Core Points - Rigel Pharmaceuticals, Inc. has granted 79,890 stock options to eleven non-executive employees as part of its Inducement Plan approved by the Compensation Committee [1] - The stock options will vest over four years with a one-year cliff, which is a common structure in employee compensation plans [1] - This action is in accordance with NASDAQ Listing Rule 5635(c)(4), indicating compliance with regulatory requirements [4] Company Overview - Rigel Pharmaceuticals, Inc. is a biotechnology company focused on discovering and developing novel therapies for hematologic disorders and cancer [2] - The company was founded in 1996 and is headquartered in South San Francisco, California [2] - For more information on Rigel's marketed products and pipeline, the company provides resources on its website [2]

Core Viewpoint - Rigel Pharmaceuticals, Inc. will implement a 1-for-10 reverse stock split to increase the per-share trading price of its common stock, effective June 27, 2024, aiming to enhance marketability and compliance with Nasdaq listing requirements [3][8]. Group 1: Reverse Stock Split Details - The reverse stock split was approved by stockholders on May 24, 2024, and the final ratio was confirmed by the Board on June 15, 2024 [1]. - The number of shares outstanding will decrease from approximately 175,582,945 to about 17,558,294 [1]. - The reverse stock split will not change the number of authorized shares or the par value of the common stock [1]. Group 2: Market Impact and Compliance - The primary objective of the reverse stock split is to raise the per-share trading price, which is currently low and affects the company's appeal to institutional investors [8]. - The split is also intended to help maintain compliance with Nasdaq's minimum bid requirement of $1.00 per share [8]. Group 3: Shareholder Actions - Registered stockholders with shares in book-entry form will not need to take action to receive post-split shares [4]. - Stockholders holding shares in "street name" will have their positions automatically adjusted, while those with certificate shares will receive instructions from Equiniti Trust Company [4].

Core Viewpoint - Rigel Pharmaceuticals has completed the transfer of U.S. commercial rights for GAVRETO (pralsetinib) and will make it available for prescription starting June 27, 2024, targeting patients with specific types of cancer [1][2][4]. Group 1: Product Information - GAVRETO is indicated for adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC) and for adult and pediatric patients aged 12 and older with advanced or metastatic RET fusion-positive thyroid cancer [5][6]. - The recommended dosage for GAVRETO is 400 mg taken orally once daily [3]. - GAVRETO is the only once-daily oral RET-inhibitor therapy designed to selectively target RET in mNSCLC and advanced or metastatic thyroid carcinoma [3]. Group 2: Pricing and Support - GAVRETO will be supplied in two configurations: 100 mg bottles of 60 capsules priced at $11,144.58 and 100 mg bottles of 90 capsules priced at $16,716.85 [3]. - Rigel offers patient assistance programs through RIGEL ONECARE, which provides support for insurance coverage and financial assistance for eligible patients [3]. Group 3: Market Context - Rigel acquired the U.S. commercial rights to GAVRETO from Blueprint Medicines Corporation in February 2024, marking a strategic expansion in its hematology and oncology business [4][2]. - The NSCLC market is significant, with over 230,000 adults expected to be diagnosed with lung cancer in the U.S. in 2024, where NSCLC accounts for 80-85% of all lung cancer cases [5].

