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APL-1202 (also known as nitroxoline) is a reversible, orally available methionine aminopeptidase 2 (MetAP2) inhibitor with anti-angiogenic and anti-tumor activities. Tislelizumab is a humanized IgG4 monoclonal antibody that targets programmed cell death protein 1 (PD-1), functioning as an immune checkpoint inhibitor. The combination of APL-1202 and tislelizumab has been investigated as neoadjuvant therapy for muscle-invasive bladder cancer (MIBC), particularly in patients who are ineligible for or refuse cisplatin-based chemotherapy. Clinical trials have demonstrated that this combination shows synergistic effects, leading to higher pathological complete response rates compared to monotherapy with tislelizumab[1][3][7]. The primary developer of APL-1202 is Asieris Pharmaceuticals.
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