BPS 2022


Discovery and Optimization of Long-Acting, Unimolecular Peptide Triple Agonists of the GLP-1, GIP, and Glucagon Receptors

Patrick Knerr

Senior Director & Site Head, Novo Nordisk Research Center Indianapolis

ABSTRACT

Concurrent activation of the GLP-1, GIP, and glucagon receptors imparts combinatorial metabolic benefits in preclinical models of diabetes and obesity through multiple pharmacological mechanisms. Unimolecular peptide triple agonists were rationally designed and optimized via sequence mutation and fatty acylation to exhibit potent agonistic activities at all three receptors and preclinical extension of time-action predicting once-weekly clinical administration. Chronic treatment of obese rodents with a balanced triple agonist exhibited weight lowering efficacy superior to GLP-1 receptor mono-agonist semaglutide and GLP-1/GIP receptor co-agonist tirzepatide, without erosion of glycemic control. Furthermore, dose escalation of this triple agonist over six weeks of chronic treatment achieved body weight normalization in obese rodents, resulting in an average weight loss of approximately 60%. These profound pre-clinical results highlight the potential of this poly-pharmacological strategy as a powerful means to combat the obesity epidemic.

BIO

Patrick Knerr is the Senior Director & Site Head of the Novo Nordisk Research Center Indianapolis (NNRCI), an interdisciplinary team focused on the discovery and maturation of disruptive research concepts for the treatment of cardiometabolic and rare diseases. After completing his PhD in peptide natural products with Wilfred van der Donk at the University of Illinois in Urbana-Champaign, Pat held a position with the former DuPont Crop Protection (now FMC) before moving to the NNRCI in 2016 to rekindle his passion in peptide medicinal chemistry. He has driven a portfolio of drug discovery projects centered on peptide poly-agonists for the treatment of metabolic diseases, resulting in three active clinical/preclinical programs and six filed international patent applications, and was promoted to Site Head in early 2022.

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.