2. A new indication for old drug Ethyl-6-bromo-4-[(dimethylamino)methyl]-5-hydroxy-1-methyl-2-[(phenylthio)methyl]-indole-3-carboxylate hydrochloride monohydrate is widely used in Russia for prevention and treatment of flu and other viral infections. 26,35 million of packs of Arbidol® were sold in 2008 .
3. A new target MC-101 inhibits protein kinase C alpha (PKCα)
4. A new target The same specificity shows major metabolite МС-109
6. A possible role of MC-101 in inflammation process МС-101 Pic. from «Targeting the NF-κB pathway in asthma and chronic obstructive pulmonary disease» M.R. Edwards et al. / Pharmacology & Therapeutics 121 (2009) 1–13
7. A possible role of MC-101 in inflammation process МС-101 Pic. from Targeting the NF-κB pathway in asthma and chronic obstructive pulmonary disease M.R. Edwards et al. / Pharmacology & Therapeutics 121 (2009) 1–13
8. The most promising new indication for MC-101 is asthma MC—101 shows anti-inflammatory activity. Viral infections cause more than half of all cases of asthma attacks. MC-101 has a huge advantage because of its antiviral activity.
9. Asthma animal model MC-101 was evaluated for possible inhibition of airway hyperresponsiveness in mice. The ovalbumin (OVA)-sensitized animals, 10 animals per group, were challenged by nasal inhalation with aerosolized 5% OVA for 25 min on Days 21, 23, and 25. The mice received vehicle, reference standard (Dexamethasone, 3 mg/kg) or MC-101 by gavage (PO) once daily from day 21 to day 26, preceding ovalbumin aerosol challenge by 60 min on days 21, 23 and 25 as well as methacholine challenge on day 26. Noninvasive measurements of airway responsiveness were performed by using whole body plethysmography, using increases in enhanced pause (Penh) as an index of airway obstruction. Responses to inhaled methacholine were measured and calculated as percentage of respective baseline values. MC-101 Dexametasone
18. Anti-asthmatic potency of MC-101 An open-label stratified randomized parallel group study conducted at the Pulmonology Research Institute (Moscow, Russia) under the direction of Prof. Alexander Chuchalin, President of Russian Association of Pulmonologists. The purpose was to evaluate anti-asthmatic potency of MC-101.
19. Trial groups The experimental group (12 patients) – Arbidol® 100 mg twice a day plus short acting beta agonists (SABA) The comparator group (12 patients) - Singular® 10 mg once a day plus short acting beta agonists (SABA) The control group (12 patients) – short acting beta agonists (SABA)
20. Trial targets Reduction of asthma attack quantity Improvement of spirography parameters Reduction of medium SABA dose.
22. Measurement of peak flow and spirographyin experimental group(Wilkinson criteria)
23. Measurement of peak flow and spirographyin control group (Wilkinson criteria)
24. Measurement of peak flow and spirographyin comparator group (Wilkinson criteria)
25. Dynamics of frequency of asthma attacks Number of patients Administration of Arbidol and Syngularreduce frequency of asthma attacks
26. Dynamics of frequency of SABA inhalations Administration of Arbidol and Syngularreduce frequency of SABA inhalations
27. Results Oral administration of MC-101 in the dose of 100 mg twice a day within 28 days improves clinical course of bronchial asthma of light and average severity, reducing the frequency of asthma attacks and requirement of using of short acting beta agonists. Effectiveness of the drug was shown by the measurement of peak flow and spirography (FVC, FEV1, FEV1%). No negative side effects have been revealed.