Asaishi K, Tominaga T, Abe O, Izuo M, Nomura Y
Dept. of Surgery I, Sapporo Medical College.
Gan To Kagaku Ryoho. 1993 Jan;20(1):91-9.
Efficacy and safety of high dose administration of NK 622 (toremifene citrate) were studied in tamoxifen (TAM)--failed patients with breast cancer. The patients included in the study were the following failure cases in TAM therapy: unresponded cases in TAM therapy (TAM unresponded cases), temporary responded (CR, PR) but progressed cases in TAM therapy (TAM temporary responded cases), and those relapsing during TAM adjuvant therapy or within 6 months after the adjuvant therapy (TAM adjuvant failed cases). NK 622 of a 120 mg/day dose were orally given daily once at least for 8 weeks. The response rates in evaluable cases were 6.3% (1/16) in TAM unresponded cases, 11.1% (1/9) in TAM temporary responded cases, 15.4% (4/26) in TAM adjuvant failed cases, and 11.8% (6/51) in total cases including 1 CR and 5 PR cases. Long NC in which duration of NC maintained for more than 6 months was observed in 18.8% (3/16) of TAM unresponded cases, 22.2% (2/9) of TAM temporary responded cases, 11.5% (3/26) of TAM adjuvant failed cases, and 15.7% (8/51) of total cases. Rates of response and long NC were 14.3 and 19.0% in postmenopausal patients with estrogen receptor positive cancer, respectively. A median value of duration to the onset of response was 34 days (15-137). Median duration of response and long NC were 127 days (39-381) and 238.5 days (178-281), respectively. Adverse effects were experienced in 3 (5.1%) of 59 patients: nausea in 1, vertigo in 1 and increase of GOT, GPT, LDH and gamma-GTP in another 1. The side effects were moderate and reversible. From these results, NK 622 seems to become a safe and effective drug for TAM-failed patients with breast cancer by using a 120 mg/day dose.
在他莫昔芬（TAM）治疗失败的乳腺癌患者中研究了高剂量服用NK 622（枸橼酸托瑞米芬）的疗效和安全性。纳入该研究的患者为TAM治疗的以下失败病例：TAM治疗无反应病例（TAM无反应病例）、TAM治疗时暂时有反应（CR、PR）但病情进展的病例（TAM暂时有反应病例），以及在TAM辅助治疗期间或辅助治疗后6个月内复发的病例（TAM辅助治疗失败病例）。以每日120mg的剂量口服NK 622，每日一次，至少服用8周。可评估病例中的反应率在TAM无反应病例中为6.3%（1/16），在TAM暂时有反应病例中为11.1%（1/9），在TAM辅助治疗失败病例中为15.4%（4/26），在包括1例CR和5例PR病例的所有病例中为11.8%（6/51）。在TAM无反应病例的18.8%（3/16）、TAM暂时有反应病例的22.2%（2/9）、TAM辅助治疗失败病例的11.5%（3/26）以及所有病例的15.7%（8/51）中观察到无进展生存期（NC）持续超过6个月的长NC。绝经后雌激素受体阳性癌症患者的反应率和长NC率分别为14.3%和19.0%。反应开始的中位持续时间为34天（15 - 137天）。反应和长NC的中位持续时间分别为127天（39 - 381天）和238.5天（178 - 281天）。59例患者中有3例（5.1%）出现不良反应：1例恶心，1例眩晕，另1例谷草转氨酶、谷丙转氨酶、乳酸脱氢酶和γ - 谷氨酰转肽酶升高。这些副作用为中度且可逆。从这些结果来看，通过使用每日120mg的剂量，NK 622似乎成为TAM治疗失败的乳腺癌患者的一种安全有效的药物。
