JIN-A02 / J Ints Bio - LARVOL DELTA

Phase 1/2 clinical trial of JIN-A02, a 4th generation EGFR-TKI in EGFR-mutated advanced/metastatic non-small cell lung cancer. (ASCO 2025) - P1/2 | "Dose-limiting toxicities (DLTs) are assessed over 21 days. Part B aims to further evaluate JIN-A02 safety to determine the RP2D using two preliminary effective dose levels from Part A. In Part C, subjects are divided into 5 cohorts based on the EGFR mutation status (both or single positive for C797S and T790M), and the anti-tumor activity of JIN-A02 is evaluated according to RECIST v1.1 at the RP2D."

Clinical • Metastases • P1/2 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Phase 1/2 clinical trial of JIN-A02, a 4th generation EGFR-TKI in EGFR mutated advanced/metastatic non-small cell lung cancer (AACR 2025) - P1/2 | "Dose-limiting toxicities (DLTs) areassessed over 21 days. Part B aims to further evaluate JIN-A02 safety todetermine the RP2D using two preliminary effective dose levels from Part A. InPart C, subjects are divided into 5 cohorts based on the EGFR mutation status(both or single positive for C797S and T790M), and the anti-tumor activity ofJIN-A02 is evaluated according to RECIST v1.1 at the RP2D."

Clinical • Metastases • P1/2 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

JIN-A02 Plus Amivantamab in EGFR-Mutant NSCLC After Third-Generation EGFR-TKI Failure (clinicaltrials.gov) - P1 | N=36 | Not yet recruiting | Sponsor: Yonsei University

New P1 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Discovery of Drug-Response Biomarkers Using Label-Free Plasma Proteomics in NSCLC Patients Treated With JIN-A02, a Fourth-Generation EGFR-TKI (IASLC-WCLC 2026) - P1/2 | "Conclusions : This study presents a framework that integrates plasma-based proteomic profiling with a generative AI approach to systematically discover drug-response biomarkers and functionally validate their relevance in NSCLC patients treated with a fourth-generation targeted therapy. This strategy has the potential to support noninvasive response monitoring, enable early detection of resistance, and inform personalized treatment decision-making."

Biomarker • Clinical • Lung Cancer • Non Small Cell Lung Cancer • Solid Tumor

AI-driven virtual transcriptome screening to identify repurposable combination partners for JIN-A02 in NSCLC. (ASCO 2026) - "Our results demonstrate the feasibility of virtual transcriptome generation as a scalable framework for discovering rational combination therapies in NSCLC. This strategy enables systematic exploration of a large target space, prioritizes clinically actionable combination hypotheses for JIN-A02, and reveals opportunities for drug repurposing. Follow-up studies will focus on experimental validation of predicted combinations and identification of biomarkers associated with combination sensitivity."

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

Phase 1/2 clinical trial of JIN-A02, a 4th generation EGFR-TKI, in patients with 3rd generation EGFR-TKI resistance in EGFR mutated advanced/metastatic non-small cell lung cancer (NSCLC) (AACR 2024) - P1/2 | "In Part B, dose exploration is carried out to evaluate the safety of JIN-A02 further and to determine the RP2D using 2 preliminary effective dose levels from Part A in subjects. In Part C dose-expansion study, subjects (n=36 for each cohort) are divided into 5 different cohorts based on the EGFR mutation (both or single positive of C797S and T790M), and the anti-tumor activity of JIN-A02 is evaluated according to RECIST v1.1 at RP2D."

Clinical • Metastases • P1/2 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

J INTS BIO Reports Fourth-Generation EGFR Inhibitor JIN-A02 in Clinical Cancer Research (PRNewswire) - "In preclinical models derived from patients with EGFR E19del/T790M/C797S mutant NSCLC that are resistant to Tagrisso, JIN-A02 demonstrated marked antitumor activity, achieving a maximum tumor growth inhibition (TGI) of 168.2%, substantially exceeding the effects observed with Tagrisso under the same conditions and indicating tumor regression...The publication also reports early clinical observations from an ongoing Phase 1/2 trial (NCT05394831) in patients with EGFR-mutant NSCLC who progressed after prior EGFR-targeted therapies and chemotherapy. As of the data cutoff, 23 patients had been treated with JIN-A02, with partial responses and stable disease observed in multiple cases. Notably, one patient in the 300 mg dose cohort achieved a partial response, with a 39.7% reduction in lung lesion size observed at the start of the third treatment cycle."

