RegulationFast Track (United States), Accelerated Approval (United States), Orphan Drug (United States), Priority Review (China), Breakthrough Therapy (China), Conditional marketing approval (China)

Structure/Sequence

Molecular FormulaC36H45N7O8

InChIKeyYXYAEUMTJQGKHS-UHFFFAOYSA-N

CAS Registry2389149-74-8

Clinical Trials associated with Mobocertinib Succinate

NCT07686185

/ Not yet recruitingNot ApplicableIIT

A Non-interventional, Real-World Study of Third-Generation EGFR-TKI Adjuvant Therapy in Chinese EGFR-Positive Stage IA Non-Small Cell Lung Cancer Patients With High-Risk Factors

This study aims to evaluate the real-world effectiveness and safety of third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs)-such as osimertinib, aumolertinib, and furmonertinib-as adjuvant therapy for patients with early-stage non-small cell lung cancer (NSCLC) in China.
Approximately 500 eligible patients are planned to be enrolled. All participants must have been diagnosed with Stage IA NSCLC (according to the 8th edition of the AJCC staging system) following surgical resection, harboring EGFR-sensitive mutations, and presenting with high-risk recurrence factors (e.g., poor differentiation, lymphovascular invasion, and spread through air spaces).
This is a non-interventional, real-world study that does not alter physicians' original prescribing habits or clinical management strategies. Patients will receive standard treatment with third-generation EGFR-TKIs according to routine clinical practice (typically for a duration of three years). The research team will periodically collect follow-up data, with a primary focus on postoperative disease-free survival (DFS) and drug safety profiles.
Through this investigation, we seek to determine whether this specific population of high-risk early-stage patients can derive clinical benefit from postoperative targeted therapy. The findings are expected to provide evidence to support the development of future clinical guidelines.

Start Date01 Sep 2026

Sponsor / Collaborator

First Affiliated Hospital of Guangxi Medical University

NCT07615348

/ RecruitingPhase 2IIT

A Phase II Trial of CD70-Targeted Immuno-PET/CT-Directed Treatment Holiday for Metastatic Clear Cell Renal Cell Carcinoma With IMDC Favorable or Intermediate Risk

The purpose of this study is to evaluate the safety and feasibility of a treatment holiday strategy directed by CD70-targeted immuno-PET/CT in patients with metastatic clear cell renal cell carcinoma (mccRCC). Specifically, the study aims to assess whether patients who achieve both anatomical disease control and metabolic response after 12 months of first-line PD-1/PD-L1 ICI + VEGFR-TKI combination therapy can safely pause their treatment, improve quality of life without compromising therapeutic efficacy.

Start Date16 Jun 2026

Sponsor / Collaborator-

NCT07637448

/ RecruitingPhase 2IIT

A Clinical Study Evaluating the Preliminary Antitumor Activity and Safety of EGFR-TKIs Combined With PD-1 Monoclonal Antibody as First-Line Therapy in Patients With EGFR-Mutant Advanced Non-Small Cell Lung Cancer

This study is an open-label, multicenter, single-arm clinical study.

Start Date21 May 2026

Sponsor / Collaborator

Nanfang Hospital

100 Clinical Results associated with Mobocertinib Succinate

100 Translational Medicine associated with Mobocertinib Succinate

100 Patents (Medical) associated with Mobocertinib Succinate

2,736

Literatures (Medical) associated with Mobocertinib Succinate

01 Dec 2026·BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Metabolic reprogramming underlying EGFR-TKI resistance in lung cancer

Review

Author: Ge, Di ; Xu, Fengkai ; Zhan, Cheng ; Huang, Xiaolong ; Cheng, Tao

Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) have significantly improved the clinical efficacy in non-small cell lung cancer (NSCLC) patients with EGFR mutations. However, acquired resistance to EGFR-TKIs remains an unavoidable therapeutic bottleneck. The metabolic reprogramming underlying this resistance is crucial for understanding the resistance mechanisms and identifying new therapeutic targets. Recently, an increasing number of studies have focused on the impact of metabolic reprogramming on acquired EGFR-TKI resistance. Collectively, this review reveals the core driving role of metabolic reprogramming in EGFR-TKI resistance, focuses on the systematic adjustments of resistant cells in terms of glucose metabolism, lipid metabolism, amino acid metabolism, and nucleotide metabolism, and also pays attention to the effects of ferroptosis and changes in the metabolic pattern of the tumor immune microenvironment on EGFR-TKI resistance. In addition, we summarize the application of potential therapeutic approaches targeting metabolic reprogramming in overcoming lung cancer resistance.

01 Nov 2026·Translational Oncology

NAT-A exhibits anti-tumor activity against acquired epidermal growth factor receptor- tyrosine kinase inhibitor-resistant non-small cell lung cancer via inhibiting the β-catenin/PKM2 axis

Article

Author: Wang, Shuping ; Sun, Yanxi ; Lin, Xiao ; Wang, Xinkai ; Wang, Xin ; Jiao, Weihua ; Zhou, Yongjun ; Liao, Yahui ; Wu, Ying ; Zhou, Guohua ; He, Qi ; Guan, Li ; Lin, Hou Wen ; Sun, Fan ; Liu, Liyun

Hyperactivation of the Wnt/β-catenin pathway is a key driver of epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI) resistance in non-small cell lung cancer (NSCLC), with pyruvate kinase M2 (PKM2) serving as a critical transcriptional coactivator of β-catenin. We show that PKM2 upregulation is associated with TKI resistance through stabilizing β-catenin and amplifying Wnt/β-catenin signaling, suggesting a non-canonical or catalytic activity-independent role of PKM2. Here, we identify Neoantimycin-A (NAT-A), a natural compound isolated from Streptomyces conglobatus by our group, as a novel therapeutic agent that suppresses EGFR-TKI-resistant NSCLC. Mechanistically, NAT-A disrupts the interaction between phosphorylated PKM2 (Ser37/Y105) and β-catenin, promoting β-catenin degradation in a PKM2-dependent manner and subsequent suppression of downstream oncogenic signaling. Both in vitro and in vivo studies confirm NAT-A's anti-tumor efficacy, including inhibition of cell proliferation and induction of apoptosis in EGFR-TKI-resistant models. Our findings demonstrate that activation of the PKM2/β-catenin axis drives EGFR-TKI resistance, and highlight NAT-A as a candidate agent that interferes with their interaction to exert anti-tumor effects against refractory EGFR-TKI-resistant NSCLC.

01 Oct 2026·COMPUTATIONAL BIOLOGY AND CHEMISTRY

Unveiling the potential mechanisms of gefitinib-induced neurotoxicity: A network toxicology approach

Article

Author: Jiang, Lan ; Wang, Xiaorong ; Jie, Wenqiao ; Ma, Cui

Gefitinib, a first-line EGFR-TKI for NSCLC, frequently causes neurotoxic side effects, yet its underlying molecular mechanism remains poorly defined. This study adopted integrated network toxicology and molecular docking to uncover key targets and pathways driving gefitinib-induced neuronal damage. Gefitinib-targeted and neurotoxicity-related genes were intersected to identify 26 shared hub genes, including EGFR, MAPK3, MAPK14, ERBB2, and CASP3. KEGG enrichment analysis indicated that the MAPK signaling pathway dominated toxic processes, and molecular docking verified stable, high-affinity binding between gefitinib and these five core proteins (binding energy: -8.0 to -6.4 kcal/mol). Collectively, gefitinib suppresses neuronal EGFR, hyperactivates MAPK cascades and triggers CASP3-dependent apoptosis, which constitutes the core mechanism of its neurotoxicity. This work provides predictive molecular evidence for subsequent experimental validation and safer clinical use of gefitinib.

