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 | "Clinical Trial Registration Number: NCT05394831 The abstract will be released to the public on May 22, 2025 at 4:00 PM CDT"

Clinical • Metastases • P1/2 data • 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

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

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

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 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

J INTS BIO Gives Presentation of Phase 1/2 study of 'JIN-A02', a Novel Oral 4th Generation EGFR TKI, at ESMO Asia 2023 (PRNewswire) - P1/2 | N=150 | NCT05394831 | Sponsor: J Ints Bio | "J INTS BIO announced that early results of the Phase 1/2 study of its novel, orally administered 4th generation EGFR-TKI 'JIN-A02' were presented at the ESMO Asia 2023 conference held in Singapore from 1st to 3rd December 2023....To-date, no dose limiting toxicities (DLTs) or maximum tolerated dose (MTD) were reported and dosing for the 3rd cohort of patients will begin very soon. According to J INTS BIO, the clinical study is progressing well and recruitment has been unexpectedly successful with no unnecessary delays between the cohorts."

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

J INTS BIO, WCLC 2023 - Presentation of Phase 1/2 study of 'JIN-A02', a Novel Oral 4th Generation EGFR TKI (PRNewswire) - "This study is divided into three parts with dose escalation (Part A), dose exploration (Part B), and dose expansion (Part C). Part A explores ascending doses of oral JIN-A02 monotherapy in 28-day cycles to evaluate the maximum tolerated dose in patients with advanced NSCLC harboring C797S or T790M mutation. Based on the results obtained in part A, a safety review committee will select 2 doses to be further evaluated in Part B by determining the safety, pharmacokinetics, and efficacy in the same way as Part A albeit in a larger cohort of patients...Dosing of the first patient with JIN-A02 was achieved in July 2023 and as of 11th of September 2023, a total of three subjects have completed MTD evaluation period for Dose Level One of Part A. There was no DLT, no treatment related AE, and no clinical disease progression was noted."

Clinical protocol • Trial status • Non Small Cell Lung Cancer

A Phase 1, 2 Study to Evaluate the Safety and Anti-tumor Activity of JIN-A02 in Patients with EGFR Mutant Advanced NSCLC (IASLC-WCLC 2023) - P1/2 | "JIN-A02, a 4th generation EGFR TKI, selectively and reversibly binds to EGFR mutations, including C797S mutation that causes resistance to Osimertinib. Primary end points include dose limiting toxicity and AE/SAE for part A, RP2D for part B, and objective response rate for part C. Part A of JIN-A02 study has begun site activation in January 2023 in US, approved in Korea and is awaiting regulatory approval in Thailand. Clinical trial information: NCT05394831"

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

J INTS BIO, Novel Oral 4th Generation EGFR TKI ’JIN-A02’ - Dosing of First Patient in the Global Multi-center Phase 1/2 Clinical Study began (PRNewswire) - "J INTS BIO announced the successful dosing of the first patient in its global multi-center Phase 1/2 clinical study of 'JIN-A02' on 31st July at Severance Hospital, Seoul, Korea....This global phase 1/2 clinical trial seeks to evaluate the safety, pharmacokinetics and anti-tumor activity of 'JIN-A02' in advanced NSCLC patients carrying EGFR mutations."

Trial status • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thoracic 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 | Not yet recruiting ➔ Recruiting | N=95 ➔ 150 | Trial completion date: Dec 2024 ➔ Nov 2025 | Trial primary completion date: Dec 2023 ➔ Jul 2024

Enrollment change • Enrollment open • Metastases • Trial completion date • Trial primary completion date • Gastrointestinal Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • EGFR

J INTS BIO, Novel Oral 4th Generation EGFR TKI 'JIN-A02' - Phase 1/2 IND approved by US FDA (PRNewswire) - "J INTS BIO announced on November 9th that it had received approval from the US FDA for its Phase 1/2 clinical trial of its Novel Oral 4th Generation EGFR TKI 'JIN-A02' in patients with advanced non-small cell lung cancer (NSCLC). IND submission is currently ongoing sequentially in territories outside of USA....J INTS BIO is expecting the first patient to be recruited in the US before the end of the year."

IND • New P1/2 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thoracic Cancer • EGFR

JIN-A02, a fourth-generation, highly effective tyrosine kinase inhibitor with intracranial activity, targeting EGFR C797S mutations in NSCLC (ESMO 2022) - "It appears to be superior to osimertinib (IC 50 >4,000 nM for both cells). Conclusions JIN-A02 is highly potent EGFR-TKI for various EGFR targeted mutations including in cis and trans EGFR ex19del/T790M/C797S and shows intracranial activity. Based on these robust activities for EGFR mutants, JIN-A02 is expected to provide a potential therapeutic opportunity for NSCLC."