Core Insights - Rigel Pharmaceuticals presented five-year efficacy data for REZLIDHIA® (olutasidenib) at the EHA 2024 Hybrid Congress, demonstrating its effectiveness in treating relapsed or refractory (R/R) mutated isocitrate dehydrogenase-1 (mIDH1) acute myeloid leukemia (AML) [1][5][6] Group 1: Efficacy Data - The oral presentation highlighted that 35% of 147 efficacy evaluable patients achieved complete remission (CR) or CR with partial hematologic recovery (CRh), with a median time to CR/CRh of 1.9 months and a median duration of 25.3 months [6] - In patients previously treated with venetoclax, 33% achieved CR/CRh, with a median overall survival of 16.2 months [7] - The overall response rate (ORR) was 48%, with a median duration of 15.5 months and a maximum duration ongoing at 54.6 months [6][9] Group 2: Safety and Tolerability - Olutasidenib was reported to have a well-characterized and manageable safety profile, with differentiation syndrome occurring in 16% of patients [13][14] - The treatment was generally well tolerated in elderly patients, with 31% achieving CR/CRh in a subgroup analysis of patients aged 75 and older [10] Group 3: Subgroup Analyses - Data presented included the efficacy of olutasidenib in elderly patients, those who failed prior venetoclax treatment, and as a bridge to allogeneic hematopoietic stem cell transplantation (HSCT) [4][10][11] - In patients with mIDH1 AML secondary to myeloproliferative neoplasms (MPN), 40% achieved CR, with a median duration of response of 15.6 months [8][11] Group 4: Future Implications - The data supports the potential of REZLIDHIA in treating patient populations with limited treatment options, particularly those with mIDH1 AML secondary to MPN [5][12] - The findings suggest that olutasidenib may serve as a bridge to allogeneic stem cell transplantation for previously ineligible patients, with 75% of those proceeding to transplant achieving CR/CRh prior to the procedure [11]

Core Insights - Rigel Pharmaceuticals presented data on REZLIDHIA® (olutasidenib) at the 2024 ASCO Annual Meeting, highlighting its long-term efficacy in treating relapsed or refractory (R/R) mutated isocitrate dehydrogenase-1 (mIDH1) acute myeloid leukemia (AML) patients, including those previously treated with venetoclax [1][2][4] - The data showed that olutasidenib achieved a complete remission (CR) or CR with partial hematologic recovery (CRh) in 35% of efficacy evaluable patients, with a median duration of CR/CRh of 25.3 months [4] - The ongoing Phase 1b trial of R289, a dual inhibitor of IRAK1 and IRAK4, is also being presented, targeting lower-risk myelodysplastic syndrome (LR-MDS) patients [2][8] Group 1: REZLIDHIA® Efficacy and Safety - The five-year results from the Phase 2 trial of olutasidenib demonstrated durable responses in heavily pretreated patients with mIDH1 AML, with an overall response rate of 48% and median overall survival of 11.6 months [4][5] - In a subgroup analysis of elderly patients aged 75 and older, 31% achieved CR/CRh, with a median duration of 25.9 months [5][6] - Among patients who were R/R to prior venetoclax, 33% achieved CR/CRh, with a median overall survival of 16.2 months [4] Group 2: R289 Trial Overview - R289 is being evaluated in a Phase 1b trial for patients with LR-MDS, an area identified as having high unmet medical needs [2][8] - The trial aims to assess the safety and preliminary efficacy of R289, with multiple dose levels already completed and active recruitment ongoing [11][12] - R289 is a prodrug of R835, which has shown potential in blocking inflammatory cytokine production linked to persistent cytopenias in lower-risk MDS patients [8]

Company Overview - Rigel Pharmaceuticals, Inc. is a biotechnology company focused on discovering, developing, and providing novel therapies for patients with hematologic disorders and cancer [3] - The company was founded in 1996 and is headquartered in South San Francisco, California [3] Upcoming Event - Raul Rodriguez, the president and CEO of Rigel, will present a company overview at the Jefferies Global Healthcare Conference on June 6, 2024, at 9:30 am ET in New York [1] - The presentation will be accessible via a live webcast, and interested parties are encouraged to connect to Rigel's website prior to the event for any necessary software downloads [2]

Group 1 - Rigel Pharmaceuticals announced upcoming presentations at the 2024 ASCO Annual Meeting and EHA 2024 Congress, showcasing their hematology and oncology portfolio [1][2] - Presentations will include data on REZLIDHIA® (olutasidenib) for mutated IDH1 acute myeloid leukemia (AML) and TAVALISSE® (fostamatinib) for chronic immune thrombocytopenia (ITP), along with a Phase 1b trial of R2891 [2][3] - The five-year data from the Phase 2 trial of REZLIDHIA indicates rapid and durable responses, particularly in difficult-to-treat populations, including elderly patients [3][6][7] Group 2 - TAVALISSE demonstrated efficacy as a second-line therapy for ITP, allowing successful tapering of corticosteroids while maintaining platelet counts above 50,000/μL [4][10] - The ASCO and EHA presentations will include various abstracts highlighting the efficacy and safety of olutasidenib in different patient populations, including those with relapsed or refractory AML [5][8][11] - Observational studies provide real-world insights into the use of fostamatinib in ITP patients, emphasizing the need for additional treatment options [10][15] Group 3 - Rigel Pharmaceuticals focuses on developing therapies for hematologic disorders and cancer, with a commitment to improving patient outcomes [36] - The company has a robust pipeline, including investigational compounds like R289, which targets IRAK1 and IRAK4 for lower-risk myelodysplastic syndrome [16][36] - Rigel's marketed products and ongoing clinical trials reflect its dedication to addressing unmet medical needs in hematology and oncology [36][37]

