A Phase 3, Multicenter, Double-Blind, Placebo-controlled Study Assessing the Efficacy and Safety of Olomorasib in Combination With Standard of Care Immunotherapy in Participants With Resected or Unresectable KRAS G12C-Mutant, Non-Small Cell Lung Cancer - SUNRAY-02

The main purpose of this study is to assess if olomorasib in combination with pembrolizumab is more effective than the pembrolizumab and placebo combination in part A in participants with resected KRAS G12C-mutant NSCLC and to assess if olomorasib in combination with durvalumab is more effective than the durvalumab and placebo combination in part B in participants with unresectable KRAS G12C-mutant non-small cell lung cancer. The study may last up to 3 years for each participant.

Start Date01 Apr 2025

Sponsor / Collaborator

Eli Lilly & Co.

NCT06719128

/ RecruitingPhase 1

An Open-Label, Nonrandomized, Single-Dose, Safety and Pharmacokinetic Study of LY3537982 in Participants With Hepatic Impairment and Healthy Participants

The main purpose of this study is to assess how olomorasib gets into the blood stream and how long it takes the body to remove it when administered to participants with mild, moderate and severe impaired liver function compared to participants with normal liver function. The safety and tolerability of olomorasib will also be evaluated. The study may last up to 6 weeks for each participant including the screening period.

Start Date06 Dec 2024

Sponsor / Collaborator

Eli Lilly & Co.

CTR20242544

/ RecruitingPhase 3

SUNRAY-01，一项比较LY3537982联合帕博利珠单抗与安慰剂联合帕博利珠单抗一线治疗PD-L1表达≥50%或LY3537982联合帕博利珠单抗、培美曲塞、铂类药物与安慰剂联合帕博利珠单抗、培美曲塞、铂类药物（无论PD-L1表达水平）一线治疗KRAS G12C突变、局部晚期或转移性非小细胞肺癌受试者的全球关键性研究

[Translation] SUNRAY-01, a global pivotal study comparing LY3537982 plus pembrolizumab versus placebo plus pembrolizumab as first-line treatment for subjects with KRAS G12C-mutated, locally advanced or metastatic non-small cell lung cancer whose PD-L1 expression is ≥50% or LY3537982 plus pembrolizumab, pemetrexed, and a platinum versus placebo plus pembrolizumab, pemetrexed, and a platinum (regardless of PD-L1 expression level) as first-line treatment

本研究的目的是评估在未经治疗的晚期 NSCLC 受试参与者中，增加LY3537982联合标准治疗抗癌药物是否比标准治疗更有效。非小细胞肺癌的基因必须发生称为KRAS G12C的突变。研究参与（包括随访）可能持续长达 3 年，具体取决于受试者和受试者的肺癌情况。

[Translation]

The purpose of this study is to evaluate whether adding LY3537982 to standard-of-care anticancer drugs is more effective than standard-of-care in participants with untreated advanced NSCLC. The NSCLC must have a mutation in a gene called KRAS G12C. Study participation, including follow-up, may last up to 3 years, depending on the participant and the subject's lung cancer.

Start Date10 Oct 2024

Sponsor / Collaborator

Eli Lilly Suzhou Pharmaceutical Co. Ltd.

[+2]

100 Clinical Results associated with Olomorasib

100 Translational Medicine associated with Olomorasib

100 Patents (Medical) associated with Olomorasib

Literatures (Medical) associated with Olomorasib

01 Oct 2024·Nature Chemical Biology

Direct RAS inhibitors turn 10

Article

Author: Ostrem, Jonathan M L ; Peters, Ulf ; Shokat, Kevan M

RAS proteins, central drivers of cancer, appeared ′undruggable′ for almost 30 years.Here we provide a personal perspective on the effort leading to our initial report of KRAS^G12C inhibitors in 2013, and the decade of discoveries that followed.

01 Apr 2024·Clinical and translational discovery

Targeting mutated KRAS in the first‐line therapy

Author: Ijichi, Hideaki

Clin. trials take time in general, especially large-scale phase 3 trials for the clin. approval of novel therapies, whereas a number of advanced cancer patients have been waiting for highly effective therapies with hope.Hence it is extremely important that novel effective therapies are approved to be available as soon as possible through the clin. trials.The first-line treatment with KRAS-specific inhibitors (in combination with EGFR inhibitors, etc.) will significantly benefit KRAS-mutated cancer patients with currently dismal prognoses.

Lancet Respiratory Medicine

Tackling KRAS^G12C-mutated non-small-cell lung cancer: iteration and exploration

Author: Luo, Jia ; Villaruz, Liza C.

