GILENYA

Product Name:       GILENYA

Code name:             FTY720

Common name:       Fingolimod

CAS No:                   162359-55-9

Indication:             Multiple sclerosis 

Mechanism of action


Fingolimod is a sphingosine 1-phosphate receptor modulator. Fingolimod is metabolised by sphingosine kinase to the active metabolite fingolimod phosphate. Fingolimod phosphate binds at low nanomolar concentrations to sphingosine 1-phosphate (S1P) receptor 1 located on lymphocytes, and readily crosses the blood-brain barrier to bind to S1P receptor 1 located on neural cells in the central nervous system (CNS). By acting as a functional antagonist of S1P receptors on lymphocytes, fingolimod phosphate blocks the capacity of lymphocytes to egress from lymph nodes, causing a redistribution, rather than depletion, of lymphocytes. Animal studies have shown that this redistribution reduces the infiltration of pathogenic lymphocytes, including pro-inflammatory Th17 cells, into the CNS, where they would be involved in nerve inflammation and nervous tissue damage. Animal studies and in vitro experiments indicate that fingolimod may also act via interaction with S1P receptors on neural cells.

Approvals

Gilenya was launched as a first-line treatment for relapsing forms of multiple sclerosis (MS) in the US and for relapsing-remitting MS in Russia. It was also approved as a first-line treatment for relapsing forms of MS in Australia, Switzerland and the United Arab Emirates. Gilenya was approved in the EU in March 2011 as a disease modifying therapy in patients with highly active relapsing-remitting multiple sclerosis (RRMS) despite treatment with beta interferon, or in patients with rapidly evolving severe RRMS. Novartis also received approval for Gilenya in September 2011 in Japan for the prevention of relapse and delay of progression of physical disability in adults with MS. Gilenya is currently approved in over 78 countries around the world.

Novartis acquired rights to Gilenya, known by the common name fingolimod (formerly known by the research number FTY720), from the Japanese pharmaceutical company Mitsubishi Tanabe Pharma Corp. in 1997.

Clinical Trials 

Remitting Multiple Sclerosis (RRMS)	Phase 3	completed
Chronic Inflammatory Demyelinating Polyradiculoneuropathy (CIDP)	Phase 3	Recruiting
Rett's Syndrome	Phase 2	Recruiting
Amyotrophic Lateral Sclerosis	Phase 2	Active, not recruiting
Schizophrenia	Phase 2	Recruiting
Acute Demylelinating Optic Neuritis	Phase 2	Terminated
Cerebral Stroke	Phase 2	Recruiting
Acute Noninfectious Posterior	Phase 2	Withdrawn

Product patent expiry

USA	February 2019*
South Korea	February 2018*
Canada	October 2013
Japan	October 2018*

* Patent expiry including patent term extension

Sales of the product (Source: From company report)

Year	2011	2012	2013	2014
Sales in US*	383	727	1023
Total Sales*	494	1195	1934	2477

*USD millions