Literature DB >> 25769658

A phase II study of single-agent RO4929097, a gamma-secretase inhibitor of Notch signaling, in patients with recurrent platinum-resistant epithelial ovarian cancer: A study of the Princess Margaret, Chicago and California phase II consortia.

Ivan Diaz-Padilla1, Michelle K Wilson1, Blaise A Clarke2, Hal W Hirte3, Stephen A Welch4, Helen J Mackay1, Jim J Biagi5, Michael Reedijk6, Johanne I Weberpals7, Gini F Fleming8, Lisa Wang1, Geoffrey Liu1, Chen Zhou1, Chantale Blattler1, S Percy Ivy9, Amit M Oza10.   

Abstract

PURPOSE: A phase II study was performed to evaluate the efficacy and safety of single-agent RO4929097 (a gamma-secretase inhibitor) in patients with recurrent platinum-resistant ovarian cancer. EXPERIMENTAL
DESIGN: Women with progressive platinum-resistant ovarian cancer treated with ≤2 chemotherapy regimens for recurrent disease were enrolled in this trial. Patients received oral RO4929097 at 20 mg once daily, 3 days on/4 days off each week in a three week cycle. The primary endpoint was progression-free survival (PFS) rate at the end of 4 cycles. Secondary objectives included assessment of the safety of RO4929097 and exploration of molecular correlates of outcome in archival tumor tissue and serum.
RESULTS: Of 45 patients enrolled, 40 were evaluable for response. Thirty-seven (82%) patients had high-grade ovarian cancer. No objective responses were observed. Fifteen patients (33%) had stable disease as their best response, with a median duration of 3.1 months. The median PFS for the whole group was 1.3 months (1.2-2.5). Treatment was generally well tolerated with 10% of patients discontinuing treatment due to an adverse event. In high grade serous ovarian cancer patients, the median PFS trended higher when the expression of intracellular Notch (NICD) protein by immunohistochemistry was high versus low (3.3 versus 1.3 months, p=0.09). No clear relationship between circulating angiogenic factors and PFS was found despite a suggestion of an improved outcome with higher baseline VEGFA levels.
CONCLUSIONS: RO4929097 has insufficient activity as a single-agent in platinum-resistant ovarian cancer to warrant further study as monotherapy. Future studies are needed to explore the potential for cohort enrichment using NICD expression.
Copyright © 2015. Published by Elsevier Inc.

Entities:  

Keywords:  Gamma-secretase inhibitor; Notch; Ovarian cancer; Phase II clinical trial; RO4929097

Mesh:

Substances:

Year:  2015        PMID: 25769658     DOI: 10.1016/j.ygyno.2015.03.005

Source DB:  PubMed          Journal:  Gynecol Oncol        ISSN: 0090-8258            Impact factor:   5.482


  23 in total

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Authors:  Tyler R McCaw; Evelyn Inga; Herbert Chen; Renata Jaskula-Sztul; Vikas Dudeja; James A Bibb; Bin Ren; J Bart Rose
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4.  RASSF1A disrupts the NOTCH signaling axis via SNURF/RNF4-mediated ubiquitination of HES1.

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Review 7.  Targeting of proangiogenic signalling pathways in chronic inflammation.

Authors:  Sander W Tas; Chrissta X Maracle; Emese Balogh; Zoltán Szekanecz
Journal:  Nat Rev Rheumatol       Date:  2015-12-03       Impact factor: 20.543

8.  Pharmacological Disruption of the Notch1 Transcriptional Complex Inhibits Tumor Growth by Selectively Targeting Cancer Stem Cells.

Authors:  William Guerrant; Luisana Astudillo; Annamil Alvarez-Trotta; Mohini Lahiry; Giulia Diluvio; Elena Shersher; Hugo Kaneku; David J Robbins; Darren Orton; Anthony J Capobianco
Journal:  Cancer Res       Date:  2021-04-05       Impact factor: 12.701

9.  Anti-myeloma effect of pharmacological inhibition of Notch/gamma-secretase with RO4929097 is mediated by modulation of tumor microenvironment.

Authors:  Alexandra Pisklakova; Eileen Grigson; Maria Ozerova; Feng Chen; Daniel M Sullivan; Yulia Nefedova
Journal:  Cancer Biol Ther       Date:  2016-03-02       Impact factor: 4.742

10.  Trichostatin A ameliorates renal tubulointerstitial fibrosis through modulation of the JNK-dependent Notch-2 signaling pathway.

Authors:  Chun-Wu Tung; Yung-Chien Hsu; Chang-Jhih Cai; Ya-Hsueh Shih; Ching-Jen Wang; Pey-Jium Chang; Chun-Liang Lin
Journal:  Sci Rep       Date:  2017-11-03       Impact factor: 4.379

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