Portrait Lars Baerfacker

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.

Discovering the right substances for unknown binding pockets sometimes feels like searching for walls in a dark basement.

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.

As a scientist, you need a lot of creativity, patience and resilience. Even after 10 years of intense research, a project can be cancelled because it doesn’t work in a disease setting.

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.

Lars Baerfacker

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

Selected Publications

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.
Read on PubMed


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.
Read on PubMed


Tandem Reaction Sequences under Hydroformylation Conditions: New Synthetic Applications of Transition Metal Catalysis.
Chem. Rev., 1999, 99 (11), pp 3329–3366
EilbrachtP, BärfackerL, BussC, HollmannC, Kitsos-RzychonBE, KranemannCL, RischeT, RoggenbuckR, SchmidtA.
Read on PubMed

Selected Patents

Substituted 4-aryl-1,4-dihydro-1,6-naphthyridinamides and use thereof
WO2008104306, 2008
Lars Bärfacker, Peter Kolkhof, Karl-Heinz Schlemmer, Rolf Grosser, Adam Nitsche, Martina Klein, Klaus Münter, Barbara Albrecht-Küpper, Elke Hartmann
Read on Google Patents


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
WO2006114213, 2006
Ingo Flamme, Jens-Kerim Ergüden, Felix Oehme, Kai Thede, Gunter Karig, Alexander Kuhl, Hanno Wild, Joachim Schuhmacher, Peter Kolkhof, Lars Bärfacker, Joachim Hütter
Read on Google Patents


Imidazopyridazines as Akt kinase inhibitors
WO2012136776, 2012.
Lars Bärfacker, William Scott, Andrea Hägebarth, Stuart Ince, Hartmut Rehwinkel, Oliver Politz, Roland Neuhaus, Hans Briem, Ulf Bömer.
Read on Google Patents

Awards

2008: Global Drug Discovery Award
2014: Otto Bayer Medal