Yokoyama, Yuta et al. published their research in Journal of Clinical Laboratory Analysis in 2022 |CAS: 380843-75-4

The Article related to photodiode dasatinib nilotinib bosutinib ponatinib high performance liquid chromatog, chronic myeloid leukemia, high-performance liquid chromatography, photodiode array detector, tyrosine kinase inhibitor and other aspects.Category: piperazines

On August 31, 2022, Yokoyama, Yuta; Nozawa, Eiji; Morita, Miho; Ishikawa, Emi; Mori, Takehiko; Sakurai, Masatoshi; Kikuchi, Taku; Matsuki, Eri; Yamazaki, Rie; Kataoka, Keisuke; Jibiki, Aya; Kawazoe, Hitoshi; Suzuki, Sayo; Nakamura, Tomonori published an article.Category: piperazines The title of the article was Simultaneous quantification of dasatinib, nilotinib, bosutinib, and ponatinib using high-performance liquid chromatography-Photodiode array detection. And the article contained the following:

Dasatinib, nilotinib, and bosutinib, second-generation tyrosine kinase inhibitors (TKIs), and ponatinib, a third-generation TKI, are approved pharmaceuticals used in the treatment of chronic myeloid leukemia (CML). Although liquid chromatog.-tandem mass spectrometry assays for simultaneous quantification of the four TKIs in human serum have been reported in the literature, a high-performance liquid chromatog. (HPLC) assay that simultaneously quantifies these compounds has not yet been developed. This study aims to establish and validate an efficient HPLC anal. method using a photodiode array (PDA) detector for the simultaneous quantification of the four TKIs. Calibration standards were prepared by serial dilution of serum samples containing the four TKIs, followed by solid-phase extraction The four TKIs were eluted in order within 10 min using a binary HPLC gradient system. The calibration ranges were 2-500 ng/mL for dasatinib, 100-5000 ng/mL for nilotinib, and 10-500 ng/mL for bosutinib and ponatinib. Intra-day and inter-day precision and accuracy values were found to be in accordance with the U. S. Food and Drug Administration guidelines. The recovery rates were 92.9%-96.0%, 80.7%-86.1%, 91.6%-99.0%, and 86.4%-92.6% for dasatinib, nilotinib, bosutinib, and ponatinib, resp. To the best of our knowledge, this is the first report of an HPLC-PDA anal. method that allows efficient simultaneous quantification of the four TKIs in the serum of patients with CML. We believe that the method developed herein can improve the efficiency of therapeutic drug monitoring in patients with CML in clin. practice. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Category: piperazines

The Article related to photodiode dasatinib nilotinib bosutinib ponatinib high performance liquid chromatog, chronic myeloid leukemia, high-performance liquid chromatography, photodiode array detector, tyrosine kinase inhibitor and other aspects.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Robin, J. B. et al. published their research in Annals of Hematology in 2022 |CAS: 380843-75-4

The Article related to chronic myeloid leukemia recurrence tyrosine kinase inhibitor discontinuation france, chronic myeloid leukemia, complete molecular response, molecular recurrence-free remission, tyrosine kinase inhibitor and other aspects.Application of 380843-75-4

On May 31, 2022, Robin, J. B.; Theron, A.; Quittet, P.; Exbrayat, C.; Gaillard, J. B.; Lavabre-Bertrand, T.; David, S.; Saad, A.; Jourdan, E.; Cartron, G. published an article.Application of 380843-75-4 The title of the article was Discontinuation of tyrosine kinase inhibitor in chronic myeloid leukemia: a retrospective cohort in East Occitania. And the article contained the following:

Tyrosine kinase inhibitor (TKI) discontinuation in chronic phase chronic myeloid leukemia (CML) patients has been examined in a real-life setting in the east occitania region of France. We have collected sex, age, prognostic scores, pre-TKI treatment, TKI length and response, relapse data from patients who had stopped TKI in prolonged complete mol. remission (CMR), and analyzed relapse risk factors. Sixty consecutive patients were included from Jan. 2010 to Dec. 2016. Sixteen received pre-TKI treatment. Fifty-three received a first-generation TKI, and seven had a second-generation TKI in first-line therapy. The median TKI time to achieve CMR was 20.5 mo [5-137]. The median TKI length before discontinuation treatment was 73 mo [12-158]. Twenty-two patients (37%) relapsed with a median time to relapse of 6 mo [3-27]. An intermediate or high Sokal score was the only relapse risk factor (HR = 3.32, p < 0.05) associated with relapse after TKI discontinuation. TKI discontinuation was possible without relapse for half of the patients in chronic phase CML. In a real-life cohort, a high-risk Sokal score at diagnosis appears to be an adverse prognosis feature for TKI discontinuation. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Application of 380843-75-4

The Article related to chronic myeloid leukemia recurrence tyrosine kinase inhibitor discontinuation france, chronic myeloid leukemia, complete molecular response, molecular recurrence-free remission, tyrosine kinase inhibitor and other aspects.Application of 380843-75-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Ma, Chen-En et al. published their research in Leukemia Research in 2021 |CAS: 380843-75-4

The Article related to dasatinib nilotinib anticancer agent chronic myeloid leukemia, chronic myeloid leukemia, chronic phase chronic myeloid leukemia, dasatinib, nilotinib, second generation tyrosine kinase inhibitor, switch and other aspects.Computed Properties of 380843-75-4

On December 31, 2021, Ma, Chen-En; Ghosh, Sunita; Leyshon, Catherine; Blosser, Nikki; Dersch-Mills, Deonne; Jupp, Jennifer; Savoie, Lynn; Liew, Elena; Jamani, Kareem published an article.Computed Properties of 380843-75-4 The title of the article was Clinical outcome of chronic myeloid leukemia patients who switch from first-line therapy with a second generation tyrosine kinase inhibitor to an alternative TKI. And the article contained the following:

While second generation tyrosine kinase inhibitors (2GTKIs) are highly effective therapies for chronic myeloid leukemia (CML), a significant minority of patients who initiate a 2GTKI will require a switch to an alternative TKI. The long-term outcomes of those who require a change in therapy after front-line 2GTKI therapy are largely undescribed. Here we describe the clin. outcomes associated with switch to an alternative TKI after first-line therapy with a 2GTKI. Of 232 patients who initiated a 2GTKI during the study period, 76 (33%) switched to an alternative TKI. Reasons for switching included intolerance (79%) and resistance (21%). Among the 60 patients who switched due to intolerance, 53 (88%) were able to achieve or maintain a major mol. response (MMR) with 5-yr progression-free survival (PFS) 90.5% (95% CI 90.4-90.6%). Amongst the 16 patients who switched due to resistance, 8 patients (50%) were able to achieve MMR with 5-yr PFS 80.4% (95% CI 80.2-80.6%). Most patients who switched due to intolerance remained on their second-line TKI. Approx. 25% of patients who initiate first-line 2GTKI in a real world setting will ultimately switch to an alternate TKI due to intolerance. Patients who switch for intolerance continue to enjoy excellent clin. outcomes. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Computed Properties of 380843-75-4

The Article related to dasatinib nilotinib anticancer agent chronic myeloid leukemia, chronic myeloid leukemia, chronic phase chronic myeloid leukemia, dasatinib, nilotinib, second generation tyrosine kinase inhibitor, switch and other aspects.Computed Properties of 380843-75-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Adiwidjaja, Jeffry et al. published their research in Pharmaceutical Research in 2020 |CAS: 380843-75-4

The Article related to mol modeling simulation drug interaction pharmacokinetic pbpk, bosutinib, curcumin, imatinib, modelling and simulation, natural product-drug interactions, physiologically-based pharmacokinetic (pbpk) and other aspects.Application In Synthesis of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

On July 31, 2020, Adiwidjaja, Jeffry; Boddy, Alan V.; McLachlan, Andrew J. published an article.Application In Synthesis of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile The title of the article was Physiologically-Based Pharmacokinetic Predictions of the Effect of Curcumin on Metabolism of Imatinib and Bosutinib: In Vitro and In Vivo Disconnect. And the article contained the following:

Abstract: Purpose: This study aimed to investigate the potential pharmacokinetic interactions between curcumin, imatinib and bosutinib, combining In Vitro and in silico methods. Methods: In Vitro metabolism of imatinib and bosutinib were investigated in pooled human liver microsomes and recombinant CYP3A4 enzyme in the presence and absence of curcumin and curcumin glucuronide using an LC-MS/MS assay for N-desmethyl metabolites. A physiol.-based pharmacokinetic (PBPK) model for curcumin formulated as solid lipid nanoparticles (SLN) was constructed using In Vitro glucuronidation kinetics and published clin. pharmacokinetic data. The potential effects of curcumin coadministration on systemic exposures of imatinib and bosutinib were predicted in silico using PBPK simulations. Results: Curcumin demonstrated potent reversible inhibition of cytochrome P 450 (CYP)3A4-mediated N-demethylation of imatinib and bosutinib and CYP2C8-mediated metabolism of imatinib with inhibitory constants (ki,u) of ≤1.5μmol. L-1. A confirmatory In Vitro study with paclitaxel, the 6α-hydroxylation of which is exclusively mediated by CYP2C8, was consistent with a potent inhibition of this enzyme by curcumin. Curcumin glucuronide also inhibited both CYP enzymes In Vitro, albeit to a lesser extent than that of curcumin. PBPK model simulations predicted that at recommended dosing regimens of SLN curcumin, coadministration would result in an increase in systemic exposures of imatinib and bosutinib of up to only 10%. Conclusion: A PBPK model for curcumin in a SLN formulation was successfully developed. Although curcumin possesses a strong In Vitro inhibitory activity towards CYP3A4 and CYP2C8 enzymes, its interactions with imatinib and bosutinib were unlikely to be of clin. importance due to curcumin’s poor bioavailability. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Application In Synthesis of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

The Article related to mol modeling simulation drug interaction pharmacokinetic pbpk, bosutinib, curcumin, imatinib, modelling and simulation, natural product-drug interactions, physiologically-based pharmacokinetic (pbpk) and other aspects.Application In Synthesis of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Baty, Roua S. et al. published their research in Saudi Journal of Biological Sciences in 2022 |CAS: 380843-75-4

The Article related to chronic myelogenous leukemia bosutinib caspase inhibitor apoptosis cancer therapy, apoptosis, boc-d-fmk, bosutinib, cell cycle arrest, cell viability, chronic myelogenous leukaemia (cml), mtt assay and other aspects.HPLC of Formula: 380843-75-4

On April 30, 2022, Baty, Roua S. published an article.HPLC of Formula: 380843-75-4 The title of the article was Protective effect of Bosutinib with caspase inhibitors on human K562 cells. And the article contained the following:

Cancer therapy has become increasingly focused on molecularly targeted medications. Despite the fact that multi-cytotoxic medication regimens have proven to be highly effective, many investigations in targeted treatments have focused on a single agent. The precise mol. mechanism of action of second-generation BCR-ABL tyrosine kinase inhibitors, which includes different targets and pathways, can help rationalize therapy in chronic myelogenous leukemia (CML) and other diseases affected by BCR-ABL tyrosine kinase inhibitors (TKIs). The purpose of this study was to analyze if bosutinib (BOS) combined with Boc-D-FMK effectively suppressed proliferation and induced apoptosis in K562 cells to a lesser extent, implying that bosutinib is an effective leukemia treatment and that its combination with Boc-D-FMK is a mild chemotherapeutic agent against leukemia. In this study, bosutinib was obtained together with other materials to perform a cell culture experiment with human cell lines, as well as addnl. drug treatment. Furthermore, cell viability (MTT assay) and flow cryometry such as viability and cell cycle assays are performed. The target profile of the dual SRC/ABL inhibitor bosutinib was studied in this study as a first kinase inhibitor to target K562 cells, which has recently been linked to the proliferation of myelogenous leukemia cells, these results suggest the effectiveness of inhibitory activity on cell viability/proliferation, alone generated a potent value of 250 nM (39.27 ± 1.17) for 48 h as optimal dose. The cytotoxic effect of bosutinib on the K562 cell line was assessed in vitro using the MTT assay, and the cytotoxicity was further clarified using cell viability and cell cycle assays. Guava Cell Assay software validated the activation of apoptosis. Sub-G1, G0/G1, S, and G2/M phases are depicted. Cell cycle research revealed that K562 cells treated with bosutinib accumulated much more in the sub-G1 phase, which was later validated by a drop peak at the G2/M phase. In conclusion, the nature of bosutinibs reduction of cancer cell growth may open the door to future research into the development of green synthesis medicines, particularly for cancer treatment. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).HPLC of Formula: 380843-75-4

