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Related Concept Videos

Pulmonary Tuberculosis V01:28

Pulmonary Tuberculosis V

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Medical management of tuberculosis (TB) patients involves a comprehensive approach that includes diagnosis, treatment, and monitoring. The specific strategies can vary depending on the type of tuberculosis (latent or active), the patient's overall health status, and other considerations.
Latent tuberculosis infection occurs when TB bacteria are present in a person's body, but are not causing illness or symptoms. It is not contagious, and preventive treatment is crucial to avoid the...
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Updated: Oct 22, 2025

An In Vitro Caseum Binding Assay that Predicts Drug Penetration in Tuberculosis Lesions
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Salts and Polymorph Screens for Bedaquiline.

Mercy Okezue1, Susan Bogdanowich-Knipp2, Daniel Smith3

  • 1Biotechnology Innovation and Regulatory Science Center, ABE, Purdue University, 225 S. University Street, Indiana, 47906, West Lafayette, USA. mokezue@purdue.edu.

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|August 26, 2021
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Summary

Researchers explored new bedaquiline salts to improve tuberculosis treatment options post-patent expiry. Five new salts, including benzoate and maleate, were successfully synthesized and characterized, offering potential for enhanced pharmacokinetic properties.

Keywords:
BedaquilinePolymorph screenSalt screenX-ray diffraction and Tuberculosis

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Area of Science:

  • Pharmaceutical Chemistry
  • Drug Discovery
  • Materials Science

Background:

  • Bedaquiline fumarate is the current treatment for multi-drug resistant tuberculosis (MDR-TB).
  • Exploring new bedaquiline salts is crucial for ensuring open access and potentially improving drug properties after patent expiration.

Purpose of the Study:

  • To screen and characterize novel bedaquiline salts.
  • To identify new salt forms with potentially improved pharmacokinetic properties for tuberculosis treatment.

Main Methods:

  • Conventional screening and small-scale experiments.
  • Crystallographic analysis (X-ray diffraction - XRD).
  • Spectroscopic (proton NMR, IR) and thermal (TGA, DSC) analyses.
  • Polymorph screening of lead candidates.

Main Results:

  • Successfully synthesized and characterized five new bedaquiline salts: benzoate, maleate, hydrochloride, besylate, and mesylate.
  • Benzoate and maleate salts were identified as initial lead candidates.
  • Polymorph screening indicated no additional polymorphs at a 1g scale for the characterized salts.

Conclusions:

  • The study successfully generated and confirmed the existence of five novel bedaquiline salts.
  • These new salts offer potential alternatives for bedaquiline formulation, possibly with enhanced pharmacokinetic profiles.
  • The findings support the development of accessible and improved treatments for multi-drug resistant tuberculosis.