302

News (Medical) associated with Mobocertinib Succinate

13 Oct 2026

·www.biospace.com

Merck Showcases First-Time Pivotal Phase 3 Results From Oncology Pipeline and Continued Innovative Potential of Existing Portfolio at ESMO 2026

INTerpath-001 data to be presented in Presidential Symposium, featuring the first Phase 3 results for investigational intismeran autogene plus KEYTRUDA ® (pembrolizumab), demonstrating improvements in recurrence-free survival and distant metastasis-free survival versus KEYTRUDA alone in patients with completely resected stage IIB-IV melanoma in the adjuvant setting Investigational sacituzumab tirumotecan (sac-TMT) data from TroFuse-005, the first and only Phase 3 trial of a TROP2-directed antibody-drug conjugate to improve overall survival and progression-free survival in certain patients with advanced or recurrent endometrial cancer, will be presented in a Presidential Symposium KEYNOTE-C93 data to be presented in Presidential Symposium suggesting important role of first-line KEYTRUDA monotherapy for certain patients with mismatch repair deficient (dMMR) advanced or recurrent endometrial cancer RAHWAY, N.J.--(BUSINESS WIRE)-- $MRK #MRK --Merck (NYSE: MRK), known as MSD outside of the United States and Canada, today announced that first-time results from three pivotal clinical trials will be presented during late-breaking Presidential Symposia at the European Society for Medical Oncology (ESMO) Congress 2026 in Madrid, Spain from Oct. 23-27. Additionally, more than 90 additional abstracts across more than 20 tumor types from the company’s pipeline and portfolio will be presented throughout the meeting. “New data at ESMO, including three Presidential Symposia from three pivotal trials, reflect the strength and depth of Merck’s industry-leading oncology portfolio and pipeline,” said Dr. Marjorie Green, senior vice president and head of oncology global clinical development, Merck Research Laboratories. "We are proud to share Phase 3 data for the first time from intismeran and sac-TMT, alongside new research from our oncology portfolio, reflecting our commitment to advancing research across a range of cancer types." Key data from Merck’s pipeline and portfolio to be presented: First presentation of data from the pivotal Phase 3 INTerpath-001 trial evaluating intismeran autogene (intismeran; V940/mRNA-4157), a novel investigational mRNA-based individualized neoantigen therapy, in combination with KEYTRUDA ® (pembrolizumab), Merck’s anti-PD-1 therapy, as adjuvant treatment for patients with completely resected stage IIB-IV melanoma, which will be featured in an ESMO Presidential Symposium (Presentation #LBA1, Proffered paper session: Presidential Symposium I). 1 First presentation of data from the pivotal Phase 3 TroFuse-005 trial evaluating sacituzumab tirumotecan (sac-TMT), an investigational trophoblast cell-surface antigen 2 (TROP2)-directed antibody-drug conjugate, for patients with advanced or recurrent endometrial cancer who have progressed after platinum-based chemotherapy and a programmed death receptor-1 (PD-1) or programmed death-ligand 1 (PD-L1) inhibitor, which will be featured in an ESMO Presidential Symposium (Presentation #LBA11, Proffered paper session: Presidential Symposium III). 2,3 First presentation of data from the Phase 3 KEYNOTE-C93 trial evaluating KEYTRUDA monotherapy as a first-line treatment for patients with mismatch repair deficient (dMMR) advanced or recurrent endometrial cancer who had not previously received systemic chemotherapy or who experienced recurrence after receiving prior adjuvant therapy, which will be featured in an ESMO Presidential Symposium (Presentation #LBA12, Proffered paper session: Presidential Symposium III). 3 Data from Phase 3 OptiTROP studies evaluating sac-TMT in non-small cell lung cancer (NSCLC), including results from the OptiTROP-Lung06 study (Presentation #LBA66) in first-line PD-L1-negative advanced non-squamous NSCLC and final overall survival data from the OptiTROP-Lung04 study (Presentation #LBA67) in epidermal growth factor receptor (EGFR)-mutated NSCLC following progression on EGFR tyrosine kinase inhibitors (TKIs) (Proffered paper session 1: NSCLC, metastatic). 4 Final analysis results from the Phase 3 LITESPARK-011 study evaluating WELIREG ® (belzutifan), Merck’s first-in-class, oral hypoxia-inducible factor-2 alpha (HIF-2α) inhibitor, in combination with LENVIMA ® (lenvatinib), an orally available multiple receptor TKI discovered by Eisai, for patients with advanced renal cell carcinoma with a clear cell component following a PD-1 or PD-L1 inhibitor (Presentation #3587O, Proffered paper session 2: Genitourinary tumours, renal and urothelial). 5 Merck investor event Merck will hold an Oncology Investor Event to coincide with the ESMO 2026 Congress on Monday, October 26, 7:30 p.m. CET/2:30 p.m. ET, during which senior management will provide an update on the company’s oncology strategy and program. The event will take place in Madrid, Spain, and will be accessible via webcast. Investors, analysts, members of the media and the general public are invited to listen to a webcast of the presentation via this weblink . All participants may join the call by dialing (800) 369-2154 (U.S. and Canada Toll-Free) or (517) 308-9422 and using the access code 8984239. Details on presentations listed above and additional key presentations for Merck Breast cancer Final OS analysis of sacituzumab tirumotecan versus chemotherapy in previously treated locally recurrent or metastatic triple-negative breast cancer: Phase III OptiTROP-Breast01. M. Li. 4 Presentation #4639RO, Rapid oral session 2: Breast cancer, advanced stage Results from KEYNOTE-B49: A Phase 3, randomized, double-blind study of pembrolizumab (pembro) vs placebo (pbo) plus chemotherapy (CT) in participants (pts) with HR+/HER2− advanced breast cancer (ABC). H. S. Rugo. Presentation #LBA51, Proffered paper session 2: Breast cancer, early and advanced stage Association between disease control and patient-reported functioning and quality of life in the ASCENT-04/KEYNOTE-D19 study. K. Kalinsky. 6 Presentation #4659P, Poster session: Triple negative breast cancer Gastrointestinal cancers Adjuvant intismeran autogene plus FOLFIRINOX in resectable pancreatic ductal adenocarcinoma: Results from a Phase I study. D. J. Pinato. 1 Presentation #3151P, Poster session: Pancreatic cancer Genitourinary cancers Final analysis of the Phase 3 LITESPARK-011 study: Belzutifan (bel) plus lenvatinib (len) versus cabozantinib (cabo) for advanced renal cell carcinoma (RCC) after anti-PD-(L)1 therapy. D. Y. Heng. 5 Presentation #3587O, Proffered paper session 2: Genitourinary tumours, renal and urothelial Final protocol-prespecified analysis of the Phase 3 KEYNOTE-564 trial of adjuvant pembrolizumab versus placebo in clear cell renal cell carcinoma (ccRCC). T. K. Choueiri. Presentation #3589RO, Rapid oral session 2: Genitourinary tumours, renal and urothelial Enfortumab vedotin (EV) with or without pembrolizumab (P) as first-line (1L) treatment for cisplatin (cis)-ineligible locally advanced or metastatic urothelial carcinoma (la/mUC): Long-term follow-up analysis from EV-103 cohorts DE/A and K. J. P. Maroto Rey. 7 Presentation #4740RO, Rapid oral session 1: Genitourinary tumours, renal and urothelial ctDNA analysis of the Phase 3 KEYNOTE-B15 trial: Neoadjuvant and adjuvant (neoadj-adj) enfortumab vedotin (EV) + pembrolizumab (pembro) for participants (pts) with muscle-invasive bladder cancer (MIBC) who are eligible for cisplatin. J. A. Chatzkel. 7 Presentation #4734O, Proffered paper session 1: Genitourinary tumour, renal and urothelial Health-related quality of life (HRQoL) with neoadjuvant and adjuvant (neoadj-adj) enfortumab vedotin (EV) plus pembrolizumab (pembro) in participants (pts) with muscle-invasive bladder cancer (MIBC) eligible for cisplatin in the Phase 3 KEYNOTE-B15 study. A. Gomez de Liano Lista. 