Pipeline

Our development program focuses on new approaches to neurological diseases and disorders.

Our portfolio has a number of compounds with multiple potential indications and multiple targets. This is an ideal portfolio for innovative, experimental medicine techniques, including state-of-the-art imaging tools, to establish rapid proof-of-concept through small, smart clinical trials. This will allow us to find in a cost-effective and efficient manner the best indication for each compound and the best compound for each indication.

Please click in the compounds for further information

SYN-111 is a potent, specific, and orally bioavailable sodium channel blocker with proven anti-epileptic and anxiolytic activity in preclinical studies that are highly predictive of clinical activity in man. In recent Phase III clinical studies in more than 1,200 patients with Lennox Gastaut Syndrome (LGS) - a severe form of epilepsy - SYN-111 resulted in a significant reduction in the incidence and severity of seizures. The onset of clinical anti-epileptic activity was rapid. Eisai was granted approval in the EU in January 2007 to market Inovelon (rufinamide) as adjunctive therapy in LGS.

SYN-111 may also be effective in rapidly relieving anxiety in patients without the risk of dependence associated with benzodiazepines or the risk of adverse sexual side effects associated with serotonin or serotonin-norepinephrine blockade.

Synosia has completed an encouraging proof-of-concept study on SYN-111 and started a Phase II study in March 2008.

Indication: Anxiety

Source: Novartis

SYN-114 is an orally bioavailable, potent and selective small molecule antagonist of the 5-HT6 receptor. 5-HT6 receptors are expressed exclusively in the brain and in regions associated with memory function.

The molecule is active in a variety of preclinical models of cognition and executive function. SYN-114 facilitates memory consolidation and demonstrates effects consistent with enhanced cholinergic function.

Synosia is investigating clinical development plans for SYN-114.

Indication: Cognitive disorders

Source: Roche

SYN-115 is a potent and selective inhibitor of the A2A receptor, which modulates the production of dopamine, glutamine and serotonin in specific regions of the brain.

In preclinical models of Parkinson's disease, A2A inhibition has resulted in increased levels of dopamine, resulting in the reversal of motor deficits.

Synosia has started a Phase IIa study on SYN-115 and plans to start a Phase IIb study in 2009.

Indication: Parkinson's disease

Source: Roche

SYN-116 is an orally bioavailable, potent and selective inhibitor of the IP-receptor, which is under evaluation for the treatment of mild to moderate acute and post-operative pain. Tissue injury results in the release of prostanoids - primarily PGE-2 and PGI-2 - that activate receptors on sensory neurons causing a painful sensation.

Selectively inhibiting the effect of PGI-2 has the potential to deliver analgesic efficacy at least comparable to the non-steroidal anti-inflammatory drugs (NSAIDs) but without the side-effects associated with the inhibition of PGE-2.

Synosia plans to initiate phase IIa studies on SYN-116.

Indication: Acute pain

Source: Roche

SYN-117 is a potent, competitive, and selective dopamine
β-hydroxylase inhibitor under investigation for the treatment of drug dependency and post-traumatic stress disorder (PTSD).

Dopamine β-hydroxylase is the main enzyme responsible for the conversion of dopamine into norepinephrine. The inhibition of this enzyme has been shown to raise dopamine levels in the CNS.

Nepicastat is orally available and well tolerated in preclinical models and in the clinic at doses significantly above the expected therapeutic range.

Synosia has started Phase IIa studies in cocaine dependency and post-traumatic stress disorder (PTSD).

Indications: Drug dependency and PTSD

Source: Roche

SYN-118 is a potent and selective inhibitor of hydroxyphenylpyruvate dioxygenase (HPPD), the primary enzyme responsible for the catabolism of tyrosine the precursor of the neurotransmitter dopamine. Preclinical studies have shown that SYN-118 is active in models of Parkinsons disease and Restless Legs Syndrome.
Clinical studies and patient experience with SYN-118 have shown pronounced and reliable elevations in the levels of tyrosine with once-daily dosing.
Swedish Orphan has gained approval for SYN-118 for the treatment of hereditary tyrosinemia type 1, which is marketed under the brand name Orfadin (nitisinone).
Synosia has started a proof-of-mechanism study on SYN-118 for Parkinson’s disease and plans to start a Phase II study in 2009. The company has also started a proof-of-concept trial on SYN-118 for Restless Legs Syndrome.

Indication: Parkinson's disease and Restless Legs Syndrome

Source: Syngenta

SYN-119 potently and selectively enhances the activity of glutamate at the mGluR-1 receptor. The molecule is under evaluation for the treatment of drug dependency.

Certain drugs of abuse cause plasticity in regions of the brain associated with pleasure and reward.

In preclinical studies, SYN-119 has been shown to prevent or reverse these changes and so has the potential to modulate the addictive properties of drugs of abuse, facilitate withdrawal from these drugs and decrease relapse rates.

SYN-119 is in preclincial studies.

Indication: Drug dependency

Source: Roche

SYN-120 is an orally bioavailable, potent and selective small molecule antagonist of the 5-HT6 receptor. 5-HT6 receptors are expressed exclusively in the brain and in regions associated with memory function. SYN-120 was in-licensed from Roche in an agreement announced in March 2009.

The molecule is active in a variety of preclinical models of cognition and executive function. SYN-114 facilitates memory consolidation and demonstrates effects consistent with enhanced cholinergic function.

Synosia is investigating clinical development plans for SYN-120.

Indication: Cognitive disorders

Source: Roche