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Changing for the Better: Discovery of the Highly Potent and Selective CDK9 Inhibitor VIP152 Suitable for Once Weekly Intravenous Dosing for the Treatment of Cancer.
Lücking U, Kosemund D, Böhnke N, Lienau P, Siemeister G, Denner K, Bohlmann R, Briem H, Terebesi I, Bömer U, Schäfer M, Ince S, Mumberg D, Scholz A, Izumi R, Hwang S, von Nussbaum F. Lücking U, et al. Among authors: izumi r. J Med Chem. 2021 Aug 12;64(15):11651-11674. doi: 10.1021/acs.jmedchem.1c01000. Epub 2021 Jul 15. J Med Chem. 2021. PMID: 34264057
First-in-Human Dose-Escalation Study of Cyclin-Dependent Kinase 9 Inhibitor VIP152 in Patients with Advanced Malignancies Shows Early Signs of Clinical Efficacy.
Diamond JR, Boni V, Lim E, Nowakowski G, Cordoba R, Morillo D, Valencia R, Genvresse I, Merz C, Boix O, Frigault MM, Greer JM, Hamdy AM, Huang X, Izumi R, Wong H, Moreno V. Diamond JR, et al. Among authors: izumi r. Clin Cancer Res. 2022 Apr 1;28(7):1285-1293. doi: 10.1158/1078-0432.CCR-21-3617. Clin Cancer Res. 2022. PMID: 35046056 Clinical Trial.
VIP152 is a selective CDK9 inhibitor with pre-clinical in vitro and in vivo efficacy in chronic lymphocytic leukemia.
Sher S, Whipp E, Walker J, Zhang P, Beaver L, Williams K, Orwick S, Ravikrishnan J, Walker B, Perry E, Gregory C, Purcell M, Pan A, Yan P, Alinari L, Johnson AJ, Frigault MM, Greer JM, Hamdy A, Izumi R, Mo X, Sampath D, Woyach J, Blachly J, Byrd JC, Lapalombella R. Sher S, et al. Among authors: izumi r. Leukemia. 2023 Feb;37(2):326-338. doi: 10.1038/s41375-022-01758-z. Epub 2022 Nov 14. Leukemia. 2023. PMID: 36376377 Free PMC article.
Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile.
Barf T, Covey T, Izumi R, van de Kar B, Gulrajani M, van Lith B, van Hoek M, de Zwart E, Mittag D, Demont D, Verkaik S, Krantz F, Pearson PG, Ulrich R, Kaptein A. Barf T, et al. Among authors: izumi r. J Pharmacol Exp Ther. 2017 Nov;363(2):240-252. doi: 10.1124/jpet.117.242909. Epub 2017 Sep 7. J Pharmacol Exp Ther. 2017. PMID: 28882879
Discovery of VIP236, an αvβ3-Targeted Small-Molecule-Drug Conjugate with Neutrophil Elastase-Mediated Activation of 7-Ethyl Camptothecin Payload for Treatment of Solid Tumors.
Lerchen HG, Stelte-Ludwig B, Heroult M, Zubov D, Gericke KM, Wong H, Frigault MM, Johnson AJ, Izumi R, Hamdy A. Lerchen HG, et al. Among authors: izumi r. Cancers (Basel). 2023 Sep 1;15(17):4381. doi: 10.3390/cancers15174381. Cancers (Basel). 2023. PMID: 37686656 Free PMC article.
Neutrophil elastase as a versatile cleavage enzyme for activation of αvβ3 integrin-targeted small molecule drug conjugates with different payload classes in the tumor microenvironment.
Rebstock AS, Wiedmann M, Stelte-Ludwig B, Wong H, Johnson AJ, Izumi R, Hamdy A, Lerchen HG. Rebstock AS, et al. Among authors: izumi r. Front Pharmacol. 2024 Mar 1;15:1358393. doi: 10.3389/fphar.2024.1358393. eCollection 2024. Front Pharmacol. 2024. PMID: 38495100 Free PMC article.
The Bruton Tyrosine Kinase (BTK) Inhibitor Acalabrutinib Demonstrates Potent On-Target Effects and Efficacy in Two Mouse Models of Chronic Lymphocytic Leukemia.
Herman SEM, Montraveta A, Niemann CU, Mora-Jensen H, Gulrajani M, Krantz F, Mantel R, Smith LL, McClanahan F, Harrington BK, Colomer D, Covey T, Byrd JC, Izumi R, Kaptein A, Ulrich R, Johnson AJ, Lannutti BJ, Wiestner A, Woyach JA. Herman SEM, et al. Among authors: izumi r. Clin Cancer Res. 2017 Jun 1;23(11):2831-2841. doi: 10.1158/1078-0432.CCR-16-0463. Epub 2016 Nov 30. Clin Cancer Res. 2017. PMID: 27903679 Free PMC article.
Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia.
Byrd JC, Harrington B, O'Brien S, Jones JA, Schuh A, Devereux S, Chaves J, Wierda WG, Awan FT, Brown JR, Hillmen P, Stephens DM, Ghia P, Barrientos JC, Pagel JM, Woyach J, Johnson D, Huang J, Wang X, Kaptein A, Lannutti BJ, Covey T, Fardis M, McGreivy J, Hamdy A, Rothbaum W, Izumi R, Diacovo TG, Johnson AJ, Furman RR. Byrd JC, et al. Among authors: izumi r. N Engl J Med. 2016 Jan 28;374(4):323-32. doi: 10.1056/NEJMoa1509981. Epub 2015 Dec 7. N Engl J Med. 2016. PMID: 26641137 Free PMC article. Clinical Trial.
355 results