Tag: M.W=300-400

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II), is researched, Molecular C6H12N2O4Pt, CAS is 41575-94-4, about Streptozocin/5-fluorouracil chemotherapy of pancreatic neuroendocrine tumours in the era of targeted therapy, the main research direction is pancreatic neuroendocrine tumor streptozocin fluorouracil chemotherapy; 5-fluorouracil; Objective response; Pancreatic neuroendocrine tumor; Streptozocin; Survival.Recommanded Product: cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II).

The role of streptozocin-based chemotherapy (STZ CTx) in advanced, well-differentiated pancreatic neuroendocrine tumors (PanNET) and the best sequence of treatments in advanced PanNET are unclear. We examined the outcomes after STZ CTx in patients who had been selected according to the current therapeutic guidelines. Data from 50 PanNET patients consecutively treated with STZ CTx between 2010 and 2018 were analyzed. The endpoints of the study were the objective-response rate (ORR), progression-free survival (PFS), and overall survival (OS). STZ CTx was the first-line treatment in 54% of patients. The PanNET grades were as follows: 6% G1, 88% G2, and 6% well-differentiated G3. The ORR was 38%. Stable disease was the best response in 38% of patients and 24% showed progressive disease. Treatment was discontinued because of toxicity in one patient. Median PFS and OS were 12 (95% confidence interval (CI), 8.5-15.5) and 38 mo (95% CI, 20.4-55.6), resp. In the Kaplan-Meier anal., the median OS was 89 mo (95% CI, 34.9-143.1) for STZ CTx as first-line therapy compared with 22 mo (95% CI, 19.3-24.7; p = 0.001, log-rank test) for subsequent lines. Bone metastases neg. impacted survival (HR, 2.71, p = 0.009, univariate anal., HR, 2.64, p = 0.015, multivariate anal., and Cox regression). In patients selected according to current guidelines, PFS, and OS after STZ CTx were lower than previously reported, whereas ORR was unchanged. First-line treatment was pos. associated with OS and the presence of bone metastases was neg. associated with OS. Pre-treatment with targeted or peptide-receptor radionuclide therapy did not alter ORR, PFS, or OS.

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Product Details of 41575-94-4. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II), is researched, Molecular C6H12N2O4Pt, CAS is 41575-94-4, about NTRK1 Fusions identified by non-invasive plasma next-generation sequencing (NGS) across 9 cancer types. Author is Rolfo, Christian; Drilon, Alexander; Hong, David; McCoach, Caroline; Dowlati, Afshin; Lin, Jessica J.; Russo, Alessandro; Schram, Alison M.; Liu, Stephen V.; Nieva, Jorge J.; Nguyen, Timmy; Eshaghian, Shahrooz; Morse, Michael; Gettinger, Scott; Mobayed, Mohammad; Goldberg, Sarah; Araujo-Mino, Emilio; Vidula, Neelima; Bardia, Aditya; Subramanian, Janakiraman; Sashital, Deepa; Stinchcombe, Thomas; Kiedrowski, Lesli; Price, Kristin; Gandara, David R..

Activating fusions of the NTRK1, NTRK2 and NTRK3 genes are drivers of carcinogenesis and proliferation across a broad range of tumor types in both adult and paediatric patients. Recently, the FDA granted tumor-agnostic approvals of TRK inhibitors, larotrectinib and entrectinib, based on significant and durable responses in multiple primary tumor types. Unfortunately, testing rates in clin. practice remain quite low. Adding plasma next-generation sequencing of circulating tumor DNA (ctDNA) to tissue-based testing increases the detection rate of oncogenic drivers and demonstrates high concordance with tissue genotyping. However, the clin. potential of ctDNA anal. to identify NTRK fusion-pos. tumors has been largely unexplored. We retrospectively reviewed a ctDNA database in advanced stage solid tumors for NTRK1 fusions. NTRK1 fusion events, with nine unique fusion partners, were identified in 37 patients. Of the cases for which clin. data were available, 44% had tissue testing for NTRK1 fusions; the NTRK1 fusion detected by ctDNA was confirmed in tissue in 88% of cases. Here, we report for the first time that minimally-invasive plasma NGS can detect NTRK fusions with a high pos. predictive value. Plasma ctDNA represents a rapid, non-invasive screening method for this rare genomic target that may improve identification of patients who can benefit from TRK-targeted therapy and potentially identify subsequent on- and off-target resistance mechanisms.

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Ester – Wikipedia,
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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《[Efficacy and survival outcomes of dose-dense carboplatin plus paclitaxel as neoadjuvant chemotherapy for triple-negative breast cancer].》. Authors are Liu, Y; Xiu, M; Wang, X; Li, Q; Wang, J Y; Fan, Y; Li, Q; Chen, S S; Cai, R G; Mo, H N; Ma, F; Luo, Y; Xu, B H; Zhang, P.The article about the compound:cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II)cas:41575-94-4,SMILESS:O=C1C2(CCC2)C(O[Pt]O1)=O.N.N).Electric Literature of C6H12N2O4Pt. Through the article, more information about this compound (cas:41575-94-4) is conveyed.

Objective: To evaluate the efficacy and survival outcomes of dose-dense (biweekly) carboplatin plus paclitaxel (PC) as neoadjuvant chemotherapy (NAC) in triple-negative breast cancer (TNBC), and to explore an optimal neoadjuvant chemotherapy regimen for TNBC. Methods: Patients diagnosed as TNBC(cT1-4N0-3M0) in Cancer Hospital, Chinese Academy of Medical Sciences & Peking Union Medical College Between January 2008 and September 2018 who received dose-dense PC and standard 3-weekly PC as NAC were 1∶1 matched using propensity score matching (PSM) to compare the efficacy, safety and survival outcomes. Results: One hundred of TNBC patients were enrolled (50 patients were divided in dose-dense group, 50 patients in standard group). The objective response rate (ORR) of dose-dense group and standard group were both 90.0% (45/50). The grade 3-4 neutropenia in dose-dense group was less than that of standard group (32.7% vs. 68.0%, P=0.001), while the rate of ALT/AST elevation in dose-dense group was higher than that of standard group (57.1% vs. 32.0%, P=0.012). The pathological complete response (pCR) rates were 34.0% (17/50) in dose-dense group and 38.0% (19/50) in standard group, without statistically significance (P=0.677). The median follow-up time was 55 months (3-150 months). The 5-year recurrence-free survival (RFS) in dose-dense group and standard group were 83.5% and 75.2%, respectively the 5-year overall survival (OS) in dose-dense and standard group were 87.9% and 84.5% the difference were not statistically significant (P=0.322 and 0.647, respectively). Patients with residual disease (tumor size≥1 cm or lymph node positive) had poor prognosis, the 5-year RFS and OS were 59.3% and 68.5%, respectively. Conclusions: Dose-dense PC has similar efficacy with standard 3-weekly PC and has a good safety profile. Since dose-dense regimen can shorten the duration of therapy, it can be an alternative in TNBC.

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Reference:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II), is researched, Molecular C6H12N2O4Pt, CAS is 41575-94-4, about Outpatient fractionated ICE protocol in relapsed/refractory lymphomas: Efficacy and safety.Recommanded Product: cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II).

Methods: In this retrospective trial, we analyzed data of patients with relapsed/refractory lymphoma who received outpatient fractionated ICE between 2011-2017 at a tertiary care center. The three weekly ICE protocol consisted of: ifosfamide 1500 mg/m2 infused over 2 h on days 1-3, carboplatin (5 AUC) on day 1, and etoposide 100 mg/m2 on days 1-3. Rituximab 375 mg/m2 was given to patients with CD20 pos. B cell Non-Hodgkin lymphoma. Results: Total of 89 patients were included in this research project. Majority of patients had Hodgkin lymphoma (64%). Mean number of ICE cycles received was 2.5. Complete remission and partial remission rates for primary refractory (62.9%) and non-primary refractory (36.4%) disease were 10.5% and 26.3% vs. 41.9% and 29.0% resp. Event free survival rate was 14.5 mo (95% CI 7.7-28.0) and overall survival rate 88.7 mo (95% CI 48.1-NR). Grade 3 hematol. toxicities were documented in 19.1% of patients with 10.1% experiencing neutropenia and 9% thrombocytopenia. 5.6% had febrile neutropenia. Conclusions: Our study included, to our knowledge, the largest number of patients treated with outpatient fractionated ICE. Results demonstrated that this regimen might be a reasonable replacement for classic ICE regimen in many patients with lymphoma. It has a favorable safety profile. However, patients with primary refractory lymphomas need more effective regimens.

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Reference:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Oxaliplatin facilitates tumor-infiltration of T cells and natural-killer cells for enhanced tumor immunotherapy in lung cancer model, published in 2022, which mentions a compound: 41575-94-4, mainly applied to , SDS of cas: 41575-94-4.

