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Cancer Chemother Pharmacol (2014) 73:595–604
DOI 10.1007/s00280-014-2389-9
ORIGINAL ARTICLE
A phase I study of olaratumab, an anti-platelet-derived growth
factor receptor alpha (PDGFRα) monoclonal antibody, in patients
with advanced solid tumors
E. Gabriela Chiorean · Christopher Sweeney ·
Hagop Youssoufian · Amy Qin · Aruna Dontabhaktuni ·
Nick Loizos · Johannes Nippgen · Robert Amato
Received: 18 December 2013 / Accepted: 13 January 2014 / Published online: 23 January 2014
© Springer-Verlag Berlin Heidelberg 2014
not identified with the doses studied. The most common
olaratumab-related adverse events (AE) were fatigue and
infusion reactions (10.5 % each). With the exception of 1
patient (20 mg/kg) experiencing two grade 3 drug-related
AEs after the dose-limiting toxicity assessment period,
all drug-related AEs were grade 1 or 2. The trough con-
centrations (C
min
) for 16 mg/kg weekly and 20 mg/kg
biweekly were higher than 155 μg/mL, and the concen-
tration found to be efficacious in preclinical xenograft
models. Twelve patients (63.2 %) had a best response of
stable disease [median duration of 3.9 months (95 % CI
2.3–8.7)].
Conclusions Olaratumab was well tolerated and showed
preliminary antitumor activity. RP2Ds are 16 mg/kg
weekly and 20 mg/kg biweekly. Phase II studies of olara-
tumab as monotherapy and in combination are ongoing in
several tumor types.
Keywords Olaratumab · IMC-3G3 · Platelet-derived
growth factor receptor · Solid tumors · Phase I
Abstract
Purpose The platelet-derived growth factor receptor
(PDGFR) has an important role in tumorigenesis and tumor
progression. Olaratumab (IMC-3G3) is a fully human
monoclonal antibody that selectively binds human
PDGFRα and blocks ligand binding. This phase I study
assessed the safety, maximum tolerated dose (MTD), rec-
ommended phase II dose (RP2D), pharmacokinetics, and
preliminary antitumor activity of olaratumab in patients
with advanced solid tumors.
Methods Patients were enrolled into five dose-escalating
cohorts of 3–6 patients each. Olaratumab was administered
intravenously weekly at 4, 8, or 16 mg/kg (cohorts 1–3) or
once every other week at 15 or 20 mg/kg (cohorts 4–5),
with 4 weeks/cycle.
Results Nineteen patients were treated in five cohorts.
There were no dose-limiting toxicities; the MTD was
Presented in part at the EORTC-NCI-AACR Annual Meeting;
October 21–24, 2008; Geneva, Switzerland [abstract 511 and
poster].
E. G. Chiorean (*)
Fred Hutchinson Cancer Research Center, University
of Washington, 825 Eastlake Ave East, G4830, Seattle, WA
98109, USA
e-mail: gchiorea@uw.edu
E. G. Chiorean
Indiana University, 535 Barnhill Drive, Indianapolis, IN, USA
C. Sweeney
Dana-Farber Cancer Institute, Harvard Medical School, Boston,
MA, USA
H. Youssoufian · A. Qin · A. Dontabhaktuni · N. Loizos
ImClone Systems LLC (a wholly owned subsidiary of Eli Lilly
and Company), Bridgewater, NJ, USA
Present Address:
H. Youssoufian
Progenics Pharmaceuticals, Tarrytown, NY, USA
J. Nippgen
ImClone Systems LLC (a wholly owned subsidiary of Eli Lilly
and Company), Heidelberg, Germany
Present Address:
J. Nippgen
Glycotope GmbH, Berlin, Germany
R. Amato
Memorial Hermann Cancer Center-Texas Medical Center,
University of Texas Health Science Center at Houston, Houston,
TX, USA