Transthera-B (02617) has announced that the first patient has been dosed in its Phase II clinical trial in China evaluating tinengotinib (Jentai®; Tinengotinib, TT-00420) combined with novel endocrine therapy (NHT) for the treatment of metastatic castration-resistant prostate cancer (mCRPC) that has progressed after prior therapy.

This study is an open-label, multi-center, Phase II clinical trial designed to assess the safety and efficacy of tinengotinib in combination with NHT in patients with mCRPC who have progressed following prior treatment. The primary target population consists of patients who experienced disease progression after receiving prior novel endocrine therapy, including abiraterone and AR inhibitors. Key endpoints of the trial include safety evaluations, the 6-month progression-free survival rate (6mo-PFS), and radiographic progression-free survival (rPFS).

In 2025, the global mCRPC drug market is valued at $16.13 billion, with projections indicating growth to $28.09 billion by 2032, reflecting a compound annual growth rate of 8.25%. The domestic market is also experiencing rapid expansion, with the Chinese CRPC treatment market reaching RMB 19.443 billion in 2025, up 12.3% year-over-year—a growth rate surpassing the average for the overall anti-tumor drug market, as clinical demand for essential treatment continues to be released.

While novel endocrine therapies significantly extend patient survival and currently serve as the core first-line treatment for mCRPC, the vast majority of patients ultimately develop acquired resistance. Tinengotinib is the world's first and only investigational drug that simultaneously inhibits both the FGFR and JAK pathways, with clinical efficacy evidence specifically in mCRPC. Recent research has revealed that activation of the FGFR and JAK pathways drives the transformation of androgen-sensitive cancer cells into neuroendocrine-like cancer cells, thereby inducing resistance. Concurrent inhibition of both the FGFR and JAK pathways can reverse this cellular state transition or lineage plasticity, restoring cancer cells' sensitivity to androgens and re-sensitizing them to NHT treatment.

Tinengotinib monotherapy has already demonstrated encouraging anti-tumor activity in patients with mCRPC who have received multiple prior lines of therapy. Additionally, tinengotinib as a single agent for mCRPC received Fast Track designation from the U.S. FDA in June 2025.