Open Label, Dose Escalation Trial of Oral 4SC-205 in Patients With Advanced Malignancies: First-In-Man Study of a Newly Developed, Oral Inhibitor of Kinesin-spindle Protein, Eg5

The purpose of the study is to investigate safety and tolerability of repeated ascending oral doses of 4SC-205 in patients with advanced and incurable solid tumors or malignant lymphomas.

开始日期2010-01-01

申办/合作机构

4SC AG

100 项与盐酸领克尼斯相关的临床结果

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100 项与盐酸领克尼斯相关的转化医学

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100 项与盐酸领克尼斯相关的专利（医药）

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项与盐酸领克尼斯相关的文献（医药）

2005-01-01·Drug Development and Industrial Pharmacy

Evaluation of Different Fast Melting Disintegrants by Means of a Central Composite Design

Article

作者: Sante Martelli ; Pascal Wehrlé ; Piera Di Martino

Fast-disintegration technologies have encountered increased interest from industries in the past decades. In order to orientate the formulators to the choice of the best disintegrating agent, the most common disintegrants were selected and their ability to quickly disintegrate direct compressed tablets was evaluated. For this study, a central composite design was used. The main factors included were the concentration of disintegrant (X1) and the compression force (X2). These factors were studied for tablets containing either Zeparox or Pearlitol 200 as soluble diluents and six different disintegrants: L-HPC LH11 and LH31, Lycatab PGS, Vivasol, Kollidon CL, and Explotab. Their micromeritics properties were previously determined. The response variables were disintegration time (Y1), tensile strength (Y2), and porosity (Y3). Whatever the diluent, the longest disintegration time is obtained with Vivasol as the disintegrant, while Kollidon CL leads to the shortest disintegration times. Exception for Lycatab PGS and L-HPC LH11, formulations with Pearlitol 200 disintegrate faster. Almost the same results are obtained with porosity: no relevant effect of disintegrant concentration is observed, since porosity is mainly correlated to the compression force. In particular, highest values are obtained with Zeparox as the diluent when compared to Pearlitol 200 and, as the type of disintegrant is concerned, no difference is observed. Tensile strength models have been all statistically validated and are all highly dependent on the compression force. Lycatab PGS concentration does not affect disintegration time, mainly increased by the increase of compression pressure. When Pearlitol 200 is used with Vivasol, disintegration time is more influenced by the disintegrant concentration than by the compression pressure, an increase in concentration leading to a significant and relevant increase of the disintegration time. With Zeparox, the interaction between the two controlled variables is more complex: there is no effect of compression force on the disintegration time for a small amount of disintegrant, but a significant increase for higher concentrations. With Kollidon CL, the main factor influencing the disintegration time is the compression force, rather than the disintegrant concentration. Increasing both the compression force and the disintegrant concentration leads to an increase of the disintegration time. For lower Kollidon CL percentages, the compression pressure increases dramatically the tablet disintegration. With the Explotab, whatever the increase of compression force, the disintegrant concentration leads to an increase of the disintegration time. According to Student's t-test, only the compression force significantly and strongly influences the disintegration time when Pearlitol 200 is used. A slight interaction and some trends nevertheless appear: above 150 MPa, increasing the disintegrant concentration leads to a shortened disintegration time, below this limit the opposite effect is observed.

1993-01-01·Pharmaceutical Research3区 · 医学

Low-substituted hydroxypropylcellulose as a sustained-drug release matrix base or disintegrant depending on its particle size and loading in formulation.

3区 · 医学

Article

作者: Tzu-Lang Lin ; Toshiyuki Niwa ; Fujio Sekigawa ; Tomoaki Hino ; Hirofumi Takeuchi ; Keiko Kawahara ; Yoshiaki Kawashima

Tablets of acetaminophen as a model drug were prepared with low-substituted hydroxypropylcellulose (L-HPC) of various particle sizes at various loadings in the formulation. Drug release into an aqueous dissolution medium (pH 1.2) was remarkably sustained from tablets prepared with fine L-HPC (LH41) at loadings of more than 20%. Tablets prepared with less than 20% LH41 or with coarse L-HPCs (LH11, LH21, and LH31) disintegrated in the medium, resulting in rapid release of the drug. The difference in behavior could not be explained in terms of differences in tablet strength, but in swelling and water uptake abilities of the tablet's polymer. Swelling work (swelling force), water penetration speed, and water uptake of LH41 (4.4-microns average particle size) were much smaller than those of coarse L-HPCs. The formation of a continuous gel-like layer on the surface of tablets containing more than 20% LH41 was another factor to sustain the drug release rate.

100 项与盐酸领克尼斯相关的药物交易

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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2期	中国台湾	广州领晟医疗科技有限公司	2019-08-05
晚期恶性实体瘤	临床2期	德国	4SC AG	2010-01-01
肝癌	临床2期	中国	广州领晟医疗科技有限公司	-
肺癌	临床2期	中国	广州领晟医疗科技有限公司	-
淋巴瘤	临床1期	中国	广州领晟医疗科技有限公司	-
淋巴瘤	临床1期	-	Takeda Pharmaceutical Co., Ltd.	-

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


CSCO2020	临床1期	浆细胞骨髓瘤难治	6	LH031 20mg	(夢簾餘夢鹹壓獵鹽憲膚) = 艱積壓簾餘選鏇鹽選壓選鹹蓋遞積糧襯觸糧壓 (積憲選願壓餘獵選製鬱 )	-	2020-09-19
NCT01065025 (ASCO2015)	临床1期	-	59	4SC-205	獵製廠醖壓製範齋艱鏇(廠獵糧蓋齋蓋襯顧憲願) = 獵齋糧壓觸窪衊獵築網蓋觸襯選鹹廠憲築壓餘 (願衊憲膚糧繭簾蓋鹹範 )	-	2015-05-20