Financial Data and Key Metrics Changes - For Q1 2024, Rigel Pharmaceuticals reported net product sales of TAVALISSE at $21.1 million, a 5% decrease compared to the same period in 2023, primarily due to a reduction in inventory levels at distributors [83][84] - REZLIDHIA generated $4.9 million in net sales for Q1 2024, significantly up from $1.5 million in the same period last year, reflecting strong growth since its launch in December 2022 [84] - Total cost and expenses for Q1 2024 were $36.5 million, down from $38.8 million in the same period for 2023, mainly due to decreased research and development costs [91] Business Line Data and Key Metrics Changes - TAVALISSE achieved its sixth consecutive quarterly record high for bottles shipped, with a 10% year-over-year growth in demand for Q1 2024 [18] - REZLIDHIA saw a 17% growth in bottles shipped compared to Q4 2023, nearly tripling the demand from the same period last year [23] - The acquisition of GAVRETO is expected to enhance the commercial product portfolio, with anticipated top-line growth and synergies with existing products [11][16] Market Data and Key Metrics Changes - GAVRETO generated $28 million in US net product sales in 2023, and the company expects to begin shipping GAVRETO to patients and clinics in July 2024 [15][42] - The market for RET fusion-positive non-small cell lung cancer is projected to expand, with approximately 3,000 new patients identified annually in the US [33][52] Company Strategy and Development Direction - The company aims to grow its Hematology and Oncology business, focusing on increasing sales of TAVALISSE and REZLIDHIA while integrating GAVRETO into its operations [94] - Rigel is pursuing additional in-licensing deals and acquisitions to expand its product portfolio, similar to its strategies with REZLIDHIA and GAVRETO [95] - The company is advancing its development programs, including olutasidenib for various cancers and R289 for lower-risk MDS, through collaborations with MD Anderson Cancer Center and the CONNECT Consortium [60][62] Management's Comments on Operating Environment and Future Outlook - Management expressed confidence in achieving financial breakeven, with expectations of revenue growth from the launch of GAVRETO and continued demand for existing products [102] - The company is focused on maintaining a disciplined financial approach while investing in clinical trials and expanding its product pipeline [93][95] - Management highlighted the importance of educating clinicians about the efficacy of GAVRETO and olutasidenib, particularly in underserved patient populations [39][60] Other Important Information - The company ended Q1 2024 with cash, cash equivalents, and short-term investments of $49.6 million [93] - Rigel has entered into an amendment to its credit agreement, extending the maturity date and interest-only period by one year [93] Q&A Session Summary Question: Cash guidance and path to breakeven - The company is burning about $8 million a quarter and is focused on increasing revenues while managing operational expenses to reach breakeven [100][102] Question: Brain activity for GAVRETO and olutasidenib - Both GAVRETO and olutasidenib have shown the ability to cross the blood-brain barrier, which is critical for their therapeutic effects [104][106] Question: Balancing current pipeline and appetite for acquisitions - The company is excited about the growth of TAVALISSE and REZLIDHIA, and sees opportunities for further clinical trials and acquisitions to enhance its pipeline [110][114]

