APG101 - CD95L-Blocker
APG101 is a human fusion protein consisting of two parts: the extracellular domain of the CD95 receptor and the Fc-domain of an IgG antibody. A Phase II clinical proof-of-concept studies with APG101 was started in December 2009 in Glioblastoma multiforme (GBM), the most common and aggressive type of primary brain tumour. Results from the trials are expected by 2011. Preparations for a Phase II trial with APG101 are currently ongoing in the second indication: acute Graft-versus-Host Disease (aGvHD), the rejection of recipient tissue by transplanted bone marrow. In May 2009 the results of a successful Phase I study demonstrated the excellent tolerability of APG101.
| Compound | Indication | Discovery | Pre-clinical | Phase I | Phase II | Phase III |
|---|---|---|---|---|---|---|
| APG101 | Glioblastoma | completed | completed | completed | 25% completed | - |
| APG101 | acute Graft-versus-Host Disease | completed | completed | completed | - | - |
APG101 blocks the CD95–ligand (CD95L) from binding to the CD95-receptor. In healthy cells, the binding of CD95L to its receptor initiates apoptosis (programmed cell death). By blocking this interaction, APG101 inhibits, among other processes, the tissue damage induced by the transplanted bone marrow and therefore opens a route for the treatment of immunological diseases like aGvHD.
Molecular structure of APG101
Mode of action of APG101
In tumour cells, however, such as gliobastoma cells, which are highly resistant to apoptosis inducing signals, the binding of CD95L to its cognate receptor enhances the invasive growth of these cells. So in this case, the inhibition of this interaction by APG101 reduces tumour cell migration. Comprehensive, preclinical studies have demonstrated the therapeutic potential of APG101 in GBM and aGvHD.
Apogenix GmbH plans to out-license worldwide marketing rights to APG101 for the treatment of GBM and aGvHD, as well as further potential indications, to commercial partners.
Contact our Business Development Manager for more information.
Dr. Jürgen Gamer - VP Business Development - Apogenix GmbH
Phonework: +49 (0) 6221 58608 0
E-mail: juergen.gamer@apogenix.com
