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HAPILA starts optimized pilot scale production of BTZ-043 anti TB agent
Gera, Germany: – High-potency active ingredient specialist HAPILA GmbH (HAPILA) has announced start of optimized pilot scale synthesis of its promising small molecule anti-tuberculosis active ingredient BTZ-043.
Following successful trails in laboratory scale, HAPILA has optimized the chemical synthesis for BTZ-043 to ensure even higher purity of intermediate products for meeting the demanding requirements for API-quality, paving the way for next clinical phases.
Based on promising results obtained from laboratory gram-scale synthesis development, the optimized synthesis process has also been successfully scaled up to kg scale. HAPILA has now commenced technical transfer of the optimized synthesis process to pilot scale as basis for process validation of BTZ-043 following GMP regulations.
A significant feature of the revised synthesis process is the splitting of a one-pot intermediate step into a two-step synthesis by isolation and analytical examination of a previously not isolated intermediate to reduce significantly the formation of impurities. Furthermore this change allows to improve quality control strategy. This is combined with optimized purification processes through crystallization of both the starting and the final intermediate to ensure a very high quality intermediate as the basis for final synthesis of BTZ-043 as small molecule API.
Combating highly resistant TB
BTZ-043 was first discovered at the Leibniz Institute for Natural Product Research and Infection Biology Hans Knöll Institute (Leibniz-HKI) in Jena, with whom HAPILA has been working in partnership throughout the program. Initial HKI studies suggested that the agent would be effective against highly resistant strains of tuberculosis, which is the most common cause of death worldwide caused by bacterial infections.
HAPILA undertook synthesis development for the tested API as well as its cGMP manufacturing, according to the Guideline of Good Manufacturing Practice, Part II – API (Manufacturing, Verification and Release).
Clinical studies are conducted under the sponsorship of the Ludwig-Maximilians-Universität (LMU) Munich, represented by Prof. Michael Hoelscher.
Studies and initial development have been supported by the InfectControl 2020 consortium and the German Center for Infection Research (DZIF), along with the Thüringer Aufbaubank.
“We have leveraged our years of experience in development of API-synthesis in getting to this point,” commented HAPILA CEO, Dr. Uwe Müller.
“Success in bringing this innovative small molecule to the point of entering cGMP manufacture underlines HAPILA’s credentials as a reliable development partner from small gram scale synthesis up to multi-kg API synthesis for market supply that is also able to support customers in terms of synthesis development, procedural challenges, several ways of purification and registration of new APIs with the relevant authorities, including EMA, and FDA,” Dr. Müller added.
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
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