PhaseIStudyofInhaledDoxorubicinforPatientswith
MetastaticTumorstotheLungs
GregoryA. Otterson,
1
Miguel A.Villalona-Calero,
1
Sunil Sharma,
3
Mark G. Kris,
3
Anthony Imondi,
2
Mirjam Gerber,
2
DorothyA.White,
3
Mark J. Ratain,
4
Joan H. Schiller,
5
Alan Sandler,
6
Michael Kraut,
7
Sridhar Mani,
8
and John R. Murren
9,c
Abstract Purpose: To evaluate the toxicity profile of inhalational doxorubicin in patients with malignant
disease in the lung.
ExperimentalDesign: The OncoMyst Model CDD-2a inhalation device aerosolizes compounds
to particles of 2 to 3 Am and prevents exhaled aerosol from escaping into the environment. Depo-
sition efficiency of inhaled Technetium 99m was used to predict deposition of doxorubicin and
calculate dose. Treatment was repeated every 3 weeks. No more than moderate pulmonary
dysfunction was permitted (forced expiratory volume in 1 s, forced vital capacity, and diffusing
capacity for carbon monoxide, all >50% predicted; resting SaO
2
>90%).
Results: Fifty-three patients were enrolled at 13 dose levels ranging from 0.4 to 9.4 mg/m
2
. The
most common histologic diagnoses were sarcoma ( n = 19) and non ^ small cell lung cancer
( n = 16). Dose-limiting toxicity (DLT) was observed at the 9.4 mg/m
2
dose level when two of
four patients experienced pulmonary DLT. Of 11 patients treated at the 7.5 mg/m
2
dose level,
only one showed DLTconsisting of a decline in forced vital capacity of >20% from baseline. No
significant systemic drug-related toxicity was observed. Several patients experienced declines in
pulmonary function test variables, which were attributed to progressive disease. Observed activ-
ity included a partial response in a patient with metastatic soft tissue sarcoma previously treated
with i.v. doxorubicin and ifosfamide.
Conclusions: Inhaled doxorubicin is safe up to a dose of 7.5 mg/m
2
every 3 weeks in patients
with cancer who had normal to moderately impaired pulmonary function.
Pulmonary metastases commonly occur in solid tumors and
are often the predominant or sole site of metastatic involve-
ment. A problem in treating these lesions is the inability to
achieve adequate therapeutic concentrations of drugs at the
tumor site without suffering substantial systemic toxicity. One
approach to improving therapeutic efficacy is targeted dose
intensification. This approach has been effectively used in a
variety of tumors, including liver, ovarian, and bladder cancer
(1–6), but there is little experience delivering chemotherapeu-
tics directly to the lungs via inhalation (7).
Inhalational chemotherapy was first described by Shev-
chenko and Resnik in 1968. (8). The concept was tested in
dogs and subsequently in 58 patients. Antitumor efficacy was
observed in 24 patients, but the data are difficult to interpret
because of the concurrent use of radiotherapy and less precise
methods for response assessment. Tatsumura et al. (9) tested
the administration of 5-fluorouracil by inhalation in dogs and
found high levels of the drug in the trachea, bronchi, and
regional nodes. Subsequently, the same authors treated 10
patients with inoperable lung tumors with 5-fluorouracil via
supersonic nebulizer at a dose of 250 mg twice daily for 2 to
3 days per week. There was notable antitumor efficacy, and the
therapy was well tolerated. Similar proof-of-principle studies
using inhaled doxorubicin or paclitaxel in dogs with macro-
scopic lung tumors showed preliminary evidence of activity
with acceptable toxicity (10).
Huland et al. (11) administered interleukin-2 by inhalation
with concomitant IFN-a given s.c. to 15 patients with
metastatic renal carcinoma. There was a marked difference in
response between lung and non-lung metastases (1 complete
response and 8 partial response in lung metastases compared
with 0 complete response and 3 partial response, in non-lung
metastases), suggesting that inhalational interleukin-2 dis-
played enhanced antitumor efficacy in pulmonary lesions.
Cancer Therapy: Clinical
Authors’Affiliations:
1
The Ohio State University Comprehensive Cancer Center
and
2
Zivena, Inc., Columbus, Ohio;
3
Memorial Sloan Kettering Comprehensive
Cancer Center, New York, New York;
4
University of Chicago, Chicago, Illinois;
5
University of Wisconsin Cancer Center, Madison, Wisconsin;
6
Vanderbilt Medical
Center, Nashville, Tennessee;
7
Karmanos Cancer Center, Detroit, Michigan;
8
Montefiore Medical Center,Weiler Division, Bronx, NewYork; and
9
Yale University
Comprehensive Cancer Center, New Haven, Connecticut
Received 5/8/06; revised 9/20/06; accepted 11/30/06.
The costs of publication of this article were defrayed in part by the payment of page
charges. This article must therefore be hereby marked advertisement in accordance
with 18 U.S.C. Section 1734 solely to indicate this fact.
c
Deceased.
Note: J. Murren died during the writing and editing of this article. This is dedicated
to him.
Requestsforreprints: Gregory A. Otterson, Division of Hematology/Oncology,
The Ohio State University, B420 Starling Loving Hall, 320 West 10th Avenue,
Columbus, OH 43210. Phone: 614-293-2887; Fax: 614-293-7529; E-mail:
greg.otterson@osumc.edu.
F 2007 American Association for Cancer Research.
doi:10.1158/1078-0432.CCR-06-1096
www.aacrjournals.org ClinCancerRes2007;13(4)February15,2007 1246
Research.
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