Category: 380843-75-4

Abaza, Yasmin; Kantarjian, Hagop; Alwash, Yasmin; Borthakur, Gautam; Champlin, Richard; Kadia, Tapan; Garcia-Manero, Guillermo; Daver, Naval; Ravandi, Farhad; Verstovsek, Srdan; Burger, Jan; Estrov, Zeev; Ohanian, Maro; Lim, Miranda; Pemmaraju, Naveen; Jabbour, Elias; Cortes, Jorge published an article in 2020, the title of the article was Phase I/II study of dasatinib in combination with decitabine in patients with accelerated or blast phase chronic myeloid leukemia.Application In Synthesis of 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:

Treatment of advanced-phase chronic myeloid leukemia (CML) remains unsatisfactory. Single-agent tyrosine kinase inhibitors have modest and short-lived activity in this setting. We conducted a phase I/II study to determine safety and efficacy of the combination of dasatinib and decitabine in patients with advanced CML. Two different dose schedules were investigated with a starting decitabine dose of either 10 mg/m2 or 20 mg/m2 daily for 10 days plus dasatinib 100 mg daily. The target dose level was decitabine 10 mg/m2 or 20 mg/m2 daily for 10 days plus dasatinib 140 mg daily. Thirty patients were enrolled, including seven with accelerated-phase CML, 19 with blast-phase CML, and four with Philadelphia-chromosome pos. acute myeloid leukemia. No dose-limiting toxicity was observed at the starting dose level with either schedule. Grade ≥3 treatment emergent hematol. adverse events were reported in 28 patients. Thirteen patients (48%) achieved a major hematol. response and six (22%) achieved a minor hematol. response, with 44% of these patients achieving a major cytogenetic response and 33% achieving a major mol. response. Median overall survival (OS) was 13.8 mo, with significantly higher OS among patients who achieved a hematol. response compared to non-responders (not reached vs 4.65 mo; P < .001). Decitabine plus dasatinib is a safe and active regimen in advanced CML. Further studies using this combination are warranted. 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 dasatinib decitabine anticancer agent chronic myeloid leukemia, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents 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

Cayssials, Emilie; Torregrosa-Diaz, Jose; Leleu, Xavier; Guilhot, Francois; Chomel, Jean-Claude published an article in 2021, the title of the article was Reply to Comment on low-dose tyrosine kinase inhibitors before treatment discontinuation do not impair treatment-free remission in chronic myeloid leukemia patients: Results of a retrospective study.SDS of cas: 380843-75-4 And the article contains the following content:

The present invention relates to a retrospective study on reply to comment on low-dose tyrosine kinase inhibitors before treatment discontinuation do not impair treatment-free remission in chronic myeloid leukemia 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).SDS of cas: 380843-75-4

The Article related to tyrosine kinase inhibitor chronic myeloid leukemia human, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.SDS of cas: 380843-75-4

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On November 25, 2021, Rea, Delphine; Mauro, Michael J.; Boquimpani, Carla; Minami, Yosuke; Lomaia, Elza; Voloshin, Sergey; Turkina, Anna; Kim, Dong-Wook; Apperley, Jane F.; Abdo, Andre; Fogliatto, Laura Maria; Kim, Dennis Dong Hwan; le Coutre, Philipp; Saussele, Susanne; Annunziata, Mario; Hughes, Timothy P.; Chaudhri, Naeem; Sasaki, Koji; Chee, Lynette; Garcia-Gutierrez, Valentin; Cortes, Jorge E.; Aimone, Paola; Allepuz, Alex; Quenet, Sara; Bedoucha, Veronique; Hochhaus, Andreas published an article.SDS of cas: 380843-75-4 The title of the article was A phase 3, open-label, randomized study of asciminib, a STAMP inhibitor, vs bosutinib in CML after 2 or more prior TKIs. And the article contained the following:

