Azasteroid Codrugs for Treatment of Tuberculosis

Compounds that increase TB therapy efficacy through a mechanism of action for increased tolerance and decreased therapy duration. Background: One third of the world’s population is infected with tuberculosis (TB). In 2014, there were 1.5 million TB related deaths. The current recommended treatment regimen for TB begins with a two-month intensive therapy using isoniazid, rifampicin, pyrazinamide, and ethambutol followed by four months of treatment with isoniazid and rifampicin. The long and complex treatment regimen leads to high levels of nonadherence. This contributes to the development of drug resistant TB that becomes more difficult and expensive to treat. Technology Overview: Researchers have identified novel compounds that are potentiators of existing TB drugs. These compounds work with both first-line and second-line TB drugs including those that are active against MDR-TB (e.g., Bedaquiline and PA-824). The drug scaffold from which these compounds were derived have high stability _in vivo_, low host toxicity, and excellent host bioavailability. The proposed therapy will reduce dose and/or time of treatment, and consequently reduce treatment costs and improve treatment outcomes. Advantages: Potentiator of both first-line and second-line TB drugs

Novel target and mechanism of action

Effective with both drug sensitive and drug resistant TB therapies

Leads are orally available with excellent PK Applications: - Tuberculosis - Anti-infective therapeutics #8775 Intellectual Property Summary: Patent application submitted Stage of Development: US 8,481,530 B2 PCT filed covering new compositions and methods of use Licensing Potential: Development partner,Licensing,University spin out Licensing Status: Additional Information: tuberculosis,second-line,drug scaffold,bioavailability,orally,mycobacterium tuberculosis,disease treatment,drug resistance,multi-drug resistant,oral bioavailability,anti-infectives,pharmacokinetics,pharmacokinetic,drug design,drug development,toxicity,third world,4g,therapeutics Please note, header image is purely illustrative. Source: CDC, Wikimedia Commons, public domain.

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