TRANSTHERA-B (02617) announced that its core product, Tinengotinib (TT00420), in combination with novel hormonal therapy (NHT) for the treatment of metastatic castration-resistant prostate cancer (mCRPC) that has progressed after prior therapy, received approval from China's National Medical Products Administration (NMPA) on May 25, 2026, to initiate a Phase II clinical trial. This trial is an open-label, multicenter, Phase II clinical study designed to evaluate the safety, efficacy, and pharmacokinetics of Tinengotinib combined with NHT in mCRPC patients who have progressed after prior treatment.

Tinengotinib is the world's first and only investigational drug that simultaneously inhibits the FGFR and JAK pathways and has clinical efficacy evidence in mCRPC. Currently, NHT is the standard treatment for mCRPC patients, but resistance often develops after a period of therapy. Recent research indicates that activation of the FGFR and JAK pathways can drive the transformation of androgen-sensitive cancer cells into neuroendocrine cancer cells, leading to drug resistance. Simultaneous inhibition of the FGFR and JAK pathways can reverse this cellular state transformation or lineage reprogramming, restoring the cancer cells' sensitivity to androgens and, consequently, their sensitivity to NHT treatment.

Tinengotinib monotherapy has already demonstrated encouraging antitumor efficacy in mCRPC patients who have received multiple prior lines of therapy. Furthermore, Tinengotinib monotherapy for mCRPC received Fast Track Designation (FTD) from the U.S. Food and Drug Administration (FDA) in June 2025.