作者
Jordi Rodon, Michael A Carducci, Juan M Sepulveda-Sánchez, Analia Azaro, Emiliano Calvo, Joan Seoane, Irene Braña, Elisabet Sicart, Ivelina Gueorguieva, Ann L Cleverly, N Sokalingum Pillay, Durisala Desaiah, Shawn T Estrem, Luis Paz-Ares, Matthias Holdhoff, Jaishri Blakeley, Michael M Lahn, Jose Baselga
发表日期
2015/2/1
期刊
Clinical Cancer Research
卷号
21
期号
3
页码范围
553-560
出版商
American Association for Cancer Research
简介
Purpose: TGFβ signaling plays a key role in tumor progression, including malignant glioma. Small-molecule inhibitors such as LY2157299 monohydrate (LY2157299) block TGFβ signaling and reduce tumor progression in preclinical models. To use LY2157299 in the treatment of malignancies, we investigated its properties in a first-in-human dose (FHD) study in patients with cancer.
Experimental Design: Sixty-five patients (58 with glioma) with measurable and progressive malignancies were enrolled. Oral LY2157299 was given as a split dose morning and evening on an intermittent schedule of 14 days on and 14 days off (28-day cycle). LY2157299 monotherapy was studied in dose escalation (part A) first and then evaluated in combination with standard doses of lomustine (part B). Safety was assessed using Common Terminology Criteria for Adverse Events version 3.0, echocardiography …
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J Rodon, MA Carducci, JM Sepulveda-Sánchez… - Clinical Cancer Research, 2015