TRANSTHERA-B(02617): First Patient Dosed in China Phase II Clinical Trial of Tinengotinib Combined with Novel Endocrine Therapy for Metastatic Castration-Resistant Prostate Cancer After Progression on Prior Treatment

TRANSTHERA-B(02617) announced that the first patient has recently been dosed in the China Phase II clinical trial of the Company's core product Tinengotinib (, Tinengotinib, TT-00420) in combination with novel endocrine therapy (NHT) for metastatic castration-resistant prostate cancer (mCRPC) that has progressed after prior treatment. This trial is an open-label, multicenter, Phase II clinical study evaluating the safety and efficacy of Tinengotinib in combination with NHT in patients with mCRPC who have progressed after prior treatment. The primary target population of the trial consists of patients who have experienced disease progression after prior treatment with novel endocrine therapy (including abiraterone and AR inhibitors). The primary endpoints of the trial include safety assessment, 6-month PFS rate (6mo-PFS), and radiographic progression-free survival (rPFS). The global mCRPC drug market was valued at US$16.13 billion in 2025 and is projected to grow to US$28.09 billion by 2032, with a compound annual growth rate of 8.25%; the domestic market is also maintaining rapid growth in tandem, with China's CRPC treatment market reaching RMB 19.443 billion in 2025, a year-on-year increase of 12.3%, outpacing the average growth rate of the overall anti-tumor drug market, as rigid clinical treatment demand continues to be released. Among these, although novel endocrine therapy drugs can significantly prolong patient survival and represent the current first-line core treatment regimen for mCRPC, the vast majority of patients will eventually develop acquired resistance. Tinengotinib is the world's first and only investigational drug that simultaneously inhibits the FGFR/JAK pathways and has clinical efficacy evidence for mCRPC. Recent studies have found that activation of the FGFR and JAK pathways promotes the transformation of androgen-sensitive cancer cells into neuroendocrine cancer cells, thereby causing drug resistance. Simultaneously inhibiting the FGFR and JAK pathways can reverse this cell state transition or lineage reprogramming, restoring the sensitivity of cancer cells to androgens and re-sensitizing them to NHT treatment. Tinengotinib monotherapy has already demonstrated encouraging anti-tumor efficacy in mCRPC patients who have received multiple prior lines of treatment. In addition, Tinengotinib monotherapy for mCRPC received Fast Track designation from the U.S. FDA in June 2025.