7 Presentation #4738RO, Rapid oral session 1: Genitourinary tumours, renal and urothelial Perioperative pembrolizumab (pembro) or enfortumab vedotin (EV) plus pembro in pts with muscle-invasive bladder cancer (MIBC) who are cisplatin-ineligible: Ad hoc analysis from KEYNOTE-905. A. Ullén. 7 Presentation #4733O, Proffered paper session 1: Genitourinary tumour, renal and urothelial Sacituzumab tirumotecan (sac-TMT) + pembrolizumab (pembro) for locally advanced or metastatic urothelial carcinoma (la/mUC): Results from a Phase 2 Study (2870-002/SKB264-II-06). X. Bian. 4 Presentation #4739RO, Rapid oral session 1: Genitourinary tumours, renal and urothelial Updated results from the Phase 1b/2 KEYNOTE-365 cohort I: Pembrolizumab (pembro) + carboplatin and etoposide chemotherapy (chemo) or chemo alone for neuroendocrine prostate cancer (NEPC). G. von Amsberg. Presentation #2217RO, Rapid oral session: Genitourinary tumours, prostate, penile and testis Gynecologic cancers Sacituzumab tirumotecan in previously treated advanced or recurrent endometrial cancer: Results from the Phase 3 TroFuse-005/ENGOT-en23/GOG-3095 study. D. Lorusso. 2,3 Presentation #LBA11, Proffered paper session: Presidential Symposium III KEYNOTE-C93/GOG-3064/ENGOT-en15: Phase 3, randomized, open-label study of first-line (1L) pembrolizumab (pembro) vs carboplatin (C) + paclitaxel (P) in mismatch repair-deficient (dMMR) advanced or recurrent endometrial carcinoma (a/rEC). B. M. Slomovitz. 3 Presentation #LBA12, Proffered paper session: Presidential Symposium III Raludotatug deruxtecan (R-DXd) + bevacizumab (bev) in participants (pts) with platinum-resistant recurrent ovarian cancer (PROC): Results for cohort B-1 of the Phase 1b/2 REJOICE-Ovarian02 study. A. Oaknin. 8 Presentation #1247RO, Rapid oral session 2: Gynaecological cancers Raludotatug deruxtecan (R-DXd) in patients (pts) with platinum-resistant ovarian cancer (PROC): An updated analysis of efficacy and tolerability from the Ph 2 part of REJOICE-Ovarian01. K. Hasegawa. 8 Presentation #1331P, Poster session: Gynaecological cancers NRG-GY020: Phase III randomized trial of radiation +/- MK-3475 (pembrolizumab) for newly diagnosed early-stage high intermediate risk (HIR) mismatch repair deficient (dMMR) endometrioid endometrial cancer. F. Backes. 9 Presentation #1239O, Proffered paper session: Gynaecological cancers Sacituzumab tirumotecan (sac-TMT) + pembrolizumab (pembro) in post-platinum advanced mismatch repair proficient (pMMR) endometrial cancer (EC): Results from a Phase 2 study (2870-002/SKB264-II-06). L. Chen. 4 Presentation #1259P, Poster session: Gynaecological cancers Head and neck cancer Practical considerations for adopting perioperative pembrolizumab in locally advanced head and neck squamous cell carcinoma (LA HNSCC) in Europe: Insights from KEYNOTE-689. M. Oliva. Presentation #1580P, Poster session: Head and neck cancer, excluding thyroid Lung cancer Sacituzumab tirumotecan (sac-TMT) plus pembrolizumab (P) versus chemotherapy (chemo) plus pembrolizumab (P) as first-line (1L) treatment for PD-L1 negative advanced non-squamous (nsq) NSCLC: Randomized Phase 3 OptiTROP-Lung06 study. C. Zhou. 4 Presentation #LBA66, Proffered paper session 1: NSCLC, metastatic Final OS analysis of sacituzumab tirumotecan (sac-TMT) versus platinum-based chemotherapy in EGFR-mutated non-small cell lung cancer (NSCLC) after progression on EGFR-TKI: Phase III OptiTROP-Lung04 study. W.F. Fang. 4 Presentation #LBA67, Proffered paper session 1: NSCLC, metastatic Calderasib (MK-1084), alone or in combination, for KRAS G12C-mutant metastatic non-small cell lung cancer (mNSCLC). M. A. N. Sendur. 10 Presentation #2680RO, Rapid oral session 2: NSCLC, metastatic Final analysis of adjuvant pembrolizumab (pembro) in resected early-stage non–small-cell lung cancer (NSCLC): Phase 3 PEARLS/KEYNOTE-091 study. M. E. O’Brien. Presentation #2511O, Proffered paper session: Non-metastatic NSCLC and other thoracic malignancies Ifinatamab deruxtecan (I-DXd) in extensive-stage small cell lung cancer (ES-SCLC): IDeate-Lung01 updated results. M. Ahn. 8 Presentation #3842P, Poster session: SCLC Melanoma INTerpath-001: Phase 3 study of the mRNA-based individualized neoantigen therapy (INT) intismeran autogene (intismeran) plus pembrolizumab (pembro) vs pembro alone for adjuvant treatment of resected stage IIB-IV melanoma (MEL). G. V. Long. 1 Presentation #LBA1, Proffered paper session: Presidential Symposium I STARBOARD Phase 3: A randomized, double-blind study of first-line (1L) encorafenib (enco), binimetinib (bini) and pembrolizumab (pembro) vs placebo (pbo) and pembro for unresectable locally advanced or metastatic BRAF V600-mutant melanoma. D. Schadendorf. 7 Presentation #2071O, Proffered paper session: Melanoma and other skin tumours Physician perspectives on defining cure in early-stage melanoma. H. M. Shaw. Presentation #2173eP, ePoster session: Melanoma Patritumab deruxtecan (HER3-DXd) in melanoma after anti-PD-(L)1 therapy: Primary analysis from HERTHENA-PanTumor01. M. McKean. 8 Presentation #2073RO, Rapid oral session: Melanoma and other skin tumours Multi-tumor Final results of the TUXEDO-3 Phase II trial of patritumab deruxtecan (HER3-DXd) in active brain metastases (BMs) and leptomeningeal disease (LMD). M. Preusser. 8 Presentation #690O, Proffered paper session: CNS tumours Calderasib monotherapy in various KRAS G12C-mutated advanced solid tumors: Results from the Phase 1 KANDLELIT-001 study. M Kwiatkowski. 10 Presentation #1039P, Poster session: Developmental therapeutics 1 In collaboration with Moderna 2 In collaboration with Kelun-Biotech 3 In collaboration with the European Network for Gynaecological Oncology Trial (ENGOT) groups and the GOG Foundation, Inc. (GOG) 4 Led by Kelun-Biotech, conducted in China 5 In collaboration with Eisai 6 In collaboration with Gilead 7 In collaboration with Astellas/Pfizer 8 In collaboration with Daiichi Sankyo 9 Sponsored by U.S. National Cancer Institute (NCI)/led by NRG Oncology 10 In collaboration with Taiho Pharmaceutical Co. Ltd and Astex Pharmaceuticals (UK), a wholly owned subsidiary of Otsuka Pharmaceutical Co., Ltd About intismeran autogene Intismeran autogene (intismeran; V940 or mRNA-4157) is a novel, potential first-in-class investigational messenger RNA (mRNA)-based individualized neoantigen therapy (INT) jointly developed by Merck and Moderna. Intismeran is designed and produced using a patient's tumor sample to identify the unique mutational signature, or "fingerprint," of their cancer and generate an anti-tumor immune response. Each therapy consists of a synthetic mRNA coding for up to 34 neoantigens and is tailored to the unique biology of an individual patient's tumor. Upon administration, the RNA-encoded neoantigen sequences are translated in the body and presented to the immune system, a key step in generating specific T-cell responses against cancer cells. Individualized neoantigen therapies are designed to train and activate an anti-tumor immune response based on the unique mutational signature of a patient's tumor. Merck and Moderna are advancing the robust INTerpath clinical development program evaluating the safety and efficacy of intismeran in combination with KEYTRUDA and other anti-cancer therapies, and as a monotherapy. About sacituzumab tirumotecan (sac-TMT) Sac-TMT is an investigational TROP2-directed ADC with a belotecan-derived topoisomerase I inhibitor payload and a unique bifunctional linker designed with the potential to maximize payload delivery to tumor cells and minimize payload loss while circulating in the body. TROP2 is overexpressed on tumor cells compared to healthy cells in many common cancers, and through the TroFuse clinical development program, Merck is evaluating sac-TMT in 18 ongoing global Phase 3 trials across multiple tumor types, the