Patients with chronic myeloid leukemia in chronic phase (CML-CP) resistant/intolerant to ≥2 tyrosine kinase inhibitors (TKIs) are at high risk of experiencing poor outcomes because of disease biol. and inadequate efficacy and/or safety of current therapies. Asciminib, a first-in-class BCR-ABL1 inhibitor Specifically Targeting the ABL Myristoyl Pocket (STAMP), has the potential to overcome resistance/intolerance to approved TKIs. In this phase 3, open-label study, patients with CML-CP previously treated with ≥2 TKIs were randomized (2:1) to receive asciminib 40 mg twice daily vs bosutinib 500 mg once daily. Randomization was stratified by major cytogenetic response (MCyR) status at baseline. The primary objective was to compare the major mol. response (MMR) rate at week 24 for asciminib vs bosutinib. A total of 233 patients were randomized to asciminib (n = 157) or bosutinib (n = 76). Median follow-up was 14.9 mo. The MMR rate at week 24 was 25.5% with asciminib and 13.2% with bosutinib. The difference in MMR rate between treatment arms, after adjusting for MCyR at baseline, was 12.2% (95% confidence interval, 2.19-22.30; 2-sided P = .029). Fewer grade ≥3 adverse events (50.6% vs 60.5%) and adverse events leading to treatment discontinuation (5.8% vs 21.1%) occurred with asciminib than with bosutinib. The study showed a superior efficacy of asciminib compared with that of bosutinib, together with a favorable safety profile. These results support the use of asciminib as a new therapy in patients with CML-CP who are resistant/intolerant to ≥2 prior TKIs. This trial was registered at www.clinicaltrials.gov as #NCT03106779. 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).SDS of cas: 380843-75-4

The Article related to bosutinib anticancer agent chronic myeloid leukemia, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.SDS of cas: 380843-75-4

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On August 31, 2021, Lakkireddy, Samyuktha; Jayaraman, Archana; Aula, Sangeetha; Kapley, Atya; Kutala, Vijay Kumar; Jamil, Kaiser published an article.Reference 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 In Silico Docking Studies of Vascular Endothelial Growth Factor-A (VEGFA): Possible Implications in Chronic Myeloid Leukemia (CML) Therapy. And the article contained the following:

Background: Dysregulated angiogenesis resulting in neovascularization is a critical event in the expansion and progression of Chronic Myeloid Leukemia (CML), hematopoietic cancer. Vascular Endothelial Growth Factor- A (VEGFA), an important angiogenesis mediator, has been a target for treating cancer. Although several anti-VEGFA drugs are available, they are associated with adverse side effects, promoting the need to identify better drugs that may be less toxic. Objective: Our aim was to investigate whether Tyrosine Kinase Inhibitors (TKIs) could be repurposed for use as VEGFA inhibitors via in silico docking software. We also investigated the potential of phytochems. as VEGFA inhibitors. Methods: We performed mol. docking using Schrodinger Maestro software suite 2014-3 to determine the most potent phytochem. and TKI VEGFA antagonists. Results: Among the TKIs investigated, Bosutinib had the best binding affinity and may be the most potent TKI against VEGFA. The order of binding affinities for the top ten docked ligands was: Ginsenoside Rg3> Bosutinib> Vitamin D> Paclitaxel> Dasatinib> Saponins> Ponatinib> Squalamine> Imatinib> Nilotinib. We found that Ginsenoside Rg3 had the highest binding affinity (MMGBSA score= -99.4 kcal/mol, glide Gscore = -9.16 kcal/mol) to VEGFA. Conclusion: Our study has shown for the first time the binding poses of these TKIs and phytochems. to VEGFA, using computational methods. We propose that the use of the top scoring ligands, in isolation or a combination of phytochems. plus TKI, could serve as potent angiogenesis inhibitors via their binding to and inhibiting VEGFA expression to prevent CML progression. We have also profiled the ligand binding residues, which may be explored in designing pharmacophores. 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).Reference of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

The Article related to chronic myeloid leukemia docking vegfa, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Reference of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

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Piperazines – an overview | ScienceDirect Topics

Lu, Xiaoxiao; Guan, Anqi; Chen, Xi; Xiao, Jian; Xie, Mingxuan; Yang, Baishuang; He, Shuya; You, Shaojin; Li, Wei; Chen, Qiong published an article in 2020, the title of the article was mPRa mediates P4/Org OD02-0 to improve the sensitivity of lung adenocarcinoma to EGFR-TKIs via the EGFR-SRC-ERK1/2 pathway.Synthetic Route of 380843-75-4 And the article contains the following content:

The discovery of epidermal growth factor receptor (EGFR) mutations has made EGFR tyrosine kinase inhibitors (EGFR-TKIs) a milestone in the treatment for advanced non-small cell lung cancer (NSCLC). However, patients lacking EGFR mutations are not sensitive to EGFR-TKI treatment and the emergence of secondary resistance poses new challenges for the targeted therapy of lung cancer. In this study, we identified that the expression of membrane progesterone receptor a (mPRa) was associated with EGFR mutations in lung adenocarcinoma patients and subsequently affected the efficacy of EGFR-TKIs. Progesterone (P4) or its derivative Org OD02-0 (Org), which is mediated by mPRa, increases the function of EGFR-TKIs to suppress the proliferation, migration, and invasion of lung adenocarcinoma cells in vitro and in vivo. In addition, the mPRa pathway triggers delayed resistance to EGFR-TKIs. Mechanistic investigations demonstrated that the mPRa pathway can crosstalk with the EGFR pathway by activating nongenomic effects to inhibit the EGFR-SRC-ERK1/2 pathway, thereby promoting antitumorigenic effects. In conclusion, our data describe an essential role for mPRa in improving sensitivity to EGFR-TKIs, thus rationalizing its potential as a therapeutic target for lung adenocarcinomas. 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).Synthetic Route of 380843-75-4

The Article related to lung adenocarcinoma membrane progesterone receptor a egfr mutation, egfr mutations, egfr-tkis, lung adenocarcinoma, mprα, sensitivity, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Synthetic Route of 380843-75-4

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Piperazines – an overview | ScienceDirect Topics

Muresan, Bogdan; Mamolo, Carla; Cappelleri, Joseph C.; Leip, Eric; Viqueira, Andrea; Heeg, Bart published an article in 2021, the title of the article was An indirect comparison between bosutinib, nilotinib and dasatinib in first-line chronic phase chronic myeloid leukemia.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:

Bosutinib, nilotinib and dasatinib are approved for the treatment of patients with newly diagnosed chronic-phase chronic myeloid leukemia (CP-CML). In the absence of head-to-head comparisons between second-generation tyrosine kinase inhibitors (TKIs), the objective of this study was to indirectly compare the efficacy of bosutinib with nilotinib and dasatinib in first-line (1L) CP-CML. Cross-trial heterogeneity in terms of patient baseline characteristics and imatinib dose escalation are difficult to adjust for in network meta-analyses and anchored matching-adjusted indirect treatment comparisons (MAICs). Therefore, an unanchored MAIC was performed using patient level data from bosutinib (BFORE trial) and published aggregated data from nilotinib (ENESTnd) and dasatinib (DASISION) trials. After matching, cytogenetic and mol. responses, and disease progression, after a min. follow-up of 24 mo were compared between nilotinib vs. bosutinb and dasatinib vs. bosutinib. The comparison of nilotinib vs. bosutinib resulted in no statistically significant differences for MMR at and by 24 mo, MR4 by 24 mo, MR4.5 at and by 24 mo, CCyR by 24 mo, and disease progression, however, a decreased odds of MR4 at 24 mo in favor of bosutinib vs. nilotinib was observed The comparison of dasatinib vs. bosutinib by 24 mo resulted in no statistically significant differences for MMR, disease progression, and CCyR, however a decreased odds of MR4.5 in favor of bosutinib vs. dasatinib was observed Overall, in these analyses bosutinib demonstrates equivalent efficacy to nilotinib and dasatinib in the treatment of patients with newly diagnosed CP-CML. 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 nilotinib dasatinib chronic phase myeloid leukemia, chronic myeloid leukemia, bosutinib, dasatinib, first line, nilotinib, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Name: 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

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Piperazines – an overview | ScienceDirect Topics

On June 30, 2022, Takahashi, Naoto; Cortes, Jorge E.; Sakaida, Emiko; Ishizawa, Kenichi; Ono, Takaaki; Doki, Noriko; Matsumura, Itaru; Garcia-Gutierrez, Valentin; Rosti, Gianantonio; Ono, Chiho; Ohkura, Masayuki; Tanetsugu, Yusuke; Viqueira, Andrea; Brummendorf, Tim H. published an article.Recommanded Product: 380843-75-4 The title of the article was Safety profile of bosutinib in Japanese versus non-Japanese patients with chronic myeloid leukemia: a pooled analysis. And the article contained the following:

Bosutinib has been investigated in multiple clin. trials globally, including Japan, for treatment of chronic myeloid leukemia (CML). A pooled anal. of seven Pfizer-sponsored clin. trials evaluated the safety of bosutinib in Japanese (n = 138) vs non-Japanese (n = 1210) patients with CML. First-line bosutinib was administered in 54.3% vs 41.4% of patients, and second-line or later bosutinib in the remainder. Median treatment duration was 1.4 vs 2.3 years, and median relative dose intensity 78.1% vs 90.0%. Any-grade treatment-emergent adverse events (TEAEs) occurred in 100.0% vs 98.9% (grade ≥ 3: 81.9% vs 75.2%). In both groups, the most common TEAEs relevant to bosutinib were gastrointestinal (92.8% vs 84.7%), liver function (72.5% vs 34.8%), rash (63.8% vs 37.4%), and myelosuppression (55.1% vs 50.7%). TEAEs led to dose reduction in 65.2% vs 50.6%, dose interruption in 78.3% vs 68.8%, and permanent treatment discontinuation in 30.4% vs 25.4% of patients. The safety profile of bosutinib in Japanese patients was generally consistent with that in non-Japanese patients, despite a higher incidence of gastrointestinal, liver function, and rash events. TEAEs were largely manageable with dose modifications and supportive care in both groups. These data may help optimize TEAE management and outcomes in Japanese patients receiving bosutinib for CML. Trial registration ClinicalTrials.gov: NCT02130557, NCT03128411, NCT00574873, NCT00261846, NCT01903733, NCT00811070, NCT02228382. 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).Recommanded Product: 380843-75-4

The Article related to bosutinib anticancer agent chronic myeloid leukemia, bosutinib, chronic myeloid leukemia, japan, safety, tyrosine kinase inhibitor, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Recommanded Product: 380843-75-4

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Piperazines – an overview | ScienceDirect Topics

Assi, Rita; Kantarjian, Hagop; Keating, Michael; Pemmaraju, Naveen; Verstovsek, Srdan; Garcia-Manero, Guillermo; Ravandi, Farhad; Borthakur, Gautam; Dahl, Jenny; Jabbour, Elias; Cortes, Jorge E. published an article in 2021, the title of the article was Management of chronic myeloid leukemia during pregnancy among patients treated with a tyrosine kinase inhibitor: a single-Center experience.Product Details of 380843-75-4 And the article contains the following content:

Tyrosine kinase inhibitors (TKIs) are teratogenic. Chronic myeloid leukemia (CML) is increasingly identified in younger patients who wish to conceive, the management of CML during pregnancy is challenging. We reviewed 51 pregnancies involving 37 patients (30 women, 10 with >1 pregnancy and 7 men) who were either diagnosed with CML during pregnancy or receiving TKI at the time of conception. Ten women were involved in >1 pregnancies. Fifteen women were diagnosed with CML during pregnancy: 10 were treated with hydroxyurea (n = 5), interferon-alfa (n = 3), leukapheresis (n = 1), or nilotinib (n = 1). There were 14 (82%) healthy babies born on term including 2 sets of twins, 2 spontaneous miscarriages (12%), and 1 elective abortion (6%). Within 1 mo of delivery or abortion, all women started TKI and achieved MR4.5 (n = 6) and MMR (n = 8) within 3-48 mo. One patient, treated with interferon during pregnancy, died of blast phase within 2 mo. Four of the 14 remaining women later conceived 5 other pregnancies while on TKI (3 unplanned, 2 planned). Twenty-six patients (7 men; 19 women) conceived while on TKI, with a total of 36 pregnancies. Fifteen women had 20 unplanned pregnancies while receiving TKI and discontinued immediately upon recognition of pregnancy. The median time of TKI exposure was 3 wk (range, 2-11). Five pregnancies ended in miscarriages and 3 in elective abortion. All 7 men fathered 7 full-term healthy babies. Of 20 babies born to men and women (including one set of twins), 1 had minor abnormality. Seven women lost their responses during pregnancy but at the end of pregnancy all but 2 resumed TKI and regained responses. Seven women involved in 9 planned pregnancies discontinued TKI prior to conception for a median of 4 mo (range, 1-20); 3 lost responses during pregnancy. Only 5 patients resumed therapy after delivery. Outcomes were 6 full-term healthy babies, one premature, and two miscarriages. Conception among CML patients while on TKI could be uncomplicated. While patients may lose response following treatment interruption, nearly all regain response upon resuming therapy. Therapy during pregnancy is rarely needed. 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).Product Details of 380843-75-4

The Article related to tyrosine kinase inhibitor human pregnancy chronic myeloid leukemia, cml, tki, malformation, pregnancy, spontaneous abortion, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Product Details of 380843-75-4