KRASG12C-mutated non-small-cell lung cancer (NSCLC) has been historically challenging to target, but the development of GDP-bound KRASG12C inhibitors has revolutionized treatment options.This study discusses the efficacy and safety of garsorasib (D-1553), a covalent allosteric inhibitor, in a phase 2, open-label, multicenter trial involving patients with advanced KRASG12C-mutated NSCLC.Results showed a 50% objective response rate (ORR), 89% disease control rate (DCR), and a median progression-free survival (PFS) of 7.6 mo. Adverse events, including elevated liver enzymes, anemia, and gastrointestinal symptoms, were reported, aligning with other KRASG12C inhibitors such as sotorasib and adagrasib.The study highlights ongoing clin. trials testing novel KRAS inhibitors and combination therapies to overcome resistance. Despite promising results, further exploratory approaches are required to develop durable and more effective KRASG12C-targeted therapies.

News (Medical) associated with Olomorasib

06 Mar 2025

·www.prnewswire.com

TEPMETKO Continues to Strengthens its Position as a Leading METex14 Skipping NSCLC Therapy | DelveInsight

With increasing biomarker-driven cancer treatments, TEPMETKO benefits from growing adoption in precision oncology. Competition from other MET inhibitors like TABRECTA (capmatinib) exists, but TEPMETKO's once-daily dosing and efficacy profile offer differentiation. LAS VEGAS, March 6, 2025 /PRNewswire/ -- DelveInsight's " TEPMETKO Market Size, Forecast, and Market Insight Report" highlights the details around TEPMETKO, a kinase inhibitor indicated for the treatment of adult patients with metastatic NSCLC harboring MET exon 14 skipping alterations. The report provides product descriptions, patent details, and competitor products (marketed and emerging therapies) of TEPMETKO. The report also highlights the historical and forecasted sales from 2020 to 2034 segmented into 7MM [the United States, the EU4 (Germany, France, Italy, and Spain), the United Kingdom, and Japan]. EMD Serono's TEPMETKO (tepotinib) Overview TEPMETKO is a kinase inhibitor prescribed for adult patients with metastatic non-small cell lung cancer (NSCLC) carrying MET exon 14 skipping alterations. The active component is Tepotinib (as hydrochloride monohydrate), administered orally. Patients should be cautioned about the heightened risk of severe or fatal interstitial lung disease/pneumonitis, liver toxicity, and potential embryo-fetal toxicity, necessitating effective contraception during and shortly after treatment. Tepotinib specifically targets MET, including variants with exon 14 skipping mutations. It blocks HGF-dependent and independent MET phosphorylation, disrupting MET-driven signaling pathways. Additionally, at clinically relevant concentrations, Tepotinib inhibits melatonin 2 and imidazoline 1 receptors. In vitro studies show that it suppresses tumor cell proliferation, anchorage-independent growth, and migration of MET-dependent cancer cells. In mouse models with MET-driven tumors, including those with MET exon 14 skipping alterations, Tepotinib reduced tumor growth, sustained MET phosphorylation inhibition, and, in one case, decreased metastasis formation. The recommended dose of TEPMETKO is 450 mg taken orally once daily until disease progression or intolerable toxicity occurs. Patients should take it at the same time each day, swallowing tablets whole without chewing, crushing, or splitting them. If a dose is missed and less than eight hours remain until the next scheduled dose, patients should skip it. In cases of vomiting after taking TEPMETKO, the next dose should be taken at the usual time. Learn more about TEPMETKO projected market size for NSCLC @ TEPMETKO Market Potential Non-small cell lung cancer (NSCLC) is the most common type of lung cancer, accounting for 81% of all diagnosed cases. Early detection greatly improves outcomes, but diagnosing NSCLC and other lung cancers is challenging because their symptoms are often mistaken for common illnesses or the long-term effects of smoking. Consequently, 80% of NSCLC cases are already at advanced stages by the time they are identified, making treatment more difficult. Around 80% of EGFR mutations in NSCLC involve either exon 19 deletions or the exon 21 L858R substitution, both of which are classified as sensitizing mutations. Until the last decade, chemotherapy was the primary treatment for advanced and metastatic lung cancer. However, this changed in 2015 with the approval of the first immune checkpoint inhibitor (ICI), KEYTRUDA (pembrolizumab), as a second-line therapy for advanced cases. This was followed by TECENTRIQ (atezolizumab) in 2016. Both therapies were later approved for first-line treatment, broadening their use to a larger patient population. In 2020, the combination of OPDIVO (nivolumab) and ipilimumab also received approval as a first-line treatment for metastatic NSCLC. According to DelveInsight, the NSCLC market size across the 7MM is projected to grow from USD 30 billion in 2024, with a substantial CAGR through 2034. This