Platinum is reported to have adjuvant immune properties, whether oxaliplatin (OXA) could be utilized to synergize with anti-programmed cell death-1 (PD-1) antibody or anti-NKG2D (natural-killer group 2, member D) antibody is investigated. S.c. A549 lung cancer and murine Lewis lung carcinoma (LLC) models were constructed, which were further i.v. injected with platinum-based drugs or concomitant administrated with anti-PD-1 antibody and or anti-NKG2D antibody. The tumor volume and the proportion of myeloid cells (CD45+CD11b+), CD3+T cells and NK (NK1.1+) cells were detected. The relative expression of chemokine (C-X-C motif) ligand 9 (CXCL9), CXCL10 and CXCL11 and C-X-C motif chemokine receptor 3 (CXCR3) was detected with the ELISA, western blot and flow cytometry. The three platinum drugs (cisplatin, DDP; carboplatin, CBP; OXA) showed similar effects to inhibit A549 tumor growth in immune-deficient mice. While OXA exhibited better antitumor efficacy in wild-type mice bearing LLC with downregulated myeloid cells proportion, upregulated concentration of CXCL9, CXCL10 and CXCL11, and upregulated proportion and CXCR3 expression on T cells and NK cells. OXA combined with anti-PD1 or anti-NKG2D synergistically improved tumor growth inhibition and survival. The combination of OXA to anti-PD1 and anti-NKG2D antibodies will provide the most appropriate treatment benefit. Oxaliplatin promotes T cells and NK cells infiltration through the CXCL9/10/11-CXCR3 axis to enhance anti-PD1 or anti-NKG2D immunotherapy in lung cancer.

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Reference:
Ester – Wikipedia,
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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Sister Mary Joseph nodule as cutaneous manifestations of metastatic ovarian cancer: A case report and review of the literature.》. Authors are Nie, Xianglin; Chen, Xing; Jiang, Yi; Zhong, Yi; Chen, Ting; Cheng, Wenjun.The article about the compound:cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II)cas:41575-94-4,SMILESS:O=C1C2(CCC2)C(O[Pt]O1)=O.N.N).Computed Properties of C6H12N2O4Pt. Through the article, more information about this compound (cas:41575-94-4) is conveyed.

RATIONALE: The Sister Mary Joseph’s nodule is an umbilical nodule resulting from the metastasis of malignant tumors in the pelvic and/or abdominal cavity. Sister Mary Joseph’s nodules are very rare, and the morphology of the skin lesions is not specific and is easily misdiagnosed. Here, we report a case of cutaneous manifestations of metastatic ovarian cancer. PATIENT CONCERNS: The patient was admitted to our hospital because of abdominal distention, and a nodule was found in the umbilicus. A computerized tomography scan of the entire abdomen showed nodular soft tissue in the subcutaneous fat space of the umbilical area and multiple pelvic masses, which were suspected metastases of peritoneal and omentum ovarian cancer. INTERVENTIONS: To confirm the pathological diagnosis, posterior fornix puncture was performed. Pathological biopsy showed adenocarcinoma. Histological examination revealed a mass arising from high-grade serous carcinoma of the ovary. The patient received 2 cycles of chemotherapy with paclitaxel liposomes and carboplatin and underwent interval debulking surgery. Postoperative pathology was consistent with high-grade serous carcinoma of the ovary. Cancer involvement was observed in umbilical lesions. After the operation, the patient was given 6 cycles of chemotherapy with paclitaxel liposomes and carboplatin. OUTCOMES: The patient underwent follow-up until October 2020. A computerized tomography scan of the entire abdomen showed that the lymph nodes in the abdominal cavity were larger than before, suggesting a platinum-sensitive relapse. After receiving the same regimen of chemotherapy, carbohydrate antigen 125 dropped to the normal range, and consolidated treatment was administered for 3 cycles. Owing to her BRCA1 mutations, olaparib was administered for maintenance treatment. Until now, she had been in the outpatient clinic for regular follow-up visits. LESSONS: The umbilicus remains an infrequently examined area, which cannot be underestimated and warrants careful clinical follow-up and histological evaluation, as appropriate.

