PBF-509 represents a novel, non-xanthine potent and selective competitive antagonist of the human A2A receptor discovered and patented by Palobiofarma S.L. The product has shown excellent efficacy in relevant animal models of PD at very safe doses. The IND-enabling studies with PBF-509 have been completed in February 2012. The Phase I clinical trials with the compound are planned to start in September 2012.

Biotech Showcase™ has provided to Palobiofarma the opportunity to present its research programs and its product's pipeline to an audience of biopharmaceutical investors and business development executives from around the world contributing to the search of new partners interested in licensing or co-development Palobiofarma’s research programs.

The approved grants are awarded by founding of the Spanish Minister for Science and Innovation (MICINN) and it covers funds for two projects: STOP-ELA based on the search for new chemical entities as novel therapeutic alternatives for the treatment of amyotrophic lateral sclerosis (ALS) and POLYFARMA: To address the development of novel therapies to treat Parkinson's disease.

The grant proposal is based in the increasing evidence about the relation of adenosine and it´s receptors in malignization and metastasis of diverse type of cells. High concentrations of adenosine have been reported in cancer tissues, it also appears to be implicated in the growth of tumors. The role of adenosine in producing pro- and anticancer effects via each of its receptor subtypes is a rapidly growing and intense area of research in drug discovery. Palobiofarma as a Reference Company in the medicinal Chemistry dealing with modulators of adenosine receptors is also interested in develops candidates that may be nominated for treatment of Cancer. The granted investigation will be developed in collaboration with two companies of huge expertise in the field: Oryzon Genomics S.L and Aromics S.L.

The PBF-680 is a novel adenosine A1 receptor antagonist proposed to be developed as “First in Class” for the oral treatment of Asthma. The discovery program has been started in 2006 with a clear goal in the development of a nonxanthine, potent and selective, non BBB-penetrable, orally available adenosine A1 antagonist as first in class treatment for allergic asthma.

The approved grant is awarded by Genoma España founding and it covers funds for the preclinical development of Palobiofarmas´s candidate (PBF-509) for the treatment of neurodegenerative diseases focusing in Parkinson’s disease. PBF-509 is a very potent adenosine A2a receptor antagonist discovered and developed by Palobiofarma. The following features make PBF-509 a “best in class” candidate in the neurodegenerative diseases treatment:

• It belongs to a different chemical class in comparison to the competitor compounds, bearing no structural alerts.
• It shows excellent PK properties in rats, with good exposure and oral bioavailability and long half-life (longer than its competitors). The compound shows also an excellent BBB penetration (B/P ratio >1)
• PBF-509 administered orally shows a dose-dependent reduction in the catalepsy induced by haloperidol in rats. Even at the lowest dose tested, PBF-509 reverts almost completely the cataleptic status. The effect is also time-dependent.