growth is largely driven by the introduction of emerging therapies during the forecast period (2025–2034). Discover more about the NSCLC market in detail @ Non-small Cell Lung Cancer Market Report Emerging Competitors of TEPMETKO The NSCLC pipeline is very robust with the promising therapies such as Telisotuzumab vedotin (AbbVie), Patritumab deruxtecan (Daiichi Sankyo/AstraZeneca), Datopotamab deruxtecan (Daiichi Sankyo/AstraZeneca), Eftilagimod alpha (Immutep), BNT311/GEN1046 (acasunlimab) (Genmab), V940 (mRNA-4157) + Pembrolizumab (Moderna Therapeutics/Merck), Plinabulin + Docetaxel (BeyondSpring), Olomorasib (LY3537982) (Eli Lilly and Company), Zipalertinib (Cullinan Oncology/Taiho Pharma), Ceralasertib (AZD6738) (AstraZeneca), TEDOPI (EP-2101; IDM 2101; OSE-2101) (OSE Immuno-therapeutics), Sigvotatug vedotin (PF08046047) (Pfizer), ANKTIVA (N-803) (ImmunityBio), Aumolertinib/Almonertinib/HS-10206 (Jiangsu Hansoh Pharmaceutical), Niraparib (GSK), Savolitinib (AstraZeneca/Hutchison MediPharma), TRODELVY (Gilead Sciences), Pyrotinib (Jiangsu HengRui Medicine), Ociperlimab (BGB-A1217) (BieGene), Volrustomig (AstraZeneca), Gotistobart (BNT316/ONC-392) (OncoC4/BioNTech), Ivonescimab (AK112/SMT112) (Akeso Biopharma/Summit Therapeutics), ZYNYZ (retifanlimab/INCMGA00012) (Incyte/Macrogenics), Divarasib (GDC-6036) (Roche/Genentech), Tiragolumab (RG6058) (Roche), Sacituzumab Tirumotecan (Merck and Kelun-Biotech), JEMPERLI (dostarlimab/TSR-042) (GSK and AnaptysBio), Zongertinib (BI-1810631) (Boehringer Ingelheim), BAY 2927088 (Bayer), Serplulimab (HLX10) (Shanghai Henlius Biotech), Rilvegostomig (AZD2936) (AstraZeneca), MK-1084 (Merck, Taiho Pharmaceutical, and Astex), Domvanalimab (Arcus Biosciences and Gilead Sciences), OPDUALAG (nivolumab and relatlimab) (Bristol-Myers Squibb), Belrestotug + JEMPERLI (iTeos Therapeutics and GSK), Firmonertinib (ArriVent BioPharma), Sunvozertinib (DZD9008) (Dizal Pharmaceutical), Cobolimab (GSK), Livmoniplimab (AbbVie), Fianlimab (REGN3767) (Regeneron Pharmaceuticals), BNT327/PM8002 (Biotheus/BioNTech), HS-20117 (Hansoh BioMedical), IO102-IO103 + Pembrolizumab (IO Biotech), Naptumomab estafenatox (NeoTX Therapeutics/Active Biotech), FF-10832 (FUJIFILM Corporation), BNT116 (BioNTechSE/Regeneron Pharmaceuticals), CAN-2409 (Candel Therapeutics), Mecbotamab Vedotin (BA3011/CAB-AXL-ADC) (BioAtla), Bemcentinib (BGB 324/BGB-3234/R-428) (BerGenBio/Rigel Pharmaceuticals), DOVBLERON (taletrectinib/AB-106/IBI-344) (Nuvation Bio/Innovent Biologics/Daiichi Sankyo/Nippon Kayaku), Lifileucel (Iovance Biotherapeutics), IBI363 (Innovent Biologics), Sotevtamab (AB-16B5) (Alethia Biotherapeutics), Avutometinib (VS6766) (Verastem Oncology), Vebreltinib (APL-101) (Apollomics), LP-300 (Lantern Pharma), JNJ-90301900 (Johnson & Johnson Innovative Medicine), AMG 193 (Amgen), Luveltamab tazevibulin (Sutro Biopharma), PRT3789 (Prelude Therapeutics), Disitamab vedotin (Seagen), PADCEV (enfortumab vedotin) (Astellas Pharma), RP1 (Replimune), TIVDAK (tisotumab vedotin) (Seagen), Zanidatamab (Jazz Pharmaceuticals), Utidelone injectable (UTD1) (Beijing Biostar Pharmaceuticals), REGN5093-M114 (Regeneron Pharmaceuticals), SLC-391 (SignalChem Lifesciences), fulzerasib (GenFleet), Davutamig (REGN5093) (Regeneron Pharmaceuticals), TAS3351 (Taiho Oncology), H002 (RedCloud Bio), JIN-A02 (J INTS BIO), FWD1509 (Forward Pharma), Sabestomig (AZD7789) (AstraZeneca), Sasanlimab (Pfizer), Selvigaltin (GB1211) (Galecto Biotech), Vepafestinib Helsinn (Healthcare/Taiho Pharmaceutical), EP0031 (A400/ KL590586) (Ellipses Pharma/Kelun-Biotech), Pamvatamig (MCLA-129) (Merus), Zidesamtinib (NVL-520) (Nuvalent), NVL-655 (Nuvalent), RMC-4630 (Revolution Medicines), REQORSA (quaratusugene ozeplasmid) (Genprex), PDC*lung01 (PDC*line Pharma), Evalstotug (BA3071) (BioAtla and BeiGene), PT-112 (Promontory Therapeutics), MRT-2359 (Monte Rosa Therapeutics), GAIA-102 (GAIA BioMedicine), Rigosertib (Traws Pharma), HMBD-001 (Hummingbird Bioscience), PLB1004 (Avistone Biotechnology), ANS03 (Avistone Biotechnology), MYTX-011 (Mythic Therapeutics), A166 (Sichuan Kelun-Biotech Bio-pharmaceutical), Atamparib (BN-2397) (Ribon Therapeutics), DELTACEL (KB-GDT-01) (Kiromic BioPharma), Carotuximab (ENV-105) (Kairos Pharma), YL202 (MediLink Therapeutics), and others. To know more about the number of competing drugs in development, visit @ TEPMETKO Market Positioning Compared to Other Drugs Key Milestones of TEPMETKO In February 2024, the FDA granted traditional approval to TEPMETKO for adult patients with metastatic NSCLC harboring MET exon 14 skipping alterations. In February 2022, the EC approved TEPMETKO as monotherapy for the treatment of adult patients with advanced NSCLC harboring alterations leading to METex14 skipping who require systemic therapy following prior treatment with immunotherapy and/or platinum-based chemotherapy. In February 2021, Merck announced that the US FDA has approved TEPMETKO following priority review for the treatment of adult patients with metastatic NSCLC harboring MET exon 14 skipping alterations. This indication