P1/2 data • Preclinical • Non Small Cell Lung Cancer

JIN-A02, a Mutant-Selective Fourth-Generation EGFR inhibitor, Overcomes C797S-Mediated Resistance and Demonstrates Intracranial Activity in NSCLC. (PubMed, Clin Cancer Res) - "These findings highlight JIN-A02 as a promising therapeutic strategy to overcome C797S- and T790M-mediated resistance in EGFR-mutant NSCLC, including intracranial disease, and support its further clinical development."

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

Effects of JIN-A02, a novel 4th generation EGFR-TKI, on multiple EGFR mutations in comparison with 3rd generation EGFR-TKIs [WITHDRAWN] (ESMO 2025) - No abstract available

Oncology

Phase 1/2 Clinical Trial of JIN-A02, a 4th Generation EGFR-TKI in EGFR Mutant Advanced/Metastatic Non-Small Cell Lung Cancer (NSCLC) (IASLC-WCLC 2025) - P1/2 | "Dose-limiting toxicities (DLTs) are assessed over 21 days. Part B aims to further evaluate JIN-A02 safety to determine the RP2D using two preliminary effective dose levels from Part A. In Part C, subjects are divided into 5 cohorts based on the EGFR mutation status (both or single positive for C797S and T790M), and the anti-tumor activity of JIN-A02 is evaluated according to RECIST v1.1 at the RP2D."

Clinical • Metastases • P1/2 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Effect of JIN-A02, a Novel 4Th-Generation EGFR-TKI, on Multiple EGFR Mutations in Comparison With 3rd-Generation EGFR-TKIs (IASLC-WCLC 2025) - P1/2 | "Methods : Docking simulation of ATP, JIN-A02, osimertinib and lazertinib were performed using Autodock Vina with the T790M/L858R (pdb: 5EM7) and the T790M/L858R/C797S(pdb: 6LUD) protein structures. In line with this enhanced binding affinity, the in vitro study showed significantly lower IC 90 value, effectively suppressing the proliferation of EGFR-mutated cell lines. These findings suggest that JIN-A02 has the potential to address the unmet therapeutic needs for NSCLC patients with heterogeneous EGFR mutations and, hence, may be a promising option for overcoming tumor tissue heterogeneity."

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

J Ints Bio unveils 4th-generation targeted anti-cancer drug candidate (KED Global) - "At the conference, J Ints Bio released preclinical results for JIN-A02, as well as early data on a Phase 1/2 trial, which is underway across several countries including South Korea, the US and Thailand. The preclinical data involves 23 patients."

P1/2 data • Preclinical • Non Small Cell Lung Cancer

Overcoming triple mutant EGFR-tyrosine kinase barriers in the therapeutics of non-small cell lung cancer: a patent review on fourth-generation inhibitors (2017-2024). (PubMed, Expert Opin Ther Pat) - "This review highlights the significance of fourth-generation EGFR tyrosine kinase inhibitors (EGFR-TKIs) in addressing acquired resistance mechanisms, such as the C797S mutation, which compromises the efficacy of third-generation inhibitors like Osimertinib and explores their potential to revolutionize NSCLC treatment through enhanced molecular specificity. Preclinical trials highlight the potential of sulfonyl and phosphine oxide-based compounds for their potency, selectivity, and favorable pharmacokinetics. Promising clinical trials with inhibitors like BDTX-1535, JIN-A02, and HS-10504 could redefine NSCLC treatment, with future success likely relying on innovative strategies, such as combination therapies, to combat resistance and enhance efficacy."

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

J INTS BIO to Present Global Clinical Results from JIN-A02, a Fourth-Generation EGFR-TKI, at ASCO 2025 (PRNewswire-Asia) - P1/2 | N=150 | NCT05394831 | Sponsor: J Ints Bio | "J INTS BIO...officially announced interim results from the global Phase 1/2 clinical trial of JIN-A02...at the American Society of Clinical Oncology 2025 (ASCO 2025)....Confirmed PRs were observed in 50mg,100mg and 300mg QD dose groups, providing clinical evidence of anti-tumor activity. In the 50 mg dose group, patients achieved a 77.3% reduction in tumor size, maintaining a PR over six consecutive treatment cycles (from cycle 3 to cycle 13). In the 300 mg dose group, a confirmed PR was observed with a 39.7% tumor size reduction, including a significant reduction in brain metastatic lesions. In the 100 mg dose group, a PR was also reported with a 35.3% reduction in tumor size, and brain metastatic lesions remained stable, further supporting the potential of JIN-A02 in treating brain metastases."

P1/2 data • Non Small Cell Lung Cancer

A Phase 1/2 Study to Evaluate the Safety, Tolerability and PK of JIN-A02 in Patients With EGFR Mutant Advanced NSCLC (clinicaltrials.gov) - P1/2 | N=150 | Recruiting | Sponsor: J Ints Bio | Trial completion date: Nov 2025 ➔ Sep 2026 | Trial primary completion date: Jul 2024 ➔ Sep 2026

Trial completion date • Trial primary completion date • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

'JIN-A02': New Hope for Overcoming Resistance – 4th Generation EGFR-TKI Clinical Results (PRNewswire) - P1/2 | N=150 | NCT05394831 | Sponsor: J Ints Bio | "In the clinical trial, a patient in the 300 mg cohort showed complete clearance of circulating tumor DNA (ctDNA) harboring either the C797S or Ex19del mutation, and ctDNA carrying the T790M mutation was reduced by over 90%. Clinically, a partial response (PR) was observed, with tumor size reductions of up to 39.7%, and notable shrinkage of intracranial metastatic lesions. These findings are particularly important for NSCLC patients, in whom brain metastases are common. Furthermore, no dose-limiting toxicities (DLTs) or serious adverse events were observed up to the 300 mg dose, highlighting the excellent safety profile of JIN-A02."

P1/2 data • Non Small Cell Lung Cancer

A clinical review on third and fourth generation EGFR tyrosine kinase inhibitors for the treatment of non-small cell lung cancer. (PubMed, Bioorg Med Chem) - "This review delves into the current clinical status, efficacy, safety profiles, and regulatory approvals of third-generation EGFR TKIs, including Osimertinib, Lazertinib, Furmonertinib, Aumolertinib, Rezivertinib, Befotertinib, Sunvozertinib...Notable fourth-generation candidates such as TQB3804, BPI-361175, BDTX-1535, WJ13404, QLH11811, H002, HS-10375, BBT-207, JIN-A02, and HS-10504 are highlighted for their potential to overcome the C797S mutation...By evaluating the therapeutic potential and limitations of these EGFR TKIs, this review aims to guide future research in the management of EGFR-mutant NSCLC. This acts as guiding beacon for the strategic design and development of third and fourth generation EGFR-TK inhibitors to overcome the drug resistance hurdles in the development of EGFR-TK inhibitors."

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

J INTS BIO Presents Interim Findings from Phase 1/2 Clinical Trial of 4th-Generation EGFR-TKI 'JIN-A02' in NSCLC: A Potential Breakthrough in Overcoming Acquired Resistance to Targeted Therapy (PRNewswire) - P1/2 | N=150 | NCT05394831 | Sponsor: J Ints Bio | "The data was presented at this year's edition of ENA (EORTC-NCI-AACR) Symposium....JIN-A02 demonstrated a very favorable tolerability across all dose levels studied so far, with no dose-limiting toxicities (DLTs) observed up to 150mg daily.....Tumor control were reported early in this study at lower doses. The first instance occurring at a relative low dose of 50mg. In this cohort, Partial Response of the lung lesions with stable disease in brain metastases was reported. Another Partial Response of the lung lesions was reported in the next cohort of 100mg, in a patient with similar primary EGFR mutation.....Reduction in the brain metastases was first reported with JIN-A02 in the 100mg Cohort, although stable disease was reported in the 50mg Cohort."

P1/2 data • Non Small Cell Lung Cancer

Phase 1/2 clinical trial of JIN-A02, a 4th generation EGFR-tyrosine kinase inhibitor (TKI), in patients with 3rd generation EGFR-TKI resistance in EGFR mutated advanced/metastatic non-small cell lung cancer (NSCLC) (EORTC-NCI-AACR 2024) - P1/2 | "JIN-A02 was well tolerated and showed preliminary antitumor activity in advanced and/or metastatic NSCLC with EGFR mutation, consistent with the expected mechanism of action. The study is active and recruiting."

Clinical • Metastases • P1/2 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Phase 1/2 Clinical Trial of JIN-A02, a 4th Generation EGFR-TKI in EGFR Mutated Advanced/metastatic Non-Small Cell Lung Cancer (NSCLC) (IASLC-WCLC 2024) - P1/2 | "Dose-limiting toxicities (DLTs) are assessed over 21 days. Part B aims to further evaluate JIN-A02 safety and to determine the RP2D using two preliminary effective dose levels from Part A. In Part C, subjects are divided into five cohorts based on the EGFR mutation status (both or single positive for C797S and T790M), and the anti-tumor activity of JIN-A02 is evaluated according to RECIST v1.1 at the RP2D."

