Characterization and phase I study of CLR457, an orally bioavailable pan-class I PI3-kinase inhibitor [0.03%]
一种口服生物可利用的泛类一PI3-激酶抑制剂CLR457的特性及Ⅰ期临床研究
James J Harding,Todd M Bauer,Daniel S W Tan et al.
James J Harding et al.
Background CLR457 is an orally bioavailable pan-phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) inhibitor. Methods CLR457 anti-tumor activity and pharmacokinetics (PK) were characterized by in vitro biochemical assays and in vivo tumo...
Clinical Trial
Investigational new drugs. 2019 Apr;37(2):271-281. DOI:10.1007/s10637-018-0627-4 2019
A natural compound derivative P-13 inhibits STAT3 signaling by covalently inhibiting Janus kinase 2 [0.03%]
天然化合物P-13通过共价抑制Janus激酶2信号转导及统计激活蛋白3信号通路
Hui Huang,Junxing Niu,Fei Wang et al.
Hui Huang et al.
We investigated the function and molecular mechanisms of 2-desoxy-4β-propylcarbamate-pulchellin (P-13), a sesquiterpene lactone derivative of 2-desoxy-4-epi-pulchellin from the traditional Chinese medicinal herb Carpesium abrotanoides L, i...
Development of apratoxin S10 (Apra S10) as an anti-pancreatic cancer agent and its preliminary evaluation in an orthotopic patient-derived xenograft (PDX) model [0.03%]
Apratoxin S10（Apra S10）作为抗胰腺癌药物的开发及其在原位患者来源异种移植模型中的初步评估
Weijing Cai,Ranjala Ratnayake,Michael H Gerber et al.
Weijing Cai et al.
Despite the significant progress in the field of cancer therapeutics, the incidence of pancreatic cancer (PC) has continuously increased. One possible mechanism for this increasing burden is impaired drug delivery and drug resistance result...
Sarcoid-like reaction mimicking disease progression in an ALK-positive lung cancer patient receiving lorlatinib [0.03%]
Lorlatinib治疗的阳性肺癌患者中类似 sarcoid反应的药物反应被误认为是疾病进展
Francesco Facchinetti,Letizia Gnetti,Valeria Balestra et al.
Francesco Facchinetti et al.
The administration of target inhibitors is paramount to grant the longest survival in patients with ALK-positive non-small cell lung cancer (NSCLC). The eventual resistance to tyrosine kinase inhibitors (TKI) is monitored clinically and rad...
HER-targeted tyrosine kinase inhibitors enhance response to trastuzumab and pertuzumab in HER2-positive breast cancer [0.03%]
针对HER2的酪氨酸激酶抑制剂可增强抗HER2阳性乳腺癌药赫赛汀和佩捷珠单抗的作用效果
Alexandra Canonici,Laura Ivers,Neil T Conlon et al.
Alexandra Canonici et al.
Despite trastuzumab and pertuzumab improving outcome for patients with HER2-positive metastatic breast cancer, the disease remains fatal for the majority of patients. This study evaluated the anti-proliferative effects of adding anti-HER2 t...
Induction of endoplasmic reticulum stress by aminosteroid derivative RM-581 leads to tumor regression in PANC-1 xenograft model [0.03%]
氨基甾体衍生物RM-581诱导内质网应激介导异种移植PANC-1肿瘤退化
Martin Perreault,René Maltais,Jenny Roy et al.
Martin Perreault et al.
The high fatality and morbidity of pancreatic cancer have remained almost unchanged over the last decades and new clinical therapeutic tools are urgently needed. We determined the cytotoxic activity of aminosteroid derivatives RM-133 (andro...
First-in-human study of the anti-HB-EGF antibody U3-1565 in subjects with advanced solid tumors [0.03%]
一项在晚期实体瘤受试者中研究抗HB-EGF抗体U3-1565的首个人体试验
Kathleen N Moore,Johanna C Bendell,Patricia M LoRusso et al.
Kathleen N Moore et al.
U3-1565 is a monoclonal antibody directed against heparin-binding epidermal growth factor-like growth factor (HB-EGF), which mediates angiogenesis via induction of vascular endothelial growth factor (VEGF-A). This first-in-human study chara...
Clinical Trial
Investigational new drugs. 2019 Feb;37(1):147-158. DOI:10.1007/s10637-018-0646-1 2019
Combination treatment of cancer cells with pan-Akt and pan-mTOR inhibitors: effects on cell cycle distribution, p-Akt expression level and radiolabelled-choline incorporation [0.03%]
泛Akt和泛mTOR抑制剂联合治疗癌细胞的影响：对细胞周期分布、p-Akt表达水平及放射性标记胆碱掺入的作用
Su Myat Phyu,Tim A D Smith
Su Myat Phyu
Signal transduction pathways, which regulate cell growth and survival, are up-regulated in many cancers and there is considerable interest in their pharmaceutical modulation for cancer treatment. However inhibitors of single pathway compone...
Absorption, metabolism, and excretion of the antiemetic rolapitant, a selective neurokinin-1 receptor antagonist, in healthy male subjects [0.03%]
健康男性受试者中止吐剂Rolapitant（一种选择性神经激肽-1受体拮抗剂）的吸收、代谢和排泄
Zhi-Yi Zhang,Jing Wang,Vikram Kansra et al.
Zhi-Yi Zhang et al.
Rolapitant is a neurokinin-1 receptor antagonist that is approved in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting (CINV) associated with initial and repeat courses of emetogenic cancer...
Clinical Trial
Investigational new drugs. 2019 Feb;37(1):139-146. DOI:10.1007/s10637-018-0638-1 2019
Hand-foot-skin reaction of grade ≥ 2 within sixty days as the optimal clinical marker best help predict survival in sorafenib therapy for HCC [0.03%]
优化的临床标记手足皮肤反应分级≥2分有助于预测索拉非尼治疗肝癌患者的生存期
Enxin Wang,Dongdong Xia,Wei Bai et al.
Enxin Wang et al.
Background & Aims Sorafenib-related adverse events have been reported as clinical surrogates for treatment response in hepatocellular carcinoma (HCC); however, no consensus has been reached regarding the definition of responders. We evaluat...