Maleate salts of bedaquiline

Salts and Polymorph Screens for Bedaquiline

Summary

Bedaquiline is used to treat multi-resistant tuberculosis in adults. The fumarate salt is commercially available and used in the product Sirturo. To provide open access to bedaquiline molecule once the patent on the chemical substance expires, new salts were screened. The current studies focus on the attempted isolation of the acetate, benzoate, benzenesulfonate, hydrobromide, succinate, hydrochloride, tartrate, lactate, maleate, malate, and mesylate salts of bedaquiline. Potential salts were screened using a unique combination of conventional screening, and small-scale experiments supplemented by crystallographic analysis and infrared microspectroscopy. The current studies focus on the attempted isolation of the acetate, benzoate, benzenesulfonate, hydrobromide, succinate, hydrochloride, tartrate, lactate, maleate, malate, and mesylate salts of bedaquiline. Potential salts were screened using a unique combination of conventional screening, and small-scale experiments supplemented by crystallographic analysis and infrared microspectroscopy.

We acknowledge the supports from Purdue University Biotechnology Innovation and Regulatory Science Program (BIRS), as well as the National Science Foundation, Directorate for Mathematical and Physical Sciences. Funding for this research was provided by: Bill and Melinda Gates Foundation (grant No. INV-017799 to SRB).

Study Objective

  1. 1.

    Carry out a standard screen to generate salts of bedaquiline.

  2. 2.

    Prepare additional quantities of crystalline materials and partially characterize them.

  3. 3.

    Conduct a polymorph screen on selected crystalline salts discovered.

Study Reprint

Okezue, M., Bogdanowich-Knipp, S., Smith, D. et al. Salts and Polymorph Screens for Bedaquiline. AAPS PharmSciTech 22, 228 (2021). 

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