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Cambridge Healthtech Institute’s 13th Annual

GLP1 & Oral Peptides

Obesity-Related Drug Discovery Advances

April 15 - 16, 2025 ALL TIMES PDT

 

The promise of anti-obesity therapeutics is generating a flurry of related research and drug development in the pharmaceutical and medical research establishment. In 2021, the FDA approved the first chronic weight-loss-specific medication, Wegovy, based on agonists of the glucagon-like peptide (GLP) receptor; GLP1 agonists were originally launched for diabetes. At CHI’s GLP1 & Oral Peptides conference, leading discovery chemists will convene to share progress and innovations spurred by GLP1R agonist-focused drug development, including the development of oral peptides. We also cover obesity-related therapeutic progress beyond GLP1 peptides such as the development of small molecules and 2nd generation compounds.

Tuesday, April 15

7:00 amRegistration Open and Morning Coffee

GLP1, GIP1 PEPTIDE-BASED DRUG DESIGN & DEVELOPMENT

8:00 amWelcome Remarks
8:05 am

Chairperson's Remarks

Hao Wu, PhD, Scientist 4, Genentech Inc.

8:10 am

Biased Agonism at GLP-1R and GIPR for Treating T2D and Obesity

Ruben Rodriguez, PhD, Senior Scientist, In Vitro Pharmacolgy, Carmot/Roche

Obesity and diabetes are major public health concerns. Incretin-like therapeutics have proven highly effective in treating both conditions and their associated complications. We are exploring the next generation of higher efficacy compounds through biased signaling of cAMP over ß-arrestin on both GLP-1R and GIPR. Our findings demonstrate that biased agonists provide longer-lasting glucose reduction, greater food intake suppression, and weight loss, highlighting their potential in treating these conditions.

8:40 am

Tuning Multi-Receptor Peptide Agonists through Molecular Design

Krishna Kumar, PhD, Professor, Chemistry, Tufts University

We describe here the design and development of potent peptide analogs that are completely refractory to hydrolytic enzyme action while retaining full biological activity, potency, and efficacy.  This lecture will describe the fundamental design principles, molecular pharmacology, and in vivo data detailing, fine tuning such activity by simple chemical modification of peptides. Some of the compounds described rival or better those used in the clinic.

9:10 am Talk Title to be Announced

Speaker to be Announced, Eurofins

9:40 amIn-Person Breakouts

See Breakouts page on the conference website for details.

10:25 amNetworking Coffee Break

10:50 am

Novel Unimolecular Tetra-Agonists for the Treatment of Obesity and Related Disorders

Cristina M. Rondinone, PhD, Founder & CEO, Pep2Tango Therapeutics

We describe the characterization of a novel long-acting peptide agonist for GLP-1, GIP, Amylin, and Calcitonin, receptors (PTT-A) and assessed its efficacy against the dual GIPR/GLP-1R agonist Tirzepatide. PTT-A decreased blood glucose and calcium levels acutely in lean rodents and dose-dependently reduced cumulative food intake. Chronic studies in diet-induced obesity (DIO) rats showed that PTT-A led to substantial reductions in body weight and cumulative food intake, primarily by decreasing fat mass while preserving muscle mass, unlike tirzepatide. The tetra-agonist peptide demonstrated robust efficacy for glucose and plasma lipid lowering, insulin sensitization, and liver benefits, outperforming Tirzepatide at equivalent doses.

11:20 am Talk Title to be Announced

Scott Pollack, PhD, Research Fellow, Peptide Therapeutics, Merck & Co., Inc.

11:50 amPresentation to be Announced

12:20 pmTransition to Lunch

12:25 pmLuncheon Presentation (Sponsorship Opportunity Available) or Enjoy Lunch on Your Own

12:55 pmSession Break

SMALL MOLECULE & OTHER ANTI-OBESITY APPROACHES

1:45 pm

Chairperson's Remarks

Robert D. Mazzola, PhD, Director & Principal Scientist, Chemical Research, Merck & Co.

1:50 pm

Developing Small Molecule Agonists of GLP-1R and Other Obesity-Related Peptide-Binding GPCRs

Yingli Y. Ma, PhD, CTO, Platform Technology, Structure Therapeutics Shanghai Basecamp Biotechnology Co.

I will present on the development of small molecule agonist versions of peptides that bind G protein-coupled receptors (GPCRs) such as GLP-1R that play a role in obesity.

2:20 pm

Discovery and Development of Orally Available GLP1 Receptor Small Molecule Agonist and Sensitizer

Jiayu Liao, PhD, Professor, Bioengineering, University of California, Riverside

Small molecule modulators for the GLP1 receptor offer complementary chemical tools and therapeutic agents as a novel mode of action. We pioneered the discovery and development of a non-peptide and orally available small molecule GLP1 receptor agonist and an utterly novel action of the GLP1 peptide sensitizer. This represents a novel opportunity for the GLP1 receptor and Class B GPCRs as therapeutics to treat metabolic diseases in the future.

2:50 pm

The Promise of Synergistic Pharmacology: LY3457263, a Novel NPY2 Receptor Agonist for Type 2 Diabetes and Obesity

Avinash Muppidi, PhD, Director, Peptide Therapeutics, Eli Lilly & Co.

3:20 pmSponsored Presentation (Opportunity Available)

3:35 pmGrand Opening Refreshment Break in the Exhibit Hall with Poster Viewing and Best of Show Voting Begins

PLENARY KEYNOTE SESSION

4:35 pm

Plenary Welcome Remarks from Lead Content Director

Anjani Shah, PhD, Senior Conference Director, Cambridge Healthtech Institute

4:50 pm PLENARY KEYNOTE:

Applying Diverse Small Molecule Strategies to Difficult Targets: Drugging BTK for (Neuro)Immunology

Christopher J. Helal, PhD, Vice President & Head, Medicinal Chemistry, Biogen

Bruton's Tyrosine Kinase (BTK) plays a central role in certain cancers which has led to the identification and approval of several covalent inhibitors. Despite this progress, challenges exist in identifying BTK inhibitors with improved safety profiles and brain penetration to address both peripheral and central immunological diseases. In this talk we will share application of diverse strategies to inhibit or degrade BTK for optimal efficacy and safety.

5:35 pmWelcome Reception in the Exhibit Hall with Poster Viewing

6:35 pmClose of Day

Wednesday, April 16

7:15 amRegistration Open and Morning Coffee

MAKING ORAL PEPTIDES

8:00 am

Chairperson's Remarks

Anastasia Velentza, PhD, Vice President, Biology, Vilya Therapeutics

8:05 am

Development of Orally Available Cyclic Peptides

Manuel L Merz, PhD, Postdoctoral Fellow, Broad Institute

I present work completed in the Christian Heinis laboratory as part of my graduate studies where we developed synthesis and screening tools for generating large chemical libraries of small cyclic peptides, enