Study in The New England Journal of Medicine Shows Novartis Corporation (NVS) Drug Afinitor(R) Reduces Size of SEGAs

Study in The New England Journal of Medicine Shows Novartis Corporation (NVS) Drug Afinitor(R) Reduces Size of SEGAs, Benign Brain Tumors Associated with Tuberous Sclerosis
EAST HANOVER, N.J., Nov. 3, 2010 /PRNewswire/ -- TheNew England Journal of Medicine (NEJM)today published a study that found patients taking Afinitor® (everolimus) tablets experienced a decrease in the size of their subependymal giant cell astrocytoma (SEGA), a benign brain tumor associated with tuberous sclerosis (TS)(1,2). This study, which was previously presented at the 46th American Society of Clinical Oncology annual meeting, is the first prospective clinical trial of a drug to show treatment benefit in these patients.

Tuberous sclerosis is a genetic disorder that is estimated to affect 25,000 to 40,000 people in the US and may cause benign tumors to form in vital organs(3). SEGAs, benign brain tumors, occur in up to 20% of patients with TS and primarily affect children and adolescents(1,4,5). SEGAs may pose a significant medical risk, including the potential for swelling in the brain, or hydrocephalus(1).

According to data published in NEJM from this Phase I/II study of 28 patients conducted by Cincinnati Children's Hospital Medical Center, treatment with everolimus was associated with a significant reduction in primary SEGA volume at six months relative to baseline on independent central review (p<0.001). Seventy-five percent of patients (21 of 28) experienced a reduction of 30% or greater in the size of their largest SEGA and 32% (9 of 28) experienced a reduction of 50% or greater at six months relative to baseline(2).

The published study findings also showed that in nine of 16 patients, everolimus therapy was associated with a reduction from baseline to six months in overall frequency of seizures per 24 hour video electroencephalograms (EEG) (n=16; median change -1 seizure, p=0.022). Additionally, no patients required surgery or developed a new SEGA while receiving everolimus(2).

The most common adverse reactions observed (incidence greater than or equal to 30%) in this trial were mouth sores, upper respiratory tract infections, sinusitis, middle ear infections and fever(2).

"This is the first clinical trial to show that a drug has the potential to provide patients with growing SEGAs, many of whom are children, another treatment option besides brain surgery," said David Franz, MD, Director, Tuberous Sclerosis Clinic at Cincinnati Children's Hospital Medical Center and principal investigator of the study.

About the study published in NEJM

In this Phase I/II study, 28 patients aged three years and above (median age=11, range 3-34) with evidence of SEGA growth initially received everolimus orally at a dose of 3 mg/m2 once-daily or on an alternate day regimen. Doses were subsequently adjusted subject to tolerability to attain a trough concentration of 5-15 ng/mL(2).

The study met its primary efficacy endpoint of change in primary SEGA lesion volume from baseline to six months (or at the last available assessment if a patient discontinued treatment prior to month six [one patient discontinued the trial before six months]). Everolimus was associated with a statistically significant reduction in primary SEGA volume at six months relative to baseline on independent central review (p<0.001). As of December 9, 2009, the median duration of treatment was 21.5 months(2).

Study findings also showed that everolimus was associated with a reduction from baseline to six months in overall frequency of seizures per 24 hour EEG (n=16; median change -1 seizure, p=0.022). Of 16 patients with seizures at the start of the study for whom EEGs were available, nine experienced decreases in seizure frequency, six reported no change and one experienced an increase at six months(2).

The reliability of the frequency of adverse reactions and laboratory abnormalities reported in this trial is limited because of the small number of patients. The most common adverse reactions reported (incidence greater than or equal to 30%) in this trial were mouth sores, upper respiratory tract infections, sinusitis, middle ear infections and fever(2).

All data reported in this study published in NEJMare based on the cut-off date of December 9, 2009(2).

About Afinitor (everolimus)

Afinitor® (everolimus) tablets is now approved in the US to treat patients with SEGA associated with tuberous sclerosis who require therapeutic intervention but are not candidates for curative surgical resection. The effectiveness of Afinitor is based on an analysis of change in SEGA volume. Improvement in disease-related symptoms or increase in survival has not been shown. A Phase III study is underway that compares everolimus to placebo to explore the clinical benefits of Afinitor for the treatment of patients with SEGA associated with TS. Afinitor is available in the US in 2.5 mg, 5 mg and 10 mg tablet strengths.

