MorphoSys’ First Lanthipeptide Completes Phase I Successfully

Lanthio Pharma MorphoSys Lanthipeptide

UPDATE (19/05/2017): MorphoSys has announced the completion of the Phase I study with MOR107, which has proved safe and showed dose-dependent pharmacokinetics. The drug, an agonist of the angiotensin II receptor type 2 (AT2-R), comes from the Dutch Lanthio Pharma and is the first lanthipeptide in MorphoSys’ pipeline.

Originally published 21/02/2017

Lanthio Pharma has initiated a Phase I clinical trial with its lanthipeptide candidate MOR107, which is being developed as a therapy for diabetic nephropathy.

Lanthio Pharma, a Dutch subsidiary of the big German antibody biotech MorphoSys, has initiated its first Phase I trial, making MOR107 MorphoSys’ first lanthipeptide in its clinical pipeline. The study will be run in the UK to test safety and tolerability in 80 to 110 healthy male volunteers, and results are expected in the second half of this year.

Although MorphoSys specializes in antibodies, the German biotech decided to acquire Lanthio Pharma back in 2015 to get hold of its lanthipeptide platform. The technology overcomes the limitations that most therapeutic peptides present in order to find alternatives for targets in which small molecules or antibodies cannot be used.

lanthipeptides Lanthio Pharma Mosphosys
Examples of lanthipeptide structures

Peptides are usually less specific than antibodies and have a very short half-life in the body. Lanthio’s strategy to circumvent this is the introduction of lanthionines, amino acids linked with a sulfur bond that lock the peptide into the optimal target-binding conformation and protect it from degradation via peptidase enzymes. Lanthipeptides are not chemically synthesized, but rather produced in Lactococcus bacteria through naturally occurring lantibiotic enzymes.

Lanthio Pharma’s main focus is G-protein coupled receptors (GPCRs), which are the target of up to 30% of approved drugs and are involved in diseases ranging from cancer to Alzheimer’s. Companies like Confo Therapeutics and Heptares Therapeutics are also going after GPCRs, but none is developing peptide therapeutics so far.

MOR107, Lanthio’s lead candidate, will be initially developed to treat diabetic nephropathy, but the company sees possibilities for the candidate in idiopathic pulmonary fibrosis (IPF) and kidney fibrosis. Its preclinical pipeline also includes indications like type 2 diabetes, heart failure and multiple sclerosis. With such a potential in big indications, Lanthio’s acquisition might end up paying off well for MorphoSys.

Images from Pakpoom Nunjui /Shutterstock; W. Tang et al., Chem. Sci., 2015, 6, 6270-6279




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