Pipeline

JIN-A02

Target Disease Information

  • Lung cancer exhibits the highest incidence and mortality rates among all cancers, and non-small cell lung cancer (NSCLC), which accounts for 85%
    of lung cancers, is a representative refractory cancer with low treatment response rates and rapid metastasis.
  • The epidermal growth factor receptor (EGFR) mutation, a representative driver mutation in NSCLC, is highly prevalent—observed in 40–55%
    of Asian NSCLC patients, including those in Korea.
  • The C797S mutation, which emerges as an acquired resistance mutation following third-generation EGFR-TKI therapies, currently has no treatment options.

Introduction of JIN-A02

  • JIN-A02 is a kinase inhibitor targeting EGFR mutations in NSCLC. It exhibits potent anticancer effects against the key acquired resistance mutation EGFR C797S,
    which emerges after third-generation EGFR-TKI therapies. Additionally, it demonstrates superior efficacy compared to third-generation EGFR-TKIs against
    compound mutations involving C797S—whether in combination with exon 19 deletions, L858R, or T790M—covering both double and triple mutation profiles.
    This highlights its potential as a promising next-generation EGFR-TKI.
  • It also shows high blood-brain barrier permeability and robust intracranial activity, addressing brain metastases—a major metastatic site in NSCLC—and
    suggests potential clinical response for brain metastases.
  • JIN-A02 exhibits high selectivity for mutant EGFR over wild-type EGFR, and maintains very favorable safety profiles even at high doses.

Mechanism of Action of JIN-A02

  • Superior efficacy against EGFR exon 19 deletions, as well as L858R, T790M, and C797S mutations
  • High selectivity for mutant EGFR compared to wild-type EGFR
  • Superior target binding affinity and efficacy compared to third-generation EGFR-TKIs

Key Research Findings of JIN-A02

  • Phase 1/2 open-label, multicenter clinical trial evaluating safety, tolerability, pharmacokinetics, and antitumor activity of JIN-A02 in patients with advanced
    EGFR-mutant NSCLC(NCT05394831)
  • Regulatory approvals obtained in Korea (2023), the US (2022), and Thailand (2022).
  • No drug-related serious adverse events or dose-limiting toxicities reported to date in enrolled patients.

JIN-A02 Conference Presentation Status

Conference Topic
2025 ASCO (Poster presentation) Clinical
2025 AACR (Poster presentation) Clinical
2024 ENA (Poster presentation) Clinical
2024 WCLC (Poster presentation) Clinical
2024 ASCO (Poster presentation) Clinical
2024 AACR (Poster presentation) Clinical
2023 ESMO Asia (Poster presentation) Clinical
2023 WCLC (Poster presentation) Clinical
2022 ESMO (Poster presentation) Preclinical
2022 WCLC (Oral presentation) Preclinical
  • AACR: American Association for Cancer Research
  • ASCO: American Society of Clinical Oncology
  • ENA: EORTC-NCI-AACR(EORTC - NCI - AACR)
  • ESMO: European Society For Medical Oncology
  • WCLC: World Conference on Lung Cancer

National Research and Development Project

  • Selection as a project in the 1st phase of the 2025 National New Drug Development Program funded by KDDF