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    DRUG:

    amezalpat (TPST-1120)

    i
    Other names: TPST-1120, TPST 1120, TPST1120
    Company:
    Tempest Therap
    Drug class:
    PPAR α antagonist
    3ms
    PROSPERO: A Study of TPST-1120 With Atezolizumab Plus Bevacizumab in Patients With Unresectable or Metastatic HCC Not Previously Treated With Systemic Therapy (clinicaltrials.gov)
    P3, N=740, Not yet recruiting, Tempest Therapeutics | Trial completion date: Dec 2029 --> Jul 2030 | Initiation date: Mar 2025 --> Dec 2025 | Trial primary completion date: Mar 2028 --> Dec 2028
    Trial completion date • Trial initiation date • Trial primary completion date
    |
    Avastin (bevacizumab) • Tecentriq (atezolizumab) • amezalpat (TPST-1120)
    6ms
    Peroxisome proliferator-activated receptor antagonists as emerging therapeutics in cancer treatment. (PubMed, Bioorg Chem)
    PPARα antagonists, such as N-(2-bromophenyl)-2-[[(3-chlorophenyl)amino]thioxomethyl]acetamide (GW6471) and TPST-1120, impair tumor metabolism and angiogenesis, reducing cancer progression...This review provides a comprehensive analysis of the medicinal chemistry, molecular mechanisms, and pharmacological development of PPAR antagonists, highlighting their potential clinical applications. Future efforts should refine drug design, develop personalized treatments, and conduct well-designed clinical trials to unlock their role in precision oncology.
    Review • Journal
    |
    CTNNB1 (Catenin (cadherin-associated protein), beta 1) • PPARA (Peroxisome Proliferator Activated Receptor Alpha)
    |
    amezalpat (TPST-1120)
    12ms
    A Study Evaluating the Efficacy and Safety of Multiple Immunotherapy-Based Treatment Combinations in Patients With Advanced Liver Cancers (Morpheus-Liver) (clinicaltrials.gov)
    P1/2, N=518, Recruiting, Hoffmann-La Roche | Trial completion date: Aug 2026 --> Dec 2026 | Trial primary completion date: Aug 2026 --> Dec 2026
    Trial completion date • Trial primary completion date • Metastases
    |
    PD-L1 (Programmed death ligand 1)
    |
    Avastin (bevacizumab) • Tecentriq (atezolizumab) • amezalpat (TPST-1120) • Actemra IV (tocilizumab) • tiragolumab (RG6058) • IO-108 • NKT2152 • muzastotug (ADG126) • tobemstomig (RG6139)
    1year
    A Study of TPST-1120 With Atezolizumab Plus Bevacizumab in Patients With Unresectable or Metastatic HCC Not Previously Treated With Systemic Therapy (clinicaltrials.gov)
    P3, N=740, Not yet recruiting, Tempest Therapeutics
    New P3 trial • Combination therapy • Metastases
    |
    Avastin (bevacizumab) • Tecentriq (atezolizumab) • amezalpat (TPST-1120)
    over1year
    A Study Evaluating the Efficacy and Safety of Multiple Immunotherapy-Based Treatment Combinations in Patients With Advanced Liver Cancers (Morpheus-Liver) (clinicaltrials.gov)
    P1/2, N=506, Recruiting, Hoffmann-La Roche | Trial completion date: Dec 2025 --> Aug 2026 | Trial primary completion date: Dec 2025 --> Aug 2026
    Trial completion date • Trial primary completion date
    |
    PD-L1 (Programmed death ligand 1)
    |
    Avastin (bevacizumab) • Tecentriq (atezolizumab) • amezalpat (TPST-1120) • Actemra IV (tocilizumab) • tiragolumab (RG6058) • NKT2152 • muzastotug (ADG126) • tobemstomig (RG6139)
    over1year
    First-in-Human Phase I Trial of TPST-1120, an inhibitor of PPARα, as Monotherapy or in Combination with Nivolumab, in Patients with Advanced Solid Tumors. (PubMed, Cancer Res Commun)
    TPST-1120 was well tolerated as monotherapy and in combination with nivolumab and the combination showed preliminary evidence of clinical activity in PD-1 inhibitor refractory and immune compromised cancers.
    Journal • Combination therapy • Metastases
    |
    PPARA (Peroxisome Proliferator Activated Receptor Alpha)
    |
    Opdivo (nivolumab) • amezalpat (TPST-1120)
    almost2years
    Pharmacodynamics and gene expression analysis of patients with renal cell carcinoma treated with combination nivolumab and TPST-1120 in a phase I clinical trial (NCT03829436). (ASCO-GU 2024)
    There is a paucity of treatment options for patients with stage IV RCC post anti-PD1 and anti-VEGF therapies. Novel therapies on this clinical scenario are needed. On this abstract we showed radiographic and pharmacodynamic data on patients with RCC who achieved a clinical partial response by RECIST on the phase I clinical trial TPST1120-001.
    PK/PD data • Clinical • PD(L)-1 Biomarker • IO biomarker
    |
    ACSL3 (Acyl-CoA Synthetase Long Chain Family Member 3) • FABP1 (Fatty Acid Binding Protein 1)
    |
    PredicineCARE™
    |
    Opdivo (nivolumab) • amezalpat (TPST-1120)
    over2years
    TPST-1120 as Monotherapy and in Combination With Nivolumab in Subjects With Advanced Cancers (clinicaltrials.gov)
    P1, N=38, Completed, Tempest Therapeutics | Active, not recruiting --> Completed | N=138 --> 38 | Trial completion date: Jun 2024 --> Sep 2022
    Trial completion • Enrollment change • Trial completion date • Combination therapy • Metastases
    |
    Opdivo (nivolumab) • amezalpat (TPST-1120)
    over2years
    Lipid and immune-based biomarkers associated with clinical response to TPST-1120: A small molecule antagonist of peroxisome-proliferator activated receptor-alpha (AACR 2023)
    TPST-1120 was well tolerated and showed signs of activity in a phase I trial as monotherapy and in combination with nivolumab (NCT03829436). TPST-1120 treated patients with PR demonstrated fatty acid oxidation perturbations and immune gene expression changes as potential biomarkers of clinical benefit. Increased frequencies of responding patients bearing PI3K pathway or IDH mutations may reveal populations likely to benefit from treatment with TPST-1120. 1.
    Clinical • PD(L)-1 Biomarker • IO biomarker
    |
    PTEN (Phosphatase and tensin homolog) • TIGIT (T Cell Immunoreceptor With Ig And ITIM Domains 2) • PVR (PVR Cell Adhesion Molecule) • APOE (Apolipoprotein E) • PPARA (Peroxisome Proliferator Activated Receptor Alpha)
    |
    PTEN mutation
    |
    PredicineCARE™ • nCounter® PanCancer Immune Profiling Panel
    |
    Opdivo (nivolumab) • amezalpat (TPST-1120)
    almost3years
    A Study Evaluating the Efficacy and Safety of Multiple Immunotherapy-Based Treatment Combinations in Patients With Advanced Liver Cancers (Morpheus-Liver) (clinicaltrials.gov)
    P1/2, N=320, Recruiting, Hoffmann-La Roche | Trial completion date: Jul 2025 --> Dec 2025 | Trial primary completion date: Jul 2025 --> Dec 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    PD-L1 (Programmed death ligand 1)
    |
    Avastin (bevacizumab) • Tecentriq (atezolizumab) • amezalpat (TPST-1120) • Actemra IV (tocilizumab) • tiragolumab (RG6058) • muzastotug (ADG126) • tobemstomig (RG6139)
    3years
    Pharmacodynamic and predictive biomarkers associated with response in cancer patients treated with TPST-1120: a first-in-class, small molecule antagonist of Peroxisome-Proliferator Activated Receptor-Alpha (SITC 2022)
    Trial Registration TPST-1120 as Monotherapy and in Combination With Nivolumab in Subjects With Advanced Cancers (NCT03829436). Patients with PR demonstrated gene expression changes that implicate immune activation and alleviation of immune suppression as potential biomarkers of clinical benefit. Increased frequencies of responding patients bearing PI3K pathway or IDH mutations may reveal populations likely to benefit from treatment with TPST-1120.
    Late-breaking abstract • PK/PD data • Clinical • PD(L)-1 Biomarker • IO biomarker
    |
    PTEN (Phosphatase and tensin homolog) • TIGIT (T Cell Immunoreceptor With Ig And ITIM Domains 2) • TNFRSF1A (TNF Receptor Superfamily Member 1A) • PVR (PVR Cell Adhesion Molecule) • FCGR2A (Fc fragment of IgG receptor IIa) • APOE (Apolipoprotein E) • ITGAX (Integrin Subunit Alpha X) • NCF4 (Neutrophil Cytosolic Factor 4) • PPARA (Peroxisome Proliferator Activated Receptor Alpha)
    |
    PTEN mutation
    |
    PredicineCARE™ • nCounter® PanCancer Immune Profiling Panel
    |
    Opdivo (nivolumab) • amezalpat (TPST-1120)
    3years
    A Study Evaluating the Efficacy and Safety of Multiple Immunotherapy-Based Treatment Combinations in Patients With Advanced Liver Cancers (Morpheus-Liver) (clinicaltrials.gov)
    P1/2, N=320, Recruiting, Hoffmann-La Roche | Trial completion date: Dec 2024 --> Jul 2025 | Trial primary completion date: Dec 2024 --> Jul 2025
    Trial completion date • Trial primary completion date
    |
    PD-L1 (Programmed death ligand 1)
    |
    Avastin (bevacizumab) • Tecentriq (atezolizumab) • amezalpat (TPST-1120) • Actemra IV (tocilizumab) • tiragolumab (RG6058) • tobemstomig (RG6139)