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    DRUG CLASS:

    TGF-β R2 kinase inhibitor

    Related drugs:
    3d
    GOLPH3 promotes papillary thyroid carcinoma by regulating the TGF-β signaling pathway. (PubMed, Mol Genet Genomics)
    However, as an inhibitor of this pathway, LY2109761 could reverse the effects induced by GOLPH3 overexpression. Collectively, these findings establish GOLPH3 as a critical driver of PTC malignancy through TGF-β pathway activation, providing a mechanistic link between Golgi function and cancer signaling. This work not only advances our understanding of PTC pathogenesis but also identifies GOLPH3 as a potential therapeutic target for aggressive PTC, offering a paradigm for exploring Golgi-associated proteins in endocrine malignancies.
    Journal
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    CDH1 (Cadherin 1) • TGFB1 (Transforming Growth Factor Beta 1) • CDH2 (Cadherin 2) • SNAI1 (Snail Family Transcriptional Repressor 1) • SMAD2 (SMAD Family Member 2) • SMAD3 (SMAD Family Member 3)
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    LY2109761
    3d
    Neoadjuvant retlirafusp alfa (anti-PD-L1/TGF-β bifunctional fusion protein) with or without chemotherapy in unresectable stage III non-small cell lung cancer: updated results from the phase 2 TRAILBLAZER trial. (PubMed, Signal Transduct Target Ther)
    Patients who underwent surgery after induction treatment achieved clinically meaningful survival gains. Our findings support the use of neoadjuvant immunotherapy with a response-adapted surgical strategy as a promising approach for unresectable stage III NSCLC.
    Clinical • P2 data • Journal • PD(L)-1 Biomarker • IO biomarker
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    EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase) • TGFB1 (Transforming Growth Factor Beta 1)
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    PD-L1 expression • PD-L1 overexpression
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    retlirafusp alfa (SHR-1701)
    17d
    SHR-1701 for Induction and Consolidation Therapy in Unresectable Stage III Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=84, Not yet recruiting, Fudan University
    New P2 trial
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    retlirafusp alfa (SHR-1701)
    18d
    Retlirafusp Alfa Plus Chemotherapy as Neoadjuvant Therapy for Thoracic ESCC (clinicaltrials.gov)
    P2, N=33, Not yet recruiting, Tang-Du Hospital
    New P2 trial
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    cisplatin • albumin-bound paclitaxel • retlirafusp alfa (SHR-1701)
    21d
    RA-A-NP: Retlirafusp Alfa Combined With Apatinib and Nab-Paclitaxel as Second-line Treatment for Gastric or Gastroesophageal Junction Cancer (clinicaltrials.gov)
    P2, N=50, Not yet recruiting, Henan Cancer Hospital
    New P2 trial
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    HER-2 (Human epidermal growth factor receptor 2)
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    HER-2 negative
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    AiTan (rivoceranib) • albumin-bound paclitaxel • retlirafusp alfa (SHR-1701)
    24d
    A Clinical Study of SHR-1701 Combined With Chemotherapy for the Perioperative Treatment of Locally Advanced Resectable Siewert Type II Adenocarcinoma of the Esophagogastric Junction (clinicaltrials.gov)
    P2, N=38, Not yet recruiting, Hebei Medical University Fourth Hospital
    New P2 trial
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    HER-2 (Human epidermal growth factor receptor 2)
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    HER-2 expression
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    oxaliplatin • retlirafusp alfa (SHR-1701)
    26d
    Optimal First-line Immune-related Therapy Selection for Advanced Gastric Cancer: A Systematic Review and Network Meta-analysis. (PubMed, J Gastrointest Cancer)
    Dual-target ICI-chemo appears to be the most effective first-line strategy for AGC based on current indirect evidence, surpassing single ICI-chemo and dual ICI-based regimens. These findings support personalized therapy selection but await confirmation by head‑to‑head trials. Future studies should address CPS < 1 and explore optimized combinations to enhance outcomes.
    Clinical • Retrospective data • Review • Journal
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    PD-L1 (Programmed death ligand 1)
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    PD-L1 expression
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    retlirafusp alfa (SHR-1701)
    1m
    Adebrelimab or Retlirafusp Alfa Plus Recaticimab and Chemotherapy for Resectable NSCLC (clinicaltrials.gov)
    P2, N=78, Not yet recruiting, Peking University Cancer Hospital & Institute
    New P2 trial
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    retlirafusp alfa (SHR-1701) • AiRuiLi (adebrelimab)
    2ms
    Relatrilfa-α Plus Single-Agent Chemotherapy as Neoadjuvant Therapy for Resectable Stage II-III NSCLC (Phase 2) (clinicaltrials.gov)
    P2, N=18, Not yet recruiting, Tianjin Medical University Cancer Institute and Hospital
    New P2 trial
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    EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase)
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    EGFR mutation
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    albumin-bound paclitaxel • retlirafusp alfa (SHR-1701)
    2ms
    Retlirafusp Alfa: First Approval. (PubMed, Drugs)
    In January 2026, retlirafusp alfa was approved for use in combination with fluorouracil and platinum-based drugs as a first-line treatment for locally advanced, unresectable, recurrent, or metastatic gastric cancer and gastroesophageal junction adenocarcinoma (GC/GEJA) with a PD-L1 positive CPS ≥ 1, as assessed by a well-validated assay in China. This article summarizes the milestones in the development of retlirafusp alfa leading to this first approval for the treatment of advanced PD-L1 positive GC/GEJA.
    Review • Journal
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    TGFB1 (Transforming Growth Factor Beta 1)
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    PD-L1 expression
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    5-fluorouracil • retlirafusp alfa (SHR-1701)
    2ms
    A clinical study of retlirafusp alfa combined with platinum-based chemotherapy and apatinib as first-line treatment for advanced NSCLC (ChiCTR2600121692)
    P4, N=35, The first affiliated hospital of anhui medical university; The first affiliated hospital of anhui medical university
    New P4 trial
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    PD-L1 (Programmed death ligand 1) • ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
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    PD-L1 expression • EGFR mutation • ALK fusion • ROS1 fusion
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    AiTan (rivoceranib) • retlirafusp alfa (SHR-1701)
    2ms
    MA-GC-II-022: PD1/TGFβ In Combination With SHR2554 or Apatinib And Chemotherapy For First - Line Treatment Of Gastric Cancer (clinicaltrials.gov)
    P2, N=78, Recruiting, The First Affiliated Hospital of Zhengzhou University | N=36 --> 78
    Enrollment change
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    AiTan (rivoceranib) • capecitabine • oxaliplatin • retlirafusp alfa (SHR-1701) • zeprumetostat (SHR-2554)