NCT03590600

A Single Ascending Dose Study of BTZ043

Completed Phase 1 Last updated 7 March 2019

What this trial tests

Phase 1 trial testing BTZ-043 in Tuberculosis in 30 participants. Completed in 5 March 2019.

Timeline

7 June 2018

Primary endpoint
14 August 2018

5 March 2019

Quick facts

Lead sponsor	Michael Hoelscher
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	randomized
Design	sequential
Masking	quadruple
Primary purpose	treatment
Enrollment	30
Start date	7 June 2018
Primary completion	14 August 2018
Estimated completion	5 March 2019
Sites	1 location across Germany

Drugs / interventions tested

• BTZ-043 — full drug profile →
• Placebo

Conditions studied

• Tuberculosis — all drugs for Tuberculosis →
• Tuberculosis, Pulmonary — all drugs for Tuberculosis, Pulmonary →
• Bacterial Infections — all drugs for Bacterial Infections →
• Lung Diseases — all drugs for Lung Diseases →

Sponsor

Michael Hoelscher — full company profile →

Who can join

Adults 18 to 55, any sex, with Tuberculosis or Tuberculosis, Pulmonary. Patients with the condition only — healthy volunteers not accepted.

Sponsor's own description

This study is a randomized, double-blind, placebo-controlled, single ascending dose study to evaluate safety, tolerability, and pharmacokinetics of single doses of BTZ043 in healthy adult volunteers. The study is conducted at a study centre in Germany. Up to 50 male and female participants will be included in this study in up to 5 cohorts; each cohort will consist of 10 subjects: in each cohort 8 subjects will be assigned to BTZ-043 and 2 to placebo. The doses tested will be: 125mg, 250mg, 500mg, 1000mg and 2000mg. Safety will be assessed via regular vital sign measurement, 12-lead ECG parameters, physical examination and safety laboratory assessments.

Subjects will be hospitalized from Day -1 until discharge in the morning of Day 3. After completion of all Day 3 assessments of a cohort, blinded safety data will be reviewed and the next dose increment will be decided by the Trial Steering Committee (TSC).

Publications & conference data

6 peer-reviewed publications reference this trial (live from Europe PMC):

1. Antibiotics in the clinical pipeline in October 2019.
   Butler MS, Paterson DL. · · 2020 · cited 174× · PMID 32152527 · DOI 10.1038/s41429-020-0291-8
2. New Drugs for the Treatment of Tuberculosis.
   Ignatius EH, Dooley KE. · · 2019 · cited 39× · PMID 31731986 · DOI 10.1016/j.ccm.2019.08.001
3. Implications of Fragment-Based Drug Discovery in Tuberculosis and HIV.
   Mallakuntla MK, Togre NS, Santos DB, Tiwari S. · · 2022 · cited 7× · PMID 36422545 · DOI 10.3390/ph15111415
4. Revolutionizing tuberculosis treatment: Breakthroughs, challenges, and hope on the horizon.
   Kufa M, Finger V, Kovar O, Soukup O, et al · · 2025 · cited 6× · PMID 40370552 · DOI 10.1016/j.apsb.2025.01.023
5. 2,5-Diazabicyclo[2.2.1]heptane in medicinal chemistry: a treasure trove of therapeutic opportunities.
   Ambast PK, Kapoor S, Das R, Chatterjee DR, et al · · 2026 · PMID 41641350 · DOI 10.1039/d5md00992h
6. First-in-human study of the benzothiazinone and DprE1 inhibitor BTZ-043, a novel drug candidate for the treatment of Tuberculosis.
   Lutchmun W, Heinrich N, Svensson EM, Kloss F, et al · · 2025 · PMID 40831749 · DOI 10.1093/jacamr/dlaf127