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    DRUG CLASS:

    DKK1 protein inhibitor

    Related drugs:
    10d
    Overcoming antigen tolerance to develop GB22-45-2, an anti-DKK1 antibody for gastric cancer. (PubMed, Antib Ther)
    In vivo, GB22-45-2 showed a modest tumor growth inhibition (31.03%) that is significant (P = 0.0175), while DKN-01 did not reach significance, in the MKN-45-Balb/c-nude mouse model. Additionally, GB22-45-2 exhibited a satisfactory developability profile, including good thermal stability, low aggregation propensity, high structural integrity, and excellent stability under various stress conditions. In summary, these preclinical results suggest that GB22-45-2 is a potential therapeutic candidate for GC, laying the foundation for its future drug development.
    Journal
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    DKK1 (dickkopf WNT signaling pathway inhibitor 1)
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    sirexatamab (DKN-01)
    1m
    Phase 2 Study Evaluating the Efficacy of the Combination of DKN-01 (DKK1 Inhibitor, Leap Therapeutics) and Pembrolizumab in the Treatment of Advanced or Recurrent Endometrial Cancer (clinicaltrials.gov)
    P2, N=8, Active, not recruiting, M.D. Anderson Cancer Center | Recruiting --> Active, not recruiting | N=60 --> 8
    Enrollment closed • Enrollment change
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    CTNNB1 (Catenin (cadherin-associated protein), beta 1) • AXIN1 (Axin 1) • RSPO2 (R-Spondin 2) • ZNRF3 (Zinc And Ring Finger 3)
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    Keytruda (pembrolizumab) • sirexatamab (DKN-01)
    2ms
    DisTinGuish: A Study of DKN-01 in Combination With Tislelizumab ± Chemotherapy in Patients With Gastric or Gastroesophageal Cancer (clinicaltrials.gov)
    P2, N=247, Terminated, Leap Therapeutics, Inc. | Trial completion date: Dec 2025 --> Mar 2025 | Active, not recruiting --> Terminated; experimental treatment will not be more efficacious than its comparator in the primary endpoint of PFS
    Trial completion date • Trial termination
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    PD-L1 (Programmed death ligand 1) • DKK1 (dickkopf WNT signaling pathway inhibitor 1)
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    5-fluorouracil • Tevimbra (tislelizumab-jsgr) • capecitabine • oxaliplatin • leucovorin calcium • sirexatamab (DKN-01)
    5ms
    DeFianCe: Phase 2 Study of DKN-01 in Colorectal Cancer (clinicaltrials.gov)
    P2, N=188, Completed, Leap Therapeutics, Inc. | Active, not recruiting --> Completed | Trial completion date: Oct 2025 --> Jul 2025 | Trial primary completion date: Oct 2025 --> Jul 2025
    Trial completion • Trial completion date • Trial primary completion date
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    Avastin (bevacizumab) • 5-fluorouracil • oxaliplatin • irinotecan • leucovorin calcium • sirexatamab (DKN-01)
    5ms
    DKN-01 and tislelizumab as second-line therapy in DKK1-high gastroesophageal adenocarcinoma: DisTinGuish trial part B. (PubMed, Nat Commun)
    The median OS was 8.2 months, median PFS 1.4 months, and DCR rate 34.8% in the overall population. Although exploratory, the results of this trial compare favorably against second-line benchmarks of Keynote-061 and RAINBOW and support the safety and tolerability of DKN-01 combined with tislelizumab.
    Journal • PD(L)-1 Biomarker • IO biomarker
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    DKK1 (dickkopf WNT signaling pathway inhibitor 1)
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    Tevimbra (tislelizumab-jsgr) • sirexatamab (DKN-01)
    6ms
    A Phase 2 Study Evaluating the Safety and Efficacy of JS207 With or Without JS015 in Combination With Chemotherapy in Patients With Colorectal Cancer (clinicaltrials.gov)
    P2, N=60, Recruiting, Shanghai Junshi Bioscience Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
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    capecitabine • oxaliplatin
    9ms
    WaKING: Wnt and checKpoint INhibition in Gastric Cancer (clinicaltrials.gov)
    P1/2, N=52, Active, not recruiting, Royal Marsden NHS Foundation Trust | Trial completion date: Sep 2025 --> Dec 2025 | Trial primary completion date: Dec 2024 --> Mar 2025
    Trial completion date • Trial primary completion date • Checkpoint inhibition • Mismatch repair • pMMR
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    HER-2 positive
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    Tecentriq (atezolizumab) • sirexatamab (DKN-01)
    9ms
    A Phase 2 Study Evaluating the Safety and Efficacy of JS207 With or Without JS015 in Combination With Chemotherapy in Patients With Colorectal Cancer (clinicaltrials.gov)
    P2, N=60, Not yet recruiting, Shanghai Junshi Bioscience Co., Ltd.
    New P2 trial
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    capecitabine • oxaliplatin
    11ms
    JS015 Combined Therapy in Gastrointestinal Tumors: A Multi-Cohort, Multi-Center, Exploratory Clinical Study (ChiCTR2400091501)
    P2, N=56, Shanghai East Hospital; Shanghai East 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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    Avastin (bevacizumab) • Loqtorzi (toripalimab-tpzi)
    12ms
    A Phase Ib/II Study Of JS015 Combination Therapy in Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=186, Recruiting, Shanghai Junshi Bioscience Co., Ltd. | Not yet recruiting --> Recruiting | Trial completion date: Apr 2026 --> Jan 2026
    Enrollment open • Trial completion date • Metastases
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    Avastin (bevacizumab) • gemcitabine • 5-fluorouracil • Loqtorzi (toripalimab-tpzi) • capecitabine • albumin-bound paclitaxel • oxaliplatin • irinotecan • leucovorin calcium
    1year
    JS015 in combination with chemotherapy and bevacizumab as second-line treatment in advanced colorectal cancer (ChiCTR2400088962)
    P2, N=37, Not yet recruiting, Shanghai East Hospital; Shanghai East Hospital
    New P2 trial • Combination therapy • Metastases
    |
    Avastin (bevacizumab)
    1year
    DKN-01 in Combination With Tislelizumab and Chemotherapy as First-Line Therapy in Advanced Gastric or Gastroesophageal Junction Adenocarcinoma: DisTinGuish. (PubMed, J Clin Oncol)
    DKN-01 can be safely combined with frontline fluoropyrimidine/oxaliplatin and tislelizumab and demonstrates encouraging activity independent of PD-L1 expression levels. A randomized phase II trial is ongoing (ClinicalTrials.gov identifier: NCT04363801).
    Journal • Combination therapy • PD(L)-1 Biomarker • IO biomarker • Metastases
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    HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • DKK1 (dickkopf WNT signaling pathway inhibitor 1)
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    PD-L1 expression • HER-2 negative
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    Tevimbra (tislelizumab-jsgr) • capecitabine • oxaliplatin • sirexatamab (DKN-01)