www.thelancet.com/child-adolescent Published online May 23, 2018 http://dx.doi.org/10.1016/S2352-4642(18)30099-3 1
Articles
Lancet Child Adolesc Health 2018
Published Online
May 23, 2018
http://dx.doi.org/10.1016/
S2352-4642(18)30099-3
See Online/Comment
http://dx.doi.org/10.1016/
S2352-4642(18)30128-7
Tor Vergata University
Hospital, Rome, Italy
(Prof P Curatolo MD);
Department of Neurology,
Cincinnati Children’s Hospital
Medical Center, Cincinnati, OH,
USA (Prof D N Franz MD);
Tuberous Sclerosis
Multidisciplinary Management
Clinic, Sydney Children’s
Hospital, Sydney, NSW,
Australia (J A Lawson MD);
Division of Child Neurology,
Department of Neurology,
Istanbul Faculty of Medicine,
Istanbul University, Istanbul,
Turkey (Prof Z Yapici MD);
National Hospital Organization
Epilepsy Center, Shizuoka
Institute of Epilepsy and
Neurological Disorders,
Shizuoka, Japan (H Ikeda MD);
Paediatric Epileptology, Mara
Hospital, Bethel Epilepsy
Center, Bielefeld, Germany
(T Polster MD); Hospital
Necker-Enfants Malades, Paris
Descartes University, Paris,
France (R Nabbout MD);
Division of Child and
Adolescent Psychiatry,
University of Cape Town,
Cape Town, South Africa
(Prof P J de Vries PhD);
Departments of Neurology and
Pediatrics, The Children’s
Hospital of Philadelphia,
Perelman School of Medicine at
the University of Pennsylvania,
Philadelphia, PA, USA
(D J Dlugos MD); Novartis
Pharmaceuticals Corporation,
East Hanover, NJ, USA
(J Fan MD, D Pelov MS,
M Voi MD); Novartis
Pharmaceuticals SAS,
Paris,France (A Ridolfi MS); and
Adjunctive everolimus for children and adolescents with
treatment-refractory seizures associated with tuberous
sclerosis complex: post-hoc analysis of the phase 3
EXIST-3 trial
Paolo Curatolo, David N Franz, John A Lawson, Zuhal Yapici, Hiroko Ikeda, Tilman Polster, Rima Nabbout, Petrus J de Vries, Dennis J Dlugos,
Jenna Fan, Antonia Ridolf, Diana Pelov, Maurizio Voi, Jacqueline A French
Summary
Background Epilepsy occurs in 70–90% of patients with tuberous sclerosis complex. We aimed to assess the efcacy
and safety of adjunctive everolimus for treatment-refractory seizures associated with tuberous sclerosis complex in
paediatric patients enrolled in the EXIST-3 trial, a double-blind, placebo-controlled, randomised, phase 3 study.
Methods This post-hoc analysis focused on paediatric patients (age <18 years) in the EXIST-3 trial, which consisted of
baseline (8 weeks), core (18 weeks), and extension phases (≥48 weeks) and was done at 99 centres in 25 countries
worldwide. Briefy, patients with tuberous sclerosis complex-associated treatment-refractory seizures, who were
receiving a stable dose of one to three antiepileptic drugs, were randomly assigned (1:1:1) to receive placebo,
low-exposure everolimus (3–7 ng/mL), or high-exposure everolimus (9–15 ng/mL). Following the core phase, patients
could enter the extension phase to receive everolimus at a targeted exposure range of 3–15 ng/mL up to 48 weeks after
the last patient had completed the core phase. Efcacy endpoints were response rate (≥50% of reduction from baseline
in average weekly seizure frequency) and median percentage reduction in seizure frequency during the 12-week
maintenance period of the core phase, and at 12-week intervals throughout the extension phase. This study is
registered with ClinicalTrials.gov, number NCT01713946.
Findings Between July 3, 2013, and May 29, 2015, 299 paediatric patients enrolled in the trial. In the younger
subgroup (<6 years; n=104), 34 received placebo, 33 low-exposure everolimus, and 37 high-exposure everolimus;
in the older subgroup (≥6 years to <18 years; n=195), 62 received placebo, 63 low-exposure everolimus, and
70 high-exposure everolimus. At the end of the core phase, response rate was higher in the treatment groups than
placebo in both the younger subgroup (17·6% [6·8–34·5] for placebo vs 30·3% [95% CI 15·6–48·7; p=0·2245]
for low-exposure everolimus vs 59·5% [42·1–75·2; p=0·0003] for high-exposure everolimus) and the older
subgroup (12·9% [5·7–23·9] vs 27·0% [16·6–39·7; p=0·0491] vs 30·0% [19·6–42·1; p=0·0179]), as were median
reduction in seizure frequency (12·3% [95% CI −10·1 to 24·8] vs 29·3% [95% CI 13·4 to 46·3; p=0·0474]
vs 54·7% [43·5 to 73·1; p<0·0001] in younger patients; 13·5% [−3·0 to 26·8] vs 31·0% [16·1 to 42·9; p=0·0128]
vs 34·8% [26·7 to 41·3; p=0·0006] in older patients). The efcacy persisted, with sustained seizure reduction
after 1 year of treatment across both paediatric subgroups (response rate 48·9% [95% CI 38·1–59·8] for the
younger subgroup vs 47·2% [39·3–55·2] for the older subgroup; median percentage reduction in seizure frequency
48·4% [95% CI 34·3–73·6] vs 48·0% [38·2–57·5]). At the cutof date for the extension phase, grade 3 or 4 adverse
events were reported in 45 (45%) younger patients (commonly pneumonia [n=16]) and 74 (38%) older patients
(commonly pneumonia [n=8] and stomatitis [n=6]). Two deaths (pneumonia, which was suspected to be treatment-
related, and sudden unexplained death due to epilepsy) were reported.
Interpretation Adjunctive everolimus resulted in sustained reductions in seizure frequency after 1 year and was well
tolerated in paediatric patients with treatment-refractory seizures associated with tuberous sclerosis complex.
Funding Novartis Pharmaceuticals Corporation.
Copyright © 2018 Elsevier Ltd. All rights reserved.
Introduction
Epilepsy is the most common presenting feature of
tuberous sclerosis complex, afecting 70–90% of pa-
tients.
1–4
The onset of seizures occurs within the frst
year of life in roughly 60% of patients, and can even be
observed in the neonatal period.
1–5
Adults with tuberous
sclerosis complex without a history of seizures continue
to be at risk (12%) for developing seizures in later years.
1
Furthermore, patients with tuberous sclerosis complex
have an 84–92% chance of having at least one seizure
during their lifetime.
6
Early seizure onset is associated
with an increased risk of refractory epilepsy, as well as