TT99000647

TT99000647 is a bone-targeting prodrug developed by Targanta Therapeutics for the treatment of osteomyelitis. It consists of the rifamycin antibiotic rifabutin covalently linked to a bisphosphonate moiety. This design utilizes the high affinity of bisphosphonates for hydroxyapatite to concentrate the antibiotic within bone tissue, potentially improving efficacy and reducing systemic toxicity in the treatment of difficult-to-reach bone infections. Once at the bone site, the prodrug is designed to release active rifabutin, which exerts its antibacterial effect by inhibiting bacterial DNA-dependent RNA polymerase. Preclinical studies in rabbit and rat models of osteomyelitis have demonstrated that TT99000647 significantly reduces bacterial load compared to rifabutin alone.

Other names

rifabutin-bisphosphonaterifabutin-bisphosphonate prodrug