Takita T, Ogino T
Institute of Microbiol Chemistry, Tokyo.
Biomed Pharmacother. 1987;41(5):219-26.
Peplomycin, derivative of Bleomycin which was developed because of a lower pulmonary toxicity and broader anti-tumor spectrum in animal study, also showed to be effective in clinical studies on adenocarcinomas such as prostatic cancer, breast cancer, etc. as well as on squamous cell carcinoma and the anti-tumor spectrum were observed to be broader than those of Bleomycin. Further, the combination therapy with other anti-cancer drugs showed higher effectiveness. Clinically lower pulmonary toxicity was also observed. Liblomycin, derivative of Bleomycin having a lipophyllic characteristics, was developed since it showed in animal studies a lower pulmonary toxicity than that of Peplomycin and broader anti-tumor spectrum. At present, this substance is under Phase I study in Japan.
培洛霉素是博来霉素的衍生物,在动物研究中因其较低的肺部毒性和更广泛的抗肿瘤谱而被研发,在前列腺癌、乳腺癌等腺癌以及鳞状细胞癌的临床研究中也显示出有效性,且观察到其抗肿瘤谱比博来霉素更广。此外,与其他抗癌药物联合治疗显示出更高的疗效。临床上也观察到较低的肺部毒性。利布洛霉素是具有亲脂性特征的博来霉素衍生物,由于在动物研究中显示出比培洛霉素更低的肺部毒性和更广泛的抗肿瘤谱而被研发。目前,该物质在日本正处于I期研究阶段。