本帖最后由 webslave 于 2011-7-27 15:40 编辑
我查了一下相关资料，是通过抑制组蛋白脱乙酰酶起作用，具体抑制剂的作用机制没弄清楚，官方报告I期对各种肿瘤进行试验的结果，有50%的病人进入无进展期，效果不错，相信这样的药会越来越多，不同的药适合不同的病人。
Resminostat (4SC-201)
Resminostat is an orally administered histone deacetylase (HDAC) inhibitor for the treatment of cancers, which modifies the DNA structure of tumour cells to cause their differentiation and programmed cell death (apoptosis). In contrast to many conventional cytotoxic drugs, because of their epigenetic mechanism the efficacy of HDAC inhibitors does not depend on the active process of cell division. As a result, HDAC inhibitors can also target cancer cells which are not actively dividing. The application of resminostat as a cancer treatment therefore opens up a broad spectrum of possibilities, in particular in combination with a number of standard chemotherapies.
Resminostat is currently in a Phase II proof-of-concept study to treat hepatocellular carcinoma (HCC) – the most common form of liver cancer –, a Phase II study in Hodgkin’s lymphoma (HL) and a Phase I / II study in advanced colorectal cancer patients with KRAS mutations (CRC).
As HDAC inhibitors modify the DNA structure of tumour cells, they offer a mechanism of action that has the potential to stop tumour progression and induce tumour regression and therefore aim to gain the therapeutic control of the cancer. In a completed Phase I trial in patients with various cancer types, stable disease was achieved in over 50% of the patients, whilst the treatment was well tolerated and showed a positive, differentiating pharmacological profile compared to other drugs in this class.
The two-arm, proof-of-concept, Phase II SHELTER study evaluates the second-line treatment with resminostat alone or in combination with sorafenib (Nexavar®), the current standard of care in advanced HCC, to see if it can induce progression free survival and tumour responses in patients who display progressive disease under treatment with sorafenib. Initial clinical data have already been published. So far, resminostat has proven to be safe and well tolerated. No pharmacokinetic interactions were observed between resminostat and sorafenib. A considerable portion of patients showed stabilisation of their disease after 6 or 12 weeks of study treatment.
The Phase II SAPHIRE trial evaluates the efficacy of resminostat for the treatment of HL patients who are refractory or who relapsed after the classical treatment method of chemotherapy. Initial preliminary trial data on the compound’s safety and efficacy have already been published. Based on the results, about half of the 18 patients included in the first recruitment cohort benefited from treatment with resminostat. Two of these patients were assessed as partial responders whilst additional patients showed a stabilisation of their disease.
The Phase I / II SHORE trial evaluates the efficacy and tolerability of resminostat in colon cancer as a third indication. In this trial resminostat is evaluated in combination with the FOLFIRI regimen, an established, frequently used form of chemotherapy to treat colon cancer, as a second-line treatment in patients with KRAS tumour mutations.
|
显身卡