The Article related to chronic myelogenous leukemia bosutinib caspase inhibitor apoptosis cancer therapy, apoptosis, boc-d-fmk, bosutinib, cell cycle arrest, cell viability, chronic myelogenous leukaemia (cml), mtt assay and other aspects.HPLC of Formula: 380843-75-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Verougstraete, Nick et al. published their research in Journal of Pharmaceutical and Biomedical Analysis in 2022 |CAS: 380843-75-4

The Article related to bosutinib dasatinib giitertinib ibrutinib anticancer agent cancer, dried blood microsampling, lc-ms/ms, therapeutic drug monitoring, tyrosine kinase inhibitors, volumetric absorptive microsampling and other aspects.Electric Literature of 380843-75-4

On January 5, 2022, Verougstraete, Nick; Stove, Christophe P. published an article.Electric Literature of 380843-75-4 The title of the article was Volumetric absorptive microsampling as a suitable tool to monitor tyrosine kinase inhibitors. And the article contained the following:

Therapeutic drug monitoring (TDM) of tyrosine kinase inhibitors (TKIs) shows significant potential in guiding personalized anticancer treatment. Dried blood microsampling could be a valuable alternative for traditional plasma sampling to provide TDM results faster and to reach a wider audience. Sample collection is easy and patient friendly as only a small volume of blood is collected via a fingerprick. This enables the possibility of home sampling by the patients themselves. Therefore, an LC-MS/MS method was developed and validated for the quantification of bosutinib, dasatinib, gilteritinib, ibrutinib, imatinib, midostaurin, nilotinib and ponatinib in dried blood samples collected via volumetric absorptive microsampling (VAMS). A VAMS device collects a fixed volume of blood (± 10μL), irresp. of the samples hematocrit (Hct). During method validation, special attention was paid to the possible impact of Hct (range 0.18-0.55) on matrix effect (ME), robustness of the extraction, and accuracy of the method. The method was successfully validated based on international guidelines in terms of calibration curves, precision (within-run CV 2.20-14.8%; between-run CV 2.40-12.3%), accuracy (within-run bias 0.34-12.5%; between-run bias -0.15 to 16.2%), carry-over and selectivity. IS-compensated ME and recovery were Hct independent and no significant impact of Hct on the accuracy of the TKI quantifications was observed All TKIs were stable in VAMS samples stored at -20°C, 4°C and room temperature for at least 4 wk and for 2 days at 60°C (except ibrutinib). Lastly, we demonstrated a good agreement between liquid blood obtained from patients on TKI treatment and VAMS samples prepared from that venous blood. As this implies that there is no methodol. impact of liquid vs. dried blood anal., the presented method can be applied in clin. follow-up studies for determining TKIs in (capillary) VAMS samples with varying Hct levels. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Electric Literature of 380843-75-4

The Article related to bosutinib dasatinib giitertinib ibrutinib anticancer agent cancer, dried blood microsampling, lc-ms/ms, therapeutic drug monitoring, tyrosine kinase inhibitors, volumetric absorptive microsampling and other aspects.Electric Literature of 380843-75-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Mulas, Olga et al. published their research in Annals of Hematology in 2020 |CAS: 380843-75-4

