Synonyms: GSK3036656 | GSK656
Compound class:
Synthetic organic
Comment: Ganfeborole (GSK3036656) is a first-in-class boron-containing antitubercular agent. It is the lead from a series of 3-aminomethylbenzoxaboroles that are potent inhibitors of Mycobacterium tuberculosis leucyl-tRNA synthetase (LeuRS) [2]. We show the (S) enantiomer, which is the most active form.
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No information available. |
Summary of Clinical Use |
Ganfeborole is being developed by GlaxoSmithKline as a treatment for tuberculosis. First-in-human safety and pharmacokinetics were reported in 2019 [3] and a Phase 2 early bacterial activities study has been completed (NCT03557281). A Phase 2 trial of ganfeborole in combination with bedaquiline or delamanid is recruiting (NCT05382312, last update January 2023). |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT05382312 | Early Bactericidal Activity, Safety & Tolerability of Oral GSK3036656 in Combination With Delamanid or Bedaquiline, Delamanid in Combination With Bedaquiline, or Standard of Care in Male and Female Participants Aged 18 to 65 Years With Pulmonary Tuberculosis | Phase 2 Interventional | GlaxoSmithKline | ||
NCT03557281 | An Early Bactericidal Activity, Safety and Tolerability of GSK3036656 in Subjects With Drug-sensitive Pulmonary Tuberculosis | Phase 2 Interventional | GlaxoSmithKline | ||
NCT03075410 | First Time in Human (FTIH) Safety and Pharmacokinetics (PK) Study of GSK3036656 in Healthy Subjects | Phase 1 Interventional | GlaxoSmithKline | Drug is well tolerated with no serious adverse events reported. | 3 |