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Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 153034-91-4, is researched, Molecular C5H2ClI2N, about Iterative and regioselective cross-couplings of 2-chloro-3,4-diiodopyridine leading to 2,3,4-triheteroarylpyridines, the main research direction is chloropyridine ortho metalation halogen dance; chlorodiiodopyridine preparation aryl boronic regioselective Suzuki Miyaura cross coupling; triheteroarylpyridine preparation; heteroaryl chloro iodopyridine preparation; chloro diheteroarylpyridine preparation; bis phenylethynylpyridinyl fluoropyridine preparation.Formula: C5H2ClI2N.

A one-pot synthesis of 2-chloro-3,4-diiodopyridine from 2-chloropyridine is described via a directed ortho metalation (DoM)/halogen dance (HD) mechanism in 26-28% yields. By performing sequential, iterative Suzuki-Miyaura cross-couplings using a variety of functionalized heteroaryl and arylboronic acids, a series of novel 2,3,4-triheteroarylpyridine scaffolds have been accessed in synthetically viable yields, including sterically hindered derivatives. 2-Chloro-4-heteroaryl-3-iodopyridines and 2-chloro-3,4-diheteroarylpyridines are also synthesized. The synthesis of 5-[3,4-bis(2-phenylethynyl)pyridin-2-yl]-2-fluoropyridine via a two-step Sonogashira/Suzuki-Miyaura reaction sequence from 2-chloro-3,4-diiodopyridine, phenylacetylene and 6-fluoropyridin-3-yl-3-boronic acid has been achieved in 48% overall yield.

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Reference:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II)( cas:41575-94-4 ) is researched.Reference of cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II).Aghajanian, Carol; Swisher, Elizabeth M; Okamoto, Aikou; Steffensen, Karina Dahl; Bookman, Michael A; Fleming, Gini F; Friedlander, Michael; Moore, Kathleen N; Tewari, Krishnansu S; O’Malley, David M; Chan, John K; Ratajczak, Christine; Hashiba, Hideyuki; Wu, Meijing; Dinh, Minh H; Coleman, Robert L published the article 《Impact of veliparib, paclitaxel dosing regimen, and germline BRCA status on the primary treatment of serous ovarian cancer – an ancillary data analysis of the VELIA trial.》 about this compound( cas:41575-94-4 ) in Gynecologic oncology. Keywords: Dose-dense paclitaxel; Homologous recombination deficiency; Ovarian cancer; PARP inhibitor; Veliparib; gBRCA. Let’s learn more about this compound (cas:41575-94-4).

OBJECTIVE: In the Phase 3 VELIA trial (NCT02470585), veliparib added to carboplatin plus paclitaxel concomitantly and as maintenance for women with newly-diagnosed advanced ovarian cancer significantly improved progression-free survival (PFS) versus chemotherapy alone. Here we present exploratory analyses by paclitaxel dosing schedule and germline BRCA (gBRCA) status. METHODS: Women with untreated ovarian carcinoma were randomized (1:1:1) to: veliparib during chemotherapy and maintenance (veliparib-throughout), veliparib during chemotherapy followed by placebo maintenance (veliparib-combination only), or placebo during chemotherapy and maintenance (control). Chemotherapy included carboplatin plus dose-dense (DD; weekly) or every-3-week (Q3W) paclitaxel (a stratification factor at randomization), selected at the investigator’s discretion pre-randomization. PFS was assessed by paclitaxel dosing schedule using a Cox proportional hazard model adjusted by treatment arm and stratification factors; safety was analyzed based on paclitaxel dosing schedule and gBRCA status. RESULTS: 1132 patients were analyzed by paclitaxel schedule. Pooled treatment arms demonstrated longer median PFS with DD (n = 586) versus Q3W (n = 546) paclitaxel (ITT: 20.5 vs 15.7 months, hazard ratio [HR] 0.77; homologous recombination proficient cancer: 15.1 vs 11.8 months, HR 0.64; BRCAwt: 18.0 vs 12.9 months, HR 0.70). Comparison between arms favored veliparib-throughout versus control in both DD (PFS, 24.2 vs 18.3 months, hazard ratio 0.67) and Q3W (19.3 vs 14.6, hazard ratio 0.69) subgroups. DD paclitaxel was associated with higher incidence of Grade 3/4 neutropenia, fatigue, and anemia versus Q3W. There were no differences in toxicity between gBRCAm (n = 211) and gBRCAwt (n = 902) subgroups. CONCLUSIONS: DD paclitaxel was tolerable and associated with longer PFS in the HR proficient and gBRCAwt groups, versus Q3W. gBRCA status did not impact safety.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Cost-Effectiveness of Pembrolizumab Versus Carboplatin and Paclitaxel in Patients With Unresectable or Metastatic Melanoma After First-Line Treatment in China., published in 2021-12-16, which mentions a compound: 41575-94-4, Name is cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II), Molecular C6H12N2O4Pt, Computed Properties of C6H12N2O4Pt.

