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Identification of side effects of COVID-19 drug candidates on embryogenesis using an integrated zebrafish screening platform.
Ernst A, Piragyte I, Mp AM, Le ND, Grandgirard D, Leib SL, Oates A, Mercader N. Ernst A, et al. Sci Rep. 2023 Oct 9;13(1):17037. doi: 10.1038/s41598-023-43911-3. Sci Rep. 2023. PMID: 37813860 Free PMC article.
Ritonavir and Baricitinib showed reduced heart functionality and Molnupiravir and Baricitinib showed effects on embryo activity. Sabizabulin was highly toxic at concentrations only 5 times higher than C(max) and led to a mean mortality of 20% at C(max). Furthermore, we tes …
Ritonavir and Baricitinib showed reduced heart functionality and Molnupiravir and Baricitinib showed effects on embryo activity. Sabizabu
Oral Sabizabulin for High-Risk, Hospitalized Adults with Covid-19: Interim Analysis.
Barnette KG, Gordon MS, Rodriguez D, Bird TG, Skolnick A, Schnaus M, Skarda PK, Lobo S, Sprinz E, Arabadzhiev G, Kalaydzhiev P, Steiner M. Barnette KG, et al. NEJM Evid. 2022 Sep;1(9):EVIDoa2200145. doi: 10.1056/EVIDoa2200145. Epub 2022 Jul 6. NEJM Evid. 2022. PMID: 38319812
BACKGROUND: Sabizabulin is an oral, novel microtubule disruptor that has dual antiviral and anti-inflammatory activities in preclinical models. ...Sabizabulin superiority was demonstrated by a planned interim analysis for the first 150 randomized patients. ...
BACKGROUND: Sabizabulin is an oral, novel microtubule disruptor that has dual antiviral and anti-inflammatory activities in preclinic …
Optimized synthesis of anti-COVID-19 drugs aided by retrosynthesis software.
Qi W, Zhai D, Song D, Liu C, Yang J, Sun L, Li Y, Li X, Deng W. Qi W, et al. RSC Med Chem. 2023 Mar 31;14(7):1254-1259. doi: 10.1039/d2md00444e. eCollection 2023 Jul 20. RSC Med Chem. 2023. PMID: 37484565 Free PMC article.
We also used the same strategy to optimize the synthesis of sabizabulin. We anticipate that these synthetic routes will contribute to the prevention and treatment of COVID-19....
We also used the same strategy to optimize the synthesis of sabizabulin. We anticipate that these synthetic routes will contribute to …
Sabizabulin, a Potent Orally Bioavailable Colchicine Binding Site Agent, Suppresses HER2+ Breast Cancer and Metastasis.
Krutilina RI, Hartman KL, Oluwalana D, Playa HC, Parke DN, Chen H, Miller DD, Li W, Seagroves TN. Krutilina RI, et al. Cancers (Basel). 2022 Oct 29;14(21):5336. doi: 10.3390/cancers14215336. Cancers (Basel). 2022. PMID: 36358755 Free PMC article.
Herein, we demonstrate the efficacy of sabizabulin in HER2(+) breast cancer. In vitro, sabizabulin inhibits the proliferation of HER2+ breast cancer cell lines with low nanomolar IC(50) values, inhibits clonogenicity, and induces apoptosis in a concentration-depende …
Herein, we demonstrate the efficacy of sabizabulin in HER2(+) breast cancer. In vitro, sabizabulin inhibits the proliferation …
Molecular structure, spectral analysis and chemical activity of sabizabulin: A computational study.
Dhasmana A, Mishra AK, Khoja UB, Mishra S. Dhasmana A, et al. J Mol Graph Model. 2023 Dec;125:108618. doi: 10.1016/j.jmgm.2023.108618. Epub 2023 Aug 30. J Mol Graph Model. 2023. PMID: 37678041
Additionally, we examine Mulliken charges and the Molecular Electrostatic Potential (MEP) plot to comprehend the electronic distribution and chemical activity of sabizabulin. Our findings provide valuable insights into the spectroscopic properties of sabizabulin, hi …
Additionally, we examine Mulliken charges and the Molecular Electrostatic Potential (MEP) plot to comprehend the electronic distribution and …
Antiandrogens for the treatment of COVID-19 patients: A meta-analysis of randomized controlled trials.
Cheema HA, Rehman AU, Elrashedy AA, Mohsin A, Shahid A, Ehsan M, Ayyan M, Ismail H, Almas T. Cheema HA, et al. J Med Virol. 2023 Apr;95(4):e28740. doi: 10.1002/jmv.28740. J Med Virol. 2023. PMID: 37185842
However, on subgroup analysis, only proxalutamide/enzalutamide and sabizabulin were found to significantly reduce mortality (RR 0.22, 95% CI: 0.16-0.30 and RR 0.42, 95% CI: 0.26-0.68, respectively), while aldosterone receptor antagonists and antigonadotropins did not show …
However, on subgroup analysis, only proxalutamide/enzalutamide and sabizabulin were found to significantly reduce mortality (RR 0.22, …
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.
Markowski MC, Tutrone R, Pieczonka C, Barnette KG, Getzenberg RH, Rodriguez D, Steiner MS, Saltzstein DR, Eisenberger MA, Antonarakis ES. Markowski MC, et al. Clin Cancer Res. 2022 Jul 1;28(13):2789-2795. doi: 10.1158/1078-0432.CCR-22-0162. Clin Cancer Res. 2022. PMID: 35416959 Free PMC article. Clinical Trial.
PURPOSE: Sabizabulin, an oral cytoskeleton disruptor, was tested in a phase Ib/II clinical study in men with metastatic castration-resistant prostate cancer (mCRPC). ...These data support the ongoing phase III VERACITY trial of sabizabulin in men with mCRPC....
PURPOSE: Sabizabulin, an oral cytoskeleton disruptor, was tested in a phase Ib/II clinical study in men with metastatic castration-re …