BIT Pharma
Overcoming the Blood-Brain Barrier

An elite team of surgeons is preparing to operate on a patient who has been wheeled in with the condition of cerebral aneurysm rupture, leading to subarachnoid haemorrhage (SAH). Clipping surgery is going to be used to prevent further bleeding of an aneurysm, which is the cause of about 85 percent of the aneurysmal subarachnoid haemorrhage cases and of about 3-5 percent of all types of strokes. But the surgeons from their experiences are keeping their fingers crossed about the chances of complete recovery after surgery. Most often, four to ten days after the clipping surgery, unfortunately, a new complication develops. Blood vessels close to the clipped aneurysm start to constrict and narrow down, thereby leading to cerebral vasospasm (CV) causing insufficient supply of oxygen to the brain. CV is one of the most severe complications after aneurysmal SAH that leads to death or permanent neurologic deficits in over 40 percent of SAH patients.

Over the decades, the use of voltage-gated calcium channel antagonists has proven to be beneficial to prevent cerebral vasospasm. The usage of this class of drugs counteracts the narrowing of blood vessels and protects the brain against periods of ischemia. However, when administered orally or intravenously, the high doses of these drugs that is necessary to exert maximum pharmacological effect result in serious side effects. Is there a way to administer medications directly to the brain?

This long-standing predicament had the team at the Graz-based BIT Pharma adopt a revolutionary approach to overcome the blood-brain barrier in the delivery of voltage-gated calcium channel antagonists, which led to the pathbreaking innovation NicaPlant^®.

NicaPlant^®, a calcium channel antagonist loaded system, is implanted into the basal cisterns in close contact to the proximal cerebrovascular system at the time of aneurysm clipping. NicaPlant^® allows the slow tailored release in situ of the calcium blocker nicardipine at a constant concentration to the cerebral blood vessel wall over a period of about 14 days at the site of action, which prevents CV. With NicaPlant^®, there’s no possibility of systemic side effects like severe drop of blood pressure.
“We have built NicaPlant^® in a way that assists surgeons in implanting it at a very precise location where it will stay and create a local concentration of the drug that will help to expand the vessel and prevent the effect of constrictions,” says Dr. Jörg Breitenbach, Managing Director of BIT Pharma. NicaPlant^® is a bio-degradable and safe product that poses no risk of side effects from that biodegradation or causes inflammation.

BIT Pharma takes pride in its drug delivery system called AIMEX^® that can successfully carry very different molecules to the brain, without hindering the function of any vessel. “The same system can deliver both small molecules and biologics to the brain, which can prove beneficial for some rare diseases,” adds Dr. Breitenbach.

While BIT Pharma awaits the further clinical trials completion, neurosurgeons and clinicians that have already been using NicaPlant^® are excited about the potential benefits for all patients with an aneurysm. “The successful prevention of vasospasm and delayed brain stroke would be an important milestone in the treatment of future aneurysm patients,” says Prof. Vajkoczy, Director of the Neurosurgical Department at the Charité, Berlin.

What sets NicaPlant^® apart is the simple and easy-to-use features, which allow for neurosurgeons to adapt to a whole new technology in no time. Besides, BIT Pharma has received appreciation from the medical community as well, after EMA accorded them with the ‘orphan medicinal product designation’ in December last year. What’s more, NicaPlant^® being cost-effective, will be a win-win for both patients and the healthcare system alike.

BIT Pharma’s next endeavor is to utilize the unique features of NicaPlant^® for the development of other specialized medicinal products in different CNS-surgically treated pathologies. On a concluding note, Dr. Breitenbach says, “For now, our focus will be on the orphan diseases, as we believe it gives us the right scope of development work that a startup company like BIT Pharma can deliver.”