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Josamycin and Rosaramicin
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Josamycin 500 mg three times a day was less effective than brodimoprim in the treatment of otitis media (de Campora et al., 1993). In a study comparing 5 days’ administration of josamycin with administration of penicillin G for 10 days for the treatment of acute group A beta-hemolytic streptococcal tonsillitis, the two regimens yielded equivalent clinical outcomes (Portier et al., 2001). A recent survey in France demonstrated that more than 95 % of S. pyogenes are still susceptible to josamycin (Auzou et al., 2015).
Dihydrofolate reductase inhibitors: patent landscape and phases of clinical development (2001–2021)
Published in Expert Opinion on Therapeutic Patents, 2022
Kavita Bhagat, Nitish Kumar, Harmandeep Kaur Gulati, Aanchal Sharma, Amandeep Kaur, Jatinder Vir Singh, Harbinder Singh, Preet Mohinder Singh Bedi
Moreover, Brodimoprim, invented by Roche, a TMP analog containing diaminopyrimidine pharmacophore, is now used for the treatment of respiratory tract infections. It was also found that it exhibited elongated elimination half time of 32–35 h, higher tissue penetration and volume of distribution as compared to TMP. But it possesses similar toxicological and bacterial properties as shown by TMP which led to withdrawal of Brodimoprim from the market in 2000. After Brodimoprim, Epiroprim, a diamonopyrimidine analog also exhibited superior antibacterial properties and lipophilicity as compared to TMP. It basically showed a synergistic effect when used with dapsone against Mycobacetrium ulcerans and leprae in vivo, but no further work was carried out to make this drug available in the market [22–24]