Literature DB >> 26098748

Safety and Efficacy of Buparlisib (BKM120) in Patients with PI3K Pathway-Activated Non-Small Cell Lung Cancer: Results from the Phase II BASALT-1 Study.

Johan F Vansteenkiste1, Jean-Luc Canon2, Filippo De Braud3, Francesco Grossi4, Tommaso De Pas5, Jhanelle E Gray6, Wu-Chou Su7, Enriqueta Felip8, Hiroshige Yoshioka9, Cesare Gridelli10, Grace K Dy11, Sumitra Thongprasert12, Martin Reck13, Paola Aimone14, Gena Atalla Vidam15, Pantelia Roussou14, Ying A Wang16, Emmanuelle Di Tomaso16, Jean-Charles Soria17.   

Abstract

INTRODUCTION: The phosphatidylinositol 3-kinase (PI3K) pathway promotes tumor growth and treatment resistance in non-small cell lung cancer (NSCLC). The aim of the open-label, two-stage, Phase II study BASALT-1 (NCT01820325) was to investigate the pan-PI3K inhibitor buparlisib (BKM120) in patients with PI3K pathway-activated, relapsed NSCLC.
METHODS: After prescreening for PI3K pathway activation, patients with PI3K pathway-activated, metastatic, squamous or nonsquamous NSCLC, who had relapsed after prior systemic antineoplastic therapy, were enrolled. In Stage 1, patients received single-agent buparlisib (100 mg/day). A futility analysis was performed independently in each histology group, based on the 12-week progression-free survival rate for the first 30 patients treated in each group being less than 50%. Exploratory biomarker analyses were performed in archival tissue samples and circulating tumor DNA (ctDNA).
RESULTS: Of 1242 prescreened patients, 13.5% exhibited PI3K pathway activation. As of June 5, 2014, 63 patients (30 squamous and 33 nonsquamous) were treated in Stage 1. The 12-week progression-free survival rates were 23.3% (95% confidence interval: 9.9-42.3) and 20.0% (95% confidence interval: 7.7-38.6) in the squamous and nonsquamous groups, respectively. Stage 2 was therefore not initiated in either group. PI3K pathway mutations in ctDNA were more concordant with metastatic tissue than with primary biopsies.
CONCLUSIONS: Despite preselecting patients for targeted treatment, BASALT-1 did not meet its primary objective during Stage 1. PI3K pathway activation can be detected using ctDNA, but may not be the main oncogenic driver in NSCLC. Combinations of PI3K inhibitors with other agents may demonstrate greater efficacy than monotherapy.

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Year:  2015        PMID: 26098748      PMCID: PMC4646607          DOI: 10.1097/JTO.0000000000000607

Source DB:  PubMed          Journal:  J Thorac Oncol        ISSN: 1556-0864            Impact factor:   15.609


  24 in total

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2.  Phase I dose-escalation and -expansion study of buparlisib (BKM120), an oral pan-Class I PI3K inhibitor, in patients with advanced solid tumors.

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Journal:  Hum Pathol       Date:  2005-07       Impact factor: 3.466

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Authors:  David A Fruman; Christian Rommel
Journal:  Nat Rev Drug Discov       Date:  2014-02       Impact factor: 84.694

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8.  Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer.

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Journal:  Proc Natl Acad Sci U S A       Date:  2009-10-05       Impact factor: 11.205

9.  PIK3CA mutations and copy number gains in human lung cancers.

Authors:  Hiromasa Yamamoto; Hisayuki Shigematsu; Masaharu Nomura; William W Lockwood; Mitsuo Sato; Naoki Okumura; Junichi Soh; Makoto Suzuki; Ignacio I Wistuba; Kwun M Fong; Huei Lee; Shinichi Toyooka; Hiroshi Date; Wan L Lam; John D Minna; Adi F Gazdar
Journal:  Cancer Res       Date:  2008-09-01       Impact factor: 12.701

10.  Multi-level targeting of the phosphatidylinositol-3-kinase pathway in non-small cell lung cancer cells.

Authors:  Christopher R Zito; Lucia B Jilaveanu; Valsamo Anagnostou; David Rimm; Gerold Bepler; Sauveur-Michel Maira; Wolfgang Hackl; Robert Camp; Harriet M Kluger; Herta H Chao
Journal:  PLoS One       Date:  2012-02-15       Impact factor: 3.240

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  66 in total

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Journal:  Transl Lung Cancer Res       Date:  2015-04

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3.  Drinking Not Drowning: How to Deal With the Deluge of Potential Predictive Biomarker Approaches in Non-Small-Cell Lung Cancer.

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Review 5.  mTOR in Lung Neoplasms.

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6.  ERK-dependent IL-6 autocrine signaling mediates adaptive resistance to pan-PI3K inhibitor BKM120 in head and neck squamous cell carcinoma.

Authors:  M R Yun; H M Choi; H N Kang; Yw Lee; H-S Joo; D H Kim; H R Kim; M H Hong; S O Yoon; B C Cho
Journal:  Oncogene       Date:  2017-09-25       Impact factor: 9.867

7.  A phase 1b dose expansion study of the pan-class I PI3K inhibitor buparlisib (BKM120) plus carboplatin and paclitaxel in PTEN deficient tumors and with dose intensified carboplatin and paclitaxel.

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8.  Prospective Comprehensive Molecular Characterization of Lung Adenocarcinomas for Efficient Patient Matching to Approved and Emerging Therapies.

Authors:  Emmet J Jordan; Hyunjae R Kim; Maria E Arcila; David Barron; Debyani Chakravarty; JianJiong Gao; Matthew T Chang; Andy Ni; Ritika Kundra; Philip Jonsson; Gowtham Jayakumaran; Sizhi Paul Gao; Hannah C Johnsen; Aphrothiti J Hanrahan; Ahmet Zehir; Natasha Rekhtman; Michelle S Ginsberg; Bob T Li; Helena A Yu; Paul K Paik; Alexander Drilon; Matthew D Hellmann; Dalicia N Reales; Ryma Benayed; Valerie W Rusch; Mark G Kris; Jamie E Chaft; José Baselga; Barry S Taylor; Nikolaus Schultz; Charles M Rudin; David M Hyman; Michael F Berger; David B Solit; Marc Ladanyi; Gregory J Riely
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Review 9.  PI3K Inhibitors in Cancer: Clinical Implications and Adverse Effects.

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Review 10.  Targeting KRAS-mutant non-small cell lung cancer: challenges and opportunities.

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