was approved under accelerated approval based on ORR and DOR. In October 2020, TEPMETKO received ODD for treating NSCLC with MET genomic tumor aberrations In March 2020, EMD Serono (the biopharmaceutical business of Merck KGaA), announced that the MHLW approved TEPMETKO for the treatment of patients with unresectable, advanced, or recurrent NSCLC with METex14 skipping alterations. In September 2019, the US FDA granted BTD for tepotinib in patients with metastatic NSCLC harboring METex14 skipping alterations who progressed following platinum-based cancer therapy Discover how TEPMETKO is shaping the NSCLC treatment landscape @ TEPMETKO NSCLC TEPMETKO Market Dynamics TEPMETKO competes in a growing but highly specialized market where MET-targeted therapies are gaining traction due to their efficacy in addressing MET-altered tumors. The market for MET inhibitors is expanding as precision oncology advances and molecular diagnostics become more widely available, enabling better identification of patients who would benefit from targeted treatments like TEPMETKO. A key factor shaping TEPMETKO's market dynamics is competition. It directly competes with Novartis' TABRECTA (capmatinib), another MET inhibitor approved for the same indication. While TEPMETKO offers the advantage of once-daily dosing compared to TABRECTA's twice-daily regimen, both drugs have similar efficacy profiles, making physician and patient preference an important differentiator. Additionally, broader competition from next-generation MET inhibitors and combination therapies in clinical trials could impact TEPMETKO's long-term market position. Regulatory approvals and market access play a crucial role in TEPMETKO's adoption. The drug has been approved in multiple regions, including the U.S., Europe, and Japan, but reimbursement and pricing strategies vary by market. Payer policies, along with the cost-benefit analysis of MET inhibitors compared to other targeted therapies, influence prescription trends. Furthermore, real-world evidence and post-marketing studies will be critical in demonstrating TEPMETKO's sustained effectiveness and safety, which could support expanded indications and increased market penetration. Looking ahead, the MET inhibitor market is expected to grow with advances in biomarker-driven therapy, further refining patient selection. TEPMETKO's success will depend on continued clinical development, potential label expansions, and strategic partnerships to strengthen its competitive edge. As new entrants emerge, Merck KGaA's ability to differentiate TEPMETKO through combination strategies or enhanced formulations may determine its long-term sustainability in this evolving landscape. Dive deeper to get more insight into TEPMETKO's strengths & weaknesses relative to competitors @ TEPMETKO Market Drug Report Table of Contents Related Reports Non-small Cell Lung Cancer Market Non-small Cell Lung Cancer Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key NSCLC companies including Daiichi Sankyo, AstraZeneca, Gilead Sciences, BieGene, AbbVie, Roche, Merck, Novartis, Pfizer, Takeda Pharmaceuticals, Eli Lilly, BerGenBio, GlaxoSmithKline, Duality biologics, among others. Non-small Cell Lung Cancer Pipeline Non-small Cell Lung Cancer Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key non-small cell lung cancer companies, including BridgeBio Pharma, Daiichi Sankyo, EMD Serono, Merck, BridgeBio Pharma, Abbvie, Pfizer, Eli Lilly and Company BioNTech SE, Shenzhen TargetRx, Taiho Pharmaceutical, Chong Kun Dang, Bristol Myers Squibb, Innovent Biologics, Xuanzhu Biopharmaceutical, Bayer, GeneScience Pharmaceuticals, InventisBio, Apollomics, Imugene, Ono Pharmaceutical, Pierre Fabre, Jiangsu Hengrui Medicine Co., Bristol-Myers Squibb, Surface Oncology, Inhibrx, Sinocelltech, Mirati Therapeutics, REVOLUTION Medicines, Yong Shun Technology Development, Iovance Biotherapeutics, Galecto Biotech, among others. C-MET Metastatic Non-small Cell Lung Cancer Market C-MET Metastatic Non-small Cell Lung Cancer Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key C-MET mNSCLC companies, including Novartis, Merck, EMD Serono, AbbVie, Regeneron Pharmaceuticals, Mythic Therapeutics, Apollomics, Johnson & Johnson Innovation, Haihe Biopharma, among others. C-MET Non-small Cell Lung Cancer Pipeline C-MET Non-small Cell Lung Cancer Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key C-MET non-small cell lung cancer companies, including AbbVie, Janssen Research & Development, Beijing Pearl Biotechnology Limited Liability Company, Novartis, among others. About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports pharma companies by providing comprehensive end-to-end solutions to improve their performance. Get hassle-free access to all the healthcare and pharma market research reports through our subscription-based platform PharmDelve . Contact Us Shruti Thakur [email protected] +14699457679 Logo: SOURCE DelveInsight Business Research, LLP WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Drug ApprovalImmunotherapyPriority Review

03 Jun 2024

·www.biopharmadive.com

ASCO24: Tagrisso in the spotlight, Caribou’s adjustment and Lilly’s KRAS competitor

BioPharma Dive is testing out a new format rounding up smaller updates from around the industry. Have thoughts on what could make this type of story better? Drop us a line!Over the weekend at the American Society of Clinical Oncologys annual meeting in Chicago, cancer researchers and doctors detailed fresh findings from hundreds of clinical trials.We covered in detail results from a few of the most significant, including for AstraZeneca and Daiichi Sankyos Enhertu and GSKs Blenrep. There were many more important studies we didnt cover with a full story, but several of which weve summarized in brief here:AstraZeneca may find another use for its top-selling drug Tagrisso based on data presented at ASCO. The so-called LAURA trial tested the drug in people whose non-small cell lung cancer had an EGFR mutation and couldnt be surgically removed. Participants had completed chemo and radiation therapy beforehand, and their cancer hadnt spread much beyond one lung. Results from the 216-person study showed Tagrisso reduced the relative risk of death or progression by 84%, compared to a placebo. Trial investigators didnt test Tagrisso against AstraZenecas own immunotherapy Imfinzi, which is approved to treat these patients. Experts said Imfinzi doesnt work well in EGFR-mutated cancer, though. Jonathan GardnerShares in Caribou Biosciences fell by nearly a quarter Monday after the biotechnology company presented updated trial data for its off-the-shelf CAR-T cell therapy. The results, from 46 patients with relapsed or refractory B cell lymphoma, showed lower rates of treatment response and remission than a previous readout last summer from about one-third as many patients. Treatment appeared to lead to longer median progression-free survival in patients whose CAR-T therapy was built from more closely matched donor cells. Caribou plans to study this approach more closely, and has delayed the start of a planned Phase 3 trial as a result. Ned PagliaruloTwo cancer drugs capable of targeting KRAS mutations once considered undruggable are on the market in the U.S. Eli Lilly hopes its experimental candidate olomorasib can join them and, at ASCO, made a case for why. Results from a Phase 1/2 study showed the drug shrank tumors in 35% of enrolled patients with solid tumors other than colon cancer. Only 1% of those participants discontinued treatment due to side effects, Lilly said. The company also tested olomorasib in combination with Keytruda, a regimen that led to responses in 77% of 17 previously untreated people with metastatic lung cancer. A larger Phase 3 trial is now enrolling. Ned PagliaruloOver the past several years, drugmakers have tested immunotherapy earlier and earlier, exploring its use during and after surgery. A study by Bristol Myers Squibb showed that before surgery, or neoadjuvant, treatment with Opdivo and Yervoy led to better outcomes than did adjuvant Opdivo treatment in people with Stage 3 melanoma. The data confirmed earlier findings from smaller studies and, researchers said, provided a template for other neoadjuvant immunotherapy trials. Ned Pagliarulo '