broadest range of disease and treatment settings compared to any TROP2-directed ADC to date. The TroFuse development program spans early-to-late-stage disease in more than nine disease areas and includes more than 15,000 patients worldwide. Numerous Phase 3 trials are exploring sac-TMT as monotherapy and in combination with immunotherapies, aiming to improve survival and quality of life for patients with advanced and earlier-stage cancers. About calderasib Calderasib (MK-1084) is an investigational, highly potent and specific next-generation KRAS G12C covalent inhibitor. Mutations in KRAS are among the most prevalent mutations found in cancer, occurring with high frequency in non-small cell lung cancer (NSCLC), pancreatic, urogenital and colorectal cancers. The KRAS G12C mutation is the most frequently observed KRAS mutation in patients, occurring in approximately 14% of patients with NSCLC (adenocarcinoma). Despite decades of research and recognition of the therapeutic importance of targeting KRAS , the development of small molecule inhibitors targeting KRAS mutations has been challenging. About KEYTRUDA ® (pembrolizumab) injection for intravenous use, 100 mg KEYTRUDA is an anti-programmed death receptor-1 (PD-1) therapy that works by increasing the ability of the body’s immune system to help detect and fight tumor cells. KEYTRUDA is a humanized monoclonal antibody that blocks the interaction between PD-1 and its ligands, PD-L1 and PD-L2, thereby activating T lymphocytes which may affect both tumor cells and healthy cells. Merck has the industry’s largest immuno-oncology clinical research program. There are currently more than 2,800 trials studying KEYTRUDA across a wide variety of cancers and treatment settings. The KEYTRUDA clinical program seeks to understand the role of KEYTRUDA across cancers and the factors that may predict a patient's likelihood of benefitting from treatment with KEYTRUDA, including exploring several different biomarkers. Selected Indications in the U.S. for KEYTRUDA ® (pembrolizumab) Melanoma KEYTRUDA is indicated for the treatment of patients with unresectable or metastatic melanoma. KEYTRUDA is indicated for the adjuvant treatment of adult and pediatric (12 years and older) patients with Stage IIB, IIC, or III melanoma following complete resection. Non-Small Cell Lung Cancer KEYTRUDA, in combination with pemetrexed and platinum chemotherapy, is indicated for the first-line treatment of patients with metastatic nonsquamous non-small cell lung cancer (NSCLC), with no EGFR or ALK genomic tumor aberrations. KEYTRUDA, in combination with carboplatin and either paclitaxel or paclitaxel protein-bound, is indicated for the first-line treatment of patients with metastatic squamous NSCLC. KEYTRUDA, as a single agent, is indicated for the first-line treatment of patients with NSCLC expressing PD-L1 [Tumor Proportion Score (TPS) ≥1%] as determined by an FDA-authorized test, with no EGFR or ALK genomic tumor aberrations, and is: Stage III where patients are not candidates for surgical resection or definitive chemoradiation, or metastatic. KEYTRUDA, as a single agent, is indicated for the treatment of patients with metastatic NSCLC whose tumors express PD-L1 (TPS ≥1%) as determined by an FDA-authorized test, with disease progression on or after platinum-containing chemotherapy. Patients with EGFR or ALK genomic tumor aberrations should have disease progression on FDA-approved therapy for these aberrations prior to receiving KEYTRUDA. KEYTRUDA is indicated for the treatment of patients with resectable (tumors ≥4 cm or node positive) NSCLC in combination with platinum-containing chemotherapy as neoadjuvant treatment, and then continued as a single agent as adjuvant treatment after surgery. KEYTRUDA, as a single agent, is indicated as adjuvant treatment following resection and platinum-based chemotherapy for adult patients with Stage IB (T2a ≥4 cm), II, or IIIA NSCLC. Head and Neck Squamous Cell Cancer KEYTRUDA is indicated for the treatment of adult patients with resectable locally advanced head and neck squamous cell carcinoma (HNSCC) whose tumors express PD-L1 [Combined Positive Score (CPS) ≥1] as determined by an FDA-authorized test, as a single agent as neoadjuvant treatment, continued as adjuvant treatment in combination with radiotherapy (RT) with or without cisplatin and then as a single agent. KEYTRUDA, in combination with platinum and fluorouracil (FU), is indicated for the first-line treatment of patients with metastatic or with unresectable, recurrent HNSCC. KEYTRUDA, as a single agent, is indicated for the first-line treatment of patients with metastatic or with unresectable, recurrent HNSCC whose tumors express PD-L1 (CPS ≥1) as determined by an FDA-authorized test. KEYTRUDA, as a single agent, is indicated for the treatment of patients with recurrent or metastatic HNSCC with disease progression on or after platinum-containing chemotherapy. Urothelial Cancer KEYTRUDA, in combination with enfortumab vedotin-ejfv, is indicated for the treatment of adult patients with locally advanced or metastatic urothelial cancer. KEYTRUDA, as a single agent, is indicated for the treatment of patients with locally advanced or metastatic urothelial carcinoma: who are not eligible for any platinum-containing chemotherapy, or who have disease progression during or following platinum-containing chemotherapy or within 12 months of neoadjuvant or adjuvant treatment with platinum-containing chemotherapy. KEYTRUDA, in combination with enfortumab vedotin-ejfv, as neoadjuvant treatment and then continued after cystectomy as adjuvant treatment, is indicated for the treatment of adult patients with muscle invasive bladder cancer (MIBC). KEYTRUDA, as a single agent, is indicated for the treatment of patients with Bacillus Calmette-Guerin (BCG)-unresponsive, high-risk, non-muscle invasive bladder cancer (NMIBC) with carcinoma in situ (CIS) with or without papillary tumors who are ineligible for or have elected not to undergo cystectomy. Renal Cell Carcinoma KEYTRUDA, in combination with axitinib, is indicated for the first-line treatment of adult patients with advanced renal cell carcinoma (RCC). KEYTRUDA, in combination with lenvatinib, is indicated for the first-line treatment of adult patients with advanced RCC. KEYTRUDA is indicated for the adjuvant treatment of patients with RCC at intermediate-high or high risk of recurrence following nephrectomy, or following nephrectomy and resection of metastatic lesions. KEYTRUDA, in combination with belzutifan, is indicated for the adjuvant treatment of adult patients with RCC with a clear cell component (ccRCC) at intermediate-high or high risk of recurrence following nephrectomy, or following nephrectomy and resection of metastatic lesions. Endometrial Carcinoma KEYTRUDA, in combination with carboplatin and paclitaxel, followed by KEYTRUDA as a single agent, is indicated for the treatment of adult patients with primary advanced or recurrent endometrial carcinoma. KEYTRUDA, in combination with lenvatinib, is indicated for the treatment of adult patients with advanced endometrial carcinoma that is mismatch repair proficient (pMMR) or not MSI-H as determined by an FDA-authorized test, who have disease progression following prior systemic therapy in any setting and are not candidates for curative surgery or radiation. KEYTRUDA, as a single agent, is indicated for the treatment of adult patients with advanced endometrial carcinoma that is MSI-H or dMMR, as determined by an FDA-authorized test, who have disease progression following prior systemic therapy in any setting and are not candidates for curative surgery or radiation. Contacts Media Contacts: Julie Cunningham julie.cunningham@merck.com Justine Moore justine.moore@merck.com Investor Contacts: Peter Dannenbaum (732) 594-1579 Steven Graziano (732) 594-1583 Read full story here

