Phase I study of Efatutazone, an oral PPARγ agonist, in patients with metastatic solid tumors

Efatutazone is a highly selective agonist of peroxisome proliferator-activated receptor gamma (PPARγ), a therapeutic target for carcinogenesis. In this phase I dose-escalation study, we assessed the safety, efficacy, and pharmacokinetics of efatutazone and the recommended dose (RD) was determined in...

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Veröffentlicht in:Anticancer research 2014-09, Vol.34 (9), p.5133-5141
Hauptverfasser: Murakami, Haruyasu, Ono, Akira, Takahashi, Toshiaki, Onozawa, Yusuke, Tsushima, Takahiro, Yamazaki, Kentaro, Jikoh, Takahiro, Boku, Narikazu, Yamamoto, Nobuyuki
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Sprache:eng
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Zusammenfassung:Efatutazone is a highly selective agonist of peroxisome proliferator-activated receptor gamma (PPARγ), a therapeutic target for carcinogenesis. In this phase I dose-escalation study, we assessed the safety, efficacy, and pharmacokinetics of efatutazone and the recommended dose (RD) was determined in Japanese patients with metastatic solid tumors using a 3+3 design. A total of 13 patients were enrolled and received efatutazone at doses of 0.25 mg, 0.50 mg, and 0.75 mg bid for multiple 3-week cycles. No dose-limiting toxicities were observed, and the maximum tolerated dose was not reached. Partial response was confirmed in one patient and stable disease in three. Efatutazone exposure was almost dose-proportional. RD was determined to be 0.50 mg bid, corresponding to the RD in previous global phase I studies. Efatutazone demonstrated acceptable toxicity and gave evidence of disease control in Japanese patients with metastatic solid tumors.
ISSN:1791-7530