Welcome to “A to Z: Drugs in Highlight”
This series is designed to delve into the intricate realm of pharmaceutical drugs. As the world of pharmaceuticals continues to evolve with new discoveries and emerging challenges, we aim to shed light on the diverse array of medications available today, ranging from blockbuster medications to those that may not be as familiar. Whether you’re a healthcare professional, a student, or simply someone with a curious mind, “A to Z: Drugs in Highlight” promises to be an enlightening and engaging series.
G is for GILENYA®
GILENYA® (from Novartis) uses fingolimod as a disease modifying therapy for highly active relapsing multiple sclerosis. It is available as capsules (0.25 mg and 0.5 mg).
How it works:
In multiple sclerosis (MS), the immune system mistakenly attacks the myelin sheath, the protective covering around nerve fibers in the central nervous system (CNS), which includes the brain and spinal cord. This leads to inflammation and damage, disrupting the normal signals.
GILENYA® contains the active substance fingolimod. Fingolimod works by modulating the immune system to reduce this damage. Specifically, fingolimod targets a receptor on T cells called the sphingosine-1-phosphate (S1P) receptor. By binding to this receptor, fingolimod prevents T cells from leaving the lymph nodes and entering the bloodstream. This action reduces the number of T cells that can reach the CNS and cause inflammation and damage.
This mechanism helps to:
· Reduce the frequency of MS relapses (flare-ups).
· Slow the progression of physical disability associated with MS.
· Decrease the number of new or enlarging brain lesions as seen on MRI scans.
GILENYA’s ability to sequester T cells in the lymph nodes is reversible, meaning that if the treatment stopped, the T cells can eventually return to normal circulation.
Market impact:
GILENYA® is approved for marketing in more than 50 countries including in the United States (approved by the FDA in September 2010) and Europe (approved by the EMA in March 2011). It has been used treat more than 300,000 patients worldwide.
GILENYA® has been a significant revenue generator for Novartis over the years. In 2023, GILENYA® generated approximately USD 925 million in net sales for Novartis, a 54% decrease compared to 2022. The decrease in net sales from 2022 to 2023 is likely due to increased competition in the market (especially in the US). However, despite increasing competition, GILENYA® continues to be a preferred choice for many patients and healthcare providers due to its convenient oral dosing and long-term efficacy.
Patent protection:
There are a number of patent rights protecting various aspects of GILENYA® in the United States and Europe (as well as in many other countries around the world).
US patent no. 9187405 relates to a method for treating Relapsing-Remitting multiple sclerosis in a subject in need thereof, comprising orally administering to said subject 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol (fingolimod), in free form or in a pharmaceutically acceptable salt form, at a daily dosage of 0.5 mg, absent an immediately preceding loading dose regimen.
In June 2022, the US Court of Appeals of the Federal Circuit invalidated US patent no. 9187405. Novartis sought to overturn this decision by petitioning for a rehearing, but the Federal Circuit denied this request. Novartis then took the case to the US Supreme Court, which also declined to hear the case. As a result, the invalidation of the patent has allowed generic manufacturers to enter the US market.
EP patent no. 2959894 was granted by the European Patent Office (EPO) in 2022 and relates a S1P receptor modulator for use in the treatment of relapsing-remitting multiple sclerosis, at a daily dosage of 0.5 mg p.o., wherein said S1P receptor modulator is 2-amino-2-[2-(4-octylphenyl) ethyl]propane-1,3-diol (fingolimod) in free form or in a pharmaceutically acceptable salt form.
No less than 23 notices of opposition were filed against the grant of European patent no. 2959894. Oral proceedings before the Opposition Division are scheduled to take place on 10th to 14th February 2025. Should the patent be revoked, and subject to any appeal, it would allow generic manufacturers to enter the European market before the 2027 expiration date.