Clinical • Metastases • P1/2 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Phase 1/2 clinical trial of JIN-A02, a 4th generation EGFR-TKI, in patients with 3rd generation EGFR-TKI resistance in EGFR mutated advanced/metastatic non-small cell lung cancer (NSCLC). (ASCO 2024) - P1/2 | "In Part B, dose exploration is carried out to evaluate the safety of JIN-A02 further and to determine the RP2D using 2 preliminary effective dose levels from Part A in subjects. In Part C dose-expansion study, subjects (n=36 for each cohort) are divided into 5 different cohorts based on the EGFR mutation (both or single positive of C797S and T790M), and the anti-tumor activity of JIN-A02 is evaluated according to RECIST v1.1 at RP2D."

Clinical • Metastases • P1/2 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

J INTS BIO, ASCO 2024 - JIN-A02 showed tumor reductions including brain metastasis in the ongoing first-in-human, dose-finding Phase 1 clinical study (PRNewswire) - P1/2 | N=150 | NCT05394831 | Sponsor: J Ints Bio | "This latest study update of JIN-A02 reported another tumor Partial Response (PR) in a patient in Cohort 4 (100mg daily)...To-date, Partial Response (PR) has been confirmed in two patients and Stable Diseases in three other, including the patient with reduction of brain metastasis in Cohort 4 and two patients from the lower Cohorts at a lower dose...The final patient in Cohort 4 (100mg) is expected to complete the dose-limiting toxicity (DLT) assessment period soon and thus far, no DLT has been detected...The next Cohort at 150mg daily will begin end of June...According to the company, JIN-A02 is scheduled to enter phase 2 clinical trial by the end of this year."

P1 data • Trial status • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

J INTS BIO announced the results of its ongoing Phase 1 clinical study of JIN-A02, a 4th generation EGFR-TKI for NSCLC treatment, at the 8th April poster session of the 2024 American Cancer Research Society (AACR) Annual Meeting (PRNewswire) - P1/2 | N=150 | NCT05394831 | Sponsor: J Ints Bio | "This ongoing Phase 1 clinical study is currently in its 4th Dose Level of 100mg daily and patients have showed increasing clinical benefits with each increasing dose levels. To-date, Partial Response (PR) was confirmed in one subject on the prior dose level of 50mg daily and stable diseases in two other subjects separately in Dose Level 50mg and 25mg daily. Despite the initial low doses, JIN-A02 has showed clinical benefits immediately, cumulating in a Partial Response at the 3rd Dose Level of 50mg....The 5th Dose Level of 150mg daily is expected to begin in 3Q 2024."

P1 data • Trial status • Non Small Cell Lung Cancer

J INTS BIO, Phase 1/2 study of 'JIN-A02', a Novel Oral 4th Generation EGFR TKI, accepted for presentation at the upcoming American Association for Cancer Research 2024 meeting in USA (AACR 2024) (PRNewswire) - "J INTS BIO announced on the 26th of month that the Phase 1/2 clinical study of its Novel Oral 4th Generation EGFR TKI 'JIN-A02' for the treatment of NSCLC has been accepted for poster presentation at the upcoming American Association for Cancer Research (AACR) meeting to be held in San Diego USA from 5 to 10 April....The topic of the presentation is 'Phase 1/2 clinical trial of JIN-A02, a 4th generation EGFR-TKI for 3rd generation EGFR-TKI resistant patients in EGFR mutated advanced/metastatic non-small cell lung cancer'."

P1/2 data • Non Small Cell Lung Cancer

A phase I/II study to evaluate the safety and anti-tumor activity of JIN-A02 in patients with EGFR TKI-refractory, EGFR-mutant advanced NSCLC (ESMO Asia 2023) - P1/2 | "JIN-A02, a 4th generation EGFR TKI, selectively and reversibly binds to EGFR mutations, including C797S mutation that results from the use of 3rd generation TKI such as osimertinib. Based on the results in Part A, two doses will be selected to be further evaluated in Part B in the same way with Part A but in a larger cohort of patients. This will determine the recommended phase 2 dose which will be studied in Part C in five cohorts based on the EGFR mutation and brain metastasis status."

Clinical • Metastases • P1/2 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor