Yochanra (tinengotinib) / TransThera Sciences - LARVOL DELTA

Tinengotinib for adults with advanced or metastatic cholangiocarcinoma: a multicentre, open-label, phase 2 trial. (PubMed, Lancet Gastroenterol Hepatol) - P2 | "These findings suggest that tinengotinib might have activity in patients with cholangiocarcinoma with FGFR2 fusions that progressed following FGFR inhibitor therapy. Anti-tumour activity was also observed in patients with other FGFR alterations. The data from this phase 2 study supported the initiation of a phase 3 registration trial."

Journal • P2 data • Biliary Cancer • Cardiovascular • Cholangiocarcinoma • CNS Disorders • Dental Disorders • Dermatology • Hypertension • Oncology • Solid Tumor • Stomatitis • FGFR2

Survival and safety of tinengotinib in pooled patients with advanced, fibroblast growth factor receptor (FGFR) inhibitor refractory/relapsed cholangiocarcinoma (CCA) (ESMO 2025) - P1, P1/2, P2 | "Conclusions Tinengotinib shows promising efficacy with an acceptable safety profile in CCA pts with notable clinical benefit in FGFR2-altered CCA with prior FGFRi(s). A global phase III study is currently open to further assess the efficacy and safety of tinengotinib in FGFR2-altered CCA pts who progressed on chemotherapy and FGFRi."

Clinical • Metastases • Biliary Cancer • Cholangiocarcinoma • Oncology • Solid Tumor • FGFR • FGFR2

The multi-kinase inhibitor tinengotinib as monotherapy or combined with atezolizumab in advanced solid tumors: a phase Ib/II trial. (PubMed, Nat Commun) - P1/2 | "In patients with cholangiocarcinoma previously treated with immune checkpoint inhibitors (n = 20), the combination regimen achieved an ORR of 20.0% and a disease control rate of 75.0%. These findings support further development of tinengotinib, both as monotherapy and in combination with immunotherapy."

Journal • Monotherapy • P1/2 data • Biliary Cancer • Biliary Tract Cancer • Cholangiocarcinoma • Oncology • Solid Tumor • FGFR1 • FGFR2 • JAK1 • JAK2

Efficacy and safety results of FGFR1-3 inhibitor, tinengotinib, as monotherapy in patients with advanced, metastatic cholangiocarcinoma: Results from phase II clinical trial. (ASCO-GI 2024) - P2 | "Tinengotinib has promising clinical benefit for FGFR2 fusion CCA after prior FGFRi and for non-fusion FGFR alterations. Tinengotinib-related toxicities were manageable. An ongoing randomized, controlled phase III study will evaluate the clinical efficacy, safety, and pharmacodynamic effect of Tinengotinib vs Physicians’ choice in subjects with FGFR2-altered refractory/relapsed CCA after prior chemotherapy and FGFRi therapy."

Clinical • Metastases • Monotherapy • P2 data • Biliary Cancer • Cholangiocarcinoma • Gastrointestinal Cancer • Oncology • Solid Tumor • FGFR2

TransThera Sciences…announced that the first batch of its core product YOCHANRA (Tinengotinib tablets) has been officially shipped through commercial channels to pharmacies across the country. (TransThera Press Release) - "As vehicles loaded with the first batch slowly departed, YOCHANRA officially commenced nationwide commercial supply, marking that the world’s first targeted therapy for cholangiocarcinoma that overcomes FGFR inhibitor resistance is about to reach patients across the country."

Commercial • Cholangiocarcinoma

TransThera Sciences…announced that the first prescription issued in China for YOCHANRA (tinengotinib tablets), a Category 1 innovative drug independently discovered and developed by the company, was written at Peking University Cancer Hospital on September 17. (TransThera Press Release) - "Professor Zhou Jun from the Department of Gastrointestinal Oncology prescribed YOCHANRA for a patient with FGFR2 fusion/rearrangement-positive advanced cholangiocarcinoma who had previously received systemic therapy and FGFR inhibitor therapy."

Launch non-US • Cholangiocarcinoma

TransThera Sciences…announces that the first patient was recently dosed in the Phase II clinical trial of the Company’s core product tinengotinib (Yochanra, Tinengotinib, TT-00420) in combination with novel hormonal therapy (NHT) for pretreated and progressed metastatic castration-resistant prostate cancer (mCRPC) in China (HKEXnews) - "This trial is an open-label, multi-center, Phase II clinical study, aimed at evaluating the safety and efficacy of tinengotinib in combination with NHT in patients with pretreated and progressed mCRPC."

Trial status • Castration-Resistant Prostate Cancer

Multikinase Inhibition with Tinengotinib in Advanced Solid Tumors: Results from a Multicenter Phase Ib/II Trial. (PubMed, Clin Cancer Res) - P1/2 | "Tinengotinib demonstrated manageable toxicity with antitumor activity across advanced solid tumors, with infrequent hyperphosphatemia and ocular toxicities. Integrated pharmacokinetic-biomarker analyses support the continued clinical development of tinengotinib and the exploration of biomarker‑informed precision oncology strategies."

Journal • P1/2 data • Biliary Cancer • Breast Cancer • Cardiovascular • Cholangiocarcinoma • Genito-urinary Cancer • Hypertension • Metabolic Disorders • Nephrology • Oncology • Prostate Cancer • Renal Disease • Solid Tumor • AR • EGFR • FGFR2 • KDR • KMT2A • ROS1

TransThera Sciences…announces that, the Guidelines for the Diagnosis and Treatment of Biliary Tract Cancers of the Chinese Society of Clinical Oncology (CSCO) (the 'Guidelines') has been officially released… (HKEXnews) - "YOCHANRA (tinengotinib), an innovative multi-target small molecule kinase inhibitor self-developed by the Company, has been included in the Guidelines as a Class II recommendation Class 2A for the treatment of advanced biliary tract cancers....Meanwhile, the efficacy data of tinengotinib in combination with atezolizumab in the treatment of patients with advanced biliary tract tumors who have received prior immunotherapy has also been written into the Guidelines in the form of 'annotations'."

Clinical guideline • Biliary Tract Cancer

Phase II study of tinengotinib in advanced cholangiocarcinoma: Analysis of molecular response and resistance mechanisms. (ASCO-GI 2026) - P2 | "These findings provide genomic evidence that tinengotinib may overcome resistance to prior FGFRi treatment in FGFR2 fus-positive CCA, as reflected by significantly reductions in ctDNA VAFs and frequent clearance of FGFR2 KD mutations. The emergence of resistance alterations including de novo FGFR2 mutations and bypass pathways activations indicates acquired resistance that may limit long-term benefit. These results support further investigation with expanded biomarker sampling to better characterize resistance evolution and guide therapy optimization in an ongoing Phase 3 trial."

Metastases • P2 data • Tumor mutational burden • Biliary Cancer • Cholangiocarcinoma • Gastrointestinal Cancer • Oncology • Solid Tumor • EGFR • FGFR2 • FUS • KRAS • TMB • TP53

Tinengotinib in patients with advanced, metastatic cholangiocarcinoma: Overall survival results and biomarker correlative analysis from a phase 2 clinical trial. (ASCO-GI 2025) - P2, P3 | "Tinengotinib has shown promising anti-tumor efficacy in CCA pts with FGFR fusion after prior FGFRi and in those with primary FGFR mutations. An ongoing randomized phase III study will investigate tinengotinib vs. chemotherapy in FGFR inhibitor refractory CCA (NCT05948475)."

Biomarker • Clinical • Metastases • P2 data • Biliary Cancer • Cholangiocarcinoma • Gastrointestinal Cancer • Oncology • Solid Tumor • ARID1A • BCOR • FGFR2 • MED12

Tinengotinib (TT-00420) in advanced/metastatic FGFR2-altered cholangiocarcinoma following prior chemotherapy and FGFR inhibitor treatment: Results from a phase II study (FIRST-08). (ASCO 2026) - P2 | "Tinengotinib demonstrated durable clinical anti-tumor activity and a manageable safety profile in heavily pretreated CCA pts with FGFR2 fusion/rearrangement following prior chemotherapy and FGFRi therapy. Efficacy outcomes by BICR and investigator."

IO biomarker • Metastases • P2 data • Biliary Cancer • Cardiovascular • Cholangiocarcinoma • Hypertension • Oncology • Solid Tumor • FGFR2

Persistent FGFR pathway dependence: where does tinengotinib fit after FGFR inhibitor therapy in advanced cholangiocarcinoma? (PubMed, J Gastrointest Oncol) - No abstract available

Journal • Biliary Cancer • Cholangiocarcinoma • Oncology • Solid Tumor

First-In-Human Phase I Study of Tinengotinib (TT-00420), a Multiple Kinase Inhibitor, as a Single Agent in Patients With Advanced Solid Tumors. (PubMed, Oncologist) - "Tinengotinib was well tolerated with favorable pharmacokinetic characteristics. Preliminary findings indicated potential clinical benefit in FGFR inhibitor-refractory cholangiocarcinoma, HER2-negative breast cancer (including TNBC), and CRPC. Continued evaluation of tinengotinib is warranted in phase II trials."

Journal • Metastases • P1 data • Biliary Cancer • Breast Cancer • Cardiovascular • Castration-Resistant Prostate Cancer • Cholangiocarcinoma • Dermatology • Gastrointestinal Cancer • Genito-urinary Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Hypertension • Oncology • Prostate Cancer • Solid Tumor • Triple Negative Breast Cancer • FGFR2 • HER-2 • JAK1

The efficacy and safety of tinengotinib in patients with advanced or metastatic HR+/HER2- breast cancer or TNBC (SABCS 2023) - P1, P1/2 | "Tinengotinib for the treatment of HR+HER2- BC or TNBC, whether as monotherapy or in combination with nab-paclitaxel, had manageable side effects. Tinengotinib has shown promising clinical benefit in heavily pre-treated pts with refractory HR+HER2- BC or TNBC. Clinical benefit was similar across the subgroups of pts with HR+ HER2-zero and HR+ HER2 low disease."

Clinical • Metastases • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • CSF1R • FGFR1 • HER-2 • JAK1 • JAK2

Yochanra, the World's First Innovative Drug to Overcome FGFR Inhibitor Resistance, Makes Its Global Debut in China (PRNewswire) - "On 6 August 2026, the National Medical Products Administration (the 'NMPA') formally approved the drug for marketing....It is indicated for adult patients with advanced, metastatic or unresectable cholangiocarcinoma harboring an FGFR2 fusion or rearrangement who have previously received systemic therapy and FGFR inhibitor therapy. The approval of this indication was based on a multicenter, open-label, single-arm, pivotal Phase II clinical trial conducted in China."

China approval • Cholangiocarcinoma

Tinengotinib (TT-00420) inhibits tumor growth and overcomes multidrug resistance in gastrointestinal cancers. (PubMed, Mol Cancer Ther) - "In addition, trastuzumab-resistant and immunotherapy-resistant models were established to assess the antitumor activity of TT-00420 in treatment-refractory settings. Mechanistically, Western blot analysis revealed that Aurora A expression was downregulated following TT-00420 treatment, and the IC50 of TT-00420 increased in AURKA-knockdown cell lines, suggesting that Aurora A contributes to the antitumor activity of TT-00420. Collectively, these findings indicate that TT-00420 is a highly promising antitumor agent with potent efficacy against gastric and colorectal cancers, providing a potential therapeutic strategy for gastrointestinal malignancies and offering valuable insights for future clinical research."

IO biomarker • Journal • Biliary Cancer • Cholangiocarcinoma • Colorectal Cancer • Gastric Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • AURKA

Enrollment Completed in the Global Multicenter Registrational Phase III Clinical Trial of Tinengotinib Monotherapy for Patients with Advanced Cholangiocarcinoma (HKEXnews) - "This clinical trial is a global multicenter, randomized, controlled Phase III clinical trial designed to evaluate the efficacy and safety of oral Tinengotinib versus Physician’s choice in patients with advanced CCA harboring fibroblast growth factor receptor (FGFR) gene aberrations who are refractory or relapsed after chemotherapy and FGFR inhibitor treatment."

Enrollment closed • Cholangiocarcinoma

FIRST-308: Study of Tinengotinib VS. Physician's Choice a Treatment of Subjects With FGFR-altered in Cholangiocarcinoma (clinicaltrials.gov) - P3 | N=200 | Active, not recruiting | Sponsor: TransThera Sciences (Nanjing), Inc. | Recruiting ➔ Active, not recruiting | Trial completion date: Aug 2026 ➔ Dec 2026 | Trial primary completion date: May 2026 ➔ Dec 2026

Enrollment closed • Trial completion date • Trial primary completion date • Biliary Cancer • Cholangiocarcinoma • Oncology • Solid Tumor • FGFR2

Beyond fibroblast growth factor receptor 2 (FGFR2) fusions: Mutations and amplifications in intrahepatic cholangiocarcinoma. (ASCO 2026) - "Among 42 patients with non-fusion FGFR2 alterations treated at a single center, 16 (38%) received FGFR-directed therapy including pemigatinib, futibatinib, tinengotinib, lirafrugatinib and derazantinib. Non-fusion FGFR2 sequence mutations and amplifications define a distinct subset of iCCA with fewer alternative actionable drivers and sensitivity to FGFR-targeted therapy. These findings support consideration of FGFR inhibition beyond FGFR2 fusions and highlight the need for refined patient selection strategies."

IO biomarker • Tumor mutational burden • Biliary Cancer • Cholangiocarcinoma • Microsatellite Instability • Oncology • Solid Tumor • BAP1 • BRAF • FGFR2 • HER-2 • HRD • IDH1 • MSI • MTAP • NF2 • PD-L1 • TMB • TSC1

TransThera to Showcase Tinengotinib Phase II Data in FGFR2-Altered Cholangiocarcinoma at 2026 ASCO (TipRanks) - "In a 50-patient Chinese phase II trial, tinengotinib showed a 28% objective response rate, 82% disease control rate, median progression-free survival of 6.1 months and median overall survival of 20.7 months, and the drug is now being evaluated in ongoing global and domestic phase III studies that could reshape second-line treatment options after chemotherapy and FGFR inhibitors."

P2 data • Real-world evidence • Cholangiocarcinoma

TransThera Wins China Phase II Trial Nod for Tinengotinib Combo in Resistant Prostate Cancer (TipRanks) - "The open-label, multicenter study will assess safety, efficacy and pharmacokinetics in patients who have developed resistance to standard hormone therapies."

New P2 trial • Castration-Resistant Prostate Cancer

The Company announced the publication of clinical results of tinengotinib as monotherapy and in combination with atezolizumab for the treatment of advanced solid tumors have been published on Nature Communications (HKEXnews) - "Tinengotinib demonstrated antitumor activity both as monotherapy (objective response rate ORR: 16.7% in Arm A) and combined with atezolizumab (ORR: 22.6% in Arm B). In predefined exploratory subgroup analysis, notable efficacy was observed in cholangiocarcinoma (ORR: 30.8% in Arm A n = 13; 25.0% in Arm B n = 28). Tinengotinib monotherapy achieved favorable response in cholangiocarcinoma harboring FGFR2 fusion progressing on prior FGFR inhibitors (ORR: 66.7%). In patients with cholangiocarcinoma previously treated with immune checkpoint inhibitors (n = 20), the combination regimen achieved an ORR of 20.0% and a disease control rate of 75.0%."

P1/2 data • Biliary Tract Cancer • Solid Tumor

Convergent FGFR-JAK signaling reprograms luminal identity and drives endocrine resistance in HR⁺ breast cancer (AACR 2026) - "Tinengotinib (TT-00420), a first-in-class dual FGFR and JAK small molecular inhibitor, restored luminal identity and resensitized resistant models to endocrine therapy in vitro and in vivo. Thus, lineage plasticity unified intrinsic/extrinsic inputs in endocrine resistance, supporting dual FGFR-JAK blockade as a translational strategy.Planned trials of tinengotinib combined with endocrine therapy in advanced HR⁺ breast cancer will assess its clinical potential, with results reported in due course."

Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • ER • FGFR

TransThera Showcases Tinengotinib Data on Endocrine Resistance in HR+ Breast Cancer at AACR 2026 (TipRanks) - "The preclinical data indicate that tinengotinib (TT-00420), a dual FGFR-JAK inhibitor, can restore luminal identity and resensitize resistant HR-positive breast cancer models to endocrine therapy in vitro and in vivo, supporting dual FGFR-JAK blockade as a strategy to overcome lineage plasticity-driven resistance."

Preclinical • Hormone Receptor Positive Breast Cancer