Clinical ResultPhase 3Phase 1Phase 2ADC

13 Oct 2026

·www.biospace.com

Kelun-Biotech to Present Multiple Study Results at ESMO 2026

CHENGDU, China , Oct. 13, 2026 /PRNewswire/ -- The 2026 European Society for Medical Oncology (ESMO) Congress will be held in Madrid, Spain, from October 23 to 27. Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. ("Kelun-Biotech" or the "Company", 6990.HK) will present results from multiple clinical studies at the congress, including data from its trophoblast cell-surface antigen 2 (TROP2)-directed antibody-drug conjugate (ADC) sacituzumab tirumotecan (sac-TMT, also known as SKB264/MK-2870) (佳泰莱 ® ) and another ADC. Among them, multiple research findings for sac-TMT have been selected for oral presentations, including the Phase III OptiTROP-Lung04 and OptiTROP-Lung06 studies, which have both been selected for the "Non-Small Cell Lung Cancer (NSCLC), Metastatic" session and will be presented in the same time slot as proffered paper reports. In addition, data from the global pivotal Phase III TroFuse-005 trial led by MSD [1] will be presented for the first time in the ESMO Presidential Symposium. The abstract titles of the above studies as well as other studies from Kelun-Biotech have been published on the official ESMO website. Details are as follows: Lung cancer Sacituzumab tirumotecan (sac-TMT) plus pembrolizumab (P) versus chemotherapy (chemo) plus pembrolizumab (P) as first-line (1L) treatment for PD-L1 negative advanced non-squamous (nsq) NSCLC: randomized phase 3 OptiTROP-Lung06 study LBA66, Proffered paper | NSCLC, metastatic October 25, 10:15 to 11:45 local time Final OS analysis of sacituzumab tirumotecan (sac-TMT) versus platinum-based chemotherapy in EGFR-mutated non-small cell lung cancer (NSCLC) after progression on EGFR-TKI: phase III OptiTROP-Lung04 study LBA67, Proffered paper | NSCLC, metastatic October 25, 10:15 to 11:45 local time SKB500 (a novel B7-H3–targeted antibody-drug conjugate) in patients with extensive-stage small cell lung cancer (ES-SCLC): Results from a Phase I study 3816RO, Rapid oral | Non-metastatic NSCLC and other thoracic malignancies October 26, 10:15 to 11:45 local time Breast cancer Final OS analysis of sacituzumab tirumotecan versus chemotherapy in previously treated locally recurrent or metastatic triple-negative breast cancer: Phase III OptiTROP-Breast01 4639RO, Rapid oral | Breast cancer, advanced stage October 26, 10:15 to 11:45 local time Gynecologic cancers Sacituzumab tirumotecan in previously treated advanced or recurrent endometrial cancer: Results from the Phase 3 TroFuse-005/ENGOT-en23/GOG-3095 study LBA11, Proffered Paper | Presidential Symposium October 26, 16:30 to 18:15 local time Sacituzumab tirumotecan (sac-TMT) + pembrolizumab (pembro) in post-platinum advanced mismatch repair proficient (pMMR) endometrial cancer (EC): Results from a Phase 2 study (2870-002/SKB264-II-06) 1259P, Poster | Gynaecological cancers October 26, 12:00 to 12:45 local time Genitourinary cancers Sacituzumab tirumotecan (sac-TMT) + pembrolizumab (pembro) for locally advanced or metastatic urothelial carcinoma (la/mUC): Results from a Phase 2 Study (2870-002/SKB264-II-06) 4739RO, Rapid oral | Genitourinary tumours, renal and urothelial October 24, 10:15 to 11:45 local time About sac-TMT ( 佳泰莱 ® ) Sac-TMT, a core product of the Company, is a novel TROP2 ADC in which the Company has proprietary intellectual property rights, targeting advanced solid tumors such as NSCLC, breast cancer (BC), gastric cancer (GC), gynecological tumors and genitourinary tumors, among others. Sac-TMT is developed with a unique, bifunctional linker that maximizes payload delivery to tumor cells both through its irreversible connection with the anti-TROP2 monoclonal antibody sacituzumab and its pH-sensitive cleavage from a belotecan-derivative topoisomerase I inhibitor payload (KL610023) in the lysosome, with a drug-to-antibody-ratio (DAR) of 7.4. Sac-TMT specifically recognizes TROP2 on the surface of tumor cells by recombinant anti-TROP2 humanized monoclonal antibodies, which is then endocytosed by tumor cells and releases the payload KL610023 intracellularly. KL610023 induces DNA damage to tumor cells, which in turn leads to cell-cycle arrest and apoptosis. In addition, it also releases KL610023 in the tumor microenvironment. Given that KL610023 is membrane permeable, it can enable a bystander effect, or in other words kill adjacent tumor cells. In May 2022, the Company licensed the exclusive rights to MSD (the tradename of Merck & Co., Inc, Rahway, NJ, USA) to develop, use, manufacture and commercialize sac-TMT in all territories outside of Greater China (which includes Mainland China, Hong Kong, Macao and Taiwan). To date, four indications for sac-TMT have been approved and marketed in China for: 1) unresectable locally advanced or metastatic triple-negative breast cancer (TNBC) who have received at least two prior systemic therapies (at least one of them for advanced or metastatic setting); 2) epidermal growth factor receptor (EGFR) mutant-positive locally advanced or metastatic non-squamous NSCLC following progression on EGFR-tyrosine kinase inhibitor (TKI) therapy and platinum-based chemotherapy; 3) EGFR mutant-positive locally advanced or metastatic non-squamous NSCLC who progressed after treatment with EGFR-TKI therapy; 4) unresectable or metastatic hormone receptor-positive (HR+)/human epidermal growth factor receptor 2-negative (HER2-) (Immunohistochemistry (IHC) 0, IHC 1+ or IHC 2+/In Situ Hybridization (ISH)-) BC who have received prior endocrine therapy and at least one line of chemotherapy in advanced setting. The first two indications above have been included in China's National Reimbursement Drug List (NRDL). This inclusion is expected to bring clinically meaningful benefits to a greater number of patients with BC and NSCLC. Additionally, sac-TMT has been granted six Breakthrough Therapy Designations by the NMPA. Sac-TMT is the world's first TROP2 ADC drug approved for marketing in lung cancer. Two new indication applications have been accepted for review by the NMPA: 1) sac-TMT in combination with pembrolizumab as first‑line treatment for locally advanced or metastatic NSCLC who have programmed cell death ligand 1 (PD-L1) tumor proportion score (TPS) ≥1% and are EGFR-negative and ALK-negative; 2) sac‑TMT as first‑line treatment for patients with recurrent or metastatic TNBC who have a PD‑L1 combined positive score (CPS) <10 or have recurred after prior programmed cell death protein 1 (PD-1)/PD‑L1 inhibitor therapy in the early stage, both of the above two applications have been included in the priority review and approval process. As of today, the Company has initiated 9 registrational clinical studies in China. MSD has initiated 18 ongoing global Phase III clinical studies of sac-TMT as a monotherapy or in combination with pembrolizumab or other anti-cancer agents for several types of cancer. These studies are sponsored and led by MSD. About SKB500 SKB500 is a B7-H3-targeted ADC independently developed by the company using its OptiDC TM platform technology, featuring a site-specific cleavable linker and a potent topoisomerase I inhibitor. In the Phase I clinical study, SKB500 demonstrated robust efficacy and manageable safety profiles across multiple advanced solid tumors. Currently, two Phase II studies of SKB500 in extensive-stage small cell lung cancer (ES-SCLC) and advanced esophageal squamous cell carcinoma (ESCC),etc. are ongoing in China. About Kelun-Biotech Kelun-Biotech (6990.HK) is a holding subsidiary of Kelun Pharmaceutical, which focuses on the R&D, manufacturing, commercialization and global collaboration of innovative biological drugs and small molecule drugs. Kelun-Biotech focuses on major disease areas such as solid tumors, autoimmune, and metabolic diseases, and in establishing a globalized drug development and industrialization platform to address the unmet medical needs in China and the rest of world. Kelun-Biotech is committed to becoming a leading global enterprise in the field of innovative drugs. At present, Kelun-Biotech has more than 30 ongoing key innovative drug projects, of which 4 projects with 8 indications have been approved for marketing, 2 projects with 3 indications are in the NDA stage and more than 10 projects are in the clinical stage. Kelun-Biotech has established one of the world's leading proprietary ADC and novel DC platforms, OptiDC TM , and has 2 ADC projects with 5 indications approved for marketing, and multiple ADC and novel DC assets in clinical or preclinical research stage. For more information, please visit: . [1] MSD is the tradename of Merck & Co., Inc, Rahway, NJ, USA. View original content to download multimedia: SOURCE Kelun-Biotech

Phase 1Phase 3Clinical ResultPhase 2Breakthrough Therapy

28 Sep 2026

·www.biospace.com

HUTCHMED Announces Submission of US NDA for ORPATHYS® plus TAGRISSO® in MET-Driven EGFR-Mutated Lung Cancer

— Filing seeks approval for a biomarker-directed, all-oral treatment option for patients whose tumors have MET overexpression or amplification, after progression on an EGFR-TKI therapy — — Application supported by SAFFRON, the first global Phase III trial to demonstrate statistically significant and clinically meaningful improvements in progression-free and overall survival in this setting — — SAFFRON builds on evidence from the SACHI Phase III and SAVANNAH Phase II trials — HONG KONG, SHANGHAI and FLORHAM PARK, N.J., Sept. 28, 2026 (GLOBE NEWSWIRE) -- HUTCHMED (China) Limited (“ HUTCHMED ”) (Nasdaq/AIM:HCM; HKEX:13) today announces that AstraZeneca has submitted a New Drug Application (“NDA”) to the US Food and Drug Administration (“FDA”) for ORPATHYS ® (savolitinib) plus TAGRISSO ® (osimertinib) for the treatment of patients with locally advanced or metastatic non-small cell lung cancer (“NSCLC”) whose tumors have MET overexpression or amplification, and who had disease progression on or after an epidermal growth factor receptor (“EGFR”) tyrosine kinase inhibitor (“TKI”) therapy. The NDA is supported by the global SAFFRON Phase III trial. SAFFRON showed ORPATHYS ® plus TAGRISSO ® demonstrated a statistically significant and clinically meaningful improvement in both progression-free survival (“PFS”) and overall survival (“OS”) versus doublet platinum-based chemotherapy in patients who progressed on treatment with TAGRISSO ® . The safety pro consistent with the known profiles of each medicine, and there were no new safety concerns. These results will be presented in a Presidential Symposium at the upcoming European Society for Medical Oncology (ESMO) Congress 2026. Third-generation EGFR tyrosine kinase inhibitors (“TKIs”) have significantly improved outcomes for patients with EGFRm NSCLC. However, MET overexpression or amplification is one of the most common mechanisms of resistance on third-generation EGFR-TKI treatment. MET-driven progression is associated with poor prognosis, and there remains a significant unmet need for effective and well-tolerated treatment options in this setting. Mr Johnny Cheng, Acting Chief Executive Officer and Chief Financial Officer of HUTCHMED , said: “This filing is an important step toward potentially bringing ORPATHYS ® plus TAGRISSO ® to patients in the US, after its approval in China based on the SACHI Phase III trial. The success of the global SAFFRON Phase III trial reflects the long-standing collaboration between HUTCHMED and AstraZeneca in addressing MET-driven progression in EGFR-mutated lung cancer. We remain committed to supporting the regulatory review and making this biomarker-directed, chemotherapy-free oral combination available to eligible patients.” ORPATHYS ® is being jointly developed by AstraZeneca and HUTCHMED and is commercialized by AstraZeneca. About NSCLC and MET aberrations Lung cancer is the leading cause of cancer death globally, accounting for almost one in four (23%) cancer deaths. 1 Lung cancer is broadly split into NSCLC and small cell lung cancer, with 80-85% of patients diagnosed with NSCLC. 2 Approximately 75% of NSCLC patients are diagnosed with advanced disease. 3 Additionally, about 10-15% of NSCLC patients in the US and Europe, and 30-40% of patients in Asia, have EGFRm NSCLC. 4 , 5 , 6 MET is a tyrosine kinase receptor that has an essential role in normal cell development. 7 MET overexpression or amplification can lead to tumor growth and the metastatic progression of cancer cells. 7 , 8 An estimated 34% of tumors will develop high levels of MET overexpression or amplification after progression on a third-generation EGFR TKI. 1 About SAFFRON SAFFRON is a randomized, open-label, multi-center, global Phase III trial studying the efficacy of ORPATHYS ® (300 mg twice daily) added to TAGRISSO ® (80 mg once daily) versus doublet platinum-based chemotherapy in 338 patients with EGFRm, locally advanced or metastatic NSCLC with MET overexpression or amplification whose disease progressed following first- or second-line treatment with TAGRISSO ® . The trial enrolled patients in 230 centers across 29 countries, including in North America, Europe, South America and Asia. The primary endpoint is PFS and key secondary endpoint includes OS. Patients were prospectively selected for SAFFRON using the high MET level cut-offs identified in the SAVANNAH Phase II trial. In SAVANNAH, MET overexpression or amplification levels were determined by two tests: immunohistochemistry (IHC), which detects if cancer cells have a particular protein or marker on their surface, and fluorescence in situ hybridization (FISH), which detects a specific DNA sequence from cancer cells. About ORPATHYS ® ORPATHYS ® (savolitinib) is an oral, potent and highly selective MET TKI that has demonstrated clinical activity in advanced solid tumors. It blocks atypical activation of the MET receptor tyrosine kinase pathway that occurs because of mutations (such as exon 14 skipping alterations or other point mutations), gene amplification or protein overexpression. ORPATHYS ® is approved in China for the treatment of adult patients with locally advanced or metastatic NSCLC with MET exon 14 skipping alteration, representing the first selective MET inhibitor approved in China. ORPATHYS ® also received a conditional approval in China for the treatment of adult patients with locally advanced or metastatic gastric cancer or gastroesophageal junction (GC/GEJ) adenocarcinoma patients with MET amplification who have failed at least two prior systemic treatments. ORPATHYS ® in combination with TAGRISSO ® is approved in China for patients with locally advanced or metastatic EGFR mutation-positive non-squamous NSCLC with MET amplification after disease progression on EGFR TKI therapy based on the SACHI Phase III trial. The combination was also granted a temporary authorization in Switzerland for the treatment of patients with locally advanced or metastatic EGFRm NSCLC and high levels of MET overexpression or amplification who progressed on prior treatment with TAGRISSO ® . This was based on results from the global SAVANNAH Phase II trial. The global, randomized, SAFFRON Phase III trial in the same treatment setting comparing the combination with doublet platinum-based chemotherapy reported positive high-level results, demonstrating a statistically significant and clinically meaningful improvement in PFS and OS in August 2026. About TAGRISSO ® TAGRISSO ® (osimertinib) is a third-generation, irreversible EGFR-TKI with proven clinical activity in NSCLC, including the treatment of central nervous system metastases. TAGRISSO ® is approved as monotherapy in more than 120 countries including the US, EU, China and Japan. Approved indications include for first-line treatment of patients with locally advanced or metastatic EGFRm NSCLC, locally advanced or metastatic EGFR T790M mutation-positive NSCLC, adjuvant treatment of early-stage EGFRm NSCLC and locally advanced, unresectable NSCLC following platinum-based chemoradiation therapy. TAGRISSO ® is also approved in combination with chemotherapy in more than 80 countries, including the US, EU, China and Japan, for first-line treatment of patients with locally advanced or metastatic EGFRm NSCLC. About HUTCHMED HUTCHMED (Nasdaq/AIM:HCM; HKEX:13) is an innovative, commercial-stage, biopharmaceutical company. It is committed to the discovery and global development and commercialization of targeted therapies and immunotherapies for the treatment of cancer and immunological diseases. Since inception it has focused on bringing drug candidates from in-house discovery to patients around the world, with its first four medicines marketed in China, the first of which is also approved around the world including in the US, Europe and Japan. For more information, please visit: or follow us on LinkedIn . Forward-Looking Statements This press release contains forward-looking statements within the meaning of the “safe harbor” provisions of the US Private Securities Litigation Reform Act of 1995. These forward-looking statements reflect HUTCHMED’s current expectations regarding future events, including its expectations regarding the therapeutic potential of ORPATHYS ® , the further clinical development for ORPATHYS ® , its expectations as to whether any studies on ORPATHYS ® would meet their primary or secondary endpoints, and its expectations as to the timing of the completion and the release of results from such studies. Forward-looking statements involve risks and uncertainties. Such risks and uncertainties include, among other things, assumptions regarding enrollment rates and the timing and availability of subjects meeting a study’s inclusion and exclusion criteria; changes to clinical protocols or regulatory requirements; unexpected adverse events or safety issues; the ability of ORPATHYS ® , including as a combination therapy, to meet the primary or secondary endpoint of a study, to obtain regulatory approval in different jurisdictions and to gain commercial acceptance after obtaining regulatory approval; the potential market of ORPATHYS ® for a targeted indication; the sufficiency of funding; HUTCHMED’s and AstraZeneca’s ability to successfully develop and commercialize ORPATHYS ® . In addition, as certain studies rely on the use of other drug products such as TAGRISSO ® as combination therapeutics with ORPATHYS ® , such risks and uncertainties include assumptions regarding the safety, efficacy, supply and continued regulatory approval of these therapeutics. Existing and prospective investors are cautioned not to place undue reliance on these forward-looking statements, which speak only as of the date hereof. For further discussion of these and other risks, see HUTCHMED’s filings with the US Securities and Exchange Commission, The Stock Exchange of Hong Kong Limited and on AIM. HUTCHMED undertakes no obligation to update or revise the information contained in this press release, whether as a result of new information, future events or circumstances or otherwise. Medical Information This press release contains information about products that may not be available in all countries, or may be available under different trademarks, for different indications, in different dosages, or in different strengths. Nothing contained herein should be considered a solicitation, promotion or advertisement for any prescription drugs including the ones under development. CONTACTS Investor Enquiries +852 2121 8200 / ir@hutch-med.com Media Enquiries FTI Consulting – +44 20 3727 1030 / HUTCHMED@fticonsulting.com Ben Atwell / Tim Stamper +44 7771 913 902 (Mobile) / +44 7779 436 698 (Mobile) Brunswick – Zhou Yi +852 9783 6894 (Mobile) / HUTCHMED@brunswickgroup.com Panmure Liberum Nominated Advisor and Joint Broker Atholl Tweedie / Emma Earl / Rupert Dearden +44 20 7886 2500 Cavendish Joint Broker Geoff Nash / Nigel Birks +44 20 7220 0500 Deutsche Numis Joint Broker Duncan Monteith / Ramin Naji +44 20 7545 8000 REFERENCES 1 World Health Organization. International Agency for Research on Cancer. Lung Fact Sheet. Available at: . Accessed August 2026. 2 American Cancer Society. What Is Lung Cancer? Available at: . Accessed August 2026. 3 Chen HJ, et al. Long-term survival of advanced lung adenocarcinoma by maintenance chemotherapy followed by EGFR-TKI. Medicine. 2021;100(6):e24688. 4 Szumera-Ciećkiewicz A, et al. EGFR Mutation Testing on Cytological and Histological Samples in Non-Small Cell Lung Cancer: a Polish, Single Institution Study and Systematic Review of European Incidence. Int J Clin Exp Pathol. 2013;6:2800-2812. 5 Keedy VL, et al. American Society of Clinical Oncology Provisional Clinical Opinion: Epidermal Growth Factor Receptor (EGFR) Mutation Testing for Patients with Advanced Non-Small-Cell Lung Cancer Considering First- Line EGFR Tyrosine Kinase Inhibitor Therapy. J Clin Oncol. 2011;29:2121-2127. 6 Ellison G, et al. EGFR Mutation Testing in Lung Cancer: a Review of Available Methods and Their Use for Analysis of Tumour Tissue and Cytology Samples. J Clin Pathol. 2013;66:79-89. 7 Uchikawa E, et al. Structural basis of the activation of c-MET receptor. Nat Commun. 2021;12(4074) 8 Wang Q, et al. MET inhibitors for targeted therapy of EGFR TKI-resistant lung cancer. J Hematol Oncol. 2019;63.

Clinical ResultPhase 3Drug ApprovalPhase 2Immunotherapy

100 Deals associated with Mobocertinib Succinate

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KEGG	Wiki	ATC	Drug Bank
D11969	-	-	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
EGFR ex20ins mutation in non-small cell lung cancer	United States	Takeda Pharmaceuticals U.S.A., Inc.	15 Sep 2021

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
metastatic non-small cell lung cancer	Phase 2	-	Takeda Pharmaceutical Co., Ltd.	30 Nov 2020
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	United States	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	China	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	Japan	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	Germany	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	Italy	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	South Korea	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	Spain	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	Taiwan Province	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016
Locally Advanced Lung Non-Small Cell Carcinoma	Phase 2	United Kingdom	Takeda Pharmaceutical Co., Ltd.	16 Jun 2016

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


WCLC2026	Not Applicable	Non-Small Cell Lung Cancer Adjuvant TP53 mutation \| EGFR copy number variation \| TYMS 3R SNP ... View more	431	First-/second-generation EGFR-TKIs	abvxfpfktn(tfjivgumkf) = Independent molecular predictors of shorter BMFS included ARID1A mutation (HR 5.79, 95% CI 1.69-19.82, P=0.005) sorahdxrpp (diugykdowt ) View more	Positive	12 Sep 2026
				Third-generation EGFR-TKIs
WCLC2026	Not Applicable	Non-Small Cell Lung Cancer EGFR alterations \| CTNNB1 mutations	97	EGFR-TKI monotherapy	kwoxcavujc(wwdgtyxyuc) = jpamjmvxqq rgpqvvddwz (yufxtawtcv, 42.55 - 74.54) View more	Positive	12 Sep 2026
				EGFR-TKIs+antiangiogenic therapy	utmykbojsp(ocimzjaqyh) = kllgusccap wlcucjwrwk (sayuhqnmzb, 20.8 - 21.6)
ESMO_ELCC2026	Not Applicable	Metastatic Malignant Neoplasm to the Leptomeninges EGFR mutation	55	EGFR-TKI-based regimen combined with intrathecal methotrexate or pemetrexed	ldzxfiteth(wzmnxxejwv) = zucssngrfv qhpmbxpanx (jvcbzjnitg ) View more	Positive	25 Mar 2026
				EGFR-TKI-based regimen combined with intrathecal methotrexate or pemetrexed (19Del)	ldzxfiteth(wzmnxxejwv) = yxswabqgsa qhpmbxpanx (jvcbzjnitg )
ESMO_ELCC2026	Not Applicable	EGFR Mutation Lung Cancer EGFR-TP53 co-mutated	115	EGFR-TKI-based regimens	dnirsybhxo(bzzvfnhtkw) = ootjamfqvk rqjsjddwmd (tudkdiwlxo ) View more	Positive	25 Mar 2026
NCT04129502 (EXCLAIM-2, Pubmed \| J Clin Oncol) Manual	Phase 3	EGFR ex20ins mutation in non-small cell lung cancer First line EGFR exon 20 insertion	354	Mobocertinib 160 mg	sjmcxjlxjk(ewritqwgnj) = ximaioxhjb erqshbgrcs (atronjelsg ) Not Met View more	Negative	29 Jan 2025
				Pemetrexed plus cisplatin or carboplatin	sjmcxjlxjk(ewritqwgnj) = buprirfibp erqshbgrcs (atronjelsg ) Not Met View more
WCLC2024	Not Applicable	Non-Small Cell Lung Cancer	-	Osimertinib	gzhgbomvif(vuaeigzgjf) = eqrujwouig piwtupjjsx (fyjovmsyde ) View more	-	07 Sep 2024
				Furmonertinib	gzhgbomvif(vuaeigzgjf) = iixkqovgps piwtupjjsx (fyjovmsyde ) View more
NCT03811834 \| NCT02716116 (phase 1 study, Pubmed \| Invest New Drugs)	Phase 1	EGFR exon 20 insertion mutations	-	Mobocertinib 160 mg	geqguqbcqo(qegnhvcnmx) = all adverse events were Grade 1 in severity cmrrvfjwaq (jrelksuiyi )	-	01 Aug 2024
				[14C]-Mobocertinib 50 µg
JPRN-jRCT2051220070 (WJOG16022M, ASCO2024)	Phase 1	Solid tumor HER2 mutations	28	Mobocertinib 80 mg	fasjmaqxfd(plvehpqaxl) = grade ≥ 3 AE occurred in 72.7% of pts; the common events (>5%) being thrombocytopenia (50.0%), diarrhea (13.6%), and anorexia (13.6%) bichgovxjg (aolgvhgpch )	Positive	24 May 2024
NCT04051827 (CTgov)	Phase 1	Advanced Lung Non-Small Cell Carcinoma	26	Midazolam (Part A: Midazolam Alone)	dbuxaajxuh(kfcayzvurl) = nsicmmdtxx laeojclsvv (xanedndcmn, 60.2) View more	-	12 Apr 2024
				Midazolam+Mobocertinib (Part A: Midazolam + Mobocertinib)	dbuxaajxuh(kfcayzvurl) = kldqphdlyj laeojclsvv (xanedndcmn, 60.7) View more
NCT04056455 (CTgov)	Phase 1	Neoplasms	26	Mobocertinib (Severe Renal Impairment: Mobocertinib 80 mg)	dntjwjipmi(btguptgwog) = swkpeaqtzl vnssviacug (xfbwajgpbx, 326) View more	-	08 Jan 2024
				Mobocertinib (Normal Renal Function: Mobocertinib 80 mg)	dntjwjipmi(btguptgwog) = ulkhcgdcvg vnssviacug (xfbwajgpbx, 69.8) View more

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