Tasisulam sodium (LY573636 sodium) as third-line treatment in patients with unresectable, metastatic non-small-cell lung cancer: a phase-II study

Journal of Thoracic Oncology : Official Publication of the International Association for the Study of Lung Cancer
Giorgio V ScagliottiChristian Manegold

Abstract

Tasisulam sodium (hereafter referred to as tasisulam) is a novel anticancer compound that induces apoptosis and exhibits antiangiogenesis activity in a broad range of cancer models, including non-small-cell lung cancer (NSCLC). Tasisulam was administered as a 2-hour infusion every 21 days as third-line treatment in patients with advanced (stage IIIB/IV) NSCLC. Thirty-two patients received a Cmax target dose of 420 µg/ml. Median time to progression was 3.12 months, median progression-free survival was 2.69 months, and median overall survival was 8.48 months. There were no objective responses; 43.8% of patients achieved stable disease. A high rate of grade-4 hematologic toxicity in the first 30 patients led to exploration of a lower Cmax target dose of 380 µg/ml. The rate of grade-4 hematologic toxicity (thrombocytopenia and/or neutropenia) at the 380-µg/ml dose (n = 20) was 20% versus 34% at the 420-µg/ml dose. Tasisulam has only modest activity as a third-line treatment of patients with unresectable/metastatic NSCLC. The high rate of grade-4 hematologic toxicity observed with this highly albumin- bound compound in this patient population provided challenges for fixed Cmax-based dosing. Alternative dosing methods, including vary...Continue Reading

References

Apr 1, 1992·Journal of Paediatrics and Child Health·S Beal
Dec 25, 2002·Lung Cancer : Journal of the International Association for the Study of Lung Cancer·E MassarelliR S Herbst
May 1, 2004·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Nasser HannaPaul A Bunn
Jul 15, 2005·The New England Journal of Medicine·Frances A ShepherdUNKNOWN National Cancer Institute of Canada Clinical Trials Group
Sep 24, 2005·Clinical Pharmacokinetics·Sarayut JanmahasatianBruce Green

❮ Previous
Next ❯

Citations

Feb 2, 2013·Cancer Chemotherapy and Pharmacology·Yutaka FujiwaraHironobu Minami
Oct 28, 2015·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Beata ŻołnowskaKrzysztof Szafrański
Nov 10, 2017·European Journal of Drug Metabolism and Pharmacokinetics·Everett J PerkinsChris Twelves
Aug 12, 2014·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Hae-Yun JungJing Yang
Nov 26, 2020·British Journal of Pharmacology·Yuewei XuHector C Keun

❮ Previous
Next ❯

Related Concepts

Related Feeds

Apoptosis

Apoptosis is a specific process that leads to programmed cell death through the activation of an evolutionary conserved intracellular pathway leading to pathognomic cellular changes distinct from cellular necrosis