Novartis has submitted marketing applications for everolimus to the European Medicines Agency (EMA) and the Swiss Agency for Therapeutic Products (Swissmedic), and additional regulatory submissions are underway worldwide. If approved in the European Union (EU) for this indication, everolimus will be made available under the trade name Votubia®.

There is no guarantee that everolimus will become commercially available for SEGA anywhere else in the world. As an investigational compound, the safety and efficacy profile of everolimus has not yet been established outside the US in patients with SEGA associated with TS.

Afinitor is also approved in the US for the treatment of patients with advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib and in the European Union (EU) for the treatment of patients with advanced RCC whose disease has progressed on or after treatment with vascular endothelial growth factor (VEGF)-targeted therapy.

In the US, everolimus is available in different dosage strengths under the trade name Zortress® for the prophylaxis of organ rejection in adult patients at low-moderate immunologic risk receiving a kidney transplant. In the EU, everolimus is available in different dosage strengths under the trade name Certican® for the prevention of organ rejection in heart and kidney transplant recipients.

Not all indications are available in every country.

Important Safety Information about Afinitor (everolimus) tablets

Patients should not take Afinitor if they are allergic to Afinitor or to any of its ingredients. Patients should tell their healthcare provider before taking Afinitor if they are allergic to sirolimus (Rapamune®) or temsirolimus (Torisel®).

Afinitor can cause serious side effects including infections or lung or breathing problems.

Afinitor may make patients more likely to develop an infection, such as pneumonia, or a bacterial, fungal or viral infection. Viral infections may include reactivation of hepatitis B in people who have had hepatitis B in the past. In some people these infections may be severe, and can even lead to death. Patients may need to be treated as soon as possible. Patients should tell their healthcare provider right away if they have a temperature of 100.5 degrees F or above, chills or do not feel well. Symptoms of hepatitis B or infection may include the following: fever, skin rash, joint pain and inflammation, tiredness, loss of appetite, nausea, pale stool or dark urine, yellowing of the skin or pain in the patient's upper right side.

In some patients lung or breathing problems may be severe, and can even lead to death. Patients should tell their healthcare provider right away if they have any of these symptoms: new or worsening cough, shortness of breath, difficulty breathing or wheezing. Patients may need to stop taking Afinitor for a while or use a lower dose.

Afinitor can cause mouth ulcers and sores. Patients should tell their healthcare provider if they have pain, discomfort or open sores in their mouth. Their healthcare provider may tell them to use a special mouthwash or mouth gel that does not contain alcohol or peroxide.

Patients will have regular blood tests before they start and during their treatment with Afinitor. These tests will monitor how their kidneys and liver are working, their blood sugar and cholesterol levels as well as the number of blood cells in their body. Patients who receive Afinitor for the treatment of SEGA will need regular blood tests to measure how much Afinitor is in their blood since this will help their doctor decide how much Afinitor they need to take.

Afinitor may affect the way other medicines work, and other medicines can affect how Afinitor works. Using Afinitor with other medicines can cause serious side effects. Patients should tell their healthcare provider about all of the medicines they take, including prescription and non-prescription medicines, vitamins, herbal supplements such as: St. John's Wort, and medicine for fungal infections, bacterial infections, tuberculosis, seizures, HIV-AIDS, heart conditions or high blood pressure and medicines that suppress their immune system. Patients should not drink grapefruit juice or eat grapefruit during their treatment.

Patients should not take Afinitor tablets which are broken or crushed. Patients should not chew or crush the tablets.

Patients should tell their healthcare provider about all their medical conditions, including if they have or have had liver problems, diabetes or high blood sugar, high cholesterol levels, infections, hepatitis B or other medical conditions.

Patients should tell their healthcare provider if they are scheduled to receive any vaccinations. Patients should not receive a live vaccine or be around people who have recently received a live vaccine during treatment with Afinitor.

It is not known if Afinitor will harm a patient's unborn baby. Patients should use effective birth control while using Afinitor and for 8 weeks after stopping treatment.

Common side effects of Afinitor in patients with SEGA include mouth ulcers, infections of the respiratory tract, sinuses and ears and fever. Common side effects of Afinitor in patients with advanced kidney cancer include mouth ulcers, infections, feeling weak or tired, cough and diarrhea.