APhase I-IIStudy to Determine the Maximum Tolerated Infusion
Rate of Rituximabwith Special Emphasis on Monitoring
theEffectofRituximabonCardiacFunction
MarcoSiano,ErikaLerch,LauraNegretti,EmanueleZucca,DelvysRodriguez-Abreu,MichelOberson,
LedaLeoncini,OresteMora,CristianaSessa,AugustoGallino,andMicheleGhielmini
Abstract
Purpose: This phase I infusion rate escalation trial was undertaken to evaluate the maximum
applicable infusion rate for rituximab without steroid premedicationinpatientshaving received
onepreviousrituximabinfusion.
Experimental Design: Cohortsofatleastthreepatientswereassignedtorituximabwithor
without concomitant chemotherapy.The initial infusion rate was 200 mg/h in the first
cohort,andwasincreasedby100mg/hineachsubsequentcohorttoamaximumof700mg/h.
Ineachpatienttheinfusionratewasincreasedby100mg/hevery30minutestothetotaldose
(375 mg/m
2
). In the first sixcohorts (21patients), two well-tolerated rituximab administrations
were required; in the 7th cohort (11patients) one previously well-tolerated rituximab infusion
was required. Patients didnot receive steroid premedication and were monitored with electro-
cardiograms(ECG),echocardiograms,HolterECGs,troponin,andbrainnatriureticpeptide(BNP).
Results: Thirty-twopatientswereincludedand128cyclesweredone,85atarateof700mg/h.
Patientstoleratedinfusionrateswithoutmajorsideeffects.Therewerenonewclinicallyrelevant
ECGalterations.Troponin(< 0.1ng/L)andmeancardiacejectionfraction(65%)remainedinthe
referencerange;BNPbaselinelevelincreasedsignificantly24hoursafterrituximabadministration
(from30.4to64.1ng/L; P < 0.0001).
Conclusions: Rituximabcanbeadministeredsafelyat700mg/hwithoutsteroidpremedication
inpatientshavingreceivedatleastonerituximabdoseintheprevious3months.
Rituximab is a monoclonal antibody against the lymphocyte
surface antigen CD20. First introduced in 1995 for the
treatment of non–Hodgkin’s B-lymphoma, rituximab has
today a broad spectrum of indications, including treatment of
rheumatoid arthritis, thrombotic thrombocytopenic purpura,
and systemic lupus erythematosis, among many others (1–6).
Treatment with rituximab is generally well tolerated and can
be combined with chemotherapy, improving response rate,
response duration, and in some cases overall survival of
patients with B-cell lymphomas (1). Infusion-related reactions
can occur in approximately one fourth of patients during
the first administration, probably due to a release of cytokines
into the blood as a consequence of the rapid destruction of
circulatingBcells(7).Thisiswhyitisrecommendedtochoose
a low initial infusion rate. The incidence and the severity of
infusion-related side effects consistently decrease in the
successive administrations; indeed after the second rituximab
infusionalmostnoBcellsareleftinthebloodforatleast2to
3 months. The reconstitution begins usually after 6 months
and is completed after a median of 12 months (8, 9). We
hypothesized that no infusion-related reaction should occur
from the second infusion, and that a faster application of
rituximab could be considered safe. Although the duration of
theinfusionisusually4to5hoursforthefirstadministration,
thepresentstudywasundertakentoevaluateiffromthesecond
infusion rituximab could be administered over 1 hour.
PatientsandMethods
Patient eligibility. Patients with any type of B-cell lymphoma were
eligible. In the first part of the study (21 patients) two previous well-
tolerated rituximab administrations (the last one given no longer then
3 mo before) were required, whereas in the second part (11 patients)
one previous rituximab infusion in the previous 3 mo was accepted.
The first rituximab administration(s) should be given according to the
manufacturer’s guidelines (10). Rituximab could be given with
chemotherapy, provided the latter (including steroids) was adminis-
tered after rituximab infusion. A left ventricular ejection fraction of
z50% (assessed by echocardiography in the month before inclusion)
was required. No severe reaction to prior rituximab infusions could
have occurred.
Cancer Therapy: Clinical
Authors’Affiliation: DepartmentsofMedicalOncologyandCardiology,Ospedale
SanGiovanni,Bellinzona,Switzerland
Received5/19/08;revised7/8/08;accepted7/27/08.
Grantsupport: RocheLtd.,Basel,andtheSwissInsuranceCompanyAssociation
(SVK),whichreimbursedthecostsofrituximab.
Thecostsofpublicationofthisarticleweredefrayedinpartbythepaymentofpage
charges.Thisarticlemustthereforebeherebymarked advertisement inaccordance
with18U.S.C.Section1734solelytoindicatethisfact.
Requests for reprints: Michele Ghielmini, Medical Oncology Department,
Oncology Institute of Southern Switzerland,Ospedale San Giovanni, CH-6500
Bellinzona,Switzerland.Phone: 419-181-18111;Fax: 419-181-18731;E-mail:
michele.ghielmini@eoc.ch.
F 2008AmericanAssociationforCancerResearch.
doi:10.1158/1078-0432.CCR-08-1124
www.aacrjournals.org ClinCancerRes2008;14(23)December1,2008 7935
Research.
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