BPS 2012
Peptide Drug Conjugates Designed to Cross the Blood-Brain Barrier
Jean Lachowicz
Chief Scientific Officer, Angiochem
ABSTRACT
The utility of numerous treatments for CNS disorders remains unrealized due to inability to cross the blood-brain barrier (BBB). With tight junctions and efflux proteins, the BBB restricts entry of many pharmaceuticals into the brain while allowing essential molecules, such as glucose, insulin, and growth hormones to penetrate. Overcoming the obstacles posed by the BBB is a critical goal for development of CNS therapeutics, particularly those involving peptides and proteins.
A new family of peptides, termed Angiopeps, derived from proteins that are efficiently transported across the BBB by the low-density lipoprotein receptor related protein (LRP1) has been designed. Binding LRP1, these peptides cross the BBB via receptor-mediated transcytosis. This technology is applicable to both small molecules and biologics and provides a non-invasive and flexible platform for creating new brain-penetrating drugs. A portfolio of new chemical entities including small molecules, peptides and proteins has been built using chemical conjugation or recombinant fusion with Angiopeps. The most advanced is GRN1005 (formerly ANG1005), formed by chemical conjugation of Angiopep-2 to three molecules of paclitaxel. GRN1005 demonstrated safety and efficacy in two phase 1/2 clinical trials for the treatment of primary and secondary brain tumors and is in Phase 2 for brain metastases (licensed to Geron Corporation).
We have created fusion proteins of Angiopep-2 with the anti-obesity hormone leptin and chemical conjugates of the peptides exendin-4 and neurotensin. These peptide drug conjugates have been demonstrated to efficiently cross the BBB in vivo in mice while retaining binding affinity to target proteins. In addition, brain-penetrant monoclonal antibodies and enzymes have been created. Results generated with these novel peptide drug conjugates further validate the utility of Angiopeps in development of new CNS therapeutics.
BIO
Information for BPS Presenters
The Boulder Peptide Foundation was established to further the science and knowledge of peptide technology to develop novel therapeutics, biomaterials, medical diagnostics and other beneficial uses for mankind. As part of this goal we run several programs to support career advancement, seminars and educational events. Join us on our mission to expand the applications of peptide science.
Information for BPS Presenters
The purpose of the Boulder Peptide Symposium is to encourage sharing of information related to peptide therapeutic development with an emphasis on the technical, scientific and regulatory aspects of the pharmaceutical development. Presentations that demonstrate original thinking or share experiences from case studies in product development shall receive priority over others.
The Boulder Peptide Symposium offers multiple opportunities for participants to present.
Oral Presentations in Scientific Sessions
The session topics for Scientific Program are Peptides in the Clinic, Drug Delivery, Chemistry of Complex Peptides, Spotlight on Discovery, and Peptide Showcase. Abstracts may be submitted via the Apply to Present page on the website. Submissions will be reviewed by the Scientific Advisory Board on a monthly basis and the speaker will be notified of a decision.
Presentation length: Format is 25-30 minutes slide presentation with 5-10 minutes for Q&A, with the exception of Peptide Showcase talks which are 10 minute slide presentations with 5 minutes for Q&A. Please confirm with your session chair to confirm the exact presentation length.
Invited Speakers: Speakers are requested to supply their presentation details 30 days after receiving an invitation to present.
Program Book Deadline: Final abstract and title must be provided no later than September 1st. No changes to the program are possible after this date.
Presentation Format: Oral presenters please provide your presentation slides to the A/V table on the day of your presentation.
Lodging: All speakers are requested to reserve their own room. Discount rates at the conference hotel are available until August 16th.
Registration: All speakers, excluding sponsored presentation speakers, receive a complimentary registration upon approval of the abstract.
Peptide Showcase Description
The Peptide Showcase is an opportunity for an individual or company to “showcase” new ideas, technology and pipeline assets. Priority shall be given to presentations from biotech and startup companies. Service providers and vendors are not eligible. Speakers in the session receive a complimentary event registration.
Posters
Posters can be presented on any topic relevant to peptides including original research, innovative products and technologies.
Eligibility- Any attendee (from academia, industry, biotech or vendor/sponsor) can present a poster. The presentation must contain original scientific thinking. To submit a poster go to the Submit a Poster link from the meeting menu. All submissions are reviewed on a rolling basis and will be notified of approval. September 1st is the last day to submit a poster abstract. Approved posters are published on the BPF website.
A 30 ” x 40″ board shall be provided with thumb tacks. Board will be on an easel and can be rotated for either landscape or portrait formats. Once you apply for a poster, you will get email confirmation that your poster was accepted. The poster session and number assignments will be emailed one week before the Symposium.
Poster boards shall be available for display from 8am to 8pm the day of your assigned poster session. See the program agenda for the poster session schedule.
Public Release
Every presentation at the Boulder Peptide Symposium is automatically recorded. Speakers are required to give consent for sharing of the presentation video with the peptide community.