Experimental and Clinical Studies on Rifacinna® - The New Effective Antituberculous Drug (Review)

Title: Experimental and Clinical Studies on Rifacinna® - The New Effective Antituberculous Drug (Review)

Volume: 5 Issue: 1

Author(s): Dimova Velichka, Atanasova Ivana, Tomioka Haruaki, Sato Katsumasa, Reddy Venkata, Geeta Nadadhur, Daneluzzi Donna, Gangadharam Patisapu, Kantardjiev Todor, Dhople Arvind, Feshchenko Yurii, Yashina Ljudmila, Toumanov Andrei, Zhivkova Zvetana and Sano Chiaki

Affiliation:

Keywords: Tuberculosis, rifamycins, rifacinna, T9, T11, Mycobacterium tuberculosis, in vitro, in vivo, pharmacokinetics, experimental tuberculosis

Abstract: A new rifamycin derivative 3-(4-cinnamyl-piperazinyl iminomethyl) rifamycin SV (T9) and its sodium salt (T11, Rifacinna®) were in vitro, in vivo, toxicologically and clinically investigated in comparison with rifampicin, rifapentine, rifabutin, rifalazil. Our experiments showed that Rifacinna exhibits excellent in vitro activity against Gram (+), Gram (-) aerobic, anaerobic pathogens and mycobacteria. Rifacinna is active against Staphylococcus, Streptococcus sp. including MRSA, with MIC90- 0.06 - 0.5mg/L; against Gram (+), Gram (-) anaerobes with MIC90 0.5 - 1mg/L; against Mycobacterium tuberculosis (MTB) with MIC90 0.062 mg/L; against MDR resistant MTB (25% - 30%) and Mycobacterium avium complex (MAC) strains with MICs 0.6-1.0mg/L. It shows high intraphagocytic activity against MAC strains (0.06-0.125mg/L). Single daily dose 10mg/kg provides complete erradication of mycobacteria in experimental generalized tuberculosis. Pharmacological studies established: excellent pharmacokinetic profile - following single oral dose 10mg/kg Tmax 5 - 6h, Cmax 5-9mg/L, T1/2 33-34 h; low toxicity; no teratogenic and embryotoxic effects. The clinical study of rifacinna shows higher therapeutic efficacy than rifampicin in patients with infiltrative, disseminated and cavitary form of pulmonary tuberculosis, good tolerability and safety profile. Some of the recent patents related to the treatment of tuberculosis are discussed in this review article.

Cite this article as:

Velichka Dimova, Ivana Atanasova, Haruaki Tomioka, Katsumasa Sato, Venkata Reddy, Nadadhur Geeta, Donna Daneluzzi, Patisapu Gangadharam, Todor Kantardjiev, Arvind Dhople, Yurii Feshchenko, Ljudmila Yashina, Andrei Toumanov, Zvetana Zhivkova and Chiaki Sano, Experimental and Clinical Studies on Rifacinna® - The New Effective Antituberculous Drug (Review), Recent Patents on Anti-Infective Drug Discovery 2010; 5 (1) . https://dx.doi.org/10.2174/157489110790112572