HAPILA’s co-developed anti-TB agent BTZ-043 named ‘Drug of the Year’

Gera, Germany: – The small molecule anti-tuberculosis active ingredient BTZ-043 has been named ‘Drug of the Year’ by the Leibniz Wirkstofftage, the Leibniz Research Network Bioactive Compounds annual conference in Braunschweig, Germany.

Discovered at the Leibniz Institute for Natural Product Research and Infection Biology (Leibniz-HKI) in Jena, the active substance, also effective against resistant bacteria, has been under development since 2014 in collaboration with the Tropical Institute at LMU Klinikum Munich and Hapila GmbH in Gera. It is currently the only new antibiotic from Germany that is being tested in clinical trials.

New mechanism

The new antibiotic BTZ-043 has a completely new mechanism of action and is a member of the nitrobenzothiazinones (BTZs) family discovered and developed at Leibniz-HKI as a highly effective class of antibiotics against the tuberculosis pathogen Mycobacterium tuberculosis, including resistant strains.  BTZ-043 was the first member of this family of compounds to obtain worldwide patent protection for its activity against the tuberculosis pathogen.

Dr. Florian Kloss., former head of the Anti-Infectives Transfer Group at Leibniz-HKI, who played a key role in the development of the active ingredient, commented: “The active ingredient irreversibly binds to an enzyme that mycobacteria need to build the bacterial cell wall.”

Promising clinical trials

In addition to Dr. Kloss, the Drug of the Year award also honors Drs. Sina Gerbach and Freddy Bernal. Dr. Gerbach led the contract research on drug safety and in-vitro studies on potential drug-drug interactions, which are required for drug approval, while Dr. Bernal developed computer models to study the relationship between the structure of benzothiazinones, their physical properties, and their efficacy.

A Phase I clinical study conducted on healthy volunteers in Germany showed that BTZ-043 was well tolerated. The subsequent Phase IIa clinical trial was conducted on tuberculosis patients in Cape Town, South Africa. It confirmed BTZ-043 as safe and effective – an important step in the development of a new drug. Further Phase II clinical trials are currently being planned to investigate BTZ-043 in combination with various standard antituberculotics. This means that the replacement of conventional antibiotics, which are often susceptible to resistance, with BTZ-043, in a combination therapy, is now within reach – and might shorten the duration of treatment for tuberculosis.

For the preclinical and clinical studies, Leibniz-HKI has been cooperating closely with the Tropical Institute at LMU Klinikum Munich since 2014. They are commissioned and supervised by the director of the Tropical Institute, Professor Michael Hoelscher and his team.

Hapila has commenced GMP production of BTZ-043 at its GMP facilities in Gera (see Resources).

Multilateral funding

The drug’s development, which has so far cost several million euros, was made possible by joint funding from the public and private sectors. In particular, the two research networks InfectControl and the German Center for Infection Research (DZIF), funded by the German Federal Ministry of Education and Research (BMBF), have been involved in the drug’s development.

The clinical trials take place within the European-African consortium PanACEA II, funded by the European & Developing Countries Clinical Trials Partnership (EDCTP), and the research consortium “Academia and Industry United Innovation and Treatment for Tuberculosis” (UNITE4TB). The latter is supported at the European level by the Innovative Medicines Initiative (IMI), a public-private collaboration now known as the Innovative Health Initiative (IHI), and at the German level by the BMBF.

About HAPILA GmbH

HAPILA GmbH is a contract developer and manufacturer (CDMO) that provides high-value services to pharma, biotech and fine chemicals client companies in the development and cGMP manufacture of active pharmaceutical ingredients (APIs).

HAPILA is an independent company with particular experience in GMP-related development and GMP manufacturing, offering full regulated service for API (IMPD, ASMF) to very high scientific and quality assurance (QA) levels.

It supports the development and manufacture of drug products with patented processes and in-depth experience in the API value-creation chain from synthesis through purification to particle design.

The company’s mission is to supply exclusive products of highest quality, potency and safety in compliance with GMP and environmental protection guidelines. All HAPILA teamwork is focused on product quality and customer satisfaction.

All HAPILA chemical synthesis is carried out at in-house at its GMP certified laboratories at Gera, Thuringia, in east-central Germany.

When combined with purification and particle design, HAPILA’s chemical synthesis services cover the complete API value-creation chain, enabling it to be a highly efficient bridge-builder between API production and pharmaceutical end-use.

For more information, visit: https://www.hapila.de/en

Resources

Click on Leibniz Drug of the year 2023 is a tuberculosis antibiotic to learn more.
Click on HAPILA BTZ-043 starts Phase II for more information.
Click on HAPILA extends BTZ 043 production capacity for further information.