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    DRUG CLASS:

    TRAIL R1 agonist

    Related drugs:
    1m
    Trial to Assess the Safety and Antitumor Activity of GEN1057 in Malignant Solid Tumors (clinicaltrials.gov)
    P1, N=45, Recruiting, Genmab | Trial completion date: Jan 2026 --> Feb 2027 | Trial primary completion date: Sep 2025 --> Nov 2026
    Trial completion date • Trial primary completion date • First-in-human
    5ms
    Trial to Assess the Safety and Antitumor Activity of GEN1057 in Malignant Solid Tumors (clinicaltrials.gov)
    P1, N=45, Recruiting, Genmab | Trial completion date: Oct 2026 --> Jan 2026 | Trial primary completion date: Oct 2026 --> Sep 2025
    Trial completion date • Trial primary completion date
    6ms
    Trial to Assess the Safety and Antitumor Activity of GEN1057 in Malignant Solid Tumors (clinicaltrials.gov)
    P1, N=45, Recruiting, Genmab | Trial completion date: Oct 2027 --> Oct 2026 | Trial primary completion date: Oct 2027 --> Oct 2026
    Trial completion date • Trial primary completion date
    7ms
    Study to Determine Recommended Phase 2 Dose of Intravenous (IV) Eftozanermin Alfa in Combination With IV or Subcutaneous (SC) Bortezomib and Oral Dexamethasone Tablet and to Assess Change in Disease Symptoms in Adult Participants With Relapsed or Refractory Multiple Myeloma (clinicaltrials.gov)
    P1, N=4, Terminated, AbbVie | N=40 --> 4 | Active, not recruiting --> Terminated; Strategic considerations
    Enrollment change • Trial termination
    |
    bortezomib • eftozanermin alfa (ABBV-621)
    9ms
    Study to Determine Recommended Phase 2 Dose of Intravenous (IV) Eftozanermin Alfa in Combination With IV or Subcutaneous (SC) Bortezomib and Oral Dexamethasone Tablet and to Assess Change in Disease Symptoms in Adult Participants With Relapsed or Refractory Multiple Myeloma (clinicaltrials.gov)
    P1, N=40, Active, not recruiting, AbbVie | Trial completion date: Jan 2025 --> Jul 2025 | Trial primary completion date: Jan 2025 --> Jul 2025
    Trial completion date • Trial primary completion date
    |
    bortezomib • eftozanermin alfa (ABBV-621)
    over1year
    Study to Determine Recommended Phase 2 Dose of Intravenous (IV) Eftozanermin Alfa in Combination With IV or Subcutaneous (SC) Bortezomib and Oral Dexamethasone Tablet and to Assess Change in Disease Symptoms in Adult Participants With Relapsed or Refractory Multiple Myeloma (clinicaltrials.gov)
    P1, N=40, Active, not recruiting, AbbVie | Trial completion date: Jul 2024 --> Jan 2025 | Trial primary completion date: Jul 2024 --> Jan 2025
    Trial completion date • Trial primary completion date • Combination therapy
    |
    bortezomib • eftozanermin alfa (ABBV-621)
    over1year
    Study to Determine Recommended Phase 2 Dose of Intravenous (IV) Eftozanermin Alfa in Combination With IV or Subcutaneous (SC) Bortezomib and Oral Dexamethasone Tablet and to Assess Change in Disease Symptoms in Adult Participants With Relapsed or Refractory Multiple Myeloma (clinicaltrials.gov)
    P1, N=40, Active, not recruiting, AbbVie | Phase classification: P1b --> P1 | Trial completion date: Oct 2024 --> Jul 2024 | Trial primary completion date: Oct 2024 --> Jul 2024
    Phase classification • Trial completion date • Trial primary completion date • Combination therapy
    |
    bortezomib • eftozanermin alfa (ABBV-621)
    over1year
    Mapatumumab, Cisplatin and Radiotherapy for Advanced Cervical Cancer (clinicaltrials.gov)
    P1/2, N=9, Completed, University Medical Center Groningen | Phase classification: P1b/2 --> P1/2
    Phase classification • Combination therapy • Metastases
    |
    cisplatin • mapatumumab (HGS-ETR1)
    almost2years
    Carboxypeptidase A4 negatively regulates HGS-ETR1/2-induced pyroptosis by forming a positive feedback loop with the AKT signalling pathway. (PubMed, Cell Death Dis)
    Specifically, CPA4 modulates AKT phosphorylation by regulating the expression of the AKT phosphatase PP2A, while inhibition of the AKT signalling pathway leads to a decreased transcription and translation levels of CPA4. Our study reveals a novel mechanism of pyroptosis induced by HGS-ETR1/2, which may provide a crucial foundation for future investigations into cancer immunotherapy.
    Journal • IO biomarker
    |
    AKT1 (V-akt murine thymoma viral oncogene homolog 1) • GSDME (Gasdermin E)
    |
    mapatumumab (HGS-ETR1)
    over2years
    Synergistic antitumor effects of circularly permuted TRAIL with doxorubicin in triple-negative breast cancer. (PubMed, Acta Biochim Biophys Sin (Shanghai))
    Collectively, our findings demonstrate that treatment with CPT in combination with Dox exerts synergistic antitumor effects through activation of the caspase cascade pathway, a mechanism that is partly dependent on the Dox-induced upregulation of death receptor 4 and death receptor 5. Therefore, CPT combined with Dox may be a feasible therapeutic strategy for the management of TNBC.
    Journal • PARP Biomarker
    |
    CASP3 (Caspase 3) • CASP8 (Caspase 8) • TNFRSF10B (TNF Receptor Superfamily Member 10b)
    |
    doxorubicin hydrochloride • CPT
    over2years
    TRAIL-mediated signaling in bladder cancer: realization of clinical efficacy of TRAIL-based therapeutics in medical oncology. (PubMed, Med Oncol)
    Certain clues of scientific evidence have provided encouraging results about efficacy of these agonistic antibodies (lexatumumab and mapatumumab) against bladder cancer cell lines. Therefore, multipronged approaches consisting of natural products, chemotherapeutics, and agonistic antibodies will realistically and mechanistically provide proof-of-concept for the translational potential of these combinatorial strategies in well-designed clinical trials.
    Review • Journal
    |
    lexatumumab (ETR2-ST01) • mapatumumab (HGS-ETR1)
    almost3years
    Synergistic activity of ABT-263 and ONC201/TIC10 against solid tumor cell lines is associated with suppression of anti-apoptotic Mcl-1, BAG3, pAkt, and upregulation of pro-apoptotic Noxa and Bax cleavage during apoptosis. (PubMed, Am J Cancer Res)
    Our data provide evidence for synergy from the combination of ONC201 and ABT-263 against human solid tumor cell lines associated with alterations in cell death and pro-survival mediators. The combination of ONC201 and ABT-263 merits further exploration in vivo and in clinical trials against a variety of solid malignancies.
    Preclinical • Journal • Tumor cell
    |
    MCL1 (Myeloid cell leukemia 1) • BCL2L1 (BCL2-like 1) • ATF4 (Activating Transcription Factor 4)
    |
    navitoclax (ABT 263) • nesuparib (JPI-547) • Modeyso (dordaviprone)