Clinical ResultPhase 3ImmunotherapyASCOCell Therapy

01 Jun 2024

·www.prnewswire.com

Updated Data from the Phase 1/2 Study of Olomorasib in KRAS G12C-Mutant Advanced Solid Tumors Presented at the 2024 ASCO® Annual Meeting

Data demonstrated promising monotherapy activity with olomorasib across a range of KRAS G12C-mutant solid tumors, including non-small cell lung cancer, and a tolerability profile in combination with pembrolizumab that is well-suited to first-line lung cancer development INDIANAPOLIS, June 1, 2024 /PRNewswire/ -- Eli Lilly and Company (NYSE: LLY) today announced updated data from the Phase 1/2 clinical trial evaluating olomorasib as a monotherapy in patients with KRAS G12C-mutant advanced solid tumors and in combination with Merck's anti-PD-1 therapy KEYTRUDA® (pembrolizumab) in patients with KRAS G12C-mutant advanced non-small cell lung cancer (NSCLC). Olomorasib is an investigational, oral, potent, and highly selective second-generation inhibitor of the KRAS G12C protein. These data will be shared in oral presentations at the 2024 American Society of Clinical Oncology (ASCO) Annual Meeting. "Despite recent advances, there remains a significant unmet need for patients with KRAS G12C-mutant cancers," said Timothy Burns, M.D., Ph.D., Associate Professor of Medicine, University of Pittsburgh Medical Center Hillman Cancer Center. "These data show efficacy with olomorasib across tumor types and, importantly, tolerability that suggests it can be combined with immunotherapy, the backbone of first-line treatment for KRAS-mutant NSCLC. In NSCLC, it is also exciting to see promising activity in patients previously treated with a KRAS G12C inhibitor as well as central nervous system (CNS) activity, consistent with the improved potency of this second generation KRAS G12C inhibitor. Collectively, these data point to a promising emerging profile for olomorasib, particularly in NSCLC where new options are needed to improve outcomes for patients." "As a second generation KRAS G12C inhibitor, olomorasib was specifically designed to offer a differentiated profile that could potentially overcome limitations of currently available treatment options," said David Hyman, M.D., chief medical officer, Lilly. "With these updated data, we are pleased to see our thesis for olomorasib continuing to translate clinically. Through our SUNRAY-01 study, we look forward to further investigating the potential of olomorasib in combination with pembrolizumab-containing regimens in first-line NSCLC, where there remains great need to further impact the disease trajectory for patients with KRAS G12C-mutant lung cancers." Data from the LOXO-RAS-20001 Phase 1/2 Study Results presented at ASCO utilized a cutoff date of March 18, 2024. Efficacy results are based on investigator response assessments, and objective response rates (ORR) include responses that are confirmed, as well as those pending confirmation and ongoing. Olomorasib as Monotherapy in KRAS G12C-Mutant Advanced Solid Tumors An oral presentation (abstract #3007) detailed updated data for olomorasib monotherapy in patients with KRAS G12C-mutant advanced solid tumors. This dataset consisted of 184 patients, including 42 with NSCLC naïve to a KRAS G12C inhibitor (six with active brain metastases), 41 with NSCLC who had received a prior KRAS G12C inhibitor, 32 with colorectal cancer (CRC), 24 with pancreatic cancer, and 45 with other solid tumors. Patients had received a median of three prior lines of therapy (range 0-11). Efficacy for olomorasib monotherapy was consistent across a range of solid tumors with an ORR of 35% (37/105) in patients with non-CRC solid tumors. Median progression free survival (PFS) in all patients with KRAS G12C inhibitor-naive non-CRC solid tumors was 7.1 months (95% CI: 5.5-8.9) and 7.9 months (95% CI: 4.1-NE) in patients with KRAS G12C inhibitor-naive NSCLC. In patients with NSCLC previously treated with a KRAS G12C inhibitor, the ORR was 41% (16/39), with 63% having received a KRAS G12C inhibitor as their immediate prior therapy, and median PFS was 8.1 months (95% CI: 5.6-15.6). Preliminary CNS activity was seen, with CNS responses observed in patients with NSCLC and measurable brain metastases. Patients were on treatment for a median of 4.7 months and treatment-related adverse events (TRAEs) were predominantly grade 1 with only diarrhea seen in greater than 15% of patients. The most common TRAEs of any grade were diarrhea (23%), nausea (11%), and fatigue (10%). The safety profile for patients who discontinued a prior KRAS G12C inhibitor due to toxicity was similar to all patients treated with olomorasib monotherapy including patients who discontinued their previous first KRAS G12C inhibitor due to toxicity. TRAEs led to discontinuation of olomorasib in 1% of patients. Olomorasib in Combination with Pembrolizumab in KRAS G12C-Mutant Advanced NSCLC An oral presentation (abstract #8510) detailed updated data for olomorasib in combination with pembrolizumab in patients with KRAS G12C-mutant advanced NSCLC, studying the two doses (50mg and 100mg BID) under ongoing investigation in first-line NSCLC. This dataset consisted of 64 patients, including patients with first-line metastatic disease and those previously treated (prior KRAS G12C inhibitor, chemotherapy, and/or immunotherapy). Patients received a median of two prior lines of therapy (range: 0-8). In patients with first-line metastatic NSCLC, across a range of PD-L1 levels, the ORR for olomorasib in combination with pembrolizumab was 77% (13/17) and median PFS was not reached with follow-up ongoing. The most common TRAEs of any grade were diarrhea (23%), increased ALT (20%), pruritus (19%), increased AST (16%), and fatigue (16%). TRAEs led to discontinuation of olomorasib only in 3% of patients (2/64), pembrolizumab only in 11% of patients (7/64) and both drugs in 5% of patients (3/64). The SUNRAY-01 trial (NCT06119581), a global, registrational study investigating olomorasib in combination with pembrolizumab or pembrolizumab plus chemotherapy in first-line NSCLC, is currently enrolling. KEYTRUDA® is a registered trademark of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc., Rahway, NJ, USA. About the LOXO-RAS-20001 Study LOXO-RAS-20001 is an open-label, multicenter, Phase 1/2 study evaluating the safety, tolerability and preliminary efficacy of olomorasib in patients with KRAS G12C-mutant advanced solid tumors (NCT04956640). The study includes a Phase 1a dose escalation phase of olomorasib monotherapy in KRAS G12C-mutant solid tumors and a Phase 1b dose expansion and optimization phase which are evaluating olomorasib as a monotherapy and in combination with other treatments. About Olomorasib Olomorasib (LY3537982) is an investigational, oral, potent, and highly selective second-generation inhibitor of the KRAS G12C protein. KRAS is the most common oncogene across all tumor types, and KRAS G12C mutations occur in 13% of patients with non-small cell lung cancer (NSCLC) and 1-3% of patients with other solid tumors.1,2 Olomorasib was specifically designed to target KRAS G12C mutations and has pharmacokinetic properties which allow for high predicted target occupancy and high potency when used as monotherapy or in combination.3 Olomorasib is currently being studied in the LOXO-RAS-20001 Phase 1/2 trial (NCT04956640) in patients with KRAS G12C-mutant NSCLC and other advanced solid tumors and in the pivotal, registrational SUNRAY-01 global study (NCT06119581) investigating olomorasib in combination with pembrolizumab with or without chemotherapy for first-line treatment of KRAS G12C-mutant advanced NSCLC. For additional information about olomorasib clinical trials, please refer to clinicaltrials.gov. About Lilly Lilly is a medicine company turning science into healing to make life better for people around the world. We've been pioneering life-changing discoveries for nearly 150 years, and today our medicines help more than 51 million people across the globe. Harnessing the power of biotechnology, chemistry and genetic medicine, our scientists are urgently advancing new discoveries to solve some of the world's most significant health challenges: redefining diabetes care; treating obesity and curtailing its most devastating long-term effects; advancing the fight against Alzheimer's disease; providing solutions to some of the most debilitating immune system disorders; and transforming the most difficult-to-treat cancers into manageable diseases. With each step toward a healthier world, we're motivated by one thing: making life better for millions more people. That includes delivering innovative clinical trials that reflect the diversity of our world and working to ensure our medicines are accessible and affordable. To learn more, visit Lilly.com and Lilly.com/news, or follow us on Facebook, Instagram and LinkedIn. P-LLY © Lilly USA, LLC 2024. ALL RIGHTS RESERVED. Cautionary Statement Regarding Forward-Looking Statements This press release contains forward-looking statements (as that term is defined in the Private Securities Litigation Reform Act of 1995) about olomorasib as a potential treatment for people with certain KRAS G12C-mutant advanced solid tumors and reflects Lilly's current beliefs and expectations. However, as with any pharmaceutical product, there are substantial risks and uncertainties in the process of drug research, development, and commercialization. Among other things, there is no guarantee that planned or ongoing studies will be completed as planned that future study results will be consistent with study results to date, that olomorasib will prove to be a safe and effective treatment for people with certain KRAS G12C-mutant advanced solid tumors, that olomorasib receive regulatory approval, or that Lilly will execute its strategy as expected. For further discussion of these and other risks and uncertainties that could cause actual results to differ from Lilly's expectations, see Lilly's Form 10-K and Form 10-Q filings with the United States Securities and Exchange Commission. Except as required by law, Lilly undertakes no duty to update forward-looking statements to reflect events after the date of this release. 1 Canon J. et al. Nature 2019, 575, 217-223 2 Salem M. et al. Ann Oncol 2021, 32 (3 Suppl): S218 3 Peng S-B, Si C, Zhang Y, et al. Abstract 1259: Preclinical characterization of Ly3537982, a novel, highly selective and potent KRAS-G12C inhibitor. Cancer Research. 2021;81(13_Supplement):1259-1259. doi:10.1158/1538-7445.am2021-1259 SOURCE Eli Lilly and Company

Clinical ResultPhase 1ASCOImmunotherapy

100 Deals associated with Olomorasib

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
KRAS G12C mutant Non-small Cell Lung Cancer	Phase 3	United States	Eli Lilly & Co.	21 Dec 2023
KRAS G12C mutant Non-small Cell Lung Cancer	Phase 3	China	Eli Lilly & Co.	21 Dec 2023
KRAS G12C mutant Non-small Cell Lung Cancer	Phase 3	Japan	Eli Lilly & Co.	21 Dec 2023
KRAS G12C mutant Non-small Cell Lung Cancer	Phase 3	Australia	Eli Lilly & Co.	21 Dec 2023
KRAS G12C mutant Non-small Cell Lung Cancer	Phase 3	Austria	Eli Lilly & Co.	21 Dec 2023
KRAS G12C mutant Non-small Cell Lung Cancer	Phase 3	Belgium	Eli Lilly & Co.	21 Dec 2023
KRAS G12C mutant Non-small Cell Lung Cancer	Phase 3	Brazil	Eli Lilly & Co.	21 Dec 2023
KRAS G12C mutant Non-small Cell Lung Cancer	Phase 3	Canada	Eli Lilly & Co.	21 Dec 2023
KRAS G12C mutant Non-small Cell Lung Cancer	Phase 3	Czechia	Eli Lilly & Co.	21 Dec 2023
KRAS G12C mutant Non-small Cell Lung Cancer	Phase 3	Denmark	Eli Lilly & Co.	21 Dec 2023

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04956640 (LOXO-RAS-20001, ASCO2024) Manual	Phase 1/2	KRAS G12C mutant Non-small Cell Lung Cancer KRAS G12C	50	OlomorasibOlomorasib 50 mg BIDpembrolizumab	veyqpnwxdo(oiqonzsgtp) = vzcseigfsi azsejxezaj (mofubczhgg, 78 - 99) View more	Positive	24 May 2024
				Olomorasib+pembrolizumab (PD-L1 ≥50%)	lukdwgfzmi(antcmjpqjg) = snjdjqibqo upvayqzizo (onvxeiozqr )
NCT04956640 (LOXO-RAS-20001, ASCO2024) Manual	Phase 1/2	KRAS G12C mutation Solid Tumors KRAS G12C	157	Olomorasib 50-200 mg BID PO	pbvpgyqggj(jydfgfbzcq) = oanlwtwblr yvqofblvuh (ltsjvmeuwl ) View more	Positive	24 May 2024
				Olomorasib (CRC)	pbvpgyqggj(jydfgfbzcq) = kpftuzcccg yvqofblvuh (ltsjvmeuwl ) View more
NCT04956640 (LOXO-RAS-20001, ASCO_GI2024) Manual	Phase 1	Gastrointestinal Neoplasms KRAS G12C	119	LY3537982	nvweepxhsp(dkgxqnujkl) = chesorkzrg ljnvwpfphn (qewkcwczln ) View more	Positive	18 Jan 2024
				LY3537982 (CRC)	trdahhhicj(iwphtyoqwj) = qhpbscxyqs favdfdcspi (phxxbitwwz ) View more
NCT04956640 (LOXO-RAS-20001, AACR 12023 \| AACR 22023) Manual	Phase 1	KRAS G12C mutation Solid Tumors KRAS G12C Mutation	56	LY3537982 (NSCLC (KRAS G12Ci naïve))	cuypyhuhga(uorqvdggfo) = No DLTs were observed dqfkygwius (qoamwitexl ) View more	Positive	15 Apr 2023
				LY3537982 (NSCLC(Prior KRAS G12Ci treated))

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