Since their addition to paclitaxel in the oncologists' armamentarium in the early 1990s, several new taxane formulations have been developed. Besides docetaxel and nab-paclitaxel, new analogs with better therapeutic profiles are being investigated. The goals of this next generation of taxanes are to improve the toxicity profile and efficacy, and to overcome resistance patterns. Several new taxanes, including cabazitaxel, paclitaxel poliglumex, paclitaxel+endotag, and polymeric-micellar paclitaxel, have shown clinical efficacy. These chemotherapeutics are part of many ongoing phase II and III studies on various cancer types. In addition, there are immunotoxins that link key antibodies to mitotic spindle inhibitors (trastuzumab emtansine and brentuximab vedotin). Through this mechanism, novel formulations increase cytotoxicity, improve specificity, and create possibilities for drug enhancement.

2012-11-01·Journal of Controlled Release1区 · 医学

Liposomal paclitaxel formulations

1区 · 医学

Review

作者: Jaroslav Turánek ; Štěpán Koudelka

Over the past three decades, taxanes represent one of the most important new classes of drugs approved in oncology. Paclitaxel (PTX), the prototype of this class, is an anti-cancer drug approved for the treatment of breast and ovarian cancer. However, notwithstanding a suitable premedication, present-day chemotherapy employing a commercial preparation of PTX (Taxol®) is associated with serious side effects and hypersensitivity reactions. Liposomes represent advanced and versatile delivery systems for drugs. Generally, both in vivo mice tumor models and human clinical trials demonstrated that liposomal PTX formulations significantly increase a maximum tolerated dose (MTD) of PTX which outperform that for Taxol®. Liposomal PTX formulations are in various stages of clinical trials. LEP-ETU (NeoPharm) and EndoTAG®-1 (Medigene) have reached the phase II of the clinical trials; Lipusu® (Luye Pharma Group) has already been commercialized. Present achievements in the preparation of various liposomal formulations of PTX, the development of targeted liposomal PTX systems and the progress in clinical testing of liposomal PTX are discussed in this review summarizing about 30 years of liposomal PTX development.

2008-01-01·Chemotherapy4区 · 医学

Nine Months to Progression Using Fourth-Line Liposomally Encapsulated Paclitaxel against Hepatocellular Carcinoma

4区 · 医学

Article

作者: Naujoks, Kurt ; Lenz, Georg ; Schalhorn, Andreas ; Christopeit, Maximilian ; Bartelheim, Kerstin ; Kuehnbach, Robert ; Forstpointner, Roswitha

Background: Hepatocellular carcinoma (HCC) is the third most common cause of cancer deaths. Difficulties to diagnose HCC at early stages remain the major obstacle to curative (surgical) therapy. Therapy in advanced stages has to be considered palliative. In this situation, a considerable amount of attention should be paid to innovative treatment strategies, e.g. including antiangiogenetic drugs. Results: We report on the successful treatment of a patient suffering from progressive HCC with a novel drug (EndoTAG®-1, formerly named LipoPac®) currently investigated in phase II studies. This drug consists of liposomally encapsulated paclitaxel. Its liposomal formulation favors the drug’s adherence to the tumor neovasculature, in effect starving the tumor. Conclusions: EndoTAG®-1 stopped tumor progression for 9 months in our patient. This, along with successes observed testing this drug against other indications, makes it a suitable candidate for future clinical trials.

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适应症	最高研发状态	国家/地区	公司	日期
实体瘤	临床3期	德国	The University of California, San Francisco	-
肿瘤	临床前	德国	Munich Biotech AG	2004-04-01
肿瘤	临床前	德国	Johann Wolfgang Goethe-Universität Frankfurt am Main	2004-04-01