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

"#JINTSBIOs Novel Oral 4th Generation #EGFRTKI #JINA02 effective against both #Cis and #Trans #Isomers of #C797S mutations at #ESMO22 https://t.co/CQQZZ0Oho7" (@1stOncology)

Oncology

J INTS BIO, poster presentation of further preclinical data of its Novel Oral 4th Generation EGFR-TKI 'JIN-A02' at the 2022 European Society for Medical Oncology Congress in Paris, France (ESMO 2022) (PRNewswire) - "J INTS BIO announced the poster presentation of its novel, orally administered 4th generation EGFR-TKI 'JIN-A02' at the 2022 edition of the European Society for Medical Oncology Congress (ESMO 2022) held in Paris, France from 9th to 13th September....Key data highlighted during this poster event was the high potency of JIN-A02 against both cis and trans isomers of C797S mutation....Also highlighted is the inhibition of EGFR autophosphorylation by JIN-A02, in a time- and dose-dependent manner in in-vivo xenograft models with both double and triple C797S mutations....J INTS BIO believes that JIN-A02 will be a game changer in the treatment of patients with EGFR mutant NSCLC harboring C797S double or triple mutations, both in cis and trans forms, and it remains on track to begin the Phase I/IIa clinical study for JIN-A02 before the end of this year."

Preclinical • Trial status • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

J INTS BIO successfully held its 1st International Advisory Board Meeting for its Novel Oral 4th Generation EGFR TKI (JIN-A02) in Vienna, Austria during WCLC (PRNewswire) - "J INTS BIO announced that it held its 1st International Advisory Board Meeting for its Novel Oral 4th Generation EGFR-TKI 'JIN-A02' on the sideline of the 2022 IASLC World Conference on Lung Cancer held in Vienna, Austria, on 7th August. This followed the 2 successful focus group meetings conducted during ASCO in June....At this meeting, J INTS BIO conducted in-depth discussions with the experts on the development plans of 'JIN-A02', with the emphasis on enhancing the planned global Phase 1/2 clinical study which expects the first patient to be enrolled before the end of the year....The experts in attendance agreed that the focus of this study should be on C797S double and triple mutations which are the current unmet medical needs without an approved therapy or treatment and against which 'JIN-A02' showed highly potent inhibition both in-vitro and in-vivo."

Clinical protocol • Trial status • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

J INTS BIO, Oral presentation of Preclinical results of its Novel Oral 4th Generation EGFR TKI ’JIN-A02’ at the 2022 World Conference on Lung Cancer in Vienna, Austria (IASLC 2022 WCLC) (PRNewswire) - "J INTS BIO announced that the pre-clinical data of its novel, orally administered 4th generation EGFR TKI 'JIN-A02' was presented on the 8th of August, at the 2022 IASLC World Conference....In-vitro and in-vivo data of 'JIN-A02' showed robust inhibitory activities against NSCLC cancer cell-lines harboring double and triple C797S mutations, with selectivity away from EGFR Wild Type, which is important for patient safety. In addition, 'JIN-A02' also effectively reduced tumor volume in a dose-dependent manner, compared to Osimertinib, in mouse model harboring EGFR C797S triple mutation, showing high brain penetrance with efficacy. Prof. Cho ended his presentation by putting forth that JIN-A02 may be the Best-In-Class 4th generation EGFR-TKI against NSCLC."

Preclinical • Lung Cancer • Non Small Cell Lung Cancer • Oncology

JIN-A02, a Highly Effective 4th Generation EGFR-TKI, Targeting EGFR C797S Triple Mutation in NSCLC (IASLC-WCLC 2022) - "It showed comparable potency to osimertinib in both double mutants (IC50=12.3 for ex19del/T790M, IC50=5.3 nM for L858R/T790M) and single mutants (IC50=3.2 nM for ex19del, IC50=9.1 nM for L858R). These preclinical studies demonstrated that JIN-A02 is a potential best-in-class fourth-generation EGFR TKI with high potency and selectivity. JIN-A02 showed robust activities against EGFR C797S mutation including single and double EGFR mutations. It was also effective against L718Q, for which there are currently no treatment alternatives."

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