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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
Influence of tumour burden on trastuzumab pharmacokinetics in HER2 positive non-metastatic breast cancer.
Bernadou G, Campone M, Merlin JL, Gouilleux-Gruart V, Bachelot T, Lokiec F, Rezai K, Arnedos M, Diéras V, Jimenez M, Paintaud G, Ternant D. Bernadou G, et al. Br J Clin Pharmacol. 2016 May;81(5):941-8. doi: 10.1111/bcp.12875. Epub 2016 Mar 7. Br J Clin Pharmacol. 2016. PMID: 26714164 Free PMC article. Clinical Trial.
Pharmacokinetic modelling of 5-FU production from capecitabine--a population study in 40 adult patients with metastatic cancer.
Urien S, Rezaí K, Lokiec F. Urien S, et al. J Pharmacokinet Pharmacodyn. 2005 Dec;32(5-6):817-33. doi: 10.1007/s10928-005-0018-2. J Pharmacokinet Pharmacodyn. 2005. PMID: 16284918 Clinical Trial.
Capecitabine oral absorption was characterized by a rapid first order input (K(a)=2.1 +/- 0.3 hr(-1)) with a lag time (0.28 +/- 0.11 hr), but related inter-occasion (IOV) and inter-subject (ISV) variabilities for these parameters, 167% and 110%, indicated that this oral ab …
Capecitabine oral absorption was characterized by a rapid first order input (K(a)=2.1 +/- 0.3 hr(-1)) with a lag time (0.28 +/- 0.11 …
A single-dose PK study of onapristone including the effect of food on absorption.
Rezai K, Chassard D, Denot C, Proniuk S, Zukiwski A, Gilles E, Ramos HL, Patat A, Bexon A, Lokiec F. Rezai K, et al. Cancer Chemother Pharmacol. 2015 Jul;76(1):171-7. doi: 10.1007/s00280-015-2754-3. Epub 2015 May 26. Cancer Chemother Pharmacol. 2015. PMID: 26006702 Clinical Trial.
Phase I Population Pharmacokinetic Assessment of the Oral Bromodomain Inhibitor OTX015 in Patients with Haematologic Malignancies.
Odore E, Lokiec F, Cvitkovic E, Bekradda M, Herait P, Bourdel F, Kahatt C, Raffoux E, Stathis A, Thieblemont C, Quesnel B, Cunningham D, Riveiro ME, Rezaï K. Odore E, et al. Clin Pharmacokinet. 2016 Mar;55(3):397-405. doi: 10.1007/s40262-015-0327-6. Clin Pharmacokinet. 2016. PMID: 26341814 Clinical Trial.
The estimated pharmacokinetic parameters were the absorption rate constant (k a) = 0.731 h(-1), V = 71.4 L and CL = 8.47 L·h(-1). ...
The estimated pharmacokinetic parameters were the absorption rate constant (k a) = 0.731 h(-1), V = 71.4 L and CL = 8.47 L·h(-1). ...
BET bromodomain inhibitor birabresib in mantle cell lymphoma: in vivo activity and identification of novel combinations to overcome adaptive resistance.
Tarantelli C, Bernasconi E, Gaudio E, Cascione L, Restelli V, Arribas AJ, Spriano F, Rinaldi A, Mensah AA, Kwee I, Ponzoni M MD, Zucca E, Carrassa L, Riveiro ME, Rezai K, Stathis A, Cvitkovic E, Bertoni F. Tarantelli C, et al. Among authors: rezai k. ESMO Open. 2018 Sep 26;3(6):e000387. doi: 10.1136/esmoopen-2018-000387. eCollection 2018. ESMO Open. 2018. PMID: 30305939 Free PMC article.
The bromodomain inhibitor OTX015 (MK-8628) exerts anti-tumor activity in triple-negative breast cancer models as single agent and in combination with everolimus.
Vázquez R, Riveiro ME, Astorgues-Xerri L, Odore E, Rezai K, Erba E, Panini N, Rinaldi A, Kwee I, Beltrame L, Bekradda M, Cvitkovic E, Bertoni F, Frapolli R, D'Incalci M. Vázquez R, et al. Oncotarget. 2017 Jan 31;8(5):7598-7613. doi: 10.18632/oncotarget.13814. Oncotarget. 2017. PMID: 27935867 Free PMC article.
Bromodomain inhibitor OTX015 (MK-8628) combined with targeted agents shows strong in vivo antitumor activity in lymphoma.
Gaudio E, Tarantelli C, Ponzoni M, Odore E, Rezai K, Bernasconi E, Cascione L, Rinaldi A, Stathis A, Riveiro E, Cvitkovic E, Zucca E, Bertoni F. Gaudio E, et al. Oncotarget. 2016 Sep 6;7(36):58142-58147. doi: 10.18632/oncotarget.10983. Oncotarget. 2016. PMID: 27494885 Free PMC article.
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.
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. Among authors: rezai k. 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.
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