1/2 basket trial will continue to focus on patients with tumors having activating GNAQ or GNA11 hotspot mutations, while plans for other indications have been suspended due to lack of supporting data[50]. - A Phase 1 sub-study initiated in January 2020 is evaluating an immediate release tablet formulation of IDE196, with ongoing enrollment to assess pharmacokinetic properties[40]. - The FDA indicated that a proposed single-arm Phase 2 portion of the IDE196-001 trial may support a new drug application for accelerated approval in MUM, targeting enrollment of 60 evaluable patients[48]. - IDE196 was initially developed by Novartis, which completed enrollment of 68 patients in a Phase 1 clinical trial for metastatic uveal melanoma as of December 31, 2019[47]. Market and Competitive Landscape - Approximately 90% of uveal melanoma patients have activating mutations in GNAQ or GNA11, with an estimated annual incidence of about 3,500 cases of metastatic uveal melanoma in major market countries[34]. - The median overall survival for untreated patients with metastatic uveal melanoma is approximately 2 to 8 months, with historical response rates ranging from 0% to 10% across treatment types[35]. - The company faces potential competition from lower-priced products in foreign markets due to price controls on pharmaceuticals[183]. - Third-party payors are increasingly reducing reimbursements for medical products, which could adversely affect sales[182]. Intellectual Property and Collaborations - As of March 15, 2020, the company holds approximately 19 distinct patent families, including four issued U.S. patents and 47 pending foreign applications across 31 jurisdictions, with nominal expirations ranging from 2035 to 2040[87]. - The IDE196 portfolio includes three issued U.S. patents and approximately 31 pending applications, with a nominal expiration in 2035, and three pending U.S. applications solely owned by the company expiring in 2040[88]. - The company has entered into a clinical trial collaboration with Pfizer to evaluate IDE196 in combination with binimetinib, targeting a Phase 1/2 clinical trial initiation in mid-2020[93]. - The exclusive option and license agreement with Cancer Research UK allows the company to develop PARG inhibitors, with the option period extended for up to four additional years[111]. - The collaboration with Cancer Research UK includes a joint research committee to govern non-clinical research activities, with a focus on PARG inhibitors[110]. Financial Overview and Funding - As of December 31, 2019, the company had cash equivalents and marketable securities totaling $100.4 million[519]. - The license agreement with Novartis includes an upfront payment of $2.5 million and potential milestone payments totaling up to $29 million, along with tiered royalty payments based on annual worldwide net sales[103]. - The company plans to pay an upfront fee of £100,000 and, if the option is exercised, an additional one-time fee of £250,000, with potential milestone payments totaling up to £28.5 million per indication[117]. Regulatory Environment - The FDA review process for a new drug application (NDA) typically takes about 10 months from the date of filing, with a goal of 12 months for a complete review[140]. - The FDA may refer a novel drug application to an advisory committee for independent evaluation and recommendations[141]. - An approval letter from the FDA authorizes commercial marketing, while a Complete Response Letter indicates deficiencies that must be addressed before approval[142]. - Orphan drug designation can provide exclusivity for seven years if the product receives FDA approval for the designated rare disease[147]. - The FDA's fast track designation allows for rolling review of NDA sections, expediting the approval process for drugs addressing serious conditions[148]. - Priority review aims to expedite applications that offer significant improvements over existing therapies, with a target review time of six months[149]. - Accelerated approval may be granted based on surrogate endpoints that predict clinical benefit, with post-marketing trials required[150]. - Breakthrough therapy designation provides intensive FDA guidance and expedited development for drugs showing substantial improvement over existing therapies[151]. Research and Development - The company is leveraging technological innovations and regulatory developments to enhance patient selection for their precision medicine approach[17]. - The team comprises experienced professionals from leading oncology organizations, guided by a scientific advisory board of key thought leaders[18]. - The company aims to establish a leading franchise in synthetic lethality by broadening its pipeline of targeted therapies and collaborating with diagnostic leaders[20]. - The prevalence of MTAP deletions is approximately 15% of all human tumors, translating to an estimated addressable population of about 90,000 annually in major market countries (US, EU5, Japan) for patients with solid tumors with MTAP deletion[59]. - The company has observed significant reduction in tumor SAM levels in terminal samples from preclinical in vivo studies following treatment with the lead MAT2A inhibitor[60]. - The lead MAT2A inhibitor is reported to be over 20 times more potent than Agios compound AGI-25696 in an engineered HCT-116 MTAP -/- xenograft model[63]. - The company expects to designate a Pol-theta inhibitor development candidate in the second half of 2020[68]. - High microsatellite instability (MSI) is present in about 15% of gastrointestinal tumor cancers, including approximately 22% of stomach adenocarcinoma and 16% of colorectal cancer[70]. - The company has identified potent, selective PARG inhibitors exhibiting a dose-dependent cellular pharmacodynamic response in a HCC1806 XRCC1 -/- cell line[76]. - The company is collaborating with several academic and research institutions to evaluate in vivo efficacy of PARG inhibitors in relevant animal models[77]. - The company has solved the crystal structure of the Pol-theta ATPase domain, enabling ongoing structure-based drug design[66]. - The company has observed synergistic in vitro and in vivo combination activity with a PARPi, Olaparib, in the DLD1 BRCA2 -/- engineered xenograft model[67]. - The company is targeting to demonstrate in vivo proof of concept for small molecule inhibitors of the WRN helicase protein in relevant animal models in 2020[73]. Manufacturing and Commercialization - The company is responsible for the manufacturing and commercialization of licensed products under the Novartis agreement, with obligations to supply IDE196 for compassionate use programs[100]. - The company currently relies on third parties for the manufacture of product candidates and biomarker diagnostics, with no plans to establish its own manufacturing facilities[123]. - For the product candidate IDE196, the company has contractual rights to API supply from Novartis, which will support ongoing preclinical research and clinical development efforts[125]. - The company plans to establish agreements with contract manufacturing organizations (CMOs) for the synthesis and manufacturing of drug products[124]. - The company holds worldwide commercialization rights to its product candidates and aims to retain significant rights in key markets[120]. - The company intends to build its own sales force to commercialize approved products in the U.S. and potentially in Europe, with plans to initiate commercial readiness activities[121].

IDEAYA Biosciences Corporate Presentation JP Morgan Conference January 2020 2 Safe Harbor Statement Certain statements in this presentation and the accompanying oral commentary are forward-looking statements. These statements relate to future events or the future financial performance of IDEAYA Biosciences, Inc. (the "Company") and involve known and unknown risks, uncertainties and other factors that may cause the actual results, levels of activity, performance or achievements of the Company or its industry ...

UNITED STATES SECURITIES AND EXCHANGE COMMISSION Washington, D.C. 20549 (Mark One) ☒ QUARTERLY REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES AND EXCHANGE ACT OF 1934 For the quarterly period ended September 30, 2019 OR ☐ TRANSITION REPORT PURSUANT TO SECTION 13 OR 15(d) OF THE SECURITIES AND EXCHANGE ACT OF 1934 For the transition period from to Commission File Number: 001-38915 IDEAYA Biosciences, Inc. (Exact name of registrant as specified in its charter) (State or other jurisdiction of incorpo ...