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    5ms
    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
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    TGRX-678
    6ms
    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
    9ms
    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
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    TGRX-678
    1year
    Safety and Efficacy of Tgrx-678, a Potent BCR-ABL Allosteric Inhibitor in Patients with Tyrosine Kinase Inhibitor (TKI) Resistant/Refractory Chronic Myeloid Leukemia (CML): Preliminary Results of Phase I Study (ASH 2023)
    There were 22 CML-CP and 23 CML-AP patients previous received 3rd Gen TKIs (ponatinib or HQP1351) or asciminib. Clinical activity of TGRX-678 was seen in all cohorts and across TKI-resistant mutations including T315I, providing a promising treatment option for CML CP/AP patients, including those who failed ponatinib or asciminib. Its unique PK properties might bring additional benefit to patients. TGRX-678 was well tolerated in heavily pretreated CML patients.
    Clinical • P1 data
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    ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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    Iclusig (ponatinib) • Scemblix (asciminib) • Nailike (olverembatinib) • TGRX-678
    1year
    Tgrx-678, a Novel Allosteric Inhibitor of BCR-ABL1, Demonstrates Preclinical Anti-Leukemia Activity, High Oral Bioavailability and Synergism with Ponatinib to Suppress the Highly Resistant Compound Mutations (ASH 2023)
    ABL1 is subject to auto-inhibition mediated by myristoylation-triggered conformational change, which can be exploited to overcome resistance, as validated by allosteric inhibitors such as GNF2, GNF5 and asciminib. Furthermore, TGRX-678 and ponatinib synergize to overcome the clinically challenging resistance conferred by T315M or T315I-inclusive compound mutations. This data warrant further clinical investigation of TGRX-678 for the treatment of resistant or refractory CML patients.
    Preclinical
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    ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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    BCR-ABL1 T315I • BCR-ABL1 E255K • BCR-ABL1 Y253H • BCR-ABL1 E255V • BCR-ABL1 G250E • ABL1 T315I • BCR-ABL1 Q252H • ABL1 E255K • ABL1 G250E • ABL1 Y253H • BCR-ABL1 T315M • BCR-ABL1 Y253H + BCR-ABL1 T315I
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    Iclusig (ponatinib) • Scemblix (asciminib) • TGRX-678
    1year
    TGRX-678 US Phase I for Subjects With Refractory or Advanced Chronic Myelogenous Leukemia (clinicaltrials.gov)
    P1, N=90, Not yet recruiting, Shenzhen TargetRx, Inc.
    New P1 trial • Metastases
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    ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
    |
    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: Dec 2022 --> Jun 2024 | Trial primary completion date: Oct 2022 --> Dec 2023
    Trial completion date • Trial primary completion date • Metastases
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    ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
    |
    TGRX-678
    over2years
    TGRX-678 Chinese Phase I in Chronic Myelogenous Leukemia (CML) Patients (clinicaltrials.gov)
    P1, N=90, Recruiting, Shenzhen TargetRx, Inc.
    New P1 trial
    |
    ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
    |
    TGRX-678