09/03/2020 Micar21

Bulgarian Innovative company Micar 21 with a break-throw in a fight with COVID-19

Discovery of the first class of dual CCR5/7 antagonists for COVID-19

CCR5/7 project Micar 21

Despite that CCR5/7 are a key targets for HIV, Coronavirus, Cancer metastasis and many other diseases only few antagonists have been developed up to date for CCR5 and non for CCR7. However, one of CCR5 antagonists is under clinical trial in US now (phase 2).

Micar 21 aimed to identify the fist class of dual CCR5/CCR7 small molecule antagonists. The company used intensive MD simulations (several 1 µs runs) to obtain the CCR5 and 7 structures

The biological response of most promising hit to the ERK path and GTPyS binding is currently under evaluation in a lab located in Belgium.

Further steps

- Lead 1 has a good ADMET profile, is not expensive and eventually can be directly used as a topical solution

- FEP+ guided Lead 1 optimization for both activity and selectivity will be further performed

- Preclinical studies of optimized molecules should be performed

- Preclinical studies and hopefully clinical studies are beyond the Micar21 capabilities at the moment. Thus, we are open and looking for collaboration, licensing and/or M&A

- A brief description of the scientific approaches which Micar21 employ can be found in the next slides. We are in a process of hit identification and lead optimization of several molecules, such as for example GlyT2 inhibitors, and look for a collaboration in these directions too.

Micar 21 scientific data, backed by the results:

- CCR5 data from ThermoFisher Scientific

- CCR5 data from Eurofins

About the company

Micar Innovation (http://micar21.com/) is a drug discovery factory. The company has found a niche where it is able to create a large societal impact by improving the quality of life through new blockbuster drug molecules for a large class of diseases. Micar Innovation focuses on non-clinical Proof-of-Concepts (POCs) in preclinical R&D and Hit-to-Lead (H2L) achievements in areas such as neuroscience, oncology, cardio-vascularity, dermatology, rare diseases. Micar21 is our drug discovery platform for small molecule drug candidates.

All improvements to the in silico process made by the team are validated with over 30 scientific publications in high-impact scientific magazines,. Some of the are:

- Micar21, is one of the world’s 130 companies in Deep Knowledge Analytics report: AI for Drug Discovery Landscape 2018 Q1,2,3,4 & 2019 Q1 Source: https://www.dka.global/

- Micar21, is one of the world’s 198 companies in Roots Analysis Study report: “In Silico/Computer-Aided Drug Discovery Services Market 2020-2030” Source: https://www.rootsanalysis.com/reports/view_document/in-silico-drug-discovery/298.html

- Micar21, is one of the world’s 250 companies in Roots Analysis Study report: “Computer-Aided Drug Discovery Services Market 2018-2030” Source: https://www.rootsanalysis.com/reports/view_document/computer-aided-drug-discovery-services-market-2018-2030/207.html

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