盐酸伊达比星的半合成研究

以柔红霉索为原料，经八步反应制得盐酸伊达比星，总收率为24．2％。本法具有反应路线短，反应条件温和，操作简单等优点，适合工业化生产。     

地西他滨联合IAG/DAG治疗急性髓系白血病的临床疗效

目的 探讨地西他滨（DAC）联合IAG/DAG治疗急性髓系白血病（AML）的临床疗效与安全性。方法 选取2017年6月至2019年12月安徽医科大学第一附属医院血液科收治的23例初治或复发AML患者,采用DAC联合IAG/DAG诱导治疗,统计分析临床疗效及安全性。结果 23例患者均予以DAC联合IAG/DAG诱导化疗,其中完全缓解13例,部分缓解2例,总有效率为65.22%。23例患者均出现Ⅲ～Ⅳ级的粒细胞和血小板减少,1例患者因严重脑出血死亡。结论 DAC联合IAG/DAG治疗AML临床疗效较好,且不良反应可耐受,安全性高,值得临床推广应用。     

阿糖胞苷分别联合柔红霉素和去甲氧柔红霉素诱导治疗初治急性髓系白血病临床效果比较

目的：比较柔红霉素联合阿糖胞苷（DA）方案和去甲氧柔红霉素联合阿糖胞苷（IA）方案诱导治疗初治急性髓系白血病（AML）的临床疗效及患者不良反应。方法回顾性分析应用 DA 方案或 IA方案诱导缓解治疗的84例初治 AML（除外 M3）患者临床资料。 DA 组32例,其中男性17例,女性15例,中位年龄46岁;IA 组52例,其中男性29例,女性23例,中位年龄49岁。疗效指标为化疗1个疗程后的完全缓解（CR）率、总有效率和不良反应发生率。结果 DA 组 CR 率为65.6％（21／32）,总有效率为75.0％（24／32）;IA 组 CR 率为71.2％（31／52）,总有效率为80.8％（42／52）,两组 CR 率和总有效率差异均无统计学意义（均 P＞0.05）。两组患者中位生存时间和5年生存率差异均无统计学意义（DA 与IA 组中位生存时间：16.8个月比24.9个月,5年生存率：26%比44%,均 P＞0.05）。两组不良反应包括血液学（主要为骨髓抑制）和非血液学不良反应,两组间各不良反应发生率差异均无统计学意义（均 P＞0.05）。结论对于初治 AML 患者,DA 方案诱导治疗1个疗程的缓解率和总有效率与 IA 方案相当,且两方案的不良反应发生率无明显不同。     

A phase I/II study of oral etoposide and idarubicin in elderly patients with high-risk acute myeloid leukemia unable to undergo intensive chemotherapy

Acute myeloid leukemia (AML) is a disease of mostly elderly patients who are often unable to undergo intensive intravenous chemotherapy. In an attempt to provide an all-oral regimen suitable for palliative treatment, we assessed the antileukemic efficacy of combination therapy of idarubicin 20 mg/m² (days 1, 3, and 5) and etoposide (EI) in increasing doses (75–125 mg/m²) on days 1–5. Eleven patients were included (median age 69 years, range: 56–77) with prognostically unfavorable characteristics (myelodysplastic syndrome, relapse, or unfavorable karyotypes). No complete remission and five partial remissions were observed whereas four patients had persistent leukemia. There were two patients who succumbed to early death. Median overall survival was 100 days (range: 8–493 days). Nonhematological toxicities were acceptable with nausea/vomiting being the predominant side effect. Hematological toxicity with grade III/IV aplasia was seen in all patients. In this study EI did not show convincing antileukemic efficacy and was unable to induce clinically useful complete remissions, with a substantial risk profile. In contrast to the situation of elderly patients with standard-risk AML in which similar oral treatment has shown promising activity, EI cannot be recommended for elderly patients with high-risk AML.     

Intensive chemotherapy with idarubicin, cytarabine, etoposide, and G-CSF priming in patients with advanced myelodysplastic syndrome and high-risk acute myeloid leukemia

In an attempt to improve the complete remission (CR) rates and to prolong the remission duration especially in elderly patients >50 years of age, we have used a combination chemotherapy of idarubicin (10 mg/m² IV×3 days), cytarabine (AraC, 100 mg/m² CIVI×7d), and etoposide (100 mg/m²×5 days) in combination with granulocyte colony-stimulating factor (G-CSF) priming [5 mg/kg SQ day 1 until absolute neutrophil count (ANC) recovery] for remission induction. Responding patients received two consolidation courses of idarubicin, AraC, and etoposide, followed by a late consolidation course of intermediate-dose AraC (600 mg/m² IV every 12 h×5 days) and amsacrine (60 mg/m² IV×5 days). A total of 112 patients (57 male/55 female) with a median age of 58 years (range: 22–75) have been entered and are evaluable for response: 19 refractory anemia with excess of blast cells in transformation (RAEB-T), 84 acute myeloid leukemia (AML) evolving from myelodysplastic syndrome (MDS), and 9 secondary AML after chemotherapy/radiotherapy. The overall CR rate was 62%, partial remission (PR) rate 10%, treatment failure 16%, and early death rate 12%. The CR rate was higher in patients 60 years (68 vs 55%), mainly due to a lower early death rate (5 vs 21%, p<0.001). After a median follow-up of 58 months, the median overall survival is 14.5% and median duration of relapse-free survival 8 months. After 60 months, the probability of CR patients to still be in CR and alive is 16% (20% in patients 60 years and 13% in patients >60 years), while the probability of overall survival is 12% (15% in patients 60 years and 9% in patients >60 years). Compared to our previous trial (AML-MDS Study 01-92) which was done with identical chemotherapy but no G-CSF priming in 110 patients with RAEB-T, AML after MDS, or secondary AML (identical median age, age range, and distribution of subtypes), the CR rate in all patients, as well as CR rate, overall survival, and relapse-free survival in patients >60 years have significantly been improved. Thus, intensive chemotherapy with G-CSF priming is both well tolerated and highly effective for remission induction in these high-risk patients.     

Results of conventional-dose cytosine arabinoside and idarubicin in elderly patients with acute myeloid leukemia

Summary Conventional-dose Ara-C (200 mg/m² d 1–5) combined with idarubicin (12 mg/m² d 1–3) was employed as remission induction and consolidation therapy in 23 elderly AML patients with a median age of 66 years (range, 60–75) with AML according to the FAB criteria (M1n=3, M2n=10, M4n=6, M5n=2, M6n=2), eligible for the study. In seven patients earlier MDS had been documented by previous bone marrow aspirates. The CR rate after one induction course was 65% (15/23). Toxicity was acceptable, with four patients dying during the chemotherapy-induced hypoplasia (4/23). Although 80% of the CR patients received two additional cycles of Ara-C and idarubicin as consolidation therapy, only two patients are still in continuous complete remission more than 12 months after achieving CR. The median disease-free survival of the CR patients was 11.5 months and the median survival of the entire group was 10 months. We conclude that conventional dose Ara-C/idarubicin is an effective protocol for inducing complete remission in elderly patients with AML, but that consolidation therapy consisting of two courses of the same regimen does not produce a relevant rate of long-term disease-free survival.     

去甲氧柔红霉素与硼替佐米治疗血液肿瘤的疗效对比观察

目的比较去甲氧柔红霉素与硼替佐米治疗血液肿瘤的疗效和不良反应。方法将68例血液肿瘤患者随机分为两组,观察组38例,采用去甲氧柔红霉素治疗,对照组60例,采用硼替佐米治疗,对两组患者的治疗过程跟踪观察,治疗结束后评价其近期疗效及不良反应。结果疗程结束后,观察组38例患者中,显效18例,有效16例,无效4例,有效率为89.5%;对照组60例患者中,显效28例,有效14例,无效18例,有效率为70.0%,两组间有效率的差异具有统计学意义(P<0.05)。观察组患者骨髓抑制的发生率显著低于对照组(P<0.05),其他不良反应的发生率无明显差异。结论采用去甲氧柔红霉素治疗血液肿瘤效果较为显著,安全性较好,值得临床推广应用。