Antibiotic macrocycle compounds and methods of manufacture and use thereof
View Patent ↗The invention encompasses an active metabolite of the 18-membered macrocyclic antimicrobial agents, specifically, a metabolite of tiacumicin B and in certain embodiments, R-Tiacumicin B or and its related compounds. In particular, the invention encompasses a compound that acts as a potent antibiotic agent for the treatment of bacterial infections, specifically GI infections caused by toxin producing strains of Clostridium difficile ( C. difficile ) and Clostridium perfringens ( C. perfringens ).
1. A method of treating a Clostridium difficile infection in a subject in need thereof comprising administering to the subject a composition comprising a therapeutically effective amount of a compound of Formula II:
in free form or in the form of a pharmaceutically acceptable salt thereof.
2. The method of claim 1 , wherein the infection is a gastrointestinal infection.
3. The method of claim 2 , wherein the subject is human.
4. The method of claim 3 , wherein the subject has previously been treated for a Clostridium difficile infection with a compound other than Formula II.
5. The method of claim 3 , wherein the subject is suffering from Clostridium difficile associated diarrhea.
6. The method of claim 3 , wherein the subject is suffering from pseudo-membranous colitis.
7. The method of claim 6 , wherein the subject is suffering from antibiotic associated diarrhea.
8. The method of claim 2 , wherein the route of administration is oral.
9. The method of claim 1 , wherein the dosage is 0.1 milligrams to 200 milligrams per kilogram of the subject's body weight.
10. The method of claim 1 , wherein the dosage is 1 milligram to 200 milligrams per kilogram of the subject's body weight.
11. The method of claim 1 , wherein the dosage is 1 milligram to 100 milligrams per kilogram of the subject's body weight.
12. The method of claim 1 , wherein the dosage is 2 milligrams to 50 milligrams per kilogram of the subject's body weight.