OBJECTIVE: This study aimed to evaluate the cost-effectiveness of pembrolizumab compared with standard-of-care chemotherapy (paclitaxel + carboplatin [PC]) in patients with unresectable or metastatic melanoma after first-line treatment from a Chinese healthcare system perspective. METHODS: We conducted a partitioned-survival model with a 1-week cycle length and a 20-year base-case time horizon. Piecewise parametric models were fitted to KEYNOTE-006 trial data to estimate progression-free survival and overall survival for pembrolizumab, and a network meta-analysis was used to estimate the clinical outcomes for standard of care. Quality-adjusted life-years (QALYs) were calculated using EQ-5D data from KEYNOTE-006, applying Chinese-specific utility tariffs. Costs included drug acquisition, administration, adverse events, and disease management, reflecting the Chinese pricing system. Chinese-specific disease management costs were estimated based on clinical opinion on health state resource use and chemotherapy-related adverse events. Costs and outcomes were discounted at 5% annually. Multiple deterministic and probabilistic sensitivity analyses were performed to test the robustness of the results. RESULTS: In the base-case analysis, the treatment of pembrolizumab is estimated to yield 2.63 life-years (LYs) and 2.24 QALYs at an incremental cost of ¥372 316.46 versus PC. The incremental costs per LY and per QALY were ¥141 771.00 and ¥165 865.69, respectively, the latter being below a threshold of 3 times the per capita gross domestic product (￥193 932) in China, deemed as cost-effective according to the World Health Organization threshold. These findings were robust against a wide range of sensitivity analyses. CONCLUSIONS: Pembrolizumab is projected as cost-effective compared with PC in patients with unresectable or metastatic melanoma after first-line treatment in China.

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Reference:
Ester – Wikipedia,
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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Cancer (Hoboken, NJ, United States) called The cumulative incidence of cisplatin-induced hearing loss in young children is higher and develops at an early stage during therapy compared with older children based on 2052 audiological assessments, Author is Meijer, Annelot J. M.; Li, Kathy H.; Brooks, Beth; Clemens, Eva; Ross, Colin J.; Rassekh, Sharad R.; Hoetink, Alex E.; van Grotel, Martine; van den Heuvel-Eibrink, Marry M.; Carleton, Bruce C., which mentions a compound: 41575-94-4, SMILESS is O=C1C2(CCC2)C(O[Pt]O1)=O.N.N, Molecular C6H12N2O4Pt, Synthetic Route of C6H12N2O4Pt.

Ototoxicity is a common adverse event of cisplatin treatment. The authors investigated the development of cisplatin-induced hearing loss (CIHL) over time in children with cancer by age and examined the influence of other clin. characteristics on the course of CIHL. Data from Canadian patients with childhood cancer were retrospectively reviewed. Hearing loss was graded according to International Society of Pediatric Oncol. criteria. The Kaplan-Meier method was applied to estimate the cumulative incidence of CIHL for the total cohort and according to age. Cox regression models were used to explore the effects of independent variables on CIHL development up to 3 years after the start of therapy. In total, 368 patients with 2052 audiol. assessments were included. Three years after initiating therapy, the cumulative incidence of CIHL was highest in patients aged ≤5 years (75%; 95% confidence interval [CI], 66%-84%), with a rapid increase observed to 27% (95% CI, 21%-35%) at 3 mo and to 61% (95% CI, 53%-69%) at 1 yr, compared with patients aged >5 years (48%; 95% CI, 37%-62%; P < .001). The total cumulative dose of cisplatin at 3 mo (per 100 mg/m2 increase: hazard ratio [HR], 1.20; 95% CI, 1.01-1.41) vincristine (HR, 2.87; 95% CI, 1.89-4.36) and the total duration of concomitantly administered antibiotics (>30 days: HR, 1.85; 95% CI, 1.17-2.95) further influenced CIHL development over time. In young children, the cumulative incidence of CIHL is higher compared with that in older children and develops early during therapy. The course of CIHL is further influenced by the total cumulative dose of cisplatin and other ototoxic (co-)medication. These results highlight the need for audiol. monitoring at each cisplatin cycle.

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Reference:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics