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    1m
    TGRX-326 Phase I Oral Pharmacokinetic Study (clinicaltrials.gov)
    P1, N=72, Not yet recruiting, Shenzhen TargetRx, Inc.
    New P1 trial
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    deulorlatinib (TGRX-326) • TGRX-678
    1m
    Safety, efficacy and biomarker analysis of deulorlatinib (TGRX-326) in ALK-positive non-small-cell lung cancer: a multicentre, open-label, phase 1/1b trial. (PubMed, J Thorac Oncol)
    Deulorlatinib showed desirable tolerability and efficacy in ALK-positive NSCLC, demonstrating the potential to become a new treatment option in this population.
    P1 data • Journal
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    ALK (Anaplastic lymphoma kinase)
    |
    ALK positive • ROS1 positive
    |
    Xalkori (crizotinib) • Lorbrena (lorlatinib) • deulorlatinib (TGRX-326)
    5ms
    TGRX-326 NSCLC Phase I study: A Phase I Dose Escalation and Dose Expansion Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of TGRX-326 Monotherapy for the Treatment of Advanced ALK-positive or ROS1-positive Non-small Cell Lung Cancer (ChiCTR2400081304)
    P1, N=185, Completed, Sun Yat-sen University Cancer Center; Shenzhen TargetRx, Inc.
    New P1 trial
    |
    ALK (Anaplastic lymphoma kinase)
    |
    deulorlatinib (TGRX-326)
    6ms
    TGRX-326 Pharmacokinetic Drug Interaction (clinicaltrials.gov)
    P1, N=34, Completed, Shenzhen TargetRx, Inc. | Recruiting --> Completed
    Trial completion
    |
    deulorlatinib (TGRX-326) • itraconazole
    7ms
    TGRX-326 Pharmacokinetic Mass Balance (clinicaltrials.gov)
    P1, N=6, Not yet recruiting, Shenzhen TargetRx, Inc.
    New P1 trial
    |
    deulorlatinib (TGRX-326)
    9ms
    TGRX-326 Chinese Phase I for Advanced Non-small Cell Lung Cancer (NSCLC) (clinicaltrials.gov)
    P1, N=198, Active, not recruiting, Shenzhen TargetRx, Inc. | Recruiting --> Active, not recruiting | N=100 --> 198 | Trial completion date: Jun 2024 --> Oct 2025 | Trial primary completion date: Dec 2023 --> Aug 2025
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date • Metastases
    |
    ALK (Anaplastic lymphoma kinase)
    |
    ALK positive • ROS1 positive
    |
    deulorlatinib (TGRX-326)
    9ms
    TGRX-326 Food Effect Pharmacokinetic Study (clinicaltrials.gov)
    P1, N=24, Completed, Shenzhen TargetRx, Inc.
    New P1 trial
    |
    deulorlatinib (TGRX-326)
    9ms
    TGRX-326 Pharmacokinetic Drug Interaction (clinicaltrials.gov)
    P1, N=32, Recruiting, Shenzhen TargetRx, Inc. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    deulorlatinib (TGRX-326) • itraconazole
    10ms
    TGRX-326 Drug-Drug Interaction Pharmacokinetic Study (clinicaltrials.gov)
    P1, N=32, Not yet recruiting, Shenzhen TargetRx, Inc.
    New P1 trial
    |
    deulorlatinib (TGRX-326) • itraconazole
    12ms
    TGRX-326 Chinese Phase III for Advanced Non-small Cell Lung Cancer (NSCLC) (clinicaltrials.gov)
    P3, N=297, Recruiting, Shenzhen TargetRx, Inc. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
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    ALK positive
    |
    Xalkori (crizotinib) • deulorlatinib (TGRX-326)
    1year
    TGRX-326 Chinese Phase III for Advanced Non-small Cell Lung Cancer (NSCLC) (clinicaltrials.gov)
    P3, N=297, Not yet recruiting, Shenzhen TargetRx, Inc.
    New P3 trial • Metastases
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    ALK positive
    |
    Xalkori (crizotinib) • deulorlatinib (TGRX-326)
    over1year
    TGRX-326 Chinese Phase II for Advanced Non-small Cell Lung Cancer (NSCLC) (clinicaltrials.gov)
    P2, N=157, Recruiting, Shenzhen TargetRx, Inc.
    New P2 trial
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    ALK positive
    |
    deulorlatinib (TGRX-326)
    over1year
    First-in-human, multicenter phase Ⅰ study of TGRX-326 in patients with advanced ALK-positive non-small cell lung cancer. (ASCO 2023)
    Background: TGRX-326, a deuterated derivative of lorlatinib (LOR), is a potent 3rd generation ALK and ROS1 dual TKI with high potency against multiple ALK-resistant mutations...In D-ESCAL and D-EXP, ALK+ pts prior failed on 2nd gen ALK-TKIs or ROS1+ pts resistant to crizotinib (CRZ) were enrolled; in C-EXP, ALK+ pts progression after CRZ (C-EXP-A1),progression after ≥1 2nd gen TKIs (C-EXP A2), ROS1+progression after CRZ (C-EXP-B) and pts with ALK TKI naïve (C-EXP-C) were enrolled... TGRX-326 was well tolerated in pts with advanced ALK+NSCLC and showed promising clinical antitumor activity irrespectively of ALK+ resistance to CRZ and 2nd gen TKIs, especially among those with brain metastases. Impressive activity was seen in ALK TKI naïve NSCLC. TGRX-326 demonstrated antitumor activity against multiple ALK mutations including G1202R.
    Clinical • P1 data • Metastases
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    ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    ALK positive • ALK mutation • ALK G1202R
    |
    Xalkori (crizotinib) • Lorbrena (lorlatinib) • deulorlatinib (TGRX-326)
    almost2years
    TGRX-326 Chinese Phase I for Advanced Non-small Cell Lung Cancer (NSCLC) (clinicaltrials.gov)
    P1, N=100, Recruiting, Shenzhen TargetRx, Inc. | Trial completion date: Mar 2023 --> Jun 2024 | Trial primary completion date: Dec 2022 --> Dec 2023
    Trial completion date • Trial primary completion date • Metastases
    |
    ALK (Anaplastic lymphoma kinase)
    |
    ALK positive • ROS1 positive
    |
    deulorlatinib (TGRX-326)
    over2years
    TGRX-326 Chinese Phase I for Advanced Non-small Cell Lung Cancer (NSCLC) (clinicaltrials.gov)
    P1, N=100, Recruiting, Shenzhen TargetRx, Inc.
    New P1 trial
    |
    ALK (Anaplastic lymphoma kinase)
    |
    ALK positive • ROS1 positive
    |
    deulorlatinib (TGRX-326)