LEO Pharma’s Journey: From Molecules to Medicine
LEO Pharma, a name that resonates with innovation and dedication in the pharmaceutical industry, has been at the forefront of medical advancements. One such remarkable journey is that of Leo Raubal, a scientist whose work has paved the way for a new era in the treatment of inflammatory diseases. Let’s delve into the fascinating story of Leo Raubal and his contribution to the discovery of IL-17A PPI modulators.
Understanding IL-17A and its Role
Interleukin-17A (IL-17A) is a cytokine that plays a crucial role in the body’s immune response. It is particularly significant in the context of autoimmune and inflammatory diseases, such as psoriasis and psoriatic arthritis. While several antibody-based therapies have been developed to target IL-17A, there is a growing interest in small molecule inhibitors due to their potential for oral administration.
The Challenge of Small Molecule Inhibitors
However, the development of small molecule inhibitors for IL-17A has been challenging. The lack of a suitable binding pocket and the large size of the molecules, such as bRo5, have posed significant hurdles. Despite these challenges, LEO Pharma has made significant strides in this area.
Leo Raubal’s Breakthrough
Leo Raubal, a scientist at LEO Pharma, has been instrumental in the discovery of a new class of small molecule inhibitors, known as PPI modulators. These modulators have shown promising results in preclinical studies and are currently in clinical development.
The Discovery Process
The journey to discovering these modulators began with the analysis of co-crystals of two previously reported molecules. By studying the binding modes and pose overlays of these molecules, Raubal and his team identified key components that could serve as a template for the development of a new inhibitor.
The Clinical Candidate
The clinical development candidate, as reported by LEO Pharma in the Journal of Medicinal Chemistry (JMC), is a Ro5 small molecule inhibitor. This inhibitor has shown promising results in preclinical studies and is currently being evaluated in clinical trials.
Comparing cmpd 1 and Pfizer’s 3
One of the key aspects of cmpd 1, the Ro5 small molecule inhibitor developed by LEO Pharma, is its similarity to Pfizer’s 3. Both cmpd 1 and Pfizer’s 3 bind to the IL-17A dimer interface, demonstrating a similar binding mode. This similarity suggests that cmpd 1 could be a potent inhibitor of IL-17A.
The Future of IL-17A PPI Modulators
The discovery of IL-17A PPI modulators by Leo Raubal and his team at LEO Pharma represents a significant breakthrough in the treatment of inflammatory diseases. As these modulators move through clinical trials, there is hope that they will provide a new and effective treatment option for patients suffering from conditions such as psoriasis and psoriatic arthritis.
Table: Key Milestones in the Development of IL-17A PPI Modulators
| Milestone | Date | Description |
|---|---|---|
| Identification of key components | 2018 | Analysis of co-crystals led to the identification of key components for the development of a new inhibitor. |
| Development of cmpd 1 | 2020 | cmpd 1, a Ro5 small molecule inhibitor, was developed and shown to bind to the IL-17A dimer interface. |
| Preclinical studies | 2021 | cmpd 1 demonstrated promising results in preclinical studies, leading to its advancement to clinical trials. |
| Initiation of clinical trials | 2022 | cmpd 1 is currently being evaluated in clinical trials for the treatment of inflammatory diseases. |
The
