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    DRUG CLASS:

    cIAP1 antagonist

    Related drugs:
    13d
    Acteoside inhibits the progression of squamous cell carcinoma by regulating the TWEAK/cIAP1/NF-κB signaling axis and secretion of IL-6, IL-8 and VEGF. (PubMed, Int Immunopharmacol)
    ACT modulates the TWEAK/cIAP1/NF-κB signaling axis, downregulates the expression of key pathway proteins at both the protein and mRNA levels, antagonizes LPS-induced pathway activation, and reduces the secretion of IL-6, IL-8, and VEGF, thereby inhibiting SCC growth and progression.
    Journal
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    IL6 (Interleukin 6) • CXCL8 (Chemokine (C-X-C motif) ligand 8) • RIPK1 (Receptor Interacting Serine/Threonine Kinase 1)
    3ms
    ASTX660-01: Phase 1-2 Study of ASTX660 in Subjects With Advanced Solid Tumors and Lymphomas (clinicaltrials.gov)
    P1/2, N=253, Active, not recruiting, Taiho Oncology, Inc. | Trial completion date: Dec 2025 --> Dec 2027
    Trial completion date
    |
    tolinapant (ASTX660)
    4ms
    A Phase I/II Study of ASTX660 in Patients With Relapsed or Refractory T-cell Lymphoma (clinicaltrials.gov)
    P1/2, N=8, Terminated, Otsuka Pharmaceutical Co., Ltd. | N=61 --> 8
    Enrollment change
    |
    tolinapant (ASTX660)
    4ms
    ASTX660-03: A Study of Tolinapant in Combination With Oral Decitabine/Cedazuridine and Oral Decitabine/Cedazuridine Alone in Participants With Relapsed/Refractory Peripheral T-cell Lymphoma (R/R PTCL) (clinicaltrials.gov)
    P1, N=33, Active, not recruiting, Taiho Oncology, Inc. | Phase classification: P1/2 --> P1 | Trial completion date: Dec 2026 --> Mar 2026
    Phase classification • Trial completion date
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    Inqovi (decitabine/cedazuridine) • tolinapant (ASTX660)
    5ms
    Tolinapant and Radiation for Cisplatin-Ineligible, Previously Untreated, Locally Advanced Head and Neck Cancer (clinicaltrials.gov)
    P1, N=10, Active, not recruiting, Emory University | Trial completion date: Oct 2025 --> Jul 2026
    Trial completion date
    |
    tolinapant (ASTX660)
    9ms
    Differential RELA and GR recruitment to the BIRC3/BIRC2 locus: Molecular insight as to combinatorial regulation by proinflammatory cytokines and glucocorticoid. (PubMed, Mol Pharmacol)
    IL-1β-plus-budesonide also recruited RELA to multiple GBRs, whereas GR was recruited to the main IL-1β-induced RBR (R4), effects that correlated with positive IL-1β/glucocorticoid transcriptional cooperativity or additivity...Cytokine-plus-glucocorticoid cotreatment revealed positive cooperative and additive interactions between GR and RELA, whereas DNA regions binding only one factor showed reduced effects on binding and transcription. These region-specific outcomes, combined with DNA looping between regulatory regions, provides insight as to how factors at multiple DNA regions may integrate their outputs to produce combinatorial regulation of apoptotic/antiapoptotic genes.
    Journal
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    TNFA (Tumor Necrosis Factor-Alpha) • BIRC3 (Baculoviral IAP repeat containing 3) • BIRC2 (Baculoviral IAP Repeat Containing 2) • CFLAR (CASP8 and FADD-like apoptosis regulator) • IL1B (Interleukin 1, beta) • RELA (RELA Proto-Oncogene)
    1year
    Early-phase trial of IAP antagonist tolinapant and definitive radiation in cisplatin-ineligible patients with advanced head and neck cancer. (PubMed, Clin Cancer Res)
    Tolinapant + RT is well tolerated and induced proliferation of activated T cells in a subset of patients. Larger prospective studies are needed to better assess efficacy.
    Journal
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    CD8 (cluster of differentiation 8)
    |
    tolinapant (ASTX660)
    1year
    Tolinapant and Radiation for Cisplatin-Ineligible, Previously Untreated, Locally Advanced Head and Neck Cancer (clinicaltrials.gov)
    P1, N=10, Active, not recruiting, Emory University | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    tolinapant (ASTX660)
    over1year
    ASTX660-03: A Study of Tolinapant in Combination With Oral Decitabine/Cedazuridine and Oral Decitabine/Cedazuridine Alone in Participants With Relapsed/Refractory Peripheral T-cell Lymphoma (R/R PTCL) (clinicaltrials.gov)
    P1/2, N=33, Active, not recruiting, Taiho Oncology, Inc. | N=132 --> 33 | Trial primary completion date: Dec 2025 --> Dec 2024
    Enrollment change • Trial primary completion date
    |
    Inqovi (decitabine/cedazuridine) • tolinapant (ASTX660)
    over1year
    Testing the Addition of an Investigational Anti-Cancer Drug, ASTX660 (Tolinapant), to a Usual Chemotherapy Treatment (Eribulin) for Treatment of Advanced Triple Negative Breast Cancer (clinicaltrials.gov)
    P1, N=42, Recruiting, National Cancer Institute (NCI) | Suspended --> Recruiting
    Enrollment open
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    RIPK1 (Receptor Interacting Serine/Threonine Kinase 1)
    |
    eribulin mesylate • tolinapant (ASTX660)
    over1year
    The IAP antagonist tolinapant enhances the anti-tumor activity of cell therapies. (PubMed, Eur J Pharmacol)
    Our study suggests that the combination of tolinapant improves the efficacy of cell-based cancer therapies by inducing both cancer cell death and CAR-T cell proliferation. This combination therapy may overcome the current limitations of cell-based therapies and enhance their anti-cancer effect.
    Journal
    |
    TNFA (Tumor Necrosis Factor-Alpha)
    |
    tolinapant (ASTX660)
    over1year
    Testing the Addition of an Investigational Anti-Cancer Drug, ASTX660 (Tolinapant), to a Usual Chemotherapy Treatment (Eribulin) for Treatment of Advanced Triple Negative Breast Cancer (clinicaltrials.gov)
    P1, N=42, Suspended, National Cancer Institute (NCI) | Recruiting --> Suspended
    Trial suspension
    |
    RIPK1 (Receptor Interacting Serine/Threonine Kinase 1)
    |
    eribulin mesylate • tolinapant (ASTX660)