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

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

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

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

A prospective, controlled Phase II clinical study on the efficacy and safety of the combination of lerotinib and bevacizumab versus lerotinib monotherapy as first - line treatment for locally advanced or recurrent metastatic non - squamous NSCLC with EGFR mutations and high PD-L1 expression. (ChiCTR) - P2 | N=136 | Not yet recruiting | Sponsor: Shanghai Chest Hospital; Shanghai Chest?Hospital

IO biomarker • Monotherapy • New P2 trial • Lung Cancer • Lung Non-Squamous Non-Small Cell Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • PD-L1

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

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

LIBRA: A Clinical Study on the Efficacy and Safety of the Combination of Limertinib and Bevacizumab Versus Limertinib as First-line Treatment for NSCLC. (clinicaltrials.gov) - P2 | N=136 | Not yet recruiting | Sponsor: Shanghai Chest Hospital

IO biomarker • Monotherapy • New P2 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • PD-L1

THE THIRD-GENERATION EGFR TKI LIMERTINIB RECEIVED APPROVAL FROM THE NATIONAL MEDICAL PRODUCTS ADMINISTRATION FOR THE FIRST-LINE TREATMENT OF LUNG CANCER (HKEXnews) - "The board of directors of the Company (the 'Board') is pleased to announce that the new drug application of limertinib, the third-generation epidermal growth factor receptor ('EGFR') tyrosine kinase inhibitor ('TKI'), received approval from the National Medical Products Administration of China ('NMPA') for the first-line treatment in adult patients with locally advanced or metastatic non-small cell lung cancer ('NSCLC') harboring EGFR exon 19 deletions or exon 21 L858R mutations. The approval of this new indication is supported by positive results from a randomized, double-blind, positive-controlled Phase 3 clinical trial. A total of 337 treatment-naïve patients with EGFR-sensitive mutation-positive locally advanced or metastatic NSCLC were enrolled and randomized at the ratio of 1:1 to receive either limertinib or gefitinib."

China approval • Non Small Cell Lung Cancer

Six new product launches in 2025 with growth momentum anticipated (PRNewswire) - "Three additional approved precision therapies to strengthen lung and hematological cancer franchises: Dovbleron; Limertinib; Jaypirca"

Commercial • Non Small Cell Lung Cancer • Non-Hodgkin’s Lymphoma

Long-term follow-up of limertinib (ASK120067) in patients with locally advanced or metastatic EGFR T790M NSCLC: A multicentre, single-arm, phase IIb study (ELCC 2025) - P1/2 | "Long-term follow-up results support the potential of Limertinib (ASK120067) as a promising treatment for EGFR T790Mmutated NSCLC. Reduced-dose limertinib demonstrated encouraging survival outcomes and is worthy of further investigation."

Clinical • Metastases • P2b data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

Innovent and ASK Pharm Jointly Announce NMPA Approval of Limertinib, a Third-generation EGFR TKI for the Treatment of Lung Cancer (PRNewswire) - "Innovent Biologics...and Jiangsu Aosaikang Pharmaceutical...jointly announce that China's National Medical Products Administration (NMPA) has approved the New Drug Application (NDA) of limertinib for the treatment of adult patients with locally advanced or metastatic EGFR T790M-mutated non-small cell lung cancer (NSCLC)....A Phase 2b pivotal study evaluating 301 patients with locally advanced or metastatic EGFR T790M-mutated NSCLC demonstrated limertinib's robust efficacy and safety profile....Additionally, limertinib met its primary endpoint in a Phase 3 clinical trial comparing it to gefitinib for first-line treatment of locally advanced or metastatic NSCLC harboring EGFR mutations. A separate NDA for the first-line treatment in adult patients with locally advanced or metastatic NSCLC carrying EGFR exon 19 deletions or exon 21 L858R mutations is currently under NMPA review."

China approval • China filing • Evidence highlight • Non Small Cell Lung Cancer • Oncology • EGFR

Innovent and Ask Pharm Announce Strategic Collaboration for Limertinib, a Third-generation EGFR TKI for the Treatment of Lung Cancer (PRNewswire) - "Innovent Biologics...and Jiangsu Aosaikang Pharmaceutical...announced that the two parties have entered into a strategic collaboration regarding limertinib, a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) for the treatment of lung cancer. Under the agreement, Innovent will obtain the exclusive commercialization rights for limertinib in mainland China, and will be entitled to receive a commercialization service fee based on the product's net sales in the region. Ask-Pharm as the MAH holder, will be responsible for the production and commercial supply of limertinib and will be eligible for upfront, regulatory and sales milestone payments."

Licensing / partnership • Non Small Cell Lung Cancer

Branched-chain amino acid transaminase 1 confers EGFR-TKI resistance through epigenetic glycolytic activation. (PubMed, Signal Transduct Target Ther) - "In this study, we conducted a comprehensive investigation utilizing high-throughput proteomics analysis on established TKI-resistant tumor models, and found a notable upregulation of branched-chain amino acid transaminase 1 (BCAT1) expression in both osimertinib- and ASK120067-resistant tumors compared with the parental TKI-sensitive NSCLC tumors. Moreover, we identified WQQ-345 as a novel BCAT1 inhibitor exhibiting antitumor activity both in vitro and in vivo against TKI-resistant lung cancer with high BCAT1 expression. In summary, our study highlighted the crucial role of BCAT1 in mediating resistance to third-generation EGFR-TKIs through epigenetic activation of glycolysis in NSCLC, thereby supporting BCAT1 as a promising therapeutic target for the treatment of TKI-resistant NSCLC."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • BCAT1

ASK120067 Versus Gefitinib as First-line Treatment for EGFRm Locally Advanced or Metastatic NSCLC (clinicaltrials.gov) - P3 | N=337 | Active, not recruiting | Sponsor: Jiangsu Aosaikang Pharmaceutical Co., Ltd. | Recruiting ➔ Active, not recruiting | Trial completion date: Dec 2023 ➔ Sep 2026 | Trial primary completion date: Mar 2023 ➔ Mar 2024

Enrollment closed • Metastases • Trial completion date • Trial primary completion date • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

AM-DMF-SCP: Integrated Single-Cell Proteomics Analysis on an Active Matrix Digital Microfluidic Chip. (PubMed, JACS Au) - "Applying the AM-DMF-SCP to characterize the proteomes of a third-generation EGFR inhibitor, ASK120067-resistant cells (67R) and their parental NCI-H1975 cells, we observed a potential correlation between elevated VIM expression and 67R resistance, which is consistent with the findings from bulk sample analyses. These results suggest that AM-DMF-SCP is an automated, robust, and sensitive platform for single-cell proteomics and demonstrate the potential for providing valuable insights into cellular mechanisms."

Journal • Oncology • VIM

Aosaikang: The combination of ASKC202 tablets and ASK120067 tablets has been approved for clinical trials [Google translation] (Stockstar) - "Securities Times e company news, Aosaikang...announced on the evening of November 12 that the clinical trial of the combination of ASKC202 tablets and ASK120067 tablets submitted by Jiangsu Aosaikang Pharmaceutical, a wholly-owned subsidiary of the company, has recently received a clinical trial certificate issued by the State Food and Drug Administration. The trial approval notice agrees to conduct a clinical trial of ASKC202 tablets in combination with ASK120067 tablets for advanced solid tumors."

New trial • Oncology • Solid Tumor

China clinical practice guideline for epidermal growth factor receptor tyrosine kinase inhibitors in stage â…£ non-small cell lung cancer (version 2023) (PubMed, Zhonghua Yi Xue Za Zhi) - "As of August 23, 2023, the first generation EGFR-TKIs, gefitinib, icotinib, and erlotinib; the second generation EGFR-TKIs, afatinib and dacomitinib; and the third generation EGFR-TKIs, osimertinib, almonertinib, furmonertinib and befotertinib were all approved for marketing by China National Medical Products Administration (NMPA). In addition, multiple domestic third-generation EGFR-TKIs are undergoing clinical trials, such as rezivertinib (BPI-7711), limertinib (ASK120067), and oritinib (SH-1028). Meanwhile, mobocertinib and sunvozertinib, which targets EGFR 20ins mutations, were also approved by NMPA. With the increasing variety of EGFR-TKIs approved for marketing subsequently, it brings confusion to clinicians when choosing specific medications, and there is an urgent need to develop relevant treatment guidelines. Hence, the Medical Oncology Branch of China International Exchange and Promotive Association for Medical and Health Care and the Chinese Association for..."

Clinical guideline • Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • EGFR

Phase 1 study to evaluate the effects of rifampin or itraconazole on the pharmacokinetics of limertinib (ASK120067), a novel mutant-selective inhibitor of the epidermal growth factor receptor in healthy Chinese subjects. (PubMed, Expert Opin Drug Metab Toxicol) - P1 | "A single dose of limertinib, administered with or without rifampin or itraconazole, is generally safe and well tolerated in healthy Chinese subjects. www.clinicaltrials.gov identifier is NCT05631678."

Journal • P1 data • PK/PD data • CYP3A4 • EGFR

Aosaikang: Subsidiary drug clinical trial application accepted [Google translation] (Daily Economic News - NBD) - "...Aosaikang announced that the clinical trial application for the combination of the subsidiary's innovative drug ASKC202 tablets and ASK120067 tablets has been accepted."

New trial • Oncology