Financial Performance - Total revenue for Q1 2024 was $29.5 million, including $21.1 million from TAVALISSE and $4.9 million from REZLIDHIA[5]. - Total revenues for Q1 2024 increased to $29,534,000, up 13.5% from $26,070,000 in Q1 2023[51]. - Product sales, net rose to $26,003,000, compared to $23,745,000 in the same period last year, reflecting an increase of 9.5%[51]. - Contract revenues from collaborations grew significantly to $3,531,000, up 51.8% from $2,325,000 in Q1 2023[51]. - Total costs and expenses for Q1 2024 were $36.5 million, a decrease from $38.8 million in the same period of 2023[10]. - Total costs and expenses decreased to $36,500,000, down 5.7% from $38,795,000 in Q1 2023[51]. - Rigel's net loss for Q1 2024 was $8.2 million, or $0.05 per share, an improvement from a net loss of $13.5 million, or $0.08 per share, in Q1 2023[11]. - Net loss for Q1 2024 was $8,247,000, an improvement of 39.5% compared to a net loss of $13,536,000 in Q1 2023[51]. - Net loss per share improved to $0.05, compared to $0.08 in the prior year[51]. - Rigel's cash, cash equivalents, and short-term investments totaled $49.6 million as of March 31, 2024, down from $56.9 million at the end of 2023[12]. - Cash, cash equivalents, and short-term investments decreased to $49,550,000 from $56,933,000 as of December 31, 2023[53]. - Total assets increased to $126,519,000, up from $117,225,000 at the end of 2023[53]. - Stockholders' deficit widened to $31,671,000 from $28,644,000 as of December 31, 2023[53]. - Stock-based compensation expense included in selling, general and administrative expenses was $4,484,000, significantly higher than $1,735,000 in Q1 2023[51]. Product Sales and Market Performance - TAVALISSE sales volume reached 2,193 bottles, the highest quarterly sales since launch, while REZLIDHIA sales grew significantly with 390 bottles sold[6]. - The company expanded its portfolio with the acquisition of GAVRETO, expected to start recognizing product sales in July 2024[5]. - Contract revenue from collaborations amounted to $3.5 million, with contributions from Kissei Pharmaceutical, Grifols, and Medison Pharma[9]. Clinical Development and Trials - Rigel is advancing its Phase 1b clinical trial for R289, a novel IRAK1/4 inhibitor, with preliminary data expected by the end of 2024[8]. - The company announced a strategic collaboration with CONNECT to evaluate REZLIDHIA in combination with temozolomide for high-grade glioma patients[7]. - Rigel Pharmaceuticals is focused on the commercialization of olutasidenib and pralsetinib for various cancers, with ongoing clinical trials[48]. Adverse Reactions and Safety - TAVALISSE patients experienced serious adverse reactions at a rate of 1%, with severe reactions including dyspnea and hypertension at 2%[31]. - Hepatotoxicity occurred in 23% of patients treated with REZLIDHIA, with 13% experiencing grade 3 or 4 hepatotoxicity[32]. - GAVRETO showed a 12% incidence of pneumonitis, with 3.3% classified as Grade 3-4 and 0.2% resulting in fatal reactions[43]. - 35% of GAVRETO patients experienced hypertension, with 18% having Grade 3 hypertension[43]. - Increased AST levels were observed in 49% of GAVRETO patients, with 7% experiencing Grade 3 or 4 increases[43]. - The median time to onset for increased AST in GAVRETO patients was 15 days, with a range from 5 days to 2.5 years[43]. - Common adverse reactions for GAVRETO included musculoskeletal pain, constipation, and fatigue, occurring in ≥25% of patients[46]. - The company advises against the use of REZLIDHIA with strong or moderate CYP3A inducers due to potential drug interactions[40]. - Rigel Pharmaceuticals emphasizes the importance of monitoring liver function tests for patients on REZLIDHIA, especially during the first two months of treatment[33]. Leadership and Management - Rigel appointed Lisa Rojkjaer, M.D. as Chief Medical Officer, bringing over 20 years of experience in clinical development and oncology[6].

