Bioasis Announces Publication of Independent Validation of the Company’s xB 3 ™
Platform Technology
Research Conducted by MedImmune Shows the xB 3 Platform
Efficiently Delivers Antibodies Across the BBB at Therapeutic Doses
xB 3 Demonstrated Sustained Systemic PK Properties of the
MedImmune Antibody Constructs and Demonstrated a Strong PK/PD Dose Dependent Relationship in a Neuropathic Pain Pre-Clinical
Model
The Research was Published in the Journal of Cerebral Blood Flow and
Metabolism 1
BIOASIS TECHNOLOGIES INC . (TSX.V:BTI; OTCQB:BIOAF), a biopharmaceutical company developing its xB3
TM proprietary platform technology for the delivery of therapeutics across the blood-brain barrier (BBB) and the treatment of
CNS disorders in areas of high unmet medical-need, including brain cancers and neurodegenerative diseases, today announced the
publication of independent research validating the ability of the company’s xB3 platform to efficiently deliver
antibodies across the blood-brain barrier to the central nervous system in therapeutically relevant doses.
Scientists at MedImmune, the global biologics research and development arm of AstraZeneca, evaluated Bioasis’ xB3
platform technology by making two xB3 antibody fusion proteins and measuring systemic pharmacokinetic (PK) and brain
exposure in mice; this was followed by a pharmacodynamic (PD) study in a mouse neuropathic pain model. This research shows that the
xB3 platform demonstrated a strong PK/PD dose dependent relationship in this pre-clinical neuropathic pain mouse model
without compromising peripheral pharmacokinetic properties. The research conducted by Thom, et al., “A peptide derived from melanotransferrin delivers a protein-based interleukin 1 receptor antagonist across the BBB
and ameliorates neuropathic pain in a pre-clinical model,” was published in the Journal of Cerebral Blood Flow and
Metabolism.
The study found that the xB3 fusion protein maintained the systemic pharmacokinetics of its payload and had
significantly improved and sustained brain exposure of the payload molecule. The PD study demonstrated dose dependent pre-clinical
effect in neuropathic pain model post single dose systemic administration.
The data presented in this publication provide evidence for the utility of xB3 peptides (previously known as MTfpep)
as a platform technology for delivery of recombinant and chemically conjugated drugs across the BBB to increase brain exposure. The
pharmacokinetic data demonstrate efficient delivery of antibodies across the BBB with peak exposure of over 4% injected dose per
gram of brain, compared to peak of 0.5% for payload alone.
The new data from MedImmune further highlights that xB3 peptides do not affect systemic pharmacokinetics of the
antibody payload compared to the payload alone. In the pharmacodynamic mouse model of neuropathic pain, the recombinant fusion
protein with interleukin-1 receptor antagonist (IL-1RA) demonstrated efficient delivery of therapeutic concentrations of IL-1RA to
the CNS and eliciting analgesia in the animal model after a single dose treatment. Systemic administration of IL-1RA itself does
not elicit analgesia.
“The results from this research independently validate the utility of our xB3 platform technology to increase
delivery of therapeutic compounds across the blood-brain barrier at levels that may help treat a variety of central nervous system
diseases. The Medimmune data are consistent with the previous antibody study where our technology successfully delivered Herceptin®
(trastuzumab) to the brain, engaged the target areas and reduced brain metastasis by 68%.” said Mei Mei Tian, Ph.D., vice
president, head of external research, Bioasis.
ABSTRACT
Delivery of biologic drugs across the blood-brain barrier is becoming a reality. However, the solutions often involve the
assembly of complex multi-specific antibody molecules. Here we utilize a simple 12 amino-acid peptide originating from the
melanotransferrin (MTf) protein that has shown improved brain delivery properties. 3D confocal fluorescence microscopic analysis
demonstrated brain parenchymal localization of a fluorescently labelled antibody (NIP228) when chemically conjugated to either the
MTf peptide or full-length MTf protein. Measurement of plasma kinetics demonstrated the MTf peptide fusions had very similar
kinetics to an unmodified NIP228 control antibody, whereas the fusion to MTf protein had significantly reduced plasma exposure most
likely due to a higher tissue distribution in the periphery. Brain exposure for the MTf peptide fusions was significantly increased
for the duration of the study, exceeding that of the fusions to full length MTf protein. Using a neuropathic pain model, we have
demonstrated that fusions to interleukin 1 receptor antagonist (IL-1RA) are able to induce significant and durable analgesia
following peripheral administration. These data demonstrate that recombinant and chemically conjugated MTf-based brain delivery
vectors can deliver therapeutic levels of drug to the central nervous system.
About Bioasis
Bioasis Technologies, Inc. is a biopharmaceutical company developing xB3, a proprietary platform technology for the
delivery of therapeutics across the blood-brain barrier (BBB) and the treatment of CNS disorders in areas of high unmet medical
need, including brain cancers and neurodegenerative diseases. The delivery of therapeutics across the BBB represents the final
frontier in treating neurological disorders. The in-house development programs at Bioasis are designed to develop symptomatic and
disease-modifying treatments for brain-related diseases and disorders. The company maintains headquarters in Richmond, Canada with
offices in Guilford, Conn., United States. Bioasis trades on the TSX Venture Exchange under the symbol “BTI” and on the OTCQB under
the symbol “BIOAF.” For more information about the company please visit www.bioasis.ca or www.bioasis.us.
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manufacturing; we may face unknown risks related to intellectual property matters; we face increased competition from
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1 Thom G, Tian MM, Hatcher JP, et al., A peptide derived from melanotransferrin delivers a protein-based interleukin
1 receptor antagonist across the BBB and ameliorates neuropathic pain in a preclinical model. Journal of Cerebral Blood Flow and
Metabolism.
Media & Investor Relations
Bioasis Technologies Inc.
Catherine London
Catherine@bioasis.us
+1 917-763-2709
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