Discoveries Within the Microcosmos
How are drugs created? Dr. Lars Baerfacker is a medicinal chemist on the quest to find new substances to treat diseases.
If I had lived in medieval times, I might have become an explorer. But there are no more countries to discover on this earth. To uncover new locations today, I’d need to travel deep into the ocean or to outer space. But I don´t like extreme conditions, so I became a chemist. I explore the tiniest of all worlds: the microcosmos.
Ping-Pong in the Lab
Every morning I come into my office, right beside my colleague´s lab, and start looking for new substances. I’m inspired to improve by recent scientific proceedings, as nowadays everyone can follow respective blogs on the internet. Well, it’s obvious why everyone looks for substances that treat diseases where there is no treatment available. I have the same goal for substances to treat diseases that remain a high burden for our society: greater effectiveness and fewer side effects can have a dramatic impact on patients’ quality of life. This goal drives my daily motivation. I design new substances and send them to my colleagues next door to receive data in return. These data will be translated into novel compounds with, hopefully, improved profiles. It´s a constant back and forth like a ping-pong game. I’ve been playing ping-pong, or table tennis, since my early childhood - even at tournament level.
The most important ‘ping-pong’ I do is with my colleagues in pharmacology. When I receive the data illustrating a substance’s therapeutic potential, my goal is to minimize side effects until the therapeutic benefits clearly outweigh them. To get the molecule we hope for, years can sometimes pass by.
Construction Manager for Chemical Structures
In medicinal chemistry, I´m the architect, stress analyst and the construction manager of molecules. I have an idea of where and how a substance should work and what characteristics this would require. Each substance needs to be tailor-made to unlock the desired pharmacological effect, but usually even more effort is required. I have also to design-in additional properties, like solubility and polarity, to max out a compound’s potential while managing all safety requirements.
None of our approaches makes it straight to approval of a drug on the market. We often have to handle setbacks. To create the first 100 substances, we might have had to consider thousands more. If we’re lucky, one of them makes it to the clinical phase, where it´s tested in patients. And this is where we are now with one of our drug candidates - a non-steroidal mineralocorticoid receptor antagonist. An international team is currently examining this antagonist as a potential treatment for diabetic kidney diseases.
When I´m not designing molecules, or exploring the microcosmos, I like to discover the world. On trips to Asia or France, I get to know new cultures and cuisines. For my physical well-being, I now try to play tennis. Since last year, I’ve been working towards my sailing license. In the upcoming years, I hope to discover the coastal waters of the world.
CV Dr. Lars Baerfacker
|1970||Born in Oberhausen, Germany|
|1990-1996||Studied chemistry at Dortmund University; Graduated with a diploma degree in chemistry|
|1999||Received the title of Doctor of Natural Sciences (Dr. rer. nat.)|
|1999-2000||Scholar of the DFG – Deutsche Forschungsgemeinschaft (The German Research Foundation) at the University of Minnesota, USA|
|2000||Joined Bayer AG as a Medicinal Chemist|
|2011-2014||Moved to Bayer’s research labs in Berlin to focus on oncology projects|
Discovery of BAY 94-8862: A Nonsteroidal Antagonist of the Mineralocorticoid Receptor for the Treatment of Cardiorenal Diseases.
ChemMedChem. 2012 Aug;7(8):1385-403.
Bärfacker L, Kuhl A, Hillisch A, Grosser R, Figueroa-Pérez S, Heckroth H, Nitsche A, Ergüden JK, Gielen-Haertwig H, Schlemmer KH, Mittendorf J, Paulsen H, Platzek J, Kolkhof P.
BAY 1125976, a selective allosteric AKT1/2 inhibitor exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models.
Int J Cancer. 2017 Jan 15;140(2):449-459
Politz O, Siegel F, Bärfacker L, Bömer U, Hägebarth A, Scott WJ, Michels M, Ince S, Neuhaus R, Meyer K, Fernández-Montalván AE, Liu N, von Nussbaum F, Mumberg D, Ziegelbauer K.
Tandem Reaction Sequences under Hydroformylation Conditions: New Synthetic Applications of Transition Metal Catalysis.
Chem. Rev., 1999, 99 (11), pp 3329–3366
Eilbracht P, Bärfacker L, Buss C, Hollmann C, Kitsos-Rzychon BE, Kranemann CL, Rische T, Roggenbuck R, Schmidt A.
Substituted 4-aryl-1,4-dihydro-1,6-naphthyridinamides and use thereof
Lars Bärfacker, Peter Kolkhof, Karl-Heinz Schlemmer, Rolf Grosser, Adam Nitsche, Martina Klein, Klaus Münter, Barbara Albrecht-Küpper, Elke Hartmann
4-(pyridin-3-yl)-2(pyridin-2yl)-1,2-dihydro-3H-pyrazol-3-one derivatives as specific HIF-pyrolyl-4-hydroxylase inhibitors for treating cardiovascular and haematological diseases
Ingo Flamme, Jens-Kerim Ergüden, Felix Oehme, Kai Thede, Gunter Karig, Alexander Kuhl, Hanno Wild, Joachim Schuhmacher, Peter Kolkhof, Lars Bärfacker, Joachim Hütter
Imidazopyridazines as Akt kinase inhibitors
Lars Bärfacker, William Scott, Andrea Hägebarth, Stuart Ince, Hartmut Rehwinkel, Oliver Politz, Roland Neuhaus, Hans Briem, Ulf Bömer.
2008: Global Drug Discovery Award
2014: Otto Bayer Medal