ANG1005

ANG1005, the Company’s lead product for the treatment of primary (glioblastoma) and metastatic brain tumors, consists of three molecules of paclitaxel conjugated to Angiopep.   Once in the brain compartment, ANG1005 again uses LRP, which is upregulated on primary and metastatic brain cancer cells, to enter tumor cells where the molecule is cleaved releasing paclitaxel to exert its antimitotic effects (preventing cell division and therefore cell proliferation).

ANG1005 is a Cremophor-free formulation that is better tolerated than Taxol® and suitable for commercialization.  It is a patented NCE with intellectual property protection on Composition of Matter (COM).

ANG1005 is the first new chemical entity to use the Angiopep technology and the first drug candidate to be tested in humans to use a physiological approach to cross the blood-brain barrier.  Promising preclinical studies and preliminary clinical safety and tolerability data provide new hope to those dealing with brain cancers and, in the future, possibly other brain diseases.

Solid preclinical data// Preclinical data demonstrated that ANG1005 delivers up to 100 times more paclitaxel to the brain, as compared to paclitaxel alone, and it achieves 10 times better brain delivery than temozolomide, the current standard of care for glioblastoma. Furthermore, after IV injection of 30 mg/kg in mice, a brain concentration of 2.1 µM of paclitaxel is obtained, about 100 times more than the level necessary for anti-cancer activity. AngioChem also conducted a brain autoradiography study in mice with metastatic brain tumours showing that ANG1005 is homogenously distributed in the brain, with some higher distribution in the tumour.

Clinical development //In October 2007, we launched two parallel phase 1/2 studies involving approximately 35 patients per study: one study treating recurrent glioblastoma, and a second study treating brain metastasis.  The primary endpoint of both studies is safety, tolerability and determination of the maximum tolerated dose (MTD).  Secondary endpoints include a preliminary assessment of efficacy, as well as the measurement of ANG1005 levels in surgically removed tumors from glioblastoma patients. Both studies are conducted at multiple sites in the United States where patient enrolment is successful and on target with objectives.  Data obtained to date confirm in humans the good tolerability observed in preclinical studies.

We expect to obtain top-line results from the Phase I/II studies during Q1:09 and will continue to fund clinical studies for ANG1005 for brain cancer in order to get the necessary data to start licensing activities.