The active ingredient is a unique substance, its pharmaceutical effect on the body allows for the necessary treatment to take place. The effectiveness of the drug depends on accurately selected AI.
Active Ingredient (AI) has an international non-proprietary name (INN). INN is selected based on the chemical name of the AI and is usually set only for the active part of the molecule. This makes it possible to avoid prolonged listing in cases where several salts, complex esters and such are used in the substance.
Over 10 years have passed from the moment of molecule creation to the release of the drug OFO7788 (directed tissue regeneration) on the market.
Numerous studies and plannings have been carried out in the course of those years.
Work process:
Research and the search of the active ingredient. Strategising of the market.
Preclinical developments.
Included: The announcement of working variations (WV); Organization of WV; Beginning of pre-clinical development.
CI or clinical trials (included 1.2.3 phases). Beginning of Phase 1: First Human Study; Beginning of Phase 2a (Proof of Concept); Beginning of Phase 2b; Phase 3.
Life cycle management of LP and pharmacological supervision following the drug approval. The phase included: application for the issuance of the certificate of registration; issuance of a certificate. Launch of OFO7788 on the market (until then,the treatment was not available to patients); making corrections.
How did the preliminary study go?
Researchers and pharmaceutical companies performed preparatory work during which the disease – cirrhosis of the liver was examined and analysed. And the unmet need for the therapy used has been proven.
This was confirmed by the fact that:
Absence of effective drugs.
Several drugs that are present on the market, but they cause significant side effects in some patients, making it impossible for them to take the drug.
The initial stage of development of OFO7788 included gathering of data on:
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principle of action;
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efficiency;
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presence of toxic effects during use.
principle of action;
efficiency;
presence of toxic effects during use.
After the drug was developed, the study was conducted in laboratory animals. We assessed the relevance of the issue, developed formulas and Active Ingredient (AI) OFO7788. The active ingredient has been tested in test tubes (in vitro) and in animals (in vivo). All the necessary technological processes were observed to prevent any errors.
What was done? As in clinical trials, a study was conducted on a large number of animals. Splitting into groups was done randomly, using a blind method (the researcher does not know the effect of which treatment is taking place – placebo, previously used or the newcompound–researcher is observing and evaluating).
During our work with the new drug OFO7788pre-clinical stage included:
1. Design of a new molecule, screening and synthesis of new
substances.
2. Pre-clinical studies:
• Study of the drug in vitro and in vivo.
• Diagnostics of absorption, distribution and excretion
kinetics of the pharmacological substances in the new
drug.
• Toxicity and safety evaluation.
• Study of mutations and carcinogenesis (if any).
• Computer modeling of the conducted study
3. Beginning of Clinical Study
Each of the steps included additional work:
• Formula Search. Inhibitor identification including target identification and validation; formula search; compound database management; toxicity screening.
•Optimization of combinations.. Included the following work stages: optimization of prototypes; a study of activity-structure dependence.
• Development of chemical composition: synthesis of active components; crystallization; particle engineering.
• Development of the production process (laboratory and pilot): testing of raw materials, mixing, grinding, testing of the final product; purity validation; safety production.
Composition and release form of OFO7788:
powder used for solution/suspension preparation and ingestion.
The suspension is viscous, opaque, color range from white to light brown.
Active Ingredient:
immobilized hyaluronate-endo-N-acetylhexosaminidase-300 mg
Inactive Ingredients, auxiliaries are used to create:
• required medicinal form,
• complex physico-chemical properties (aiding in a correct distribution of the drug in the body)
• collective effect in support of Active Ingredient (AI);
• smoothing out of possible side effects.
Rational use of excipients made it possible to increase the effectiveness of pharmacotherapy with the help of the drug OFO7788:
• Citric acid (anhydrous) – 2.015 mg. Stabilizer pH.
• Sodium citrate (anhydrous) – 7.2 mg. The substance reduces coagulation and increases the alkaline blood reserves, leaches urine, makes hemocoagulation (in vitro) impossible. Increases the concentration of sodium ions (Na+) in the blood plasma.
• Sodium benzoate – 1.83 mg. Preservative.
• MCC and sodium carmellosis 125.4 mg. MCC is a natural source of food fibres, natural enterosorbent with high detoxifying and adsorption properties.
Kameda xanthane – 7.9 mg; silicon colloid dioxide – 13.733 mg; silicon dioxide – 0.186 g. Listed substances are enterosorbents that bind and remove toxins including heavy metal salts.
• Mannitol – 80 mg. Diuretic, that promotes fluid elimination from the body.
1 bottle of OFO7788 contains 5 daily dosages of 20 ml/60 mg.
Carefully selected combination of AI and auxiliary components open possibilities for highly effective treatment schemes for patients with cirrhosis.
OFO 7788 was prescribed in a daily dose of 20 mg/ml, the duration of the therapy – 4 weeks.
Favorable safety profile and to lernace were reported.
The half-life period is:
in 1st phase of two-phase model (T1/2ka) – 1.84 h,
in the second phase (T1/2ke) – 5.26 h.
Time of reaching max blood level:
Tmax – 1.0 h,
Cmax – 50 ng/ml.
The degree of binding to blood plasma proteins reaches 78%.
OFO7788 has proved in its initial development prospects.
Institutional Review Board has approved the program for clinical research of the drug.
We have also submitted an application for registration of a new drug to the Agency for Drug Administration and Control.
After OFO7788 was approved for clinical trials and human testings.