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    DRUG CLASS:

    ERN1 inhibitor

    Related drugs:
    3ms
    The Role of Endoplasmic Reticulum Stress and Unfolded Protein Response in Gynecological Cancers: A Narrative Review. (PubMed, Cureus)
    Therapeutically, IRE1 RNase inhibitors (e.g., MKC-8866, B-I09), PERK/EIF2AK3 pathway modulators, protein-disulfide isomerase inhibition, and agents that trigger irrecoverable ER stress show preclinical efficacy, including synergy with platinum, poly (ADP-ribose) polymerase (PARP) inhibitors, HDAC6 blockers, and PD-1 inhibitors...Thus, ER-stress/UPR signaling is a convergent, targetable axis in gynecologic cancers. Priorities include validating UPR-based prognostic signatures, defining context-specific vulnerabilities (e.g., genotype-informed IRE1/XBP1 dependence), and executing biomarker-driven clinical trials that combine UPR-targeted agents with standard chemotherapy, PARP inhibition, and immunotherapy to overcome resistance and improve patient outcomes.
    Review • Journal • PARP Biomarker • PD(L)-1 Biomarker • IO biomarker
    |
    HSPA5 (Heat Shock Protein Family A (Hsp70) Member 5) • ATF4 (Activating Transcription Factor 4) • ATF6 (Activating Transcription Factor 6) • ERN1 (Endoplasmic Reticulum To Nucleus Signaling 1) • XBP1 (X-box-binding protein 1) • EIF2AK3 (Eukaryotic Translation Initiation Factor 2 Alpha Kinase 3)
    8ms
    Evaluation of Oral ORIN1001 in Subjects With Idiopathic Pulmonary Fibrosis (IPF) (clinicaltrials.gov)
    P1, N=24, Suspended, Orinove, Inc. | Trial completion date: Dec 2024 --> Dec 2025 | Trial primary completion date: Dec 2024 --> Dec 2025
    Trial completion date • Trial primary completion date
    |
    ORIN1001
    8ms
    ORIN1001-C1: Treatment of Patients With Advanced Solid Tumors With Oral Agent ORIN1001 and in Combination With Standard of Care. (clinicaltrials.gov)
    P1/2, N=150, Completed, Orinove, Inc. | Trial completion date: Jan 2023 --> Jan 2025
    Trial completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor) • ERN1 (Endoplasmic Reticulum To Nucleus Signaling 1)
    |
    HER-2 negative
    |
    ORIN1001
    11ms
    The transcription factor XBP1 regulates mitochondrial remodel and autophagy in spontaneous abortion. (PubMed, Int Immunopharmacol)
    XBP1s inhibition restored mitochondrial homeostasis and promoted autophagy by modulating the TRAF6/mTORC2 axis under ERS conditions, providing novel mechanistic insights into SA pathogenesis and potential therapeutic targets.
    Journal
    |
    IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL18 (Interleukin 18) • IL1B (Interleukin 1, beta) • XBP1 (X-box-binding protein 1) • TRAF6 (TNF Receptor Associated Factor 6)
    |
    STF-083010 • chloroquine phosphate
    1year
    ORIN1001 in Patients with Advanced Solid Tumors and Relapsed Refractory Metastatic Breast Cancer (clinicaltrials.gov)
    P1/2, N=58, Completed, Orinove, Inc. | Active, not recruiting --> Completed | N=150 --> 58
    Trial completion • Enrollment change
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    HER-2 negative
    |
    albumin-bound paclitaxel • ORIN1001
    1year
    Evaluation of Oral ORIN1001 in Subjects with Idiopathic Pulmonary Fibrosis (IPF) (clinicaltrials.gov)
    P1, N=24, Suspended, Orinove, Inc. | Active, not recruiting --> Suspended
    Trial suspension
    |
    IL6 (Interleukin 6)
    |
    ORIN1001
    1year
    ORIN1001-C1: Treatment of Patients with Advanced Solid Tumors with Oral Agent ORIN1001 and in Combination with Standard of Care. (clinicaltrials.gov)
    P1/2, N=150, Completed, Orinove, Inc. | Active, not recruiting --> Completed | N=350 --> 150
    Trial completion • Enrollment change
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor) • ERN1 (Endoplasmic Reticulum To Nucleus Signaling 1)
    |
    HER-2 negative
    |
    ORIN1001
    1year
    ORIN1001-C1: Treatment of Patients with Advanced Solid Tumors with Oral Agent ORIN1001 and in Combination with Standard of Care. (clinicaltrials.gov)
    P1/2, N=150, Completed, Orinove, Inc. | Active, not recruiting --> Completed | N=350 --> 150
    Trial completion • Enrollment change
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor) • ERN1 (Endoplasmic Reticulum To Nucleus Signaling 1)
    |
    HER-2 negative
    |
    ORIN1001
    1year
    Evaluation of Oral ORIN1001 in Subjects with Idiopathic Pulmonary Fibrosis (IPF) (clinicaltrials.gov)
    P1, N=24, Suspended, Orinove, Inc. | Active, not recruiting --> Suspended
    Trial suspension
    |
    IL6 (Interleukin 6)
    |
    ORIN1001
    almost2years
    Population pharmacokinetic model for oral ORIN1001 in Chinese patients with advanced solid tumors. (PubMed, Front Pharmacol)
    The necessity of dose adjustments based on these two covariates remains to be validated in a larger population. The first PopPK model of ORIN1001 was successfully constructed, which may provide some important references for future research.
    PK/PD data • Journal • Metastases
    |
    ERN1 (Endoplasmic Reticulum To Nucleus Signaling 1) • XBP1 (X-box-binding protein 1)
    |
    ORIN1001
    almost2years
    ORIN1001 in Patients With Advanced Solid Tumors and Relapsed Refractory Metastatic Breast Cancer (clinicaltrials.gov)
    P1/2, N=150, Active, not recruiting, Orinove, Inc. | Trial completion date: Dec 2023 --> Dec 2024 | Trial primary completion date: Jan 2023 --> Jan 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    HER-2 negative
    |
    albumin-bound paclitaxel • ORIN1001
    almost2years
    ORIN1001-C1: Treatment of Patients With Advanced Solid Tumors With Oral Agent ORIN1001 and in Combination With Standard of Care. (clinicaltrials.gov)
    P1/2, N=350, Active, not recruiting, Orinove, Inc. | Trial completion date: Dec 2023 --> Dec 2024 | Trial primary completion date: Dec 2023 --> Dec 2024
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor) • ERN1 (Endoplasmic Reticulum To Nucleus Signaling 1)
    |
    HER-2 negative
    |
    ORIN1001