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Poster display session

1405 - A phase 1 study of BYL719, an α-isoform selective PI3K inhibitor, in Japanese patients with advanced solid malignancies


11 Sep 2017


Poster display session


Clinical Research;  Breast Cancer


Junichi Tomomatsu


Annals of Oncology (2017) 28 (suppl_5): v74-v108. 10.1093/annonc/mdx365


J. Tomomatsu1, S. Iwasa2, H. Saka3, S. Takahashi1, K. Nakano1, S. Morita4, M. Inoue4, H. Nakahama2, Y. Kogure3, T. Kakizume5, K. Natsume5, T. Aoki5, C. Quadt6, Y. Yamada2, Y. Ando4

Author affiliations

  • 1 Department Of Medical Oncology, The Cancer Institute Hospital of Japanese Foundation for Cancer Research, 135-8550 - Tokyo/JP
  • 2 Department Of Gi Medical Oncology, National Cancer Center Hospital, Tokyo/JP
  • 3 Department Of Respiratory Medicine, Nagoya Medical Center, Nagoya/JP
  • 4 Department Of Clinical Oncology And Chemotherapy, Nagoya University Hospital, Nagoya/JP
  • 5 Oncology, Novartis Pharmaceuticals KK, Tokyo/JP
  • 6 Oncology, Novartis Pharmaceuticals AG, Basel/CH


Abstract 1405


BYL719 is an oral inhibitor that selectively targets the α-isoform of class l PI3K. In a first-in-human ph1 study in mostly Western patients (pts) with PIK3CA alteration, the maximum tolerated dose for once-daily (qd) BYL719 was declared as 400 mg and preliminary antitumor activity was observed. Previous preliminary findings showed tolerability, safety, and pharmacokinetic (PK) results in dose escalation of the first-in-Japanese ph1 study. Here, we report results of the food effect on the PK profile of BYL719 at steady state, additional safety, and preliminary efficacy in Japanese pts.


Pts were aged ≥18 years with histologically confirmed, advanced solid tumors. Pts received BYL719 qd in 28-day cycles until disease progression, unacceptable toxicity, or investigator/pts decision. The objectives in the expansion part were to assess food effect on PK profile, preliminary antitumor activity, and safety. Pts with PIK3CA alteration were selected in the expansion part and were randomized to receive BYL719 at the recommended dose 350 mg qd in fasted or fed condition on cycle 1 day 22 and cycle 2 day 1 in a crossover fashion. Pts received BYL719 ∼1 hr following a light breakfast and continued to be fasted for 1 hr after each dose.


Thirty-three pts were enrolled and all pts discontinued treatment. The median duration of exposure was 71.0 days (range, 6-462). The common BYL719-related all-grade (Gr) AEs (>30%) were hyperglycemia, rash maculopapular (48.5%, each), diarrhea (45.5%), and decreased appetite (33.3%). BYL719-related Gr 3 or 4 AEs (≥20%) were rash maculopapular (24.2%) and hyperglycemia (21.2%). Eight pts were enrolled in the expansion part; six of them were eligible for PK analysis. The geometric mean values of dose-normalized Cmax and AUC0-24 in fed state were 78% and 56% higher than those in fasted state, respectively. One pt experienced Gr 4-infected neoplasm meeting DLT criteria, 1 pt with uterus cancer and PIK3CA mutation had an unconfirmed partial response, and 18 pts had a stable disease.


In this ph1 study of BYL719 in Japanese pts, a positive food effect and preliminary antitumor activity were observed at steady state in pts with PIK3CA mutation status.

Clinical trial identification


Legal entity responsible for the study

Novartis Pharmaceuticals KK, Tokyo, Japan


Novartis Pharmaceuticals KK, Tokyo, Japan


H. Saka: Grants from Novartis, KHK, Daiichi Sankyo, Merck, Esai, Bristol-Myers Squibb, Taiho, Ono, Chugai, Eli Lilly, Beyer, MSD, Quintiles, West JCOG. Personal fees Chugai, Kyorin, NU, BI, Eli Lilly, Astellas, Nobelpharma, JSRE, Ono, Chunichi Shimbun, Taiho. S. Takahashi: Grants from Novartis, during the conduct of the study; grants from Chugai, grants from Astrazeneka, grants from Daiichisankyo, grants from Bayer, grants from Parexel, outside the submitted work. K. Natsume, T. Kakizume: Personal fees from Novartis Pharmaceuticals KK, during the conduct of the study; Y. Ando: Grants and personal fee: Chungai, Takeda, KHK, Eisai, Taiho, Nippon, YakultHonsya, Mochida, Merck, Ono, Eli Lilly, Novartis, Janssen, Hisamitsu, GSK, Terumo, Bayel, Meiji, BSC, Boehringer Ingelheim, Bristol-Myers Squibb, Sawai, Otsuka, Shionogi, outside the submitted work. All other authors have declared no conflicts of interest.

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