^
    12d
    Study of TT-00420 (Tinengotinib) Tablet as Monotherapy and Combination Therapy in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=203, Completed, TransThera Sciences (Nanjing), Inc. | Active, not recruiting --> Completed
    Trial completion • Combination therapy • Metastases
    |
    FGFR (Fibroblast Growth Factor Receptor)
    |
    albumin-bound paclitaxel • tinengotinib (TT-00420)
    12d
    Study to Evaluate the Efficacy and Safety of TT-00420 (Tinengotinib) in Cholangiocarcinoma (clinicaltrials.gov)
    P2, N=55, Completed, TransThera Sciences (Nanjing), Inc. | Active, not recruiting --> Completed
    Trial completion • Metastases
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR (Fibroblast Growth Factor Receptor)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR mutation • FGFR1 mutation • FGFR1 fusion • FGFR wild-type
    |
    tinengotinib (TT-00420)
    21d
    Rollover Study to Provide Continued Access to TT-00420 (Tinengotinib) for Subjects With Advanced Solid Tumors (clinicaltrials.gov)
    P=N/A, N=0, Available, TransThera Sciences (Nanjing), Inc.
    New trial • Metastases
    |
    tinengotinib (TT-00420)
    3ms
    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.
    P1 data • Journal • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • FGFR2 (Fibroblast growth factor receptor 2) • JAK1 (Janus Kinase 1)
    |
    HER-2 positive • HR positive • HER-2 negative • FGFR2 mutation • FGFR2 fusion • HR positive + HER-2 negative • PTEN mutation + HR positive
    |
    tinengotinib (TT-00420)
    4ms
    Safety and Efficacy of TT-00420 Tablets Combined With Toripalimab Injection in Advanced Urological Tumors (clinicaltrials.gov)
    P1/2, N=42, Not yet recruiting, The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School
    New P1/2 trial • Metastases
    |
    Loqtorzi (toripalimab-tpzi) • tinengotinib (TT-00420)
    4ms
    Safety of TT-00420 (Tinengotinib) Monotherapy in Patients With Advanced Solid Tumors and Triple Negative Breast Cancer (clinicaltrials.gov)
    P1, N=48, Active, not recruiting, TransThera Sciences (Nanjing), Inc. | Trial completion date: Dec 2021 --> Feb 2024 | Trial primary completion date: Jun 2021 --> Jan 2023
    Trial completion date • Trial primary completion date • Metastases
    |
    STAT3 (Signal Transducer And Activator Of Transcription 3)
    |
    tinengotinib (TT-00420)
    4ms
    Study of TT-00420 (Tinengotinib) in Subjects With Cholangiocarcinoma Who Failed or Relapsed to Chemotherapy and FGFR Inhibitor (clinicaltrials.gov)
    P2, N=50, Recruiting, TransThera Sciences (Nanjing), Inc. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    tinengotinib (TT-00420)
    5ms
    The efficacy and safety of tinengotinib in patients with heavily pretreated metastatic castration-resistant prostate cancer (mCRPC). (ASCO-GU 2024)
    All patients had at least 2 prior therapies including 77% prior docetaxel, 87% prior abiraterone, and 30% prior enzalutamide. Tinengotinib safety profile was tolerable and manageable. The preliminary efficacy data showed promising clinical benefit of tinengotinib monotherapy in patients with heavily pretreated mCRPC. Further study of tinengotinib in this disease is warranted.
    Clinical • Metastases
    |
    FGFR (Fibroblast Growth Factor Receptor)
    |
    docetaxel • Xtandi (enzalutamide capsule) • abiraterone acetate • tinengotinib (TT-00420)
    5ms
    FIRST-308: Study of Tinengotinib VS. Physician's Choice a Treatment of Subjects With FGFR-altered in Cholangiocarcinoma (clinicaltrials.gov)
    P3, N=200, Recruiting, TransThera Sciences (Nanjing), Inc. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    FGFR2 fusion
    |
    5-fluorouracil • irinotecan • tinengotinib (TT-00420)
    5ms
    First-308: Phase III study of tinengotinib versus physician's choice in patients with FGFR-altered, chemotherapy- and FGFR inhibitor–refractory/relapsed cholangiocarcinoma. (ASCO-GI 2024)
    The first generation FGFR inhibitors (FGFRi) pemigatinib and futibatinib, have been approved for the treatment of advanced CCA with FGFR2 fusions or rearrangements after systemic chemotherapy...The study includes Part A and Part B. The Part A is to select a dose for Part B. Eligible subjects will be randomized in a 2:2:1 ratio to receive tinengotinib 8 mg QD, tinengotinib 10 mg QD or Physician's Choice (FOLFOX or FOLFIRI) in Part A or 2:1 in Part B to receive the recommended Part B dose or Physician's Choice...Study is open for enrollment. Clinical trial information: NCT05948475.
    Clinical • P3 data
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR mutation
    |
    5-fluorouracil • Lytgobi (futibatinib) • irinotecan • Pemazyre (pemigatinib) • tinengotinib (TT-00420) • leucovorin calcium
    5ms
    Tinengotinib (TT-00420) in combination with atezolizumab in Chinese patients (pts) with biliary tract carcinoma (BTC): Preliminary efficacy and safety results from a phase Ib/II study. (ASCO-GI 2024)
    Clinical Trial Registration Number NCT05253053 Sponsored by No funding sources reported Background: Programmed Cell Death Ligand 1 (PD-L1) inhibitor durvalumab in combination with gemcitabine and cisplatin has been approved as first-line therapy for BTC...Another pt with prior immunotherapy (sintilimab), target therapy (donafenib) and chemotherapy had a tumor reduction of 39.1% (tinengotinib 10 mg QD plus atezo)... Tinengotinib in combination with atezo was well-tolerated for the treatment of Chinese BTC pts. Preliminary encouraging efficacy of tinengotinib in combination with atezo was observed in pts with heavily pre-treated BTC. The ongoing study is to further evaluate the safety and efficacy of tinengotinib in combination with atezo in pts with BTC who had prior immunotherapy and/or chemotherapy.
    Clinical • P1/2 data • Combination therapy
    |
    cisplatin • Tecentriq (atezolizumab) • Imfinzi (durvalumab) • gemcitabine • Tyvyt (sintilimab) • tinengotinib (TT-00420) • Zepsun (donafenib)
    5ms
    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)
    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 • P2 data • Metastases
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR fusion • FGFR wild-type
    |
    tinengotinib (TT-00420)
    5ms
    In vitro and in vivo pharmacokinetics, disposition, and drug-drug interaction potential of tinengotinib (TT-00420), a promising investigational drug for treatment of cholangiocarcinoma and other solid tumors. (PubMed, Eur J Pharm Sci)
    Major metabolic pathways include oxidation, oxidative cleavage of the morpholine ring, glucuronide and glutathione conjugations. The overall preclinical pharmacokinetics profile supported the selection and development of tinengotinib as a clinical candidate.
    PK/PD data • Preclinical • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • FGFR (Fibroblast Growth Factor Receptor) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
    |
    HER-2 negative
    |
    tinengotinib (TT-00420)
    5ms
    To Evaluate Efficacy and Safety of TT-00420 as Monotherapy and Combination Therapy in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=114, Recruiting, TransThera Sciences (Nanjing), Inc. | Trial completion date: Aug 2024 --> Dec 2024 | Trial primary completion date: Aug 2023 --> Sep 2024
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • FGFR2 (Fibroblast growth factor receptor 2)
    |
    PD-L1 expression • HER-2 negative
    |
    Tecentriq (atezolizumab) • albumin-bound paclitaxel • tinengotinib (TT-00420)
    6ms
    The efficacy and safety of tinengotinib in patients with advanced or metastatic HR+/HER2- breast cancer or TNBC (SABCS 2023)
    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
    |
    HER-2 (Human epidermal growth factor receptor 2) • FGFR1 (Fibroblast growth factor receptor 1) • JAK2 (Janus kinase 2) • JAK1 (Janus Kinase 1) • CSF1R (Colony stimulating factor 1 receptor)
    |
    HR positive • HER-2 negative
    |
    albumin-bound paclitaxel • tinengotinib (TT-00420)
    7ms
    Study of TT-00420 Tablet as Monotherapy and Combination Therapy in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=225, Active, not recruiting, TransThera Sciences (Nanjing), Inc. | Recruiting --> Active, not recruiting | Trial completion date: Dec 2022 --> Feb 2024 | Trial primary completion date: Oct 2022 --> Feb 2024
    Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    albumin-bound paclitaxel • tinengotinib (TT-00420)
    7ms
    Study to Evaluate the Efficacy and Safety of TT-00420 in Cholangiocarcinoma (clinicaltrials.gov)
    P2, N=55, Active, not recruiting, TransThera Sciences (Nanjing), Inc. | Recruiting --> Active, not recruiting | N=80 --> 55 | Trial completion date: Sep 2023 --> May 2024 | Trial primary completion date: Sep 2023 --> May 2024
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date • Metastases
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR (Fibroblast Growth Factor Receptor)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR mutation • FGFR1 mutation • FGFR1 fusion • FGFR wild-type
    |
    tinengotinib (TT-00420)
    7ms
    Study of TT-00420 (Tinengotinib) in Subjects With Cholangiocarcinoma Who Failed or Relapsed to Chemotherapy and FGFR Inhibitor (clinicaltrials.gov)
    P2, N=50, Not yet recruiting, TransThera Sciences (Nanjing), Inc.
    New P2 trial
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    tinengotinib (TT-00420)
    10ms
    Preliminary efficacy and safety of tinengotinib (TT-00420) monotherapy in Chinese patients (pts) with advanced solid tumors: Results from a phase Ib/II study (ESMO 2023)
    One responder with prior treatment of erdafitinib achieved tumor reduction of 44%, the other with no prior FGFR inhibitor treatment achieved 69% reduction. Promising efficacy has been observed, especially in CCA with FGFR2 alteration. The ongoing study is to further evaluate the safety and efficacy of monotherapy and combination therapy.
    Clinical • P1/2 data • Metastases
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    Balversa (erdafitinib) • tinengotinib (TT-00420)
    10ms
    Tinengotinib in patients with advanced, fibroblast growth factor receptor (FGFR) inhibitor refractory/relapsed cholangiocarcinoma (ESMO 2023)
    Notable clinical benefit was noted with tinengotinib in FGFR-altered CCA pts with acquired resistance to prior FGFRi. A global phase III clinical trial is planned to further evaluate the efficacy and safety of tinengotinib for CCA with FGFRi resistance.
    Clinical • Metastases
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR (Fibroblast Growth Factor Receptor)
    |
    FGFR2 mutation
    |
    tinengotinib (TT-00420)
    10ms
    FIRST-308: Study of Tinengotinib VS. Physician's Choice a Treatment of Subjects With FGFR-altered in Cholangiocarcinoma (clinicaltrials.gov)
    P3, N=200, Not yet recruiting, TransThera Sciences (Nanjing), Inc.
    New P3 trial
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    FGFR2 fusion
    |
    5-fluorouracil • irinotecan • tinengotinib (TT-00420)
    1year
    Tinengotinib, a novel fibroblast growth factor receptor (FGFR) inhibitor, is potent against resistance mutations in FGFR1/2/3 (AACR 2023)
    First generation of FGFR inhibitors, such as erdafitinib and pemigatinib, have already demonstrated promising efficacy on multiple cancers with prespecified FGFRalt. Retrospective analysis showed early promising efficacy in treating patients with various solid tumors bearing FGFRalt . It provides an opportunity to investigate tinengotinib as a tumor agnostic therapy in patients with prespecified FGFR 1/2/3 alterations (pan-FGFRalt).
    Late-breaking abstract
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR1 (Fibroblast growth factor receptor 1)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR mutation • FGFR1 mutation • FGFR2 N549K
    |
    Balversa (erdafitinib) • Pemazyre (pemigatinib) • tinengotinib (TT-00420)
    over1year
    Study to Evaluate the Efficacy and Safety of TT-00420 in Cholangiocarcinoma (clinicaltrials.gov)
    P2, N=80, Recruiting, TransThera Sciences (Nanjing), Inc. | Trial primary completion date: Dec 2022 --> Sep 2023
    Trial primary completion date • Metastases
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR (Fibroblast Growth Factor Receptor)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR mutation • FGFR1 mutation • FGFR1 fusion • FGFR wild-type
    |
    tinengotinib (TT-00420)
    over1year
    Tinengotinib (TT-00420), a Novel Spectrum-Selective Small Molecule Kinase Inhibitor, Is Highly Active Against Triple Negative Breast Cancer. (PubMed, Mol Cancer Ther)
    Tinengotinib represents a novel combinatorial inhibitory mechanism to treat TNBC. The phase I trial of tinengotinib was completed (ClinicalTrials.gov identifier: NCT03654547).
    Journal
    |
    FGFR1 (Fibroblast growth factor receptor 1) • JAK2 (Janus kinase 2) • CXCL10 (Chemokine (C-X-C motif) ligand 10) • JAK1 (Janus Kinase 1) • CSF1R (Colony stimulating factor 1 receptor)
    |
    tinengotinib (TT-00420)
    over1year
    Novel protein kinase inhibitor TT-00420 inhibits gallbladder cancer by inhibiting JNK/JUN-mediated signaling pathway. (PubMed, Cell Oncol (Dordr))
    TT-00420 shows potent antitumor efficacy and may serve as a novel agent to improve GBC prognosis.
    Journal
    |
    FGFR1 (Fibroblast growth factor receptor 1) • FASLG (Fas ligand)
    |
    FGFR1 expression
    |
    tinengotinib (TT-00420)
    over1year
    To Evaluate Efficacy and Safety of TT-00420 as Monotherapy and Combination Therapy in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=114, Recruiting, TransThera Sciences (Nanjing), Inc. | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    Tecentriq (atezolizumab) • albumin-bound paclitaxel • tinengotinib (TT-00420)
    2years
    Study to Evaluate the Efficacy and Safety of TT-00420 as Monotherapy and Combination Therapy in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=114, Not yet recruiting, TransThera Sciences (Nanjing), Inc.
    New P1/2 trial • Combination therapy
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    Tecentriq (atezolizumab) • albumin-bound paclitaxel • tinengotinib (TT-00420)
    2years
    Study to Evaluate the Efficacy and Safety of TT-00420 in Cholangiocarcinoma (clinicaltrials.gov)
    P2, N=80, Recruiting, TransThera Sciences (Nanjing), Inc. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR (Fibroblast Growth Factor Receptor)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR mutation • FGFR1 mutation • FGFR1 fusion • FGFR wild-type
    |
    tinengotinib (TT-00420)
    over2years
    Study to Evaluate the Efficacy and Safety of TT-00420 in Cholangiocarcinoma (clinicaltrials.gov)
    P2, N=80, Not yet recruiting, TransThera Sciences (Nanjing), Inc. | Trial completion date: Jun 2023 --> Sep 2023
    Clinical • Trial completion date
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR mutation • FGFR1 mutation • FGFR1 fusion • FGFR wild-type
    |
    tinengotinib (TT-00420)
    almost3years
    Study to Evaluate the Efficacy and Safety of TT-00420 in Cholangiocarcinoma (clinicaltrials.gov)
    P2, N=80, Not yet recruiting, TransThera Biosciences Co., Ltd
    Clinical • New P2 trial
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR mutation • FGFR1 mutation • FGFR1 fusion
    |
    tinengotinib (TT-00420)