Morgan R J, Doroshow J H, Venkataraman K, Chang K, Raschko J, Somlo G, Leong L, Tetef M, Shibata S, Hamasaki V, Margolin K, Forman S, Akman S, Coluzzi P, Ahn C, Weiss L, Gadgil U, Harrison J
Department of Medical Oncology, City of Hope National Medical Center, Duarte, California 91010, USA.
Clin Cancer Res. 1997 Dec;3(12 Pt 1):2337-45.
The purpose of this study was to determine the maximally tolerated dose of doxorubicin administered during two cycles of intensive chemotherapy with cyclophosphamide and doxorubicin without stem cell support in patients with advanced cancer and to assess the cumulative cardiac toxicity of the regimen by noninvasive radionuclide imaging and by pre-and postchemotherapy endomyocardial biopsies. Thirty-eight patients (thirty-six with high risk or metastatic breast cancer) were treated in a dose-escalation trial using a fixed dose of i.v. cyclophosphamide (4.2 g/m2) administered over 2 h on day 5 and escalating doses of doxorubicin (50-175 mg/m2) given as a 96-h continuous i.v. infusion on days 1-4, using Filgrastim (granulocyte colony-stimulating factor) for hematological support beginning on day 6. All patients underwent pretreatment, and 28 patients underwent postchemotherapy endomyocardial biopsies. Twenty-nine of 38 patients received two cycles of treatment (median number of days between cycles, 44; range, 34-62). Twenty-one patients had received doxorubicin previously at cumulative dose levels </=150 mg/m2; all patients had pretreatment endomyocardial biopsy scores less than 1. One patient treated at the highest dose level of doxorubicin (175 mg/m2) developed symptoms of mild congestive heart failure following two cycles of chemotherapy. Pre- and posttreatment radionuclide ejection fractions were 65 and 45%, respectively; this patient had a posttreatment endomyocardial biopsy score of 1 (damage to <5% of myocytes). One additional patient at this dose level had an asymptomatic biopsy score of 1, with a decrease in ejection fraction from 62 to 43%; this recovered to 58% 5 months after completion of chemotherapy. Six additional patients treated at lower dose levels had abnormal posttreatment endomyocardial biopsies without abnormal posttreatment ejection fractions. Nine patients received only one cycle of chemotherapy: five patients due to decreased cardiac ejection fraction following cycle 1 (two of these patients had normal endomyocardial biopsies, and two patients had biopsy scores of 1); one patient secondary to tumor progression following cycle one; one patient due to persistently detectable Clostridium difficile toxin in the stool; one patient refused cycle two; and one patient died following cycle one of complications related to sepsis. A single patient experienced a grand mal seizure associated with orthostatic hypotension, which was considered the dose-limiting toxicity. The median duration (over two cycles) of granulocytopenia (absolute granulocyte count <500/microliter) at the maximally tolerated dose level of 150 mg/m2 was 8.5 days (range, 5-13 days), and the median duration of thrombocytopenia (platelets <20,000/microliter) was 2.5 days (range, 0-9 days). The median duration of hospitalization including chemotherapy administration was 23 days (range, 19-36 days). Other toxicities included stomatitis, fever, diarrhea, and emesis. One patient developed acute leukemia 54 months posttreatment. We conclude that two courses of high-dose cyclophosphamide and doxorubicin using granulocyte colony-stimulating factor are feasible and safe with tolerable myocardial toxicity as evidenced by serial endomyocardial biopsies. The dose-limiting toxicity encountered was a grand mal seizure. The recommended Phase II dose is doxorubicin 150 mg/m2 administered as a 96-h infusion on days 1-4, with cyclophosphamide 4. 2 g/m2 on day 5 and G-CSF 5 microgram/kg/day started on day 6 and administered until the total WBC is above 10,000/microliter for three consecutive days.
本研究的目的是确定在晚期癌症患者中,在不进行干细胞支持的情况下,环磷酰胺和阿霉素强化化疗两个周期期间给予阿霉素的最大耐受剂量,并通过无创放射性核素成像以及化疗前后的心内膜活检来评估该方案的累积心脏毒性。38例患者(36例高危或转移性乳腺癌患者)参加了剂量递增试验,在第5天静脉注射固定剂量的环磷酰胺(4.2 g/m²),持续2小时,第1 - 4天静脉持续输注递增剂量的阿霉素(50 - 175 mg/m²),从第6天开始使用非格司亭(粒细胞集落刺激因子)进行血液学支持。所有患者均接受了预处理,28例患者进行了化疗后的心内膜活检。38例患者中有29例接受了两个周期的治疗(周期之间的中位天数为44天;范围为34 - 62天)。21例患者之前接受过累积剂量≤150 mg/m²的阿霉素治疗;所有患者预处理时的心内膜活检评分均小于1。1例接受最高剂量阿霉素(175 mg/m²)治疗的患者在两个周期化疗后出现轻度充血性心力衰竭症状。治疗前和治疗后的放射性核素射血分数分别为65%和45%;该患者化疗后的心内膜活检评分为1(心肌细胞损伤<5%)。该剂量水平的另外1例患者无症状活检评分为1,射血分数从62%降至43%;化疗完成后5个月恢复至58%。另外6例接受较低剂量治疗的患者化疗后心内膜活检异常,但治疗后射血分数无异常。9例患者仅接受了一个周期的化疗:5例患者因第1周期后心脏射血分数降低(其中2例患者心内膜活检正常,2例患者活检评分为1);1例患者因第1周期后肿瘤进展;1例患者因粪便中持续检测到艰难梭菌毒素;1例患者拒绝第2周期治疗;1例患者在第1周期后死于与败血症相关的并发症。1例患者发生了与体位性低血压相关的癫痫大发作,被认为是剂量限制性毒性。在最大耐受剂量水平150 mg/m²时,粒细胞减少(绝对粒细胞计数<500/微升)的中位持续时间(超过两个周期)为8.5天(范围为5 - 13天),血小板减少(血小板<20,000/微升)的中位持续时间为2.5天(范围为0 - 9天)。包括化疗给药在内的住院中位持续时间为23天(范围为19 - 36天)。其他毒性包括口腔炎、发热、腹泻和呕吐。1例患者在治疗后54个月发生急性白血病。我们得出结论,使用粒细胞集落刺激因子进行两个疗程的高剂量环磷酰胺和阿霉素治疗是可行且安全的,连续的心内膜活检证明心肌毒性可耐受。遇到的剂量限制性毒性是癫痫大发作。推荐的II期剂量为阿霉素150 mg/m²,在第1 - 4天进行96小时输注,第5天给予环磷酰胺4.2 g/m²,第6天开始给予G - CSF 5微克/千克/天,持续给药直至白细胞总数连续三天高于10,000/微升。