limertinib (ASK120067) / Aosaikang Pharma, Innovent Biologics - LARVOL DELTA

Exploration of the Efficacy and Safety of Limertinib as Adjuvant Therapy in Patients with Stage II-IIIA Non-Small Cell Lung Cancer Harboring EGFR Uncommon Mutations After Radical Resection. (ChiCTR) - P4 | N=18 | Not yet recruiting | Sponsor: The Fourth Hospital of Hebei Medical University; The Fourth Hospital of Hebei Medical University

New P4 trial • Lung Cancer • Lung Non-Squamous Non-Small Cell Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Efficacy and safety of ASK120067 (limertinib) in patients with locally advanced or metastatic EGFR T790M-mutated non–small cell lung cancer: A multicenter, single-arm, phase IIb study. (ASCO 2022) - P1/2 | "ASK120067 demonstrated promising efficacy and an acceptable safety profile for the treatment of patients with locally advanced or metastatic EGFR T790M mutated NSCLC."

Clinical • P2b data • Anemia • Hematological Disorders • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

ASKC202 Combined With Limertinib Versus Platinum-based Chemotherapy in Treatment of Locally Advanced or Metastatic NSCLC With MET Amplification/Overexpression After Failure of EGFR-TKI Therapy (clinicaltrials.gov) - P3 | N=286 | Recruiting | Sponsor: Jiangsu Aosaikang Pharmaceutical Co., Ltd. | Not yet recruiting ➔ Recruiting

Enrollment open • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • MET

First-line third-generation EGFR-TKIs for advanced EGFR-mutated non-small cell lung cancer: a systematic review and network meta-analysis of randomized controlled trials. (PubMed, J Thorac Dis) - "All investigated third-generation agents (aumolertinib, osimertinib, furmonertinib, befotertinib, limertinib, rilertinib, lazertinib, and rezivertinib) demonstrated superior PFS compared to first-generation TKIs. Most third-generation TKIs offer superior PFS compared to first-generation agents, with comparable efficacy observed across the third-generation agents. Safety profiles, specifically regarding high-grade adverse events, appear similar between third- and first-generation TKIs."

Journal • Retrospective data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

ASKC202 Combined With Limertinib Versus Platinum-based Chemotherapy in Treatment of Locally Advanced or Metastatic NSCLC With MET Amplification/Overexpression After Failure of EGFR-TKI Therapy (clinicaltrials.gov) - P3 | N=286 | Not yet recruiting | Sponsor: Jiangsu Aosaikang Pharmaceutical Co., Ltd.

New P3 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Sphingosine-1-phosphate receptor 3 confers tumor metastasis in lung cancer resistant to third-generation EGFR inhibitor (EACR 2026) - "Trans-well assay, chromatin immunoprecipitation assay, promoter luciferase reporter assay and in vivo luciferase imaging assay were employed to explore the mechanisms that mediated metastasis in EGFR TKI-resistant tumors.Result and Using transcriptomics analyses on established ASK120067-resistant and AZD9291-resistant tumor models, we identified an aberrant upregulation of S1PR3 in resistant cells, which conferred enhanced metastatic potential to lung cancer. Our findings identify S1PR3 as a critical driver of metastatic progression in third-generation EGFR inhibitor-resistant lung cancer, highlighting targeting S1PR3 as a potential therapeutic strategy that could be employed to prevent tumor progression."

Lung Cancer • Oncology • Solid Tumor • RAC1

Study of IBI3005 Combination Therapy in Participants With Unresectable, Locally Advanced or Metastatic Solid Tumors (clinicaltrials.gov) - P1/2 | N=282 | Not yet recruiting | Sponsor: Innovent Biologics (Suzhou) Co. Ltd.

New P1/2 trial • Lung Cancer • Lung Non-Squamous Non-Small Cell Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK • ROS1

Sphingosine-1-Phosphate Receptor 3 Confers Tumor Metastasis in Lung Cancer Resistant to Third-Generation EGFR Inhibitor. (PubMed, MedComm (2020)) - "The third-generation EGFR tyrosine kinase inhibitor (TKI) osimertinib (AZD9291) has significantly improved the survival in EGFR-mutant lung cancer patients. Our team developed limertinib (ASK120067), a novel third-generation EGFR inhibitor with remarkable antitumor effects, which has been launched in China...Further studies identified that the overexpression of fibroblast growth factor receptor 1 (FGFR1) increased S1PR3 expression through signal transducer and activator of transcription 4 (STAT4) to promote the emergence of metastatic-resistant cells. Importantly, targeting S1PR3 or FGFR1 blocks metastasis in EGFR TKI-resistant models."

Journal • Lung Cancer • Oncology • Solid Tumor • FGFR1 • RAC1 • STAT4

A randomised phase II study of limertinib and bevacizumab versus limertinib alone as second-line targeted treatment in locally advanced or metastatic NSCLC with EGFR mutations and resistance to third-generation EGFR-TKIs (ChiCTR) - P2 | N=40 | Sponsor: Anhui Chest Hospital; Anhui Chest Hospital

New P2 trial • Lung Cancer • Lung Non-Squamous Non-Small Cell Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

First-line limertinib versus gefitinib in EGFR-mutated advanced NSCLC: Updated overall survival results from a randomized, double-blind, phase III trial (ELCC 2026) - P3 | "No new safety signals were identified with long-term exposure to limertinib.Conclusions With over 41 months of follow-up, limertinib had a clinically substantial OS benefit, with a 9-month improvement in median OS and a 10% increase in 3-year OS rate compared with gefitinib, and a manageable long-term safety profile. These results demonstrated limertinib as a preferred first-line treatment option for patients with EGFR-mutated advanced NSCLC."

Clinical • Metastases • P3 data • Lung Cancer • Non Small Cell Lung Cancer • Solid Tumor • EGFR

Limertinib Plus Carboplatin and Etoposide for EGFR-mutant NSCLC With SCLC Transformation After EGFR-TKI Progression (clinicaltrials.gov) - P2 | N=30 | Not yet recruiting | Sponsor: Hunan Province Tumor Hospital | Initiation date: Oct 2025 ➔ May 2026

Trial initiation date • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Small Cell Lung Cancer • Solid Tumor

Epidermal growth factor receptor tyrosine kinase inhibitor for the treatment of non-small cell lung cancer in the past 30 years (1997-2026). (PubMed, Chin Med J (Engl)) - "Since 1997, EGFR tyrosine kinase inhibitors (EGFR-TKIs) have evolved from first-generation agents, such as gefitinib, erlotinib, and icotinib, to second-generation agents like afatinib and dacomitinib, now to third-generation agents, including osimertinib, aumolertinib, furmonertinib, befotertinib, rezivertinib, rilertinib, limertinib, lazertinib, mifanertinib for EGFR L858R, sunvozertinib for EGFR exon 20 insertion (20ins), and zorifertinib for EGFR-sensitive mutation with brain metastases. Over the past 30 years, substantial advancements have been made in the comprehensive management of EGFR-mutant NSCLC. This systemic review provides the history of the development of EGFR-TKI therapy for NSCLC from 1997 to 2026, highlighting clinical milestones, emerging therapies, and future directions in this rapidly evolving field."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Limertinib Plus Radiotherapy for EGFR-Mutant NSCLC With Brain Metastases (clinicaltrials.gov) - P2 | N=45 | Not yet recruiting | Sponsor: The First Affiliated Hospital of Guangzhou Medical University

New P2 trial • Brain Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Limertinib Plus Platinum-Based Chemotherapy in Patients with Advanced EGFR-Mutated Non-Squamous NSCLC after Progression on First-Line EGFR-TKI Therapy : A Single-Arm, Multicenter Study (ChiCTR) - P2 | N=61 | Not yet recruiting | Sponsor: Qilu Hospital of Shandong University; Qilu Hospital of Shandong University

New P2 trial • Lung Cancer • Lung Non-Squamous Non-Small Cell Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Neoadjuvant Sacituzumab Tirumotecan and Limertinib for Potentially Resectable Stage Ⅲ EGFR-mutant Non-small Cell Lung Cancer (clinicaltrials.gov) - P2 | N=36 | Recruiting | Sponsor: Shanghai Pulmonary Hospital, Shanghai, China

New P2 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

ASKC202-001: Study to Assess the Safety, Tolerability, Pharmacokinetics and Preliminary Anti-tumor Activity of ASKC202 With or Without ASK120067 (clinicaltrials.gov) - P1 | N=150 | Recruiting | Sponsor: Jiangsu Aosaikang Pharmaceutical Co., Ltd. | Trial completion date: May 2025 ➔ Dec 2027 | Trial primary completion date: May 2024 ➔ Dec 2026

Trial completion date • Trial primary completion date • Oncology • Solid Tumor • MET

In the updated NRDL, limertinib is newly listed for: 1) the treatment of adult patients with locally advanced or metastatic EGFR T790M-mutated…NSCLC, who have previously experienced disease progression during or after treatment with EGFR TKI; and 2) the first-line treatment of adult patients with locally advanced or metastatic NSCLC carrying EGFR exon 19 deletions or exon 21 L858R mutations (PRNewswire)

Reimbursement • Non Small Cell Lung Cancer

​Efficacy and Safety of Limertinib Combined with Radioactive Iodine-125 Seed Implantation in Patients with EGFR-Mutant Advanced Non-Squamous Non-Small Cell Lung Cancer Exhibiting Oligoprogression After Prior EGFR-TKI Therapy: A Prospective, Single-Arm, Multicenter, Observational Study​ (ChiCTR) - P4 | N=33 | Not yet recruiting | Sponsor: Hebei General Hospital​; Hebei General Hospital

New P4 trial • Lung Cancer • Lung Non-Squamous Non-Small Cell Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

ASKC202 plus limertinib in EGFR-mutated advanced or metastatic NSCLC patients with MET amplification or MET overexpression following EGFR-TKI (ESMO 2025) - P1 | "Conclusions ASKC202 plus Limertinib showed excellent antitumor activity and a manageable safety profile in patients with EGFRm NSCLC with MET amplification or MET overexpression who have progressed after EGFR TKI therapy. Legal entity responsible for the study Jiangsu Aosaikang Pharmaceutical Co., Ltd, Jiangsu, China."

Clinical • Metastases • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • MET

Chemical Adaptation in Drug Discovery: The Medicinal Chemistry Journey of Olverembatinib and Limertinib in Overcoming Kinase Drug Resistance. (PubMed, Acc Chem Res) - "Building on this success, we are advancing next-generation inhibitors designed to overcome additional resistance mutations such as EGFRL858R/T790M/C797S.In summary, this Account highlights the medicinal chemistry strategies underlying the approvals of olverembatinib and limertinib, illustrating how chemical adaptation can be harnessed to overcome kinase inhibitor resistance. Moving forward, we aim to expand this concept across broader drug modalities and therapeutic targets to address ongoing clinical challenges."

Journal • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Multicenter Phase II Randomized Trial of Limertinib Followed by Sintilimab and Chemotherapy vs. Limertinib Followed by Limertinib and Chemotherapy as Neoadjuvant Therapy in Resectable Stage II–IIIB EGFR-Mutant NSCLC (ChiCTR) - P2 | N=134 | Not yet recruiting | Sponsor: Guangdong Provincial People's Hospital(Guangdong Academy of Medical Sciences); Guangdong Provincial People's Hospital(Guangdong Academy of Medical Sci

New P2 trial • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR • PD-L1

NEO-LISI: A Multicenter Phase II Randomized Trial of Limertinib Followed by Sintilimab and Chemotherapy vs. Limertinib Followed by Limertinib and Chemotherapy as Neoadjuvant Therapy in Resectable Stage II-IIIB EGFR-Mutant NSCLC (clinicaltrials.gov) - P2 | N=134 | Not yet recruiting | Sponsor: Wen-zhao ZHONG

New P2 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Limertinib for EGFR mutation-positive NSCLC treatment. (PubMed, Lancet Respir Med) - No abstract available

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Limertinib: First Approval. (PubMed, Drugs) - "In April 2025, limertinib was also approved in China for first-line treatment for adult patients with locally advanced or metastatic NSCLC harbouring EGFR exon 19 deletions or exon 21 L858R mutations. This article summarizes the milestones in the development of limertinib leading to this first approval."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Efficacy and safety of limertinib versus gefitinib as first-line treatment for locally advanced or metastatic non-small-cell lung cancer with EGFR-sensitising mutation: a randomised, double-blind, double-dummy, phase 3 trial. (PubMed, Lancet Respir Med) - P3 | "Limertinib showed superior efficacy compared with gefitinib and a manageable safety profile for locally advanced or metastatic NSCLC patients with EGFR-sensitising mutation and should be considered as another first-line treatment option for this patient population."

Journal • P3 data • Infectious Disease • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pneumonia • Respiratory Diseases • Solid Tumor • EGFR