^
    9d
    Targeting high-risk MYC-overexpressed osteosarcoma with an Aurora kinase inhibitor:--results from a pilot umbrella trial. (PubMed, NPJ Precis Oncol)
    Patients were assigned to three arms: (A) PD-1 antibody plus gemcitabine and docetaxel; (B) PARP inhibitor combined with temozolomide; or (C) tinengotinib (TT-00420), a small-molecule aurora kinase inhibitor currently in clinical trials. This study demonstrated the feasibility of using genomic molecular subtyping to guide the precise treatment of osteosarcoma. We also revealed that the abnormal genomic and transcriptomic profiles caused by MYC amplification could be suppressed by tinengotinib.
    Journal
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • HRD (Homologous Recombination Deficiency)
    |
    HRD
    |
    gemcitabine • docetaxel • temozolomide • tinengotinib (TT-00420)
    14d
    Tinengotinib for adults with advanced or metastatic cholangiocarcinoma: a multicentre, open-label, phase 2 trial. (PubMed, Lancet Gastroenterol Hepatol)
    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.
    P2 data • Journal
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    FGFR2 mutation • FGFR2 fusion
    |
    Lytgobi (futibatinib) • Pemazyre (pemigatinib) • 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, Active, not recruiting, TransThera Sciences (Nanjing), Inc. | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    tinengotinib (TT-00420)
    5ms
    Safety of TT-00420 (Tinengotinib) Monotherapy in Patients With Advanced Solid Tumors and Triple Negative Breast Cancer (clinicaltrials.gov)
    P1, N=48, Completed, TransThera Sciences (Nanjing), Inc. | Active, not recruiting --> Completed
    Trial completion
    |
    tinengotinib (TT-00420)
    6ms
    A Phase II Clinical Study of AK104/AK112 in Combination With TT-00420 Tablet for Advanced HCC. (clinicaltrials.gov)
    P2, N=100, Not yet recruiting, Akeso
    New P2 trial
    |
    tinengotinib (TT-00420) • Kaitanni (cadonilimab) • Yidafan (ivonescimab)
    6ms
    To Evaluate Efficacy and Safety of TT-00420 (Tinengotinib) as Monotherapy and Combination Therapy in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=84, Completed, TransThera Sciences (Nanjing), Inc. | Recruiting --> Completed | Trial completion date: Dec 2024 --> Aug 2024
    Trial completion • Trial completion date
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    Tecentriq (atezolizumab) • albumin-bound paclitaxel • tinengotinib (TT-00420)
    11ms
    Multiple Kinase Small Molecule Inhibitor Tinengotinib (TT-00420) Alone or With Chemotherapy Inhibit the Growth of SCLC. (PubMed, Cancer Sci)
    When combined with etoposide/cisplatin, it synergistically inhibited SCLC growth. Mechanistic studies revealed that c-Myc expression may be a key factor influencing the effect of tinengotinib in SCLC-N. This study provides reliable preclinical data and a new direction for tinengotinib as a promising therapy for SCLC, either alone or in combination with chemotherapy.
    Journal
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • NEUROD1 (Neuronal Differentiation 1)
    |
    MYC expression
    |
    cisplatin • etoposide IV • tinengotinib (TT-00420)
    12ms
    A Model for Decoding Resistance in Precision Oncology: Acquired Resistance to FGFR inhibitors in Cholangiocarcinoma. (PubMed, Ann Oncol)
    Our multimodal analysis led to a model characterizing the biology of acquired resistance, informing the rational design of next-generation FGFR inhibitors. FGFR inhibitors should be small, high-affinity, and selective for specific FGFR family members. Tinengotinib, a novel small molecule inhibitor with these characteristics, exhibited preclinical and clinical activity against key resistance mutations. This integrated approach offers a blueprint for advancing drug resistance research across cancer types.
    Preclinical • Journal
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    FGFR2 mutation
    |
    tinengotinib (TT-00420)
    over1year
    A Study of Tinengotinib (TT-00420) in Combination With Standard Treatments in People With Prostate Cancer (clinicaltrials.gov)
    P1/2, N=50, Recruiting, Memorial Sloan Kettering Cancer Center
    New P1/2 trial • Combination therapy • Metastases
    |
    Xtandi (enzalutamide) • abiraterone acetate • prednisone • tinengotinib (TT-00420)
    over1year
    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)
    over1year
    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)
    over1year
    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)