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KDDF-201712-07 Discovery of novel anti-tubercular agent for the treatment of multidrug-resistant/extensively drug-resistant tuberculosis(Infectious Diseases, Chemical) [2019-06-24]

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Ongoing Project
Section Lead
Generation
Lead
Optimization
Preclinical Phase I Phase II Phase III

Development and Market Objectives

Innovative tuberculosis drug candidates for control of drug-resistant Mycobacterium tuberculosis

Unmet Medical Need & Target Patients

Target patient group

- Patients with multiple drug resistance (MDR) including rifampicin resistance and extensively drug resistance (XDR) Mycobacterium tuberculosis infections

- Drug-sensitive TB patients

 

Unmet Medical Needs

- According to the WHO report, patients with MDR-TB and XDR-TB are increasing year by year, 480,000 MDR-TB patients were reported.

- Patients with rifampicin-resistant tuberculosis (RR-TB) who are resistant to rifampicin ― an essential drug in the treatment of tuberculosis ― have been reported.

- The medical cost of treatment for drug-resistant tuberculosis is more than 50 times that of general tuberculosis treatment.

- The recently approved TB drugs, Bedaquiline (Sirturo®) and delamanid (Deltyba™), have been reported to be clinically resistant, and the safety of cardiac toxicity has not yet been secured.

- In view of the low cure rate and high mortality rate of patients with resistant tuberculosis infection, it is urgent to develop new drug-resistant tuberculosis drugs with safety that can effectively cope with them.

Status

- Lead TTCA compound has a superior in vivo efficacy in comparison with the control drug (INH) in the experimental animal model of chronic tuberculosis infection.

- In dose proportional animal experiments, in vivo efficacy close to sterilization was confirmed.

- In vitro as well as in vivo safety is secured.

- Excellent activity against MDR-TB was confirmed in vitro.

- Activity against latent M. tuberculosis was confirmed in vitro.

- Excellent activity was observed in M. tuberculosis inside macrophages.

Intellectual Property

We have obtained patents for materials and uses about 360 TTCA derivatives, and patent registration is currently in progress in ten countries (PCT / EP2015 / 063982).

Competitive Advantages

- Lead TTCA compound is active against both M. tuberculosis in broth and M. tuberculosis inside macrophages. Especially, the lead compound shows 4 - 100 times more potent biological activity against M. tuberculosis inside macrophages than M. tuberculosis in broth.

- Many TTCA compounds show excellent anti-tuberculosis activity at nanomolar (nM) level, and the in vivo drug characteristics that is appropriate to be orally administered once a day are secured through optimization.

Contact & Company Overview

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