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Lofarma patent: sublingual allergoid. An invention against allergies

To date many dozens of thousand people have been treated with an anti-allergy vaccine based on the sublingual monomeric allergoid, with their great satisfaction and that of the physicians treating them: this is the best acknowledgement that Lofarma can get, as Italian company with had office in Milan and specialized in the allergy sector, manufacturing medicinal products aiming at prevention, diagnosis and treatment of allergic diseases.

Let’s go back over the story of such invention, worthy of taking out a patent. The term “allergoid” comes from the combination of the word “allergen” with suffix “-oid”, which in medicine sector scientists assigned to certain molecules that must be chemically changed before being used due to their toxicity.
Tetanus “toxin”, for instance, become a “toxoid” when it is treated with formaldehyde so that its poisoning property is destroyed but its capacity to stimulate the formation of toxin antibodies, i.e. to vaccinate, remains.
In allergic patients allergens may cause sneezes, lacrimation, rhinitis, short breath, asthma and even anaphylactic shock, although they are not toxic. This is due to the existing antibodies that trigger the allergic reaction while reacting with the allergen. How can therefore such antibodies be eluded in order to get a vaccine that is effective without inducing any harmful allergic reaction?

The strategy is the same as that adopted for the formation of “toxoids” from toxins: chemical modification of allergens in order to achieve “allergoids”.
The first allergoids were prepared by treating allergens with substances binding 50- 100 allergenic molecules together. Such “polymeric” allergoids are suitable for the injectable anti-allergy vaccine that proves to be safer than other anti-allergy vaccines relating to side effects, but certainly not welcome by patients, especially children. It is impossible to suppose an oral administration of such an allergoid, because its large molecular “size” does not allow the oral mucosa and gastrica to absorb it, thus exposing it to the proteolytic enzyme attack and nullifying every therapeutic efficacy.


The goal of Lofarma research was therefore to find a new way to get an allergoid suitable for the absorption by oral mucosa and gastrica with a molecular “size” almost identical to that of the natural allergen and resistant to the destructive action of enzymes.
And it was really Lofarma that discovered a special chemical modification, the so-called carbamylation, which keeps the molecular size of the allergoid unchanged, if carried out in certain conditions, thus allowing it to be absorbed: the goal was reached.
The carbamylated allergoid moreover eludes the proteolytic enzyme attack, such as the gastroenteric enzymes, thus allowing the allergenic molecule to remain intact and to keep its own therapeutic properties.

The monomeric allergoid
Laboratory reports show that such allergoid – since then called “monomeric” as opposed to “polymeric” – does not cause the allergic reaction, while improving and strengthening immunologic capacities.
The patent application was filed in Italy and extended to all industrialised countries worldwide. After carrying out rigorous analysis that lasted some years, Lofarma invention was acknowledged as valid since it held the three requirements of novelty, industrializability and description. The patent was finally issued being the crowning achievement of the huge investments that Lofarma makes to improve the quality of life of allergic patients.

Lofarma