Financial Performance - For the three months ended March 31, 2024, net product sales of TAVALISSE were $21.1 million, a decrease of $1.2 million or 5% compared to $22.3 million in the same period in 2023[123]. - Net product sales of REZLIDHIA for the same period were $4.9 million, an increase of $3.4 million compared to $1.5 million in the same period in 2023, primarily due to increased quantities sold[124]. - Total revenues for the three months ended March 31, 2024, were $29.534 million, an increase of $3.464 million or 13.3% compared to $26.070 million in the same period in 2023[199]. - Cost of product sales for the three months ended March 31, 2024, was $2.025 million, an increase of $1.048 million compared to $977,000 in the same period in 2023[202]. - Revenue from collaborations for the three months ended March 31, 2024, included $2.3 million from Kissei, $1.1 million from Grifols, and $0.1 million from Medison[200]. Product Development and Trials - The company has a Phase 1b trial for its IRAK1/4 inhibitor program, which is expected to enroll approximately 40 patients, with preliminary data anticipated by the end of 2024[137]. - The company has strategic collaborations to expand the evaluation of REZLIDHIA in AML and other hematologic cancers[122]. - A collaboration with CONNECT was announced to conduct a Phase 2 clinical trial for REZLIDHIA in HGG, with funding of up to $3.0 million over four years[139]. - The Phase 2 registrational trial of REZLIDHIA demonstrated a CR+CRh rate of 35% and a median duration of overall response of 11.7 months[173]. - The major portion of total research and development expense in Q1 2024 was associated with the IRAK 1/4 inhibitor program[214]. Strategic Agreements and Collaborations - The company entered into an Asset Purchase Agreement to acquire GAVRETO (pralsetinib) for $15.0 million, with $10.0 million payable upon the first commercial sale and an additional $5.0 million on the first anniversary of the agreement[127]. - The company entered into a Strategic Collaboration Agreement with MDACC to evaluate REZLIDHIA (olutasidenib) in AML and other hematologic cancers, providing $15.0 million in milestone payments over five years[138]. - The company has established a reimbursement and patient support program called Rigel OneCare (ROC) to assist eligible patients with access to TAVALISSE[158]. - The commercialization license agreement with Grifols for fostamatinib includes exclusive rights in Europe, the UK, and other regions[160]. - The company entered into a commercial license agreement with Knight Therapeutics for fostamatinib in Latin America, receiving a $2.0 million upfront payment and potential for up to $20.0 million in milestones[169]. Financial Position and Cash Flow - As of March 31, 2024, the company had approximately $49.6 million in cash, cash equivalents, and short-term investments, down from $56.9 million at the end of 2023[222]. - Net cash used in operating activities was $(5,013,000) in Q1 2024 compared to $(4,074,000) in Q1 2023, reflecting an increase in cash outflow of $939,000[223]. - The company anticipates significant additional funding requirements in the foreseeable future, potentially impacting its ability to operate as a going concern[231]. - The company has a fully funded $60.0 million term loan credit facility with MidCap as of March 31, 2024[230]. - The outstanding principal amount of the loan under the credit facility with MidCap was $60.0 million[242]. Market and Competitive Landscape - GAVRETO is one of only two approved RET inhibitors on the market, with FDA approvals for metastatic RET fusion-positive NSCLC and advanced thyroid cancer[130]. - The competitive landscape includes TIBSOVO® (ivosidenib) as the only other approved product in the US for patients with IDH1 mutation[182]. - TAVALISSE is competing with existing therapies for ITP, including corticosteroids and thrombopoietin receptor agonists[151]. - REZLIDHIA was added to the NCCN Clinical Practice Guidelines for AML as a recommended targeted therapy in January 2023[177]. Sales and Marketing - TAVALISSE's sales decrease was partly due to a reduction in distributor inventory and increased revenue reserves from higher government and private payor rebates[123]. - The company plans to commercialize GAVRETO later in 2024, which is expected to contribute to future revenues[201]. - The company expects to incur significant selling, general and administrative expenses as it expands commercial activities for existing products and prepares for the commercialization of GAVRETO later this year[216]. Research and Development Expenses - Research and development expense decreased to $6,026,000 in Q1 2024 from $10,089,000 in Q1 2023, a reduction of $4,063,000 or 40.3%[204]. - The decrease in research and development expense was partly due to a $1.1 million reduction in clinical trial-related expenses and a $1.0 million decrease in personnel-related costs[205]. - Selling, general and administrative expense increased to $28,449,000 in Q1 2024 from $27,729,000 in Q1 2023, an increase of $720,000 or 2.6%[215].