Cited by 154PI3K/AKT/mTOR signaling in cancerAdvanced Breast Cancer TherapiesMetabolism, Diabetes, and Cancer

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Phase I Safety, Pharmacokinetic, and Pharmacodynamic Study of SAR245408 (XL147), an Oral Pan-Class I PI3K Inhibitor, in Patients with Advanced Solid Tumors

Shapiro, Geoffrey I., Rodon, Jordi, Bedell, Cynthia, Kwak, Eunice L., Baselga, Jose, Braña, Irene, Pandya, Shuchi S., Scheffold, Christian, Laird, A. Douglas, Nguyen, Linh T., Xu, Yi, Egile, Coumaran, Edelman, Gerald·2014·Clinical Cancer Research

DOI 10.1158/1078-0432.ccr-13-1777

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Abstract

Purpose: SAR245408 is a pan-class I phosphoinositide 3-kinase (PI3K) inhibitor. This phase I study determined the maximum tolerated dose (MTD) of two dosing schedules [first 21 days of a 28-day period (21/7) and continuous once-daily dosing (CDD)], pharmacokinetic and pharmacodynamic profiles, and preliminary efficacy. Experimental Design: Patients with refractory advanced solid malignancies were treated with SAR245408 using a 3 + 3 design. Pharmacokinetic parameters were determined after single and repeated doses. Pharmacodynamic effects were evaluated in plasma, hair sheath cells, and skin and tumor biopsies. Results: Sixty-nine patients were enrolled. The MTD of both schedules was 600 mg; dose-limiting toxicities were maculopapular rash and hypersensitivity reaction. The most frequent drug-related adverse events included dermatologic toxicities, diarrhea, nausea, and decreased appetite. Plasma pharmacokinetics showed a median time to maximum concentration of 8 to 22 hours, mean terminal elimination half-life of 70 to 88 hours, and 5- to 13-fold accumulation after daily dosing (first cycle). Steady-state concentration was reached between days 15 and 21, and exposure was dose-proportional with doses up to 400 mg. SAR245408 inhibited the PI3K pathway (∼40%–80% reduction in phosphorylation of AKT, PRAS40, 4EBP1, and S6 in tumor and surrogate tissues) and, unexpectedly, also inhibited the MEK/ERK pathway. A partial response was seen in one patient with advanced non–small cell lung cancer. Eight patients were progression-free at 6 months. Pharmacodynamic and clinical activity were observed irrespective of tumor PI3K pathway molecular alterations. Conclusions: SAR245408 was tolerable at doses associated with PI3K pathway inhibition. The recommended phase II dose of the capsule formulation is 600 mg administered orally with CDD. Clin Cancer Res; 20(1); 233–45. ©2013 AACR.

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Authors: Shapiro, G. I., Rodon, J., Bedell, C., Kwak, E. L., Baselga, J., Braña, I., Pandya, S. S., Scheffold, C., Laird, A. D., Nguyen, L. T., Xu, Y., Egile, C., & Edelman, G.
Affiliations: Beth Israel Deaconess Medical Center (US)
Authors' Affiliations: 1Dana-Farber Cancer Institute; 2Massachusetts General Hospital; 3Beth Israel Deaconess Medical Center, Boston, Massachusetts; 4Vall d'Hebron Institute of Oncology (VHIO), Barcelona, Spain; 5Mary Crowley Cancer Research Centers, Dallas, Texas; 6Exelixis Inc., South San Francisco, California; and 7Sanofi, Cambridge, Massachusetts, and Vitry-sur-Seine, France
ORCID: Shapiro, Geoffrey I.
Rodon, Jordi
Baselga, Jose
Braña, Irene
Laird, A. Douglas
Nguyen, Linh T.
Xu, Yi
Venue: Clinical Cancer Research
Publisher: American Association for Cancer Research (AACR)
Published: 2014-01-01
Volume: 20
Issue: 1
Pages: 233-245
ISSN: 1078-0432 (ISSN-L)
1557-3265
DOI: 10.1158/1078-0432.ccr-13-1777
OpenAlex: W1979937839
Cited by: 152
References: 28
Citations by year: 2025: 1 · 2024: 8 · 2023: 5 · 2022: 6 · 2021: 9 · 2020: 10 · 2019: 7 · 2018: 9 · 2017: 24 · 2016: 21 · 2015: 28 · 2014: 24
FWCI: 10.89
Type: journal article
Language: en
Open access: closed
Locations: Clinical Cancer Research (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › PI3K/AKT/mTOR signaling in cancer
Health Sciences › Medicine › Oncology › Advanced Breast Cancer Therapies
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
Keywords: phosphatidylinositol 3-kinase, maximum tolerated dose, dose-limiting toxicity, maculopapular rash, pharmacokinetics, pharmacodynamics, Akt phosphorylation, advanced solid tumors, non-small cell lung cancer, dose proportionality, tumor biopsy
MeSH terms: Phosphoinositide-3 Kinase Inhibitors, Administration, Oral, Adult, Aged, Aged, 80 and over, Antineoplastic Agents, Carcinoma, Non-Small-Cell Lung, Dose-Response Relationship, Drug, Female, Humans, Lung Neoplasms, Male, Middle Aged, Neoplasm Staging, Quinoxalines, Skin Diseases, Sulfonamides, Signal Transduction, Treatment Outcome, Area Under Curve, Maximum Tolerated Dose, Phosphatidylinositol 3-Kinase

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Phase I Safety, Pharmacokinetic, and Pharmacodynamic Study of SAR245408 (XL147), an Oral Pan-Class I PI3K Inhibitor, in Patients with Advanced Solid Tumors

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