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    DRUG CLASS:

    NRP1 modulator

    Related drugs:
    3ms
    A Study of CEND-1 With Chemotherapy as First-Line Therapy in Patients With Pancreatic Ductal Adenocarcinoma (clinicaltrials.gov)
    P2, N=120, Not yet recruiting, Qilu Pharmaceutical Co., Ltd.
    New P2 trial • Combination therapy • Metastases
    |
    gemcitabine • albumin-bound paclitaxel • certepetide (LSTA1)
    4ms
    A Randomised, double-blinded phase II study of gemcitabine and nab-paclitaxel with CEND-1 or placebo in patients with untreated metastatic pancreatic ductal adenocarcinoma (ACTRN12621001290886)
    P2, N=155, Active, not recruiting, Australasian Gastro-Intestinal Cancer Trials Group | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    |
    gemcitabine • albumin-bound paclitaxel • certepetide (LSTA1)
    5ms
    BOLSTER: A Study of LSTA1 When Added to Standard of Care Versus Standard of Care Alone in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P2, N=80, Recruiting, Lisata Therapeutics, Inc. | N=120 --> 80
    Enrollment change • Metastases
    |
    cisplatin • Imfinzi (durvalumab) • gemcitabine • paclitaxel • certepetide (LSTA1)
    6ms
    BOLSTER: A Study of LSTA1 When Added to Standard of Care Versus Standard of Care Alone in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P2, N=120, Recruiting, Lisata Therapeutics, Inc.
    Trial completion date • Trial primary completion date • Metastases
    |
    cisplatin • Imfinzi (durvalumab) • gemcitabine • paclitaxel • docetaxel • certepetide (LSTA1)
    6ms
    BOLSTER: A Study of LSTA1 When Added to Standard of Care Versus Standard of Care Alone in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P2, N=120, Recruiting, Lisata Therapeutics, Inc. | Phase classification: P2a --> P2
    Phase classification • Metastases
    |
    cisplatin • Imfinzi (durvalumab) • gemcitabine • paclitaxel • docetaxel • certepetide (LSTA1)
    almost1year
    BOLSTER: A Study of LSTA1 When Added to Standard of Care Versus Standard of Care Alone in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P2a, N=120, Recruiting, Lisata Therapeutics, Inc. | Trial completion date: May 2026 --> Dec 2025 | Trial primary completion date: May 2026 --> Dec 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    cisplatin • Imfinzi (durvalumab) • gemcitabine • paclitaxel • docetaxel • certepetide (LSTA1)
    1year
    A phase Ib/II, open-label, multicenter study to evaluate the safety, efficacy, and pharmacokinetics/pharmacodynamics of αvβ3/5 integrin and neuropilin-1 targeting peptide LSTA1 in patients with metastatic pancreatic ductal adenocarcinoma. (ASCO 2023)
    Here we report the safety and efficacy results from a Phase Ib/II, multicenter study of LSTA1 plus (SoC) gemcitabine and locally produced nab-paclitaxel in patients with metastatic pancreatic ductal adenocarcinoma (mPDAC). LSTA1 combined with SoC showed an acceptable safety profile in patients with mPDAC. Compared with historical SoC data, LSTA1 plus SoC numerically improved ORR and PFS. Higher NRP1 expression is associated with better ORR and PFS, suggesting NRP1 may be a potential biomarker of LSTA1 plus chemotherapy for mPDAC treatment.
    Clinical • P1/2 data • PK/PD data • Metastases
    |
    NRP1 (Neuropilin 1)
    |
    gemcitabine • albumin-bound paclitaxel • certepetide (LSTA1)
    over1year
    Hepatocellular carcinoma cells loss lenvatinib efficacy in vitro through autophagy and hypoxia response-derived neuropilin-1 degradation. (PubMed, Acta Pharmacol Sin)
    Under hypoxia, HIF-1α directly modulated NRP1 expression; HIF-1α silencing not only enhanced the anticancer effects of combined lenvatinib and hypoxia, but also prevented the loss of effectiveness caused by bafilomycin A1, highlighting the potential role of HIF-1α-derived hypoxia response in the adaptive cellular response to lenvatinib and promoting resistance acquisition by autophagy modulation. Overall, NRP1 may constitute a potential therapeutic target to prevent lenvatinib failure derived from a hypoxia-associated modulation of autophagy in advanced HCC.
    Preclinical • Journal
    |
    HIF1A (Hypoxia inducible factor 1, alpha subunit) • NRP1 (Neuropilin 1)
    |
    HIF1A expression
    |
    Lenvima (lenvatinib)
    over1year
    Neuropilin-1 modulates the 3D invasive properties of glioblastoma stem-like cells. (PubMed, Front Cell Dev Biol)
    From a mechanistic standpoint, this biological effect might rely on the expression of the β3 subunit integrin cell-extracellular matrix adhesive receptor. Our data, therefore, propose a reliable approach to explore invasive properties of patient glioma cells ex vivo and identify NRP1 as a mediator in this malignant process.
    Journal
    |
    NRP1 (Neuropilin 1)
    almost2years
    Preclinical assessment of the pharmacokinetics, disposition, and duration of action of the dual alphav-integrin and neuropilin-1 targeting peptide CEND-1 (ESMO 2022)
    The duration of the tumor-penetrating effect of CEND-1 was evaluated by assessing tumor accumulation of Evans Blue and Doxorubicin in two different models of hepatocellular carcinoma (HCC): TGFα/c-myc-double transgenic mice and HepG2 xenografted mice. Conclusions These results indicate a favourable in vivo PK profile of CEND-1 after intravenous administration and demonstrate a specific and long-lasting tumour homing and tumor penetrability. Therefore, even single injections of CEND-1 may elicit long-lasting tumor PK improvements for co-administered anti-cancer agents.
    PK/PD data • Preclinical
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • NRP1 (Neuropilin 1) • TGFA (Transforming Growth Factor Alpha)
    |
    doxorubicin hydrochloride • certepetide (LSTA1)