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On July 31, 2021, Chuah, Charles; Koh, Liang Piu; Numbenjapon, Tontanai; Zang, Dae Young; Ong, Kiat Hoe; Do, Young Rok; Ohkura, Masayuki; Ono, Chiho; Viqueira, Andrea; Cortes, Jorge E.; Brummendorf, Tim H. published an article.Category: piperazines The title of the article was Efficacy and safety of bosutinib versus imatinib for newly diagnosed chronic myeloid leukemia in the Asian subpopulation of the phase 3 BFORE trial. And the article contained the following:

Bosutinib is approved in the United States, Europe, Japan, and other countries for treatment of newly diagnosed chronic phase (CP) chronic myeloid leukemia (CML), and CML resistant/intolerant to prior therapy. In the phase 3 BFORE trial (Clinicaltrials.gov, NCT02130557), patients were randomized 1:1 to first-line bosutinib or imatinib 400 mg once daily. We examined efficacy, safety, and patient-reported outcomes of bosutinib vs imatinib and pharmacokinetics of bosutinib in the Asian (n = 33 vs 34) and non-Asian (n = 235 vs 234) subpopulations of BFORE followed for at least 24 mo. At the data cutoff date, 72.7 vs 66.7% of Asian and 70.6 vs 66.4% of non-Asian patients remained on treatment. The major mol. response rate at 24 mo favored bosutinib vs imatinib among Asian (63.6 vs 38.2%) and non-Asian (60.9 vs 52.6%) patients, as did the complete cytogenetic response rate by 24 mo (86.7 vs 76.7%, 81.5 vs 76.3%). Treatment-emergent adverse events in both subpopulations were consistent with the primary BFORE results. Trough bosutinib concentration levels tended to be higher in Asian patients. Health-related quality of life was maintained after 12 mo of bosutinib in both subpopulations. These results support bosutinib as a first-line treatment option in Asian patients with CP CML. 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 bosutinib imatinib human cml efficacy safety diagnosis, asian, bosutinib, chronic myeloid leukemia, first-line, imatinib, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Category: piperazines

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Piperazines – an overview | ScienceDirect Topics

On July 31, 2020, Hino, Masayuki; Matsumura, Itaru; Fujisawa, Shin; Ishizawa, Kenichi; Ono, Takaaki; Sakaida, Emiko; Sekiguchi, Naohiro; Tanetsugu, Yusuke; Fukuhara, Kei; Ohkura, Masayuki; Koide, Yuichiro; Takahashi, Naoto published an article.Formula: C26H29Cl2N5O3 The title of the article was Phase 2 study of bosutinib in Japanese patients with newly diagnosed chronic phase chronic myeloid leukemia. And the article contained the following:

Abstract: This open-label, single-arm, phase 2 study (ClinicalTrials.gov, NCT03128411) evaluated the efficacy, safety, and pharmacokinetics of bosutinib at a starting dose of 400 mg once daily (QD) in Japanese patients with newly diagnosed chronic phase chronic myeloid leukemia (CP CML). The primary endpoint was major mol. response (MMR) at Month 12 in the modified as-treated population (Philadelphia chromosome-pos. [Ph+] patients with e13a2/e14a2 transcripts). Sixty Japanese patients with CP CML were treated with bosutinib; median age was 55 years (range 20-83), 60.0% were males, and all were Ph+ and had e13a2/e14a2 transcripts. After median follow-up of 16.6 mo (range 11.1-21.9), 41 (68.3%) patients remained on bosutinib. The MMR rate at Month 12 was 55.0% (2-sided 90% confidence interval: 44.4-65.6). There were no on-treatment transformations to accelerated/blast phase, and no patient died on treatment or within 28 days of the last bosutinib dose. The most common treatment-emergent adverse events were diarrhea (86.7%), increased alanine aminotransferase (55.0%), and increased aspartate aminotransferase (46.7%). The primary objective of this phase 2 study was met, and there were no new safety signals for bosutinib. These data suggest bosutinib is an effective first-line treatment option for Japanese patients with newly diagnosed CP CML. 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).Formula: C26H29Cl2N5O3

The Article related to bosutinib human phase chronic myeloid leukemia, bosutinib, chronic myeloid leukemia, japan, tyrosine kinase inhibitor, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Formula: C26H29Cl2N5O3

Referemce:
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Piperazines – an overview | ScienceDirect Topics