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Year Number of Results
2016 9
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2019 7
2020 3
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2023 6
2024 2

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42 results

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Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction.
Yin M, Guo Y, Hu R, Cai WL, Li Y, Pei S, Sun H, Peng C, Li J, Ye R, Yang Q, Wang N, Tao Y, Chen X, Yan Q. Yin M, et al. Nat Commun. 2020 Apr 14;11(1):1833. doi: 10.1038/s41467-020-15290-0. Nat Commun. 2020. PMID: 32286255 Free PMC article.
Here we report the discovery and characterization of NHWD-870, a BET inhibitor that is more potent than three major clinical stage BET inhibitors BMS-986158, OTX-015, and GSK-525762. NHWD-870 causes tumor shrinkage or significantly suppresses tumor growth in nine xe …
Here we report the discovery and characterization of NHWD-870, a BET inhibitor that is more potent than three major clinical stage BET inhib …
Insights into the cellular pharmacological properties of the BET-inhibitor OTX015/MK-8628 (birabresib), alone and in combination, in leukemia models.
Astorgues-Xerri L, Vázquez R, Odore E, Rezai K, Kahatt C, Mackenzie S, Bekradda M, Coudé MM, Dombret H, Gardin C, Lokiec F, Raymond E, Noel K, Cvitkovic E, Herait P, Bertoni F, Riveiro ME. Astorgues-Xerri L, et al. Leuk Lymphoma. 2019 Dec;60(12):3067-3070. doi: 10.1080/10428194.2019.1617860. Epub 2019 Jun 17. Leuk Lymphoma. 2019. PMID: 31204545 No abstract available.
From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors.
Koravovic M, Mayasundari A, Tasic G, Keramatnia F, Stachowski TR, Cui H, Chai SC, Jonchere B, Yang L, Li Y, Fu X, Hiltenbrand R, Paul L, Mishra V, Klco JM, Roussel MF, Pomerantz WC, Fischer M, Rankovic Z, Savic V. Koravovic M, et al. Eur J Med Chem. 2023 May 5;251:115246. doi: 10.1016/j.ejmech.2023.115246. Epub 2023 Mar 4. Eur J Med Chem. 2023. PMID: 36898329
This effort led to the discovery of potent BET inhibitors displaying overall improved profiles when compared to JQ1 and birabresib. A thiadiazole derived 1q (SJ1461) displayed excellent BRD4 and BRD2 affinity and high potency in the panel of acute leukaemia and medulloblas …
This effort led to the discovery of potent BET inhibitors displaying overall improved profiles when compared to JQ1 and birabresib. A …
Synergistic activity of BET inhibitor MK-8628 and PLK inhibitor Volasertib in preclinical models of medulloblastoma.
Han Y, Lindner S, Bei Y, Garcia HD, Timme N, Althoff K, Odersky A, Schramm A, Lissat A, Künkele A, Deubzer HE, Eggert A, Schulte JH, Henssen AG. Han Y, et al. Cancer Lett. 2019 Mar 31;445:24-33. doi: 10.1016/j.canlet.2018.12.012. Epub 2019 Jan 4. Cancer Lett. 2019. PMID: 30611741
We here assessed the therapeutic efficacy of the orally bioavailable BRD4 inhibitor, MK-8628, in preclinical models of medulloblastoma. MK-8628 showed therapeutic efficacy against in vitro and in vivo models of MYC-amplified medulloblastoma by inducing …
We here assessed the therapeutic efficacy of the orally bioavailable BRD4 inhibitor, MK-8628, in preclinical models of medullo …
BET Bromodomain Inhibition Suppresses Human T Cell Function.
Georgiev P, Wang Y, Muise ES, Bandi ML, Blumenschein W, Sathe M, Pinheiro EM, Shumway SD. Georgiev P, et al. Immunohorizons. 2019 Jul 11;3(7):294-305. doi: 10.4049/immunohorizons.1900037. Immunohorizons. 2019. PMID: 31356159 Free article.
MK-8628 reduces the expression of canonical transcripts directing the proliferation, activation, and effector function of T lymphocytes. ...This antiproliferative phenotype partially results from T lymphocyte apoptosis, which is exacerbated by MK-8628. …
MK-8628 reduces the expression of canonical transcripts directing the proliferation, activation, and effector function of T ly …
OTX015 (MK-8628), a novel BET inhibitor, displays in vitro and in vivo antitumor effects alone and in combination with conventional therapies in glioblastoma models.
Berenguer-Daizé C, Astorgues-Xerri L, Odore E, Cayol M, Cvitkovic E, Noel K, Bekradda M, MacKenzie S, Rezai K, Lokiec F, Riveiro ME, Ouafik L. Berenguer-Daizé C, et al. Int J Cancer. 2016 Nov 1;139(9):2047-55. doi: 10.1002/ijc.30256. Epub 2016 Jul 30. Int J Cancer. 2016. PMID: 27388964 Free article.
BRD2 and BRD4, members of the BET family, are significantly increased in glioblastoma multiforme (GBM), the most common primary adult brain cancer. OTX015 (MK-8628), a novel BRD2/3/4 inhibitor, is under evaluation in dose-finding studies in solid tumors, including G …
BRD2 and BRD4, members of the BET family, are significantly increased in glioblastoma multiforme (GBM), the most common primary adult brain …
Metabolic rewiring in MYC-driven medulloblastoma by BET-bromodomain inhibition.
Graziani V, Garcia AR, Alcolado LS, Le Guennec A, Henriksson MA, Conte MR. Graziani V, et al. Sci Rep. 2023 Jan 23;13(1):1273. doi: 10.1038/s41598-023-27375-z. Sci Rep. 2023. PMID: 36690651 Free PMC article.
To this end, we employed an NMR-based metabolomics approach applied to the MYC-driven MB D283 and D458 cell lines before and after the treatment with the BETi OTX-015. We found that OTX-015 triggers a metabolic shift in both cell lines resulting in inc …
To this end, we employed an NMR-based metabolomics approach applied to the MYC-driven MB D283 and D458 cell lines before and after the treat …
Phase Ib Trial With Birabresib, a Small-Molecule Inhibitor of Bromodomain and Extraterminal Proteins, in Patients With Selected Advanced Solid Tumors.
Lewin J, Soria JC, Stathis A, Delord JP, Peters S, Awada A, Aftimos PG, Bekradda M, Rezai K, Zeng Z, Hussain A, Perez S, Siu LL, Massard C. Lewin J, et al. J Clin Oncol. 2018 Oct 20;36(30):3007-3014. doi: 10.1200/JCO.2018.78.2292. Epub 2018 May 7. J Clin Oncol. 2018. PMID: 29733771 Clinical Trial.
PURPOSE: Birabresib (MK-8628/OTX015) is a first-in-class bromodomain inhibitor with activity in select hematologic tumors. ...Pharmacokinetic analysis indicated a dose-proportional increase in birabresib exposure and rapid absorption. CONCLUSION: The r …
PURPOSE: Birabresib (MK-8628/OTX015) is a first-in-class bromodomain inhibitor with activity in select hematologic tumo …
OTX015 (MK-8628), a novel BET inhibitor, exhibits antitumor activity in non-small cell and small cell lung cancer models harboring different oncogenic mutations.
Riveiro ME, Astorgues-Xerri L, Vazquez R, Frapolli R, Kwee I, Rinaldi A, Odore E, Rezai K, Bekradda M, Inghirami G, D'Incalci M, Noel K, Cvitkovic E, Raymond E, Bertoni F. Riveiro ME, et al. Oncotarget. 2016 Dec 20;7(51):84675-84687. doi: 10.18632/oncotarget.13181. Oncotarget. 2016. PMID: 27835869 Free PMC article.
Inhibitors targeting epigenetic control points of oncogenes offer a potential mean of blocking tumor progression in small cell and non-small cell lung carcinomas (SCLC, NSCLC). OTX015 (MK-8628) is a BET inhibitor selectively blocking BRD2/3/4. OTX015 was evaluated i …
Inhibitors targeting epigenetic control points of oncogenes offer a potential mean of blocking tumor progression in small cell and non-small …
42 results