^
    3ms
    TGRX-678 Pharmacokinetic Mass Balance (clinicaltrials.gov)
    P1, N=6, Completed, Shenzhen TargetRx, Inc. | Not yet recruiting --> Completed | Trial completion date: Dec 2025 --> Aug 2025
    Trial completion • Trial completion date
    |
    TGRX-678
    4ms
    Preclinical characterization of TGRX-678, a brain-penetrant allosteric inhibitor of BCR::ABL1. (PubMed, Blood)
    When combined with ponatinib, TGRX-678 synergistically re-sensitizes the highly resistant compound mutants and T315M to growth inhibition at clinically achievable concentrations...It also demonstrates a markedly improved in vivo pharmacokinetic (PK) profile and higher oral bioavailability compared to asciminib. Importantly, TGRX-678 penetrates the blood-brain barrier (BBB) and exhibits in vivo efficacy in a murine CNS blast crisis leukemia model. Collectively, these findings suggest that TGRX-678 is a novel BCR::ABL1 allosteric inhibitor with high selectivity, potency and unique pharmacologic features, which has the potential to treat relapse or refractory CML and Ph+ ALL, even with CNS involvement.
    Preclinical • Journal
    |
    ABL1 (ABL proto-oncogene 1) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2)
    |
    Iclusig (ponatinib) • Scemblix (asciminib) • TGRX-678
    5ms
    Management of chronic myeloid leukemia in 2025. (PubMed, Cancer)
    Today, the six approved BCR::ABL1 TKIs, five in frontline therapy (imatinib, dasatinib, bosutinib, nilotinib, and asciminib) and all six in later line therapy (including ponatinib), fulfill in one form or another these requirements. Third-generation TKIs that target the ABL1 kinase domain (olverembatinib and ELVN-001) or the myristoyl pocket (TGRX-678 and TERN-701) are under development...However, serious complications, such as graft-vs-host disease, or death could occur. This review summarizes relevant information concerning the management of CML in 2025, and addresses some CML treatment pathways that became entrenched in the management of CML in the first 15-20 years of TKI experience, which may need to be revisited.
    Review • Journal
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    ABL1 (ABL proto-oncogene 1)
    |
    dasatinib • imatinib • Iclusig (ponatinib) • Tasigna (nilotinib) • bosutinib • Scemblix (asciminib) • Nailike (olverembatinib) • TGRX-678 • ELVN-001 • TERN-701
    7ms
    TGRX-678 Pharmacokinetic Mass Balance (clinicaltrials.gov)
    P1, N=6, Not yet recruiting, Shenzhen TargetRx, Inc.
    New P1 trial
    |
    TGRX-678
    7ms
    TGRX-678-1002: TGRX-678 Phase I Oral Pharmacokinetic Study (clinicaltrials.gov)
    P1, N=76, Completed, Shenzhen TargetRx, Inc. | Active, not recruiting --> Completed | Trial completion date: Jul 2025 --> Feb 2025
    Trial completion • Trial completion date
    |
    TGRX-678
    9ms
    TGRX-678-1001: TGRX-678 Chinese Phase I in Chronic Myelogenous Leukemia (CML) Patients (clinicaltrials.gov)
    P1, N=90, Active, not recruiting, Shenzhen TargetRx, Inc. | Recruiting --> Active, not recruiting | Trial completion date: Jun 2025 --> Sep 2026 | Trial primary completion date: Dec 2024 --> Mar 2026
    Enrollment closed • Trial completion date • Trial primary completion date
    |
    TGRX-678
    10ms
    TGRX-678-1002: TGRX-678 Phase I Oral Pharmacokinetic Study (clinicaltrials.gov)
    P1, N=72, Active, not recruiting, Shenzhen TargetRx, Inc. | Not yet recruiting --> Active, not recruiting | Trial completion date: Feb 2025 --> Jul 2025
    Enrollment closed • Trial completion date
    |
    TGRX-678
    10ms
    TGRX-678 Chinese Phase II in Chronic Myelogenous Leukemia (CML) Patients (clinicaltrials.gov)
    P2, N=40, Recruiting, Shenzhen TargetRx, Inc. | Not yet recruiting --> Recruiting | Trial completion date: Dec 2027 --> Apr 2028
    Enrollment open • Trial completion date
    |
    TGRX-678
    1year
    TGRX-326 Phase I Oral Pharmacokinetic Study (clinicaltrials.gov)
    P1, N=72, Not yet recruiting, Shenzhen TargetRx, Inc.
    New P1 trial
    |
    deulorlatinib (TGRX-326) • TGRX-678
    over1year
    TGRX-678 Chinese Phase II in Chronic Myelogenous Leukemia (CML) Patients (clinicaltrials.gov)
    P2, N=40, Not yet recruiting, Shenzhen TargetRx, Inc.
    New P2 trial
    |
    TGRX-678
    over1year
    TGRX-678 US Phase I for Subjects With Refractory or Advanced Chronic Myelogenous Leukemia (clinicaltrials.gov)
    P1, N=90, Recruiting, Shenzhen TargetRx, Inc. | Not yet recruiting --> Recruiting | Initiation date: Mar 2024 --> Jun 2024
    Enrollment open • Trial initiation date • Metastases
    |
    TGRX-678
    almost2years
    TGRX-678 Chinese Phase I in Chronic Myelogenous Leukemia (CML) Patients (clinicaltrials.gov)
    P1, N=90, Recruiting, Shenzhen TargetRx, Inc. | Trial completion date: Jun 2024 --> Jun 2025 | Trial primary completion date: Dec 2023 --> Dec 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    TGRX-678