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    DRUG CLASS:

    KRAS G12D inhibitor

    Related drugs:
    3d
    HDAC5 deficiency induces intrinsic resistance to KRAS inhibition by disrupting c-Myc acetylation-ubiquitination homeostasis. (PubMed, J Clin Invest)
    Our data further demonstrated that pharmacological or genetic inhibition of c-Myc effectively reversed the resistance phenotype mediated by HDAC5 loss, suggesting a therapeutic strategy centered on "KRAS-MYC dual-node blockade." Furthermore, the expression levels of HDAC5 and the acetylation status of c-Myc may serve as potential biomarkers for predicting the therapeutic response to MRTX1133. These findings provide insights into overcoming resistance to KRASG12D inhibitors and offer potential biomarkers and combinatorial therapeutic strategies for precision treatment of PDAC.
    Journal
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    KRAS (KRAS proto-oncogene GTPase) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • HDAC5 (Histone Deacetylase 5) • NEDD4 (NEDD4 E3 Ubiquitin Protein Ligase)
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    KRAS mutation • KRAS G12D
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    MRTX1133
    9d
    Phase 1 Study to Investigate TCRTs KRAS Mutation in Unresectable, Advanced, and/or Metastatic Solid Tumors (clinicaltrials.gov)
    P1, N=24, Recruiting, AstraZeneca | Trial completion date: Apr 2044 --> Nov 2043
    Trial completion date
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    KRAS (KRAS proto-oncogene GTPase)
    11d
    Phase III Study to Compare GFH375 and Chemotherapy in Patients With KRAS G12D-Mutant Metastatic Pancreatic Cancer (clinicaltrials.gov)
    P3, N=320, Not yet recruiting, Genfleet Therapeutics (Shanghai) Inc.
    New P3 trial
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    KRAS (KRAS proto-oncogene GTPase)
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    gemcitabine • paclitaxel • 5-fluorouracil • irinotecan • leucovorin calcium • Teysuno (gimeracil/oteracil/tegafur)
    12d
    A Study of GFH375 Combined With Cetuximab or Chemotherapy in Participants With Solid Tumors Harboring KRAS G12D Mutation (clinicaltrials.gov)
    P1/2, N=126, Recruiting, Genfleet Therapeutics (Shanghai) Inc.
    New P1/2 trial
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    KRAS (KRAS proto-oncogene GTPase)
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    Erbitux (cetuximab) • gemcitabine • paclitaxel
    12d
    A targeted combination therapy achieves effective pancreatic cancer regression and prevents tumor resistance. (PubMed, Proc Natl Acad Sci U S A)
    Likewise, a combination of selective inhibitors of KRAS (RMC-6236/daraxonrasib), EGFR family (afatinib), and STAT3 (SD36) induced the complete regression of orthotopic PDAC tumors with no evidence of tumor resistance for over 200 d posttreatment...Of importance, this combination therapy was well tolerated. In sum, these results should guide the development of new clinical trials that may benefit PDAC patients.
    Journal
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    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53)
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    TP53 mutation • KRAS mutation
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    Gilotrif (afatinib) • MRTX1133 • daraxonrasib (RMC-6236)
    18d
    iEXPLORE: iExosomes in Treating Participants With Metastatic Pancreas Cancer With KrasG12D Mutation (clinicaltrials.gov)
    P1/2, N=28, Recruiting, M.D. Anderson Cancer Center | Phase classification: P1 --> P1/2
    Phase classification
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    KRAS (KRAS proto-oncogene GTPase)
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    KRAS mutation • KRAS G12D • KRAS G12
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    Undisclosed MSC-derived Exosomes with KrasG12D siRNA
    18d
    A Study to Assess the Effect of Itraconazole, Rifampin, and Acid-Reducing Agents on INCB161734 Pharmacokinetics When Administered Orally in Healthy Participants (clinicaltrials.gov)
    P1, N=63, Completed, Incyte Corporation | Recruiting --> Completed
    Trial completion
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    itraconazole • rifampicin
    23d
    HRS-4642 in Combination With Nimotuzumab and Chemotherapy for BRPC With KRAS G12D Mutation (clinicaltrials.gov)
    P2, N=40, Not yet recruiting, Zhejiang University
    New P2 trial
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    KRAS (KRAS proto-oncogene GTPase)
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    paclitaxel • TheraCIM (nimotuzumab) • HRS-4642
    26d
    HRS 4642 Injection Combined With AG Versus Placebo Combined With AG Therapy in First-Line Advanced or Metastatic Pancreatic Cancer (clinicaltrials.gov)
    P3, N=588, Not yet recruiting, Jiangsu HengRui Medicine Co., Ltd.
    New P3 trial
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    KRAS (KRAS proto-oncogene GTPase)
    |
    HRS-4642
    27d
    GFH375X1201: A Phase II Study to Evaluate GFH375 in Patients With KRAS G12D Mutant Metastatic Pancreatic Cancer (clinicaltrials.gov)
    P2, N=0, Withdrawn, Genfleet Therapeutics (Shanghai) Inc. | N=83 --> 0 | Not yet recruiting --> Withdrawn | Trial primary completion date: Dec 2027 --> Aug 2027
    Enrollment change • Trial withdrawal • Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase)
    27d
    HRS-4642 Combined With Nimotuzumab in the Treatment of Recurrent or Metastatic Pancreatic Ductal Adenocarcinoma (clinicaltrials.gov)
    P1/2, N=20, Recruiting, West China Hospital | N=10 --> 20
    Enrollment change
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    TheraCIM (nimotuzumab) • HRS-4642
    1m
    ALAFOSS-01: A Phase I/IIa Study to Investigate the Safety, Tolerability, Pharmacokinetics, and Efficacy of AZD0022 as Monotherapy and in Combination With Anti-cancer Agents in Adult Participants With Tumours Harbouring a KRASG12D Mutation (clinicaltrials.gov)
    P1/2, N=17, Active, not recruiting, AstraZeneca | Recruiting --> Active, not recruiting | N=430 --> 17 | Trial completion date: Jan 2028 --> Jun 2026 | Trial primary completion date: Jan 2028 --> Oct 2025
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    Erbitux (cetuximab)