The Article related to anticancer ace inhibitor angiotensin receptor blocker thrombosis hypertension leukemia, arterial occlusive events, chronic myeloid leukemia, hypertension, renin angiotensin system inhibitors, tki and other aspects.Category: piperazines

On July 31, 2020, Mulas, Olga; Caocci, Giovanni; Stagno, Fabio; Bonifacio, Massimiliano; Annunziata, Mario; Luciano, Luigiana; Orlandi, Ester Maria; Abruzzese, Elisabetta; Sgherza, Nicola; Martino, Bruno; Albano, Francesco; Galimberti, Sara; Pregno, Patrizia; Bocchia, Monica; Castagnetti, Fausto; Tiribelli, Mario; Binotto, Gianni; Gozzini, Antonella; Capodanno, Isabella; Fozza, Claudio; Luzi, Debora; Efficace, Fabio; Simula, Maria Pina; Scaffidi, Luigi; De Gregorio, Fiorenza; Elena, Chiara; Trawinska, Malgorzata Monika; Cattaneo, Daniele; Attolico, Imma; Barate, Claudia; Pirillo, Francesca; Sicuranza, Anna; Gugliotta, Gabriele; Stella, Rossella; Scalzulli, Emilia; Iurlo, Alessandra; Foa, Robin; Breccia, Massimo; La Nasa, Giorgio published an article.Category: piperazines The title of the article was Renin angiotensin system inhibitors reduce the incidence of arterial thrombotic events in patients with hypertension and chronic myeloid leukemia treated with second- or third-generation tyrosine kinase inhibitors. And the article contained the following:

Hypertension is a commonly reported comorbidity in patients diagnosed with chronic myeloid leukemia (CML), and its management represents a challenge in patients treated with 2nd- or 3rd-generation tyrosine kinase inhibitors (TKIs), considering their addnl. cardiovascular (CV) toxicity. The renin angiotensin system (RAS) contributes to hypertension genesis and plays an important role in atherosclerosis development, proliferation, and differentiation of myeloid hematopoietic cells. We analyzed a cohort of 192 patients with hypertension at CML diagnosis, who were treated with 2nd- or 3rd-generation TKIs, and evaluated the efficacy of RAS inhibitors (angiotensin-converting enzyme inhibitors (ACEi) and angiotensin-II receptor blockers (ARBs)) in the prevention of arterial occlusive events (AOEs), as compared with other drug classes. The 5-yr cumulative incidence of AOEs was 32.7 ± 4.2%. Patients with SCORE ≥ 5% (high-very-high) showed a significantly higher incidence of AOEs (33.7 ± 7.6% vs 13.6 ± 4.8%, p = 0.006). The AOE incidence was significantly lower in patients treated with RAS inhibitors (14.8 ± 4.2% vs 44 ± 1%, p < 0.001, HR = 0.283). The difference in the low and intermediate Sokal risk group was confirmed but not in the high-risk group, where a lower RAS expression has been reported. Our data suggest that RAS inhibitors may represent an optimal treatment in patients with hypertension and CML, treated with 2nd or 3rdG TKIs. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Category: piperazines

The Article related to anticancer ace inhibitor angiotensin receptor blocker thrombosis hypertension leukemia, arterial occlusive events, chronic myeloid leukemia, hypertension, renin angiotensin system inhibitors, tki and other aspects.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Cortes, Jorge E. et al. published their research in European Journal of Haematology in 2021 |CAS: 380843-75-4

The Article related to bosutinib drug safety toxicity philadelphia chromosome pos leukemia patient, bosutinib, cardiovascular events, chronic myeloid leukemia, clinical trial, effusion events, tyrosine kinase inhibitor and other aspects.Name: 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

Cortes, Jorge E.; Kantarjian, Hagop M.; Mauro, Michael J.; An, Fiona; Nick, Sonja; Leip, Eric; Gambacorti-Passerini, Carlo; Bruemmendorf, Tim H. published an article in 2021, the title of the article was Long-term cardiac, vascular, hypertension, and effusion safety of bosutinib in patients with Philadelphia chromosome-positive leukemia resistant or intolerant to prior therapy.Name: 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile And the article contains the following content:

Long-term follow-up (≥4 years) demonstrated a low incidence of cardiac and vascular treatment-emergent adverse events (TEAEs) with bosutinib treatment. We evaluated cardiac, vascular, hypertension, and effusion TEAEs after ≥ 7 years of follow-up in patients with Philadelphia chromosome-pos. (Ph+) leukemia. This retrospective anal. of a phase I/II study and its ongoing extension study included data from patients with chronic phase chronic myeloid leukemia (CML) treated with bosutinib after resistance/intolerance to imatinib (CP2L) or to imatinib plus dasatinib and/or nilotinib (CP3L), and those with accelerated/blast phase CML or acute lymphoblastic leukemia after treatment with, at a min., imatinib (ADV). In all, 570 patients were treated with bosutinib; median treatment duration was 11.1 mo (range: 0.03-133.1). The incidence of cardiac, vascular, hypertension, and effusion-related TEAEs was 10.9%, 8.8%, 9.1%, and 13.3%, resp. Few patients had maximum grade 3-4 TEAEs (cardiac, 3.9%; vascular, 4.0%; hypertension, 3.0%; effusion, 4.6%). Grade 5 TEAEs occurred in the cardiac (0.7%) and vascular (1.8%) clusters only. In years 5-7, fewer than 5% of patients each year had newly occurring cardiac, vascular, hypertension, or effusion TEAEs. The exposure-adjusted TEAE rates (patients with TEAEs/total patient-year) pooled across CP2L, CP3L, and ADV cohorts were as follows: cardiac, 0.044; vascular, 0.035; hypertension, 0.038; and effusion, 0.056, of which, correspondingly, 0.9%, 1.2%, 0%, and 2.1% required treatment discontinuation. The incidence of cardiac, hypertension, vascular, and effusion events was low in patients with Ph+ CML resistant or intolerant to prior therapy who were treated with bosutinib. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Name: 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

The Article related to bosutinib drug safety toxicity philadelphia chromosome pos leukemia patient, bosutinib, cardiovascular events, chronic myeloid leukemia, clinical trial, effusion events, tyrosine kinase inhibitor and other aspects.Name: 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Koller, Dora et al. published their research in Talanta in 2020 |CAS: 380843-75-4

The Article related to tyrosine kinase inhibitor therapeutic drug monitoring hplc mass spectrometry, blood plasma analysis, caffeine, liquid chromatography-tandem mass spectrometry, phospholipids, solid phase extraction, therapeutic drug monitoring, tyrosine kinase inhibitors and other aspects.Computed Properties of 380843-75-4

On February 1, 2020, Koller, Dora; Vaitsekhovich, Viktoryia; Mba, Cecile; Steegmann, Juan L.; Zubiaur, Pablo; Abad-Santos, Francisco; Wojnicz, Aneta published an article.Computed Properties of 380843-75-4 The title of the article was Effective quantification of 11 tyrosine kinase inhibitors and caffeine in human plasma by validated LC-MS/MS method with potent phospholipids clean-up procedure. application to therapeutic drug monitoring. And the article contained the following:

Therapeutic drug monitoring (TDM) help to improve treatment efficacy and safety. Therefore, a simple and sensitive liquid chromatog.-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous monitoring of 11 tyrosine kinase inhibitors (TKIs) in human plasma. TKIs included in the assay are used in the treatment of chronic myeloid leukemia (CML: imatinib, dasatinib, nilotinib, bosutinib, ponatinib), polycythemia vera (ruxolitinib), chronic lymphocytic leukemia (ibrutinib) and rheumatoid arthritis (filgotinib, tofacitinib, baricitinib, peficitinib). Caffeine was also included in the method. Caffeine increases the acidity of the stomach and decreases its pH as well as is a competitive inhibitor of cytochrome P 450 isoenzymes. Thus, it may influence absorption and metabolism of some TKIs, by modifying their plasma levels. The analytes of interest and their stable isotope-labeled internal standards were extracted from 200μL of human plasma. Microelution-solid phase extraction (μ-SPE) was optimized for method validation and compared to simple protein precipitation (PPT). A gradient elution on a Poroshell 120 EC-C18 column at 60°C and a flow rate of 0.5 mL/min was applied for analyte separation The anal. run lasted 8 min and it was followed by a re-equilibration time of 4 min. Dynamic multiple reaction monitoring scan in the pos. ionization mode was applied to improve method sensitivity. Endogenous plasma phospholipids can strongly affect MS anal. Hence, the monitoring of endogenous phospholipids was included in the assay. Full validation of the method was achieved, including tests of precision, accuracy, trueness, linearity, extraction recovery, matrix effect, process efficiency, stability, sensitivity (with excellent LLOQs), selectivity, identity confirmation and carry-over effect. Regarding sample cleanup, more than 91% of early eluting and more than 96% of late eluting endogenous phospholipids were eliminated by μ-SPE when compared to PPT. This method enables the simultaneous plasma monitoring of 11 TKIs and caffeine and ensures high effectiveness in phospholipids elimination. The present approach is currently used in our clin. practice, being applied to TDM of dasatinib, imatinib, nilotinib and ponatinib. TKIs plasma monitoring helps to individualize dose adjustment and manage adverse effects in CML patients. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Computed Properties of 380843-75-4

The Article related to tyrosine kinase inhibitor therapeutic drug monitoring hplc mass spectrometry, blood plasma analysis, caffeine, liquid chromatography-tandem mass spectrometry, phospholipids, solid phase extraction, therapeutic drug monitoring, tyrosine kinase inhibitors and other aspects.Computed Properties of 380843-75-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Pushpam, Deepam et al. published their research in Daru, Journal of Pharmaceutical Sciences in 2020 |CAS: 380843-75-4

The Article related to meta analysis chronic myeloid leukemia tyrosine kinase pharmacol, gene polymorphism and imatinib, pharmacology of tyrosine kinase inhibitors, selection of tyrosine kinase inhibitors, tyrosine kinase inhibitors in chronic myeloid leukemia and other aspects.Computed Properties of 380843-75-4

On June 30, 2020, Pushpam, Deepam; Bakhshi, Sameer published an article.Computed Properties of 380843-75-4 The title of the article was Pharmacology of tyrosine kinase inhibitors in chronic myeloid leukemia; a clinician’s perspective. And the article contained the following:

Meta-anal. of tyrosine kinase inhibitors pharmacol. in chronic myeloid leukemia patients. Upcoming concepts and related trials in the management of chronic myeloid leukemia (CML) along with future directions have been touched upon. Evidence acquisition: PubMed, Embase, Google, Cochrane library and Medline were searched to identify relevant literature for the review. Clinicaltrial.gov was searched for upcoming data and trials. Results: There are lot of gap in pharmacokinetics and pharmacodynamics of TKI. Imatinib appears to be the safest TKI. Newer TKI’s achieve better achievement of therapeutic milestones, deeper mol. response and less chances of progression of CML compared to imatinib. Newer TKI appears to be better choice for achieving TFR. When the objective is survival, imatinib is still the TKI of choice. Primary prophylaxis with antiplatelet drugs for TKI having cardiovascular and thromboembolic side effects should be considered. Conclusion: Pharmacogenetic data of TKI is still immature to guide in therapeutic decision making in clin. practice. There is need for further research in pharmacol. and pharmacogenomics of newer TKI’s. Randomized controlled trials are required to decide the optimum TKI for TFR. Safe and effective TKI for targeting T315I mutation, CML accelerated phase and blast crisis are an active area of research. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Computed Properties of 380843-75-4

The Article related to meta analysis chronic myeloid leukemia tyrosine kinase pharmacol, gene polymorphism and imatinib, pharmacology of tyrosine kinase inhibitors, selection of tyrosine kinase inhibitors, tyrosine kinase inhibitors in chronic myeloid leukemia and other aspects.Computed Properties of 380843-75-4

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics