LY573636-sodium (tasisulam) is a small molecule antitumor agent with a novel mechanism of action currently being investigated in a variety of human cancers. In vitro, tasisulam induced apoptosis via the intrinsic pathway, resulting in cytochrome c …

Tasisulam enhances TRAIL-induced apoptosis by activating both extrinsic and intrinsic apoptotic pathways, achieved through upregulation of death receptor 5 (DR5) and downregulation of B-cell lymphoma 2 (Bcl-2).

Tasisulam is a thiophene substituted by a 2,4-dichlorobenzamide -N-sulfonyl and bromo groups at positions 2 and 4, respectively. It induces tumour cell apoptosis via ROS induction and mitochondrial membrane potential loss and currently in clinical development for the treatment of …

This phase I study was carried out to determine the phase II recommended dose of tasisulam sodium (hereafter, tasisulam), a novel anticancer agent with a unique mechanism of action. Tasisulam was administered intravenously, every 21 days, in ...

在Calu-6非小细胞肺癌异种移植模型中Tasisulam (25或者50mg/kg，i.v.)表现出剂量依赖性的抗肿瘤活性，诱导细胞凋亡，使与肿瘤相关的血管正常化。 此外，Tasisulam对一系列体内异种移 …

Purpose: To determine the recommended/maximum tolerated dose (MTD), pharmacokinetics (PK), and safety profile of tasisulam sodium (hereafter tasisulam), a novel anticancer agent. Methods: In this phase I study, tasisulam was administered as a 24-h continuous intravenous infusion on day 1, every 28 days, to patients with advanced solid tumors.

2016年10月20日 · Get severity rating, description, and management advice. Tasisulam has been used in trials studying the treatment and basic science of Melanoma, Lymphoma, Solid Tumors, Breast Cancer, and Ovarian Cancer, among others.

Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic progression and induces vascular normalization [1].

2011年4月1日 · Tasisulam, a TGF-β/TGF-β type I receptor kinase (ALK5) inhibitor, has been tested in two phase I clinical trials in patients with refractory or malignant solid tumors, including ovarian cancer, to determine the recommended dose for phase II trials [269, 270].

Tasisulam Sodium is the sodium salt of an acyl-sulfonamide with potential antineoplastic activity. Selectively toxic towards tumor cells, tasisulam appears to induce tumor cell apoptosis by a mitochondrial-targeted mechanism involving the loss of mitochondrial membrane potential and induction of reactive oxygen species (ROS).