<%@LANGUAGE="VBSCRIPT" CODEPAGE="1252"%> Sun Pharma Advanced Research Company Ltd. - Annual Report 07-08
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  Allergy  
  Anti-inflammatory for
Asthma/ COPD
 
  Antiepileptic -
modification of absorption
 
  Muscle relaxant -
modification of absorption
 
     
   
  Perennial allergic rhinitis starts in early childhood and occurs all year round. It is caused by allergy to the aerosolised droppings (faeces) of house dust mites and pet skin flakes (dander).  
   
     
Amongst other pathways it is involved in, a histamine mediated pathway is thought to be directly involved in the mechanisms that lead to allergy related manifestations - allergic rhinitis and urticaria.
Currently available drugs such as loratadine, terfenadine, diphenhydramine, chlorpheniramine, and cetirizine, known as H1 receptor antagonists, prevent the binding of histamine to the cell and the consequent synthesis and release of chemical mediators that produce the symptoms of allergy. Unfortunately the classical antihistamines like diphenhydramine and chlorpheniramine are highly sedating, and since these drugs do not selectively bind to H1 receptor alone, they result in also other side effects like dry mouth, blurred vision etc. Later developed antihistamines such as terfenadine and astemizole produce serious side effects like arrythmia or irregular heart beats. The relatively newer drugs are also not without problems, for example cetirizine is known to cause sedation in about 25% of the population, and loratadine has a slower onset of action. Thus there is a need for drugs that bind with high selectivity to H1 histamine receptors and provide potent, effective action without long term side effects.
SUN-1334H, the first lead molecule from our NCE program, is a selective histamine H1 receptor antagonist.
SUN-1334H has now finished Phase II clinical trials for seasonal allergic rhinitis in the US. The data from these trials is being collected and analyzed.
Like most antiallergics, this can be given as an oral drug, and will be eventually be formulated as a tablet or capsule. Current data indicates that it can be formulated as a once-a-day medication, making it easier for patients to take.
Features designed in SUN-1334H, provide desired characteristics to the molecule so as to make it fast acting and less sedating.
The findings of chronic toxicity studies in animals indicate that the molecule is well tolerated, effective and safe for use even at doses that are over 35 times the effective dose. SUN-1334H seems devoid of cardiac toxicity issues.
Phase II clinical studies on patients for proof of concept and dose titration for seasonal allergic rhinitis have been completed. Phase II studies for chronic idiopathic urticaria have also been completed.