^
    26d
    Fulzerasib: First Approval. (PubMed, Drugs)
    This conditional approval was based on the positive results of a single-arm, phase II study. This article summarizes the milestones in the development of fulzerasib leading to this first approval for KRAS G12C-mutated advanced NSCLC.
    Review • Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C
    |
    Dupert (fulzerasib)
    1m
    An open, multicentre, phase I/II study to evaluate the effectiveness and safety of IBI351 combined with platinum-containing chemotherapy and ⻉vazumab in subjects of KRAS G12C mutation or metastatic non-squamous non-small cell lung cancer subjects (ChiCTR2400090974)
    P1/2, N=28, Not yet recruiting, HenanCancerHospital; HenanCancerHospital
    New P1/2 trial • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Dupert (fulzerasib)
    2ms
    Study of the mass balance, biotransformation, and safety of [ 14C]IBI351 in healthy Chinese subjects. (PubMed, J Biomed Res)
    IBI351 and its metabolites were primarily excreted through feces. Taken together, this is the first study on the metabolism and safety of IBI351 in Chinese subjects, and these findings may guide future clinical development of IBI351 as a novel anti-tumor drug.
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS G12C • KRAS G12
    |
    Dupert (fulzerasib)
    3ms
    Potent covalent irreversible inhibitor of KRAS G12C IBI351 in patients with advanced solid tumors: First-in-human phase I study. (PubMed, Eur J Cancer)
    IBI351 was well tolerated in patients with advanced solid tumors and showed promising antitumor activity in advanced NSCLC patients with KRAS G12C mutation.
    P1 data • Journal • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C
    |
    Dupert (fulzerasib)
    4ms
    Efficacy and safety of KRAS G12C inhibitor IBI351 monotherapy in patients with advanced non-small cell lung cancer: results from a phase 2 pivotal study. (PubMed, J Thorac Oncol)
    IBI351 monotherapy demonstrated promising and sustained efficacy with manageable safety, supporting its potential as a new treatment option for KRAS G12C-mutant NSCLC.
    P2 data • Journal • PD(L)-1 Biomarker • IO biomarker • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53) • STK11 (Serine/threonine kinase 11) • KEAP1 (Kelch Like ECH Associated Protein 1) • SMAD4 (SMAD family member 4) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • BRINP3 (BMP/Retinoic Acid Inducible Neural Specific 3)
    |
    Dupert (fulzerasib)
    12ms
    A Study of [14C]IBI351 in Healthy Subjects (clinicaltrials.gov)
    P1, N=6, Completed, Innovent Biologics (Suzhou) Co. Ltd. | Not yet recruiting --> Completed
    Trial completion
    |
    Dupert (fulzerasib)
    1year
    A Study of IBI351 in Healthy Subjects (clinicaltrials.gov)
    P1, N=24, Completed, Innovent Biologics (Suzhou) Co. Ltd. | Not yet recruiting --> Completed | Trial completion date: Jun 2023 --> Oct 2023 | Trial primary completion date: Apr 2023 --> Oct 2023
    Trial completion • Trial completion date • Trial primary completion date
    |
    Dupert (fulzerasib)
    1year
    A Study of IBI351 in Healthy Subjects (clinicaltrials.gov)
    P1, N=24, Completed, Innovent Biologics (Suzhou) Co. Ltd. | Not yet recruiting --> Completed | Trial completion date: May 2023 --> Oct 2023 | Trial primary completion date: Apr 2023 --> Oct 2023
    Trial completion • Trial completion date • Trial primary completion date
    |
    Dupert (fulzerasib) • itraconazole
    1year
    Efficacy and safety of IBI351 (GFH925) monotherapy in metastatic colorectal cancer harboring KRASG12C mutation: Updated results from a pooled analysis of two phase I studies (ESMO Asia 2023)
    Conclusions The updated results of IBI351 (GFH925) monotherapy showed promising durable efficacy and manageable safety in metastatic CRC harboring KRASG12C mutation. During longer follow-up, these two ongoing studies are expected to provide more robust evidence.
    P1 data • Retrospective data • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Dupert (fulzerasib)
    1year
    Efficacy and safety of IBI351 (GFH925), a selective KRASG12C inhibitor, monotherapy in patients (pts) with advanced non-small cell lung cancer (NSCLC): Initial results from a registrational phase II study (ESMO Asia 2023)
    Conclusions IBI351 continues to demonstrate encouraging efficacy with manageable safety. These results support IBI351 monotherapy as a potential new treatment option for advanced KRASG12C mutant NSCLC pts.
    Clinical • P2 data • Late-breaking abstract • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C
    |
    Dupert (fulzerasib)
    over1year
    A Study of GFH925 in Patients With Advanced Solid Tumors With KRAS G12C Mutations (clinicaltrials.gov)
    P1/2, N=264, Recruiting, Innovent Biologics (Suzhou) Co. Ltd. | N=128 --> 264
    Enrollment change • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Dupert (fulzerasib)
    over1year
    Efficacy and Safety of IBI351 in Combination With Sintilimab ± Chemotherapy in Advanced Non-squamous Non-small Cell Lung Cancer Subjects With KRAS G12C Mutation (clinicaltrials.gov)
    P1, N=144, Recruiting, Innovent Biologics (Suzhou) Co. Ltd. | Not yet recruiting --> Recruiting | Trial primary completion date: May 2023 --> May 2024
    Enrollment open • Trial primary completion date • Combination therapy • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    carboplatin • Tyvyt (sintilimab) • pemetrexed • Dupert (fulzerasib)
    over1year
    A Study of GFH925 in Combination With Cetuximab in Previously Untreated Advanced NSCLC Harboring KRAS G12C Mutation (clinicaltrials.gov)
    P1/2, N=45, Recruiting, Zhejiang Genfleet Therapeutics Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Erbitux (cetuximab) • Dupert (fulzerasib)
    over1year
    Efficacy and safety of IBI351 (GFH925) monotherapy in metastatic colorectal cancer harboring KRASG12C mutation: Preliminary results from a pooled analysis of two phase I studies. (ASCO 2023)
    IBI351 (GFH925) monotherapy demonstrated promising anti-tumor activity with manageable safety profile in metastatic CRC patients harboring KRASG12C mutation. These two studies are still ongoing and longer follow-up will provide more solid evidence. Updated data will be presented at the meeting.
    P1 data • Retrospective data • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Dupert (fulzerasib)
    almost2years
    A Study of GFH925 in Combination With Cetuximab in Previously Untreated Advanced NSCLC Harboring KRAS G12C Mutation (clinicaltrials.gov)
    P1/2, N=45, Not yet recruiting, Zhejiang Genfleet Therapeutics Co., Ltd.
    New P1/2 trial • Combination therapy • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Erbitux (cetuximab) • Dupert (fulzerasib)
    2years
    A Study of IBI351 in Combination With Cetuximab in Subjects With KRAS G12C Mutated Metastatic Colorectal Cancer (clinicaltrials.gov)
    P1, N=80, Recruiting, Innovent Biologics (Suzhou) Co. Ltd. | Not yet recruiting --> Recruiting | Trial primary completion date: Aug 2022 --> Aug 2023
    Enrollment open • Trial primary completion date • Combination therapy • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Erbitux (cetuximab) • Dupert (fulzerasib)
    over2years
    Efficacy and Safety of IBI351 in Combination With Sintilimab ± Chemotherapy in Advanced Non-squamous Non-small Cell Lung Cancer Subjects With KRAS G12C Mutation (clinicaltrials.gov)
    P1, N=144, Not yet recruiting, Innovent Biologics (Suzhou) Co. Ltd.
    New P1 trial • Combination therapy
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Erbitux (cetuximab) • carboplatin • Tyvyt (sintilimab) • pemetrexed • Dupert (fulzerasib)
    over2years
    A Study of GFH925 in Patients With Advanced Solid Tumors With KRAS G12C Mutations (clinicaltrials.gov)
    P1/2, N=128, Recruiting, Zhejiang Genfleet Therapeutics Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Dupert (fulzerasib)
    over3years
    A Study of GFH925 in Patients With Advanced Solid Tumors With KRAS G12C Mutations (clinicaltrials.gov)
    P1/2, N=128, Not yet recruiting, Zhejiang Genfleet Therapeutics Co., Ltd.
    Clinical • New P1/2 trial
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12
    |
    Dupert (fulzerasib)