ArticleEClinicalMedicine2025
Safety, pharmacokinetic, pharmacodynamic, and efficacy properties of orally administered APG-2449 in patients with advanced
Article in EClinicalMedicine, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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2 citing papers in PubMed.
- Adaptive epithelial-mesenchymal bi-directional transition: A key invasive plasticity for tumor metastasis.iScience · 2026Review
- Targeting Cytoskeleton and Cell Motility: Past and Novel Strategies for Cancer Therapy.Oncology research · 2026Review
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26 authors.
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Abstract
Background: APG-2449 is a focal adhesion kinase (FAK) inhibitor and a third-generation anaplastic lymphoma kinase (ALK)-proto-oncogene receptor tyrosine kinase ROS (ROS1) tyrosine kinase inhibitor (TKI). The aim of this first-in-human study was to evaluate safety and efficacy of APG-2449 in patients with advanced non-small-cell lung cancer (NSCLC). Methods: This single-arm, multicentre, phase 1 clinical trial included a dose escalation to determine maximum tolerated dose (MTD) and recommended phase 2 dose (RP2D), followed by a dose-expansion stage at RP2D to evaluate safety. Secondary endpoints included pharmacokinetics, pharmacodynamics, and preliminary efficacy. APG-2449 was administered once daily in 28-day cycles through a 3 + 3 dose escalation. Eligible patients were aged 18 years or older and had advanced ALK or ROS1 fusion gene-positive NSCLC and other solid tumours (during the dose escalation). Patients with Findings: 144 patients were enrolled from May 27, 2019, to April 2, 2024, and received APG-2449 (150-1500 mg/day). MTD was not reached, and RP2D was 1200 mg. The most common grade ≥3 treatment-emergent adverse events (TEAE) were anaemia [6 (4.2%)], alanine aminotransferase (ALT) increased [6 (4.2%)], electrocardiogram QT prolonged [5 (3.5%)], and pneumonia [5 (3.5%)]. The most common grade ≥3 treatment-related adverse events (TRAEs) were ALT increased [5 (3.5%)], QT prolonged [5 (3.5%)], and vomiting [2 (1.4%)]. There were no treatment-related deaths. Pharmacokinetic analyses indicated a dose-proportional increase in plasma exposure, and that APG-2449 penetrated the blood-brain barrier (cerebrospinal fluid [CSF]-to-free plasma ratio 0.65-1.66). Of patients with Interpretation: APG-2449 demonstrated favourable preliminary safety, pharmacokinetics, and efficacy in TKI-untreated or second-generation ALK-resistant NSCLC. Higher baseline tumour phosphorylated FAK levels were associated with greater APG-2449 treatment benefit. Targeting FAK signalling may provide a feasible strategy for overcoming second-generation ALK TKI resistance. Funding: Ascentage Pharma Group Corp Ltd. (Hong Kong).
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