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    DRUG CLASS:

    SOS1 inhibitor

    Related drugs:
    6d
    KQB198 in Combination With Imatinib in Participants With Advanced/Metastatic GIST in 1st Line Setting (clinicaltrials.gov)
    P2, N=46, Recruiting, Kumquat Biosciences Inc. | Not yet recruiting --> Recruiting
    Enrollment open
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    KIT (KIT proto-oncogene, receptor tyrosine kinase)
    |
    KIT mutation
    |
    imatinib
    9d
    Discovery of a potent and orally available SOS1 inhibitor with antitumor efficacy in KRAS-mutant colorectal cancers. (PubMed, Bioorg Chem)
    In an HCT116 xenograft model, oral administration of SL43 (20 and 40 mg/kg) also significantly suppressed tumor growth (TGI = 57.2% and 74.9%, respectively), outperforming MRTX0902 (60 mg/kg, TGI = 47.1%) with no observable systemic toxicity. In conclusion, SL43 represents a potent and orally bioavailable SOS1 inhibitor that effectively suppresses KRAS signaling and exerts strong antitumor efficacy, highlighting its potential as a promising candidate for KRAS-mutant colorectal cancer.
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation • KRAS G12C • KRAS G12D • KRAS wild-type • RAS wild-type • KRAS G12
    |
    MRTX0902
    28d
    KQB198-102: A Study to Investigate the Safety and Efficacy of KQB198 as Monotherapy and in Combination in Participants With Advanced Hematologic Malignancies (clinicaltrials.gov)
    P1, N=13, Active, not recruiting, Kumquat Biosciences Inc. | Recruiting --> Active, not recruiting | N=122 --> 13 | Trial completion date: Feb 2028 --> Mar 2027 | Trial primary completion date: Aug 2027 --> Mar 2027
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
    |
    dasatinib
    2ms
    CA247-0004: A Phase 1 Study of MRTX0902 in Solid Tumors With Mutations in the KRAS MAPK Pathway (clinicaltrials.gov)
    P1, N=64, Terminated, Mirati Therapeutics Inc. | Phase classification: P1/2 --> P1 | N=228 --> 64 | Trial completion date: Jul 2026 --> Feb 2026 | Active, not recruiting --> Terminated | Trial primary completion date: Jun 2026 --> Feb 2026; business objectives have changed
    Phase classification • Enrollment change • Trial completion date • Trial termination • Trial primary completion date • First-in-human
    |
    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NF1 (Neurofibromin 1) • PTPN11 (Protein Tyrosine Phosphatase Non-Receptor Type 11)
    |
    KRAS mutation • EGFR mutation • KRAS G12C • BRAF mutation • KRAS G12
    |
    Krazati (adagrasib) • MRTX0902
    2ms
    KQB198 in Combination With Imatinib in Participants With Advanced/Metastatic GIST in 1st Line Setting (clinicaltrials.gov)
    P2, N=46, Not yet recruiting, Kumquat Biosciences Inc.
    New P2 trial
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase)
    |
    KIT mutation
    |
    imatinib
    3ms
    A Study to Test Different Doses of BI 1701963 Alone and Combined With Trametinib in Patients With Different Types of Advanced Cancer (Solid Tumours With KRAS Mutation) (clinicaltrials.gov)
    P1, N=71, Active, not recruiting, Boehringer Ingelheim | Trial completion date: Dec 2025 --> Dec 2027 | Trial primary completion date: Dec 2025 --> Dec 2027
    Trial completion date • Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
    |
    Mekinist (trametinib) • BI 1701963
    4ms
    A Phase I/II Study of HYP-6589 Monotherapy in Treating Advanced Solid Tumors and in Combination With Tyrosine Kinase Inhibitors in Treating Patients With Advanced NSCLC Positive for Driver Genes (clinicaltrials.gov)
    P1/2, N=115, Recruiting, Sichuan Huiyu Pharmaceutical Co., Ltd | Trial completion date: Jul 2026 --> Apr 2028 | Trial primary completion date: Jul 2026 --> Apr 2028
    Trial completion date • Trial primary completion date
    5ms
    Wild-type KRAS activation drives evasion of interferon-mediated immunity and resistance to immunotherapy in hepatocellular carcinoma. (PubMed, Nat Commun)
    Notably, combination therapy with SOS1 inhibitor MRTX0902, Trametinib, and anti-PD-1 antibody effectively increased intratumoural CD8+ T cell infiltration and improved survival. Our study thus reveals that targeting wild-type KRAS signalling in combination with ICIs may serve as an effective treatment strategy for advanced HCC patients.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    KRAS (KRAS proto-oncogene GTPase) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • CD8 (cluster of differentiation 8) • CXCL9 (Chemokine (C-X-C motif) ligand 9)
    |
    KRAS wild-type • RAS wild-type
    |
    Mekinist (trametinib) • MRTX0902
    7ms
    A Phase 1/2 Study of MRTX0902 in Solid Tumors With Mutations in the KRAS MAPK Pathway (clinicaltrials.gov)
    P1/2, N=228, Active, not recruiting, Mirati Therapeutics Inc. | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • NF1 (Neurofibromin 1) • PTPN11 (Protein Tyrosine Phosphatase Non-Receptor Type 11)
    |
    KRAS mutation • EGFR mutation • KRAS G12C • KRAS G12
    |
    Krazati (adagrasib) • MRTX0902
    8ms
    A Phase I Study of BAY3498264 Given Together With Sotorasib in Participants Who Have Advanced Solid Cancers With Specific Genetic Changes Called KRASG12C Mutation (clinicaltrials.gov)
    P1, N=104, Recruiting, Bayer | Trial completion date: Nov 2027 --> Mar 2028 | Trial primary completion date: Jan 2027 --> Jul 2027
    Trial completion date • Trial primary completion date
    |
    Lumakras (sotorasib)
    9ms
    Development and biological evaluation of novel SOS1 inhibitors featuring 5,8-dihydropyrido[4,3-d]pyrimidin-7(6H)-one scaffold. (PubMed, Bioorg Med Chem Lett)
    Among these, A15f and B5a emerged as the most potent compounds comparable to BI-3406...Molecular docking revealed that these two compounds shared a conserved binding mode with SOS1, similar to the reported inhibitors. These findings provide foundation for further development of SOS1-targeted anticancer therapeutics and offer valuable insights for structural optimization of this novel class of inhibitors.
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
    |
    BI-3406
    1year
    A Study to Test Different Doses of BI 1701963 Alone and Combined With Trametinib in Patients With Different Types of Advanced Cancer (Solid Tumours With KRAS Mutation) (clinicaltrials.gov)
    P1, N=71, Active, not recruiting, Boehringer Ingelheim | Trial completion date: Apr 2025 --> Dec 2025 | Trial primary completion date: Apr 2025 --> Dec 2025
    Trial completion date • Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
    |
    Mekinist (trametinib) • BI 1701963