ArticleMolecular cancer therapeutics2020
An Orally Available Tubulin Inhibitor, VERU-111, Suppresses Triple-Negative Breast Cancer Tumor Growth and Metastasis and Bypasses Taxane Resistance.
Article in Molecular cancer therapeutics, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed.
- A Phase Ib/II Study of Sabizabulin, a Novel Oral Cytoskeleton Disruptor, in Men with Metastatic Castration-resistant Prostate Cancer with Progression on an Androgen Receptor-targeting Agent.Clinical cancer research : an official journal of the American Association for Cancer Research · 2022Trial
- Therapeutic potential of colchicine-binding site inhibitors in breast cancer brain metastasis.Cancer letters · 2026Review
- Decoding triple negative breast cancer bone metastasis: from 3D bioprinted models to clinical translation.Journal of nanobiotechnology · 2026Review
- The secreted protein SPARCL1 suppresses tumor progression in papillary thyroid carcinoma via SLC3A2-mediated ferroptosis.Endocrine-related cancer · 2026Article
- A novel colchicine-binding site inhibitor suppresses triple-negative breast cancer growth and metastasis and synergizes with anti-PD-L1 immunotherapy in an immunogenic cancer model.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2026Article
- QW-5-70 targets the colchicine site and demonstrates antitumor activity in P-gp-overexpressing cancer models.Molecular cancer therapeutics · 2026Article
- Discovery of Potent and Brain-Penetrable Tubulin Inhibitors that Effectively Suppress Breast Cancer Brain Metastasis.Molecular cancer therapeutics · 2026Article
- Novel Triazoloquinoxaline-Based Tubulin Polymerization Inhibitor Induces Necroptosis and Significantly Inhibits Metastatic Melanoma Tumor Growth.Journal of medicinal chemistry · 2026Article
- Discovery of New Quinazolinone and Benzimidazole Analogs as Tubulin Polymerization Inhibitors with Potent Anticancer Activities.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Article
- Design and synthesis of novel 4-aryl-2-benzoyl-imidazoles as colchicine binding site inhibitors.European journal of medicinal chemistry · 2025Article
- Quantum chemical modeling, molecular docking, and ADMET evaluation of imidazole phenothiazine hybrids.Scientific reports · 2025Article
- VERU-111, an orally available tubulin inhibitor, suppresses ovarian tumor growth and metastasis.The Journal of pharmacology and experimental therapeutics · 2025Article
- Biological activity of a stable 6-aryl-2-benzoyl-pyridine colchicine-binding site inhibitor, 60c, in metastatic, triple-negative breast cancer.Cancer letters · 2024Article
- Novel Antimitotic Agent SP-1-39 Inhibits Head and Neck Squamous Cell Carcinoma.Journal of dental research · 2024Article
- Recent Advances in Drug Discovery for Triple-Negative Breast Cancer Treatment.Molecules (Basel, Switzerland) · 2023Review
- Antiproliferative and Tubulin-Destabilising Effects of 3-(Prop-1-en-2-yl)azetidin-2-Ones and Related Compounds in MCF-7 and MDA-MB-231 Breast Cancer Cells.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Design, Synthesis, and Biological Evaluation of Pyrimidine Dihydroquinoxalinone Derivatives as Tubulin Colchicine Site-Binding Agents That Displayed Potent Anticancer Activity Both In Vitro and In Vivo.ACS pharmacology & translational science · 2023Article
- SB226, an inhibitor of tubulin polymerization, inhibits paclitaxel-resistant melanoma growth and spontaneous metastasis.Cancer letters · 2023Article
- Sabizabulin, a Potent Orally Bioavailable Colchicine Binding Site Agent, Suppresses HER2+ Breast Cancer and Metastasis.Cancers · 2022Article
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
Triple-negative breast cancer (TNBC) accounts for approximately 15% of breast cancer cases in the United States. TNBC has poorer overall prognosis relative to other molecular subtypes due to rapid onset of drug resistance to conventional chemotherapies and increased risk of visceral metastases. Taxanes like paclitaxel are standard chemotherapies that stabilize microtubules, but their clinical efficacy is often limited by drug resistance and neurotoxicities. We evaluated the preclinical efficacy of a novel, potent, and orally bioavailable tubulin inhibitor, VERU-111, in TNBC models. VERU-111 showed potent cytotoxicity against TNBC cell lines, inducing apoptosis and cell-cycle arrest in a concentration-dependent manner. VERU-111 also efficiently inhibited colony formation, cell migration, and invasion. Orally administered VERU-111 inhibited MDA-MB-231 xenograft growth in a dose-dependent manner, with similar efficacies to paclitaxel, but without acute toxicity. VERU-111 significantly reduced metastases originating from the mammary fat pad into lung, liver, and kidney metastasis in an experimental metastasis model. Moreover, VERU-111, but not paclitaxel, suppressed growth of luciferase-labeled, taxane-resistant, patient-derived metastatic TNBC tumors. In this model, VERU-111 repressed growth of preestablished axillary lymph node metastases and lung, bone, and liver metastases at study endpoint, whereas paclitaxel enhanced liver metastases relative to vehicle controls. Collectively, these studies strongly suggest that VERU-111 is not only a potent inhibitor of aggressive TNBC phenotypes, but it is also efficacious in a taxane-resistant model of metastatic TNBC. Thus, VERU-111 is a promising new generation of tubulin inhibitor for the treatment of TNBC and may be effective in patients who progress on taxanes.Results presented in this study demonstrate the efficacy of VERU-111
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Registered trials
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