Request Demo

Last update 27 Mar 2026

Osimertinib mesylate

Last update 27 Mar 2026

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

[11C]osimertinib, ADAURA, Mereletinib

+ [16]

Target

EGFR L858R x EGFR T790M x EGFR-Ex19del

Action

inhibitors

Mechanism

EGFR T790M inhibitors(Epidermal Growth Factor Receptor T790M inhibitors), EGFR exon 19 deletion inhibitors, EGFR exon 21 L858R mutation inhibitors

Therapeutic Areas

NeoplasmsRespiratory DiseasesNervous System Diseases+ [4]

Active Indication

Non-Small Cell Lung CancerEGFR positive non-small cell lung cancerEGFR exon 19 Deletions Mutant Non-small Cell Lung Cancer+ [34]

Inactive Indication

Adenocarcinoma of LungMetastatic Lung CancerMetastatic Malignant Neoplasm to the Leptomeninges+ [4]

Originator Organization

AstraZeneca Pharmaceuticals Co. Ltd.

Active Organization

AstraZeneca Investment (China) Co. Ltd.AstraZeneca AB

AstraZeneca PLC

+ [9]

Inactive Organization

AstraZeneca GmbHRoche Pharma AG

License Organization

Suzhou Genhouse Bio Co., Ltd.

Thermo Fisher Scientific, Inc.

EpimAb Biotherapeutics, Inc.

+ [6]

Drug Highest PhaseApproved

First Approval Date

United States (13 Nov 2015),

EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma

RegulationPriority Review (United States), Breakthrough Therapy (United States), Accelerated Approval (United States), Orphan Drug (United States), Priority Review (China), Breakthrough Therapy (China), Priority Review (Australia), Accelerated assessment (European Union), Special Review Project (China), Fast Track (United States)

Structure/Sequence

Molecular FormulaC29H37N7O5S

InChIKeyFUKSNUHSJBTCFJ-UHFFFAOYSA-N

CAS Registry1421373-66-1

359

Clinical Trials associated with Osimertinib mesylate

NCT07486648

/ Not yet recruitingPhase 1/2IIT

The Safety and Efficacy of Osimertinib Plus Capivasertib in EGFRm Advanced Non-small Cell Lung Cancer (NSCLC) Participants With PIK3CA/AKT1/PTEN Alterations Who Had Progressed on First-line Osimertinib Monotherapy or Plus Chemotherapy: a First-in-human, Phase Ib/Ⅱa Study (PRECISION)

The goal of this clinical trial is to learn if Osimertinib plus Capivasertib works to treat EGFRm advanced non-small cell lung cancer (NSCLC) in participants with PIK3CA/AKT1/PTEN alterations after progression on first-line Osimertinib (monotherapy or plus chemotherapy).
The main questions it aims to answer are:
Part A:
* Number of Dose-limiting toxicities (DLTs)
* Adverse events (AEs)/serious adverse events (SAEs) (graded by CTCAE Version 5.0)
* Recommended combined dose (RCD)
Part B:Confirmed ORR assessed by the Investigator per RECIST 1.1 criteria.
Participants will:
Part A:Take Capivasertib twice daily from day 1 to 4 of a 7-day cycle, Osimertinib will be given orally QD(once daily) at 80 mg throughout the study treatment period.
Part B: Take Osimertinib (80mg QD, continuously) and Capivasertib(RCD,orally BID from day1-day 4 in 7-day cycle , 4 days on /3 days off) till disease progression (PD) or unacceptable toxicity.

Start Date15 May 2026

Sponsor / Collaborator

Shanxi Province Cancer Hospital

[+1]

NCT07153055

/ Not yet recruitingPhase 1/2IIT

Phase I/II Trial of Lurbinectedin With Osimertinib in Transformed Small Cell Lung Cancer

This open-label, Phase I/II trial is studying the safety and effectiveness of an experimental drug combination, lurbinectedin with osimertinib, against a rare type of cancer known as transformed small cell lung cancer (SCLC).

Start Date01 May 2026

Sponsor / Collaborator

Indiana University

[+1]

NCT07485452

/ Not yet recruitingPhase 2IIT

Boosting Osimertinib Blood Brain Barrier Penetration in Patients With Epidermal Growth Factor Receptor Mutated Non-small Cell Lung Cancer

The goal of this proof-of-concept clinical study is to determine the effect of combining osimertinib with febuxostat on cerebrospinal fluid concentrations of osimertinib in patients with epidermal growth factor receptor (EGFR) mutated non-small cell lung cancer (NSCLC). The main question it aims to answer is: what is the effect of combining osimertinib with the ABCG2 inhibitor febuxostat on cerebrospinal fluid to unbound plasma osimertinib concentration ratio in patients with EGFR mutated NSCLC without central nervous system (CNS) metastases and without the ABCG2 34G>A single nucleotide polymorphism (SNP)?

Start Date01 Apr 2026

Sponsor / Collaborator

Netherlands Cancer Insitute

[+1]

100 Clinical Results associated with Osimertinib mesylate

100 Translational Medicine associated with Osimertinib mesylate

100 Patents (Medical) associated with Osimertinib mesylate

4,352

Literatures (Medical) associated with Osimertinib mesylate

31 Dec 2026·RENAL FAILURE

A tri-scale in silico framework integrating pharmacovigilance and mechanistic modeling suggests tepotinib-associated acute kidney injury risk

Article

Author: Bai, Zhixun ; Wang, Qin ; Zheng, Rubin ; Han, Jinfen ; Lyu, Jiayi ; Lu, Jing ; Deng, Miao ; Chen, Jiaxi

Proactive safety evaluation of molecularly targeted therapies requires generalizable frameworks that integrate real-world evidence with mechanistic insights. As a case in point, tepotinib, a mesenchymal-epithelial transition (MET) inhibitor for non-small cell lung cancer, has a known pulmonary toxicity profile, but its link to acute kidney injury (AKI) and underlying mechanism remain unclear. We devised a tri-scale in silico strategy encompassing population-scale pharmacovigilance signal extraction from the FDA Adverse Event Reporting System (FAERS) (2020-2025) via disproportionality analysis (Reporting Odds Ratio, ROR, and Proportional Reporting Ratio, PRR), network toxicology-based multi-target exploration for shared target and hub gene identification, and mechanistic docking-based molecular plausibility assessment using the Cavity-detection guided Blind Docking (CB-Dock2) platform. Pharmacovigilance analysis identified a significant renal impairment signal (ROR = 20.60). Network toxicology suggested potential nephrotoxicity and revealed 173 shared targets and prioritizing six hub genes (HSP90AA1, AKT1, EGFR, CASP3, TNF, SRC). These genes were shown to be critically involved in PI3K-Akt and MAPK pathways. Molecular docking revealed high-affinity binding between tepotiniband all six hub targets (Vina scores: -8.0 to -10.6 kcal/mol), providing a structural basis for the postulated mechanistic link to AKI. These findings not only highlight the necessity for enhanced renal monitoring in tepotinib-treated patients but, more broadly, establish the FAERS-NetDock Pipeline as a reusable, generalizable and hypothesis-generating framework for evaluating tyrosine kinase inhibitors (TKIs)-induced nephrotoxicity; this framework is immediately applicable to profiling the safety of other TKIs (e.g. crizotinib, capmatinib, savolitinib, afatinib and osimertinib) and is readily adaptable for de-risking a wider spectrum of targeted therapies.

01 Jul 2026·Value in Health Regional Issues

Cost-Utility Analysis of Adjuvant Osimertinib in Resected Epidermal-Growth-Factor-Receptor-Mutated Early-Stage Non-Small Cell Lung Cancer

Article

Author: Phisalprapa, Pochamana ; Changsatja, Supitchaya ; Komonpaisarn, Touchanun ; Kositamongkol, Chayanis ; Thamlikitkul, Lucksamon

OBJECTIVES:

Lung cancer is the most common cancer and the leading cause of cancer death worldwide. One-third of non-small cell lung cancer (NSCLC) patients are diagnosed at a resectable stage, for which surgery is the standard curative treatment. However, most patients recur within 2 years. Adjuvant osimertinib, a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, significantly reduces recurrence and prolongs survival in completely resected EGFR-mutated NSCLC. This study assessed the cost-utility and budget impact of adjuvant osimertinib versus placebo for resected stage IB-IIIA EGFR-mutated NSCLC from Thailand's societal perspective.

METHODS:

A Markov model with a lifetime horizon and 4-week cycle was developed, including 3 health states: disease-free, recurrent disease, and death. Patients received osimertinib or placebo in the disease-free state, with recurrence categorized as locoregional or distant. Subsequent treatments were modeled based on recurrence timing. Health outcomes were obtained from a systematic review, and costs followed Thai health technology assessment guidelines. Results were reported as incremental cost-effectiveness ratios in 2023 USD per quality-adjusted life-years (QALY) gained. Sensitivity analyses addressed uncertainty.

RESULTS:

Osimertinib yielded 2.36 additional QALYs at an incremental cost of USD 62 604.90, with an incremental cost-effectiveness ratio of USD 26 474.02/QALY, exceeding Thailand's willingness-to-pay threshold (USD 4619). An 85.07% price reduction is required for cost-effectiveness. Probabilistic sensitivity analysis showed 0% probability of cost-effectiveness at the current threshold, increasing to 52% at USD 25 981.97/QALY. The 5-year budget impact analysis was estimated at USD 678.73 million.

CONCLUSIONS:

Adjuvant osimertinib is not cost-effective in Thailand under current pricing but could be with major price reductions or risk-sharing strategies.

01 Jun 2026·BIOORGANIC CHEMISTRY

Synthesis and evaluation of methoxyquinazoline sulfonamide derivatives as bifunctional molecular targeting tumor related inflammation and anti-EGFR triple-mutation

Article

Author: Yao, Han ; Li, Xingshu ; Peng, Jun ; Zeng, Wei ; Cao, Longcai ; Tan, Zhenyou

The development of novel anti-cancer compounds that overcome acquired resistance to third-generation EGFR inhibitors such as osimertinib is of great significance. This study designed and synthesized eighteen methoxyquinazoline sulfonamide derivatives, and evaluated their anti-tumor activity using three EGFR triple-mutant tumor cell lines. Among them, the optimal compound 9f exhibited IC₅₀ values of 33.3-95.3 nM against Baf3-L858R/C797S/T790M, Baf3-Del19/C797S/T790M, and H1975-L858R/C797S/T790M cancer cell lines, which were consistent with the results of colony formation assays and 3D spheroid suspension culture assays. In anti-tumor experiments in mice bearing H1975-L858R/C797S/T790M tumors, compound 9f achieved a tumor growth inhibition rate of 67.3%. Mechanistic studies showed that 9f exerts excellent anti-inflammatory effects, including downregulating the expression of inflammation-related proteins iNOS, COX-2, and NF-κB (p65) in Raw264.7 cells (Western blot assay), increasing NO secretion in LPS-stimulated Raw264.7 cells (fluorescence intensity assay), and reducing IL-6 secretion in Raw264.7 and THP-1 cells (ELISA). Mechanistic studies also indicated that 9f promotes apoptosis of tumor cells and inhibits phosphorylation of the key tumor growth protein EGFR.

903

News (Medical) associated with Osimertinib mesylate

24 Mar 2026

·www.prnewswire.com

KELUN-BIOTECH ANNOUNCED 2025 ANNUAL RESULTS: MULTIPLE PRODUCTS SUCCESSFULLY LAUNCHED WITH TIERED PIPELINE READY FOR TAKE-OFF

Revenue amounted to approximately RMB2057.92 million, and gross profit amounted to approximately RMB1478.78 million, representing a year-on-year increase. R&D Expenses was approximately RMB1319.68 million. Loss for the period was RMB381.97 million, adjusted annual loss[1] was approximately RMB211.28 million. Cash and financial assets[2] amounted to approximately RMB4559.36 million, with ample cash reserves. The debt-to-asset ratio[3] further declined to 18.7%. CHENGDU, China, March 23, 2026 /PRNewswire/ -- Sichuan Kelun-Biotech Pharmaceutical Co., Ltd. (" Kelun-Biotech" or the " Company", Stock Code: 6990.HK) announced its audited consolidated results for the year ended 31 December 2025 (the " Reporting Period"). Kelun-Biotech is leveraging its core strengths and proprietary OptiDC™ technology platform to continue deepening its presence in the ADC and novel DC drug field. The company is actively advancing cutting-edge modalities including bispecific ADCs, RDCs, iADCs, and DACs, building a differentiated pipeline with strong global competitiveness. At the same time, Kelun-Biotech is steadily advancing product commercialization, achieving transformational growth across its business. To date, the company has four products with eight indications approved for marketing in China, including Sacituzumab Tirumotecan (佳泰莱®), Trastuzumab Botidotin (舒泰莱®), Tagitanlimab (科泰莱®), and Cetuximab N01 (达泰莱®). Among them, three products with five indications have been included in the 2025 National Reimbursement Drug List (NRDL), establishing a fully integrated drug development ecosystem that spans R&D through commercialization. As of now, the company has built a robust pipeline of more than 30 drug candidates, with over 10 in the clinical stage, and are gradually expanding into broader non-oncology therapeutic areas such as autoimmune diseases and metabolic disorders. Looking ahead, the company will leverage its innovative and differentiated pipeline to deliver high-quality therapeutic solutions for major unmet medical needs worldwide. Core ADC Products' Commercialization Realized to Solidify Long-term Performance Foundation Sac-TMT (sacituzumab tirumotecan, TROP2 ADC) (also known as SKB264/MK-2870) (佳泰莱® ) TNBC: The Company received marketing authorization in China from the NMPA for sac-TMT in adult patients with unresectable locally advanced or metastatic TNBC who have received at least two prior systemic therapies (at least one of them for advanced or metastatic setting). The Company has initiated a Phase 3 registrational study of sac-TMT monotherapy versus ICC for 1L advanced TNBC. HR+/HER2- BC : In February 2026, a new indication application for sac-TMT for the treatment of adult patients with HR+/HER2- BC who have received prior endocrine therapy (ET) and at least one line of chemotherapy in advanced setting has been approved for marketing by the NMPA. A Phase 3 registrational study of sac-TMT versus ICC for treatment of patients with HR+/HER2- BC who received prior ET is in progress. EGFR-mutant NSCLC: In March 2025, the Company received marketing authorization in China from the NMPA for sac-TMT for the treatment of adult patients with EGFR mutant-positive NSCLC following progression on EGFR-TKI therapy and platinum-based chemotherapy. This is the first TROP2 ADC drug approved for marketing in LC globally. In October 2025, the company received marketing authorization in China from the NMPA for sac-TMT for the treatment of adult patients with EGFR mutant-positive NSCLC who progressed after treatment with EGFR-TKI therapy. This is the first ADC globally to show an OS benefit compared with platinum doublet chemotherapy and be approved for advanced NSCLC following progression on only TKI therapy (2L). The Phase 3 registrational study of sac-TMT combined with osimertinib as first-line treatment of EGFR-mutant NSCLC and a Phase 2 study of sac-TMT monotherapy or in combination with osimertinib as neoadjuvant therapy for EGFR-mutant NSCLC are in progress. EGFR-wild type NSCLC: The Phase 3 registrational study of sac-TMT in combination with KEYTRUDA®[1] (pembrolizumab) versus pembrolizumab as first-line treatment of PD-L1 positive NSCLC met its primary endpoint. This is the first Phase 3 clinical trial of ADC combined with immune checkpoint inhibitor to achieve its primary endpoint in the first-line treatment of NSCLC. In January 2026, sac-TMT in combination with pembrolizumab for the first-line treatment of PD-L1 positive NSCLC were granted Breakthrough Therapy Designation by the NMPA. The Phase 3 registrational study of sac-TMT in combination with pembrolizumab as first-line treatment of PD-L1 negative NSCLC is in progress. Other indications: The company is actively exploring the potential of sac-TMT both as a monotherapy and in combination with other therapies for treating other solid tumors, including GC, EC, CC, OC, UC, CRPC, HNSCC, and TC, etc. Trastuzumab botidotin (HER2 ADC, also known as A166, 舒泰莱 ® ) In October 2025, trastuzumab botidotin was approved for marketing by the NMPA for adult patients with HER2+ BC who have received one or more prior anti-HER2 therapy. This is the first domestically developed HER2 ADC approved for 2L+ HER2+ BC in China. An open, multicenter Phase 2 clinical study of trastuzumab botidotin in the treatment of HER2+ BC that previously received a topoisomerase inhibitor ADC is in progress. Key Clinical Data Highlighted at International Academic Conferences and in Top Journals Results from the Phase 3 study of sac-TMT for the treatment of 2L EGFR-mutant NSCLC were selected for LBA and presented as an oral report in the Presidential Symposium session at the 2025 ESMO Congress. Sac-TMT achieved statistically significant and clinically meaningful improvements in ORR, PFS, and OS compared to chemotherapy. The study findings were published simultaneously online at the New England Journal of Medicine and in the first issue of 2026. Results from the study of sac-TMT for the treatment of 3L EGFR-mutant NSCLC were presented as an oral report at the ASCO Annual Meeting and published at the British Medical Journal. The final OS analysis of this study will be selected for LBA and presented as a mini oral report at the 2026 ELCC. Results from the Phase 3 study of sac-TMT for the treatment of 2L+ HR+/HER2-BC were selected for LBA and presented as an oral report at the 2025 ESMO Congress. Results from the Phase 3 study of trastuzumab botidotin for the treatment of 2L+ HER2+ BC were selected for LBA and presented as an oral report at the 2025 ESMO Congress. Sustained Value Release of ADCs Under Development with Tiered Advancement of Innovation Pipeline Phase 2 clinical stage SKB315 (CLDN18.2 ADC): The Phase 1b clinical trial of SKB315 is in progress, for the treatment of GC/GEJC/PDAC, etc. Results of a Phase 1 study of SKB315 in patients with advanced solid tumors including GC/GEJC were presented at 2025 ESMO Congress in October 2025. SKB410/MK-3120 (Nectin-4 ADC): Its partner MSD has launched 4 global Phase 1/2 clinical trial of SKB410/MK-3120 in advanced solid tumor including bladder cancer, etc. SKB571/MK-2750 (novel bsADC): The Phase 2 clinical trial in China is ongoing. SKB518 (novel ADC with a potential FIC target): The Phase 2 clinical trials are ongoing in China. SKB500 (novel ADC): The Phase 2 study is ongoing in China. Phase 1 clinical stage SKB107 (RDC) [2] : The Phase 1 study is ongoing. SKB535/MK-6204 (novel ADC with potential FIC target): The Phase 1 clinical trial for SKB535 is ongoing in China. SKB445 (novel ADC with potential FIC target): The Phase 1 clinical trials for SKB445 is ongoing in China. SKB105/CR-003 (ITGB6 ADC): In January 2026, an IND application was approved by the CDE of NMPA for the treatment of advanced solid tumor. A Phase 1/2 trial is ongoing in China. Strategic Layout of Non-DC Assets with Focus on Combination Therapy & Indication Expansion Drug candidates for oncology Tagitanlimab (PD-L1 mAb, also known as A167) ( 科泰莱 ® ): In January 2025, the Company received marketing authorization of tagitanlimab used in combination with cisplatin and gemcitabine for the first-line treatment of NPC from NMPA. Tagitanlimab is the first PD-L1 mAb globally to receive authorization for the first-line treatment of NPC. In May 2025, the results of a Phase 3 clinical study of tagitanlimab in combination with cisplatin and gemcitabine for the first-line treatment of NPC were presented at the ASCO Annual Meeting. Cetuximab N01 (EGFR mAb, also known as A140) ( 达泰莱 ® ): In February 2025, the Company received marketing authorization in China from the NMPA for Cetuximab N01 Injection used in combination with FOLFOX or FOLFIRI regimens for first-line treatment of RAS wild-type mCRC. Lunbotinib Fumarate Capsules (RET inhibitor, also known as A400/EP0031)( 宁泰莱 ® ) [3] ： An NDA was accepted for review by the CDE of the NMPA of China for the 1L+ treatment of RET-fusion positive NSCLC. The company is also conducting a Phase 1b/2 clinical study for RET+ MTC and solid tumor in China. Ellipses Pharma is progressing their phase 2 clinical study globally outside of China. In May 2025, results from the Phase 1 study of Lunbotinib Fumarate Capsules in patients with advanced RET-mutant MTC were presented at the ASCO Annual Meeting. SKB118/CR-001 (PD-1/VEGF bsAb): In January 2026, Crescent Biopharma announced the regulatory clearance of the IND application for SKB118 by FDA to initiate its global ASCEND Phase 1/2 clinical trial for the treatment of advanced solid tumors, and the first patient has been dosed in February, 2026. The company is planning to initiate the Phase 1/2 clinical study for SKB118 in China in the first half of 2026. Drug candidates for autoimmune diseases SKB378/WIN378 (TSLP mAb): In January 2025, an IND application for SKB378 for the treatment of COPD was approved by the NMPA. Its collaboration partner, Windward Bio, has launched the Phase 2 POLARIS global trial in patients with asthma. SKB575 (TSLP/ undisclosed target bsAb ): In March 2026, an IND application for SKB575 for the treatment of atopic dermatitis was approved by the NMPA. Drug candidates for other non-oncology diseases SKB336 (FXI/FXIa mAb): The company completed Phase 1 clinical trial in China. Multiple Products First Included in National Reimbursement Drug List with Accelerated Market Coverage In 2025, the Company witnessed an explosive growth in the commercialization of its innovative achievements. The Company has also filed an NDA for Lunbotinib Fumarate Capsules and expects to commence its commercialization in the second half of 2026 or the first half of 2027, subject to regulatory communications and marketing approval. To date, the company's initial commercial product portfolio, consisting of five products, has taken shape. Supported by national innovation policies, the Company has successfully secured the first-time inclusion of three of its commercialized products, namely 佳泰莱®, 科泰莱® and 达泰莱®, in the National Reimbursement Drug List (國家醫保藥品目錄), which officially took effect on January 1, 2026, and is expected to benefit more patients faster and better. Steady Advancement of Global Collaboration and Comprehensive Strength Authoritatively Recognized Collaboration with MSD: As at the date of this announcement, MSD is evaluating initiated 17 ongoing Phase 3 global clinical studies of sac-TMT as a monotherapy or with pembrolizumab or other agents for several types of cancer, including BC, LC, gynecological cancers, GI cancer and GU cancer. In addition to sac-TMT, the company is also collaborating with MSD on certain ADC assets to continuously explore favorable ADC pipeline portfolios. Collaboration with Ellipses Pharma: The Company has deepened its collaboration with Ellipses Pharma on A400/EP0031, which has cleared by the FDA to progress into Phase 2 clinical development. As at December 31, 2025, a total of 39 clinical sites in the United States, Europe and UAE were set up for Lunbotinib Fumarate Capsules. Collaboration with Windward Bio: In January 2025, the Company and Harbour BioMed had entered into an exclusive license agreement with Windward Bio, under which the Company and Harbour BioMed granted Windward Bio an exclusive license for the research, development, manufacturing and commercialization of SKB378/WIN378 globally (excluding Greater China and several Southeast and West Asian countries). Windward Bio has launched the Phase 2 POLARIS global trial in patients with asthma. Collaboration with Crescent Biopharma. In December 2025, the company and Crescent Biopharma entered into a strategic collaboration for SKB105/CR-003 and SKB118 (a PD1 x VEGF bsAb, also known as CR-001). Under the collaboration, the company granted Crescent Biopharma exclusive rights to research, develop, manufacture and commercialize SKB105/CR-003 in the United States, Europe and all other markets outside of Greater China. In return, the compamy obtained exclusive rights from Crescent Biopharma to research, develop, manufacture and commercialize SKB118/CR-001 in Greater China. In January 2026, Crescent Biopharma announced the regulatory clearance of the IND application for SKB118 by FDA to initiate its global ASCEND Phase 1/2 clinical trial for the treatment of advanced solid tumors, and the first patient has been dosed in February, 2026. Continuous Improvement of ESG Capabilities to Consolidate the Foundation for Sustainable Development Through the establishment and continuous improvement of the ESG governance structure, the Company comprehensively enhances ESG performance ability and ensures the Company's sustainable development. In May 2025, the company was awarded "Best ESG" by Extel. In March 2026, the Company had received a rating of "AA" in the MSCI ESG Rating Assessment. Outlook In 2026, Kelun-Biotech will continue to drive innovation and strengthen its operational capabilities, steadily advancing towards becoming a world-class biopharmaceutical company. Specifically, the Company will implement the following development strategies: advancing differentiated pipelines targeting indications with significant medical needs; innovating on and optimizing payload-linker strategies and novel DC designs and structures, while expanding applications in non-oncology diseases; enhancing its end-to-end drug development and commercialization capabilities; expanding business landscape and strategic partnerships and improve our capabilities for the development, registration and commercialization of our products in ex-China market; and optimizing its operational systems with the aim of becoming a leading global biopharmaceutical company. About Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. (referred to as "Kelun-Biotech" Stock Code: 6990.HK) is a subsidiary of Sichuan Kelun Pharmaceutical Co., Ltd., specializing in the R&D, manufacturing, commercialization, and global collaboration of innovative biological drugs and small molecule drugs. The Company focuses on addressing unmet clinical needs both globally and in China, with a strategic emphasis on major disease areas such as oncology, autoimmune disorders, and metabolic diseases. It is dedicated to building an international platform for drug R&D and industrialization, with the aim of becoming a global leader in the innovative drug sector. Currently, Kelun-Biotech has over 30 key innovative drug projects, including 4 projects covering 8 indications that have received market approval, 1 project at the NDA stage, and more than 10 projects in clinical trials. The Company has also successfully established its internationally renowned proprietary ADC and novel conjugated drug platform, OptiDCTM, with 2 ADC projects covering 5 indications approved for market launch, and several ADC or novel conjugated drug projects in clinical or preclinical development. SOURCE Kelun-biotech 21% more press release views with Request a Demo

Phase 1Phase 2Phase 3Drug ApprovalLicense out/in

23 Mar 2026

·www.fiercepharma.com

Dizal's Zegfrovy clinches landmark phase 3 win in NSCLC subtype, setting up challenge to J&J's Rybrevant

Dizal's global phase 3 Wu-Kong28 trial, which tested Zegfrovy (sunvozertinib) as a monotherapy, has met its primary endpoint in first-line non-small cell lung cancer harboring EGFR exon 20 insertion mutations. Watch out, Johnson & Johnson. Dizal has reported positive phase 3 results for its oral Zegfrovy that could put more pressure on the pharma giant’s injectable Rybrevant in non-small cell lung cancer (NSCLC).The global phase 3 Wu-Kong28 trial, which tested Zegfrovy (sunvozertinib) as a monotherapy, has met its primary endpoint, Dizal announced Saturday. The EGFR tyrosine kinase inhibitor (TKI) significantly improved progression-free survival (PFS) versus platinum-based chemotherapy in treatment-naïve patients with NSCLC harboring EGFR exon 20 insertion mutations.In addition to the “statistically significant and clinically meaningful” improvement in PFS, Dizal also reported “superior results” for Zegfrovy in all secondary endpoints, which are measuring tumor response rates and duration as well as a safety profile that’s consistent with previous studies.The success of the Wu-Kong28 study positions Zegfrovy as the first oral, chemo-free regimen to demonstrate superior clinical benefit over standard chemo in the first-line EGFR exon 20 NSCLC setting. The positive readout sets the stage for a continued market battle with Johnson & Johnson’s Rybrevant. While Rybrevant got its first-line FDA approval two years ago, it is an injectable bispecific antibody that needs to be used in combination with chemo. As a single-agent oral regimen, Dizal’s Zegfrovy could offer a potentially more convenient and less toxic alternative. However, before Dizal can claim a competitive edge, the Wu-Kong28 results need to be benchmarked against J&J’s Papillon trial, which showed Rybrevant plus chemo resulted in a 61% reduction in the risk of disease progression or death versus chemo alone. Detailed data from Wu-Kong28 will be presented at an upcoming medical meeting, and Dizal said it plans to engage with regulatory authorities about potential drug applications. “Finding a drug targeting EGFR exon 20 insertion mutations is especially challenging due to their enormous heterogeneity,” Dizal CEO Xiaolin Zhang, Ph.D., said in a March 21 statement. “Despite tremendous efforts, there is no success yet in finding an effective target drug that can spare patients from chemotherapies. WU-KONG28 study has the potential to change all that.” Before Zegfrovy, Takeda’s small-molecule TKI Exkivity (mobocertinib) failed a study in the first-line EGFR exon 20 setting, leading to a global market withdrawal in 2023. Depending how the FDA views the Wu-Kong28 results, Dizal could also turn Zegfrovy’s accelerated approval in previously treated patients into a full nod. Dizal also recently launched what currently appears to be a China-only phase 3 trial testing Zegfrovy as an adjuvant therapy in stage 1b to 3a NSCLC with EGFR exon 20 insertion mutations or PACC mutations.A spinout from AstraZeneca, Dizal reported 2025 revenue of 801 million Chinese yuan ($116 million), which represents a 123% jump over the prior year after the company’s two commercial products—Zegfrovy and c-Met/VEGFR2 inhibitor golvatinib—landed coverage on China’s national insurance scheme. With an expanding pipeline that also includes the pivotal-stage, potential first-in-class noncovalent LYN/BTK dual inhibitor birelentinib, the Chinese biotech is seeking a second listing on the Hong Kong Stock Exchange. Meanwhile, other than the rare exon 20 setting, J&J is spending much energy on a high-stakes battle with AZ’s EGFR king Tagrisso in the bigger exon 19/exon 21 market. After a delay, J&J managed to improve Rybrevant’s convenience and safety profile—and seemingly also efficacy—with an FDA approval for a subcutaneous version.

Phase 3Clinical ResultDrug Approval

20 Mar 2026

·www.genfleet.com

Innovative Therapeutic Modalities for RAS-Mutant and Co-Mutated Tumors: GenFleet Announces Data from Three Preclinical Studies Selected for Poster Presentation of 2026 AACR Annul Meeting

GenFleet Therapeutics (2595.HK) announced today that preclinical data of three novel drug candidates have been selected for the poster presentation at the 2026 Annual Meeting of the American Association for Cancer Research (AACR), which is scheduled to take place in San Diego, US from April 17 to 22, 2026. GenFleet’s RAS-targeted matrix encompasses multiple selective and Pan RAS inhibitors, as well as targeted therapies for potential co-mutations associated with the RAS pathway. This matrix includes small and large molecules with diversified modalities and mechanisms; preclinical research data of three compounds - GFH276 (non-degrading molecular glue), GFS784 (novel ADC linking functional antibody with synergistic targeted payload) and GFH603 (molecular glue-like covalent allosteric activator) - will be featured at this upcoming conference. Title: Preclinical evaluation of GFH276 monotherapy and combination therapy for RAS-mutant tumors Session Category: Experimental and Molecular Therapeutics Session Start: 4/21/2026 9:00:00 AM Session End: 4/21/2026 12:00:00 PM Poster Number: 4565 GFH276, a molecular glue Pan (ON) RAS inhibitor with favorable oral bioavailability, showed potent suppression of most activated wild-type and mutant RAS subtypes. Preclinical research conducted across multiple KRAS-mutant models demonstrated GFH276's significant and dose-dependent anti-tumor efficacy in tumor types including non-small cell lung cancer, colorectal cancer, pancreatic cancer, cholangiocarcinoma and endometrial carcinoma. Furthermore, GFH276 also exhibited notable synergistic effects when administered in combination with cetuximab or anti-PD-1 monoclonal antibody, highlighting broad therapeutic potential of both monotherapy and combinational treatments. Title: GFS784, a next-generation ADC with a novel Pan RAS (ON) inhibitor payload Session Category: Experimental and Molecular Therapeutics Session Start: 4/21/2026 9:00:00 AM Session End: 4/21/2026 12:00:00 PM Poster Number: 4536 GFS784, linking a Pan RAS inhibitor payload to cetuximab, was the first candidate developed from GenFleet's globally innovative FAScon™ ADC platform combining functional antibodies with synergistic targeted payloads. Preclinical studies showed GFS784’s potent activity in both DXd-sensitive and Dxd-resistant RAS-mutant tumor models, while also exerting anti-tumor activity in EGFR-mutant and osimertinib-resistant models, bringing a potential next-generation ADC therapeutic regimen to patients. Title：GFH603: A molecular glue-like allosteric activator of the KEAP1-CUL3 E3 ligase complex for targeting NRF2-activated tumors Session Category: Experimental and Molecular Therapeutics Session Start: 4/19/2026 2:00:00 PM Session End: 4/19/2026 5:00:00 PM Poster Number: 348 KEAP1 is a frequently co-mutated gene in RAS-mutant tumors. Dysfunction of the KEAP1 protein can lead to aberrant activation of its downstream NRF2, causing resistance to various cancer treatments. Designed to restore the KEAP1-CUL3 E3 ligase activity and promote the NRF2 degradation, GFH603 demonstrated potent anti-tumor efficacy across multiple preclinical models in single-agent research and in combination with Pan RAS inhibitors. The molecular glue-like allosteric activator holds the potential to provide a novel targeted therapy for NRF2-driven malignancies. Forward-looking Statements Specific information in this press release may contain or constitute forward-looking words that are not historical facts. They can be identified by using forward-looking terminology, such as "predict", "believe", "plan", "predict", "expect", "will", "may", "should" and other words of similar meanings. Based on the management's current beliefs, plans, estimates and expectations of the company's operation and market trends subject to changes beyond control, the forward-looking terminology reflects GenFleet Therapeutics' beliefs, plans, estimates and expectations of future development. Actual outcome in the future may differ significantly from forward-looking words owing to market, policy, and R&D uncertainties, among others. Subject to the above-mentioned uncertainties, GenFleet Therapeutics makes no expressed or implied guarantee as to the accuracy, completeness or feasibility of this presentation, and you are cautioned not to solely rely on such forward-looking words. Neither the company nor any of its directors, officers, employees, shareholders, agents, related parties, consultants or representatives will be liable to you or any other person for consequences resulting from using this presentation. Investors are advised to exercise due diligence with reference to the company's official disclosures for decision-making.

AACR

100 Deals associated with Osimertinib mesylate

External Link

KEGG	Wiki	ATC	Drug Bank
D10766	Osimertinib mesylate	L01XE	DB09330

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Non-Small Cell Lung Cancer	Canada	AstraZeneca Canada, Inc.	05 Jul 2016
EGFR positive non-small cell lung cancer	Japan	AstraZeneca Pharmaceuticals Co. Ltd.	28 Mar 2016
EGFR exon 19 Deletions Mutant Non-small Cell Lung Cancer	European Union	AstraZeneca AB	01 Feb 2016
EGFR exon 19 Deletions Mutant Non-small Cell Lung Cancer	Iceland	AstraZeneca AB	01 Feb 2016
EGFR exon 19 Deletions Mutant Non-small Cell Lung Cancer	Liechtenstein	AstraZeneca AB	01 Feb 2016
EGFR exon 19 Deletions Mutant Non-small Cell Lung Cancer	Norway	AstraZeneca AB	01 Feb 2016
EGFR exon 21 Substitution Mutant Non-small Cell Lung Cancer	European Union	AstraZeneca AB	01 Feb 2016
EGFR exon 21 Substitution Mutant Non-small Cell Lung Cancer	Iceland	AstraZeneca AB	01 Feb 2016
EGFR exon 21 Substitution Mutant Non-small Cell Lung Cancer	Liechtenstein	AstraZeneca AB	01 Feb 2016
EGFR exon 21 Substitution Mutant Non-small Cell Lung Cancer	Norway	AstraZeneca AB	01 Feb 2016
EGFR-mutated non-small Cell Lung Cancer	European Union	AstraZeneca AB	01 Feb 2016
EGFR-mutated non-small Cell Lung Cancer	Iceland	AstraZeneca AB	01 Feb 2016
EGFR-mutated non-small Cell Lung Cancer	Liechtenstein	AstraZeneca AB	01 Feb 2016
EGFR-mutated non-small Cell Lung Cancer	Norway	AstraZeneca AB	01 Feb 2016
metastatic non-small cell lung cancer	European Union	AstraZeneca AB	01 Feb 2016
metastatic non-small cell lung cancer	Iceland	AstraZeneca AB	01 Feb 2016
metastatic non-small cell lung cancer	Liechtenstein	AstraZeneca AB	01 Feb 2016
metastatic non-small cell lung cancer	Norway	AstraZeneca AB	01 Feb 2016
EGFR T790M Mutation Positive Non-Small Cell Lung Carcinoma	United States	AstraZeneca Pharmaceuticals LP	13 Nov 2015

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
EGFR positive Non-squamous non-small cell lung cancer	Phase 3	United States	AstraZeneca AB	09 Jan 2025
EGFR positive Non-squamous non-small cell lung cancer	Phase 3	China	AstraZeneca AB	09 Jan 2025
EGFR positive Non-squamous non-small cell lung cancer	Phase 3	Australia	AstraZeneca AB	09 Jan 2025
EGFR positive Non-squamous non-small cell lung cancer	Phase 3	Brazil	AstraZeneca AB	09 Jan 2025
EGFR positive Non-squamous non-small cell lung cancer	Phase 3	Canada	AstraZeneca AB	09 Jan 2025
EGFR positive Non-squamous non-small cell lung cancer	Phase 3	France	AstraZeneca AB	09 Jan 2025
EGFR positive Non-squamous non-small cell lung cancer	Phase 3	Germany	AstraZeneca AB	09 Jan 2025
EGFR positive Non-squamous non-small cell lung cancer	Phase 3	Hong Kong	AstraZeneca AB	09 Jan 2025
EGFR positive Non-squamous non-small cell lung cancer	Phase 3	India	AstraZeneca AB	09 Jan 2025
EGFR positive Non-squamous non-small cell lung cancer	Phase 3	Italy	AstraZeneca AB	09 Jan 2025

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03778229 (SAVANNAH, CTgov)	Phase 2	Non-squamous non-small cell lung cancer	367	Savo (Savo 300 mg BID + Osi)	kymrqpzsav = aqqvzxhtkn wjjxodyfgl (oegrgscydi, ykmlzukirq - xysnqbhzrb) View more	-	10 Feb 2026
				Savo (Savo 300 mg QD + Osi)	raalijzfli = lhpyepnslh ttrdwpqndu (bbfhthmgdl, ekucjlderg - vkyjvbdciv) View more
NCT05163249 (FLOWERS, Pubmed \| Nat Commun)	Phase 2	EGFR mutation MET positive Non-small Cell Lung Cancer First line EGFR mutations \| MET amplification or overexpression	44	Osimertinib 80 mg	ogvlmaueqx(ighlnmyrfz) = udqczzdkst qxkestyphi (tyamimhxjk, 38.5 - 80.3) View more	Positive	13 Jan 2026
				Osimertinib 80 mg + Savolitinib 300 mg	ogvlmaueqx(ighlnmyrfz) = ubnogkswbv qxkestyphi (tyamimhxjk, 69.6 - 98.8) View more
NCT04765059 (COMPEL, CTgov)	Phase 3	Non-Small Cell Lung Cancer \| Squamous non-small cell lung cancer \| Recurrent Non-Small Cell Lung Cancer	98	Carboplatin+Pemetrexed+Cisplatin+Osimertinib (AZD9291) (Treatment Arm A: Osimertinib (AZD9291), Pemetrexed, Cisplatin or Carboplatin)	aygqppofdk(grnyhhrelp) = gntpurzlqj qzryokyzbz (ehdivsnvnf, eakpcvglyv - ytkkpzeaai) View more	-	13 Jan 2026
				Placebo+Carboplatin+Pemetrexed+Cisplatin+Osimertinib (AZD9291) (Treatment Arm B: Placebo for Osimertinib (AZD9291), Pemetrexed, Cisplatin or Carboplatin)	aygqppofdk(grnyhhrelp) = lvuqxgtdlx qzryokyzbz (ehdivsnvnf, jhouinidtv - hxdfsrjcva) View more
NCT03497767 \| NCT03769103 (OUTRUN, Pubmed \| J Thorac Oncol)	Phase 2	EGFR Mutation Lung Cancer \| Brain metastases EGFR-Mutated	79	Stereotactic Radiosurgery (SRS) + Osimertinib	juearlohbt(nbqcnilyfu) = kuzplslupp xxzirrfixr (zdszfdovvc ) View more	Negative	01 Jan 2026
				Osimertinib	juearlohbt(nbqcnilyfu) = aythasquec xxzirrfixr (zdszfdovvc ) View more
NCT03778229 (SAVANNAH, Pubmed \| Clin Lung Cancer)	Phase 2	MET gene amplification Non-small Cell Lung Cancer MET Amplified \| EGFR Mutated	30	Savolitinib 300 mg QD + Osimertinib 80 mg QD	zytghtalpd(fawpucpjml) = ozasxguaru vgngqlngbo (kpwspxgwiq, 29 - 82) View more	Positive	01 Jan 2026
				Savolitinib + Placebo	zytghtalpd(fawpucpjml) = aeitgpclfr vgngqlngbo (kpwspxgwiq, 2 - 38) View more
NCT06194448 (NEOLA, ESMO_ASIA2025)	Phase 2	Non-small cell lung cancer stage IIIB EGFRm	55	Osimertinib 80 mg QD (unresectable stage III EGFRm NSCLC)	vicymcnozg(htntwaicnp) = nukdzwqqyf nbnqcquvkz (vckhetxijp ) View more	Positive	06 Dec 2025
JPRN-jRCT2080225059 (ESMO_ASIA2025)	Phase 2	EGFR-mutated non-small Cell Lung Cancer EGFR mutations	79	Osimertinib (common EGFR mutation)	pymhtcnzid(iapjlaweiu) = pylubwoodj jiogchbwqt (qldvogxpaq, 75 - 92) View more	Positive	05 Dec 2025
				Osimertinib (detectable plasma EGFRm)	pymhtcnzid(iapjlaweiu) = izmgedqbbe jiogchbwqt (qldvogxpaq, 82 - 97) View more
ESMO_ASIA2025	Not Applicable	EGFR-mutated non-small Cell Lung Cancer First line EGFR mutated	18	Osimertinib combined with chemotherapy (pemetrexed plus carboplatin)	lctbrpxrck(bklakmxvzh) = kujbklaeqy kkjyidvknk (cuicegwyit ) View more	Positive	05 Dec 2025
ESMO_ASIA2025	Not Applicable	Adenocarcinoma of Lung EGFR mutations	477	Osimertinib	nwimutagft(dxxdjlxqrw) = ckndszvzve wdelcsmvuu (hdibqbmqma ) View more	Positive	05 Dec 2025
ESMO_ASIA2025	Not Applicable	EGFR Mutation Lung Cancer EGFR-mutated	91	Osimertinib 80mg once daily	alodqivdna(tpndcqndpa) = elpcmenrzh iqkwbfwbda (qgmsmytumh ) View more	Negative	05 Dec 2025

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

AI Agents Built for Biopharma Breakthroughs

Accelerate discovery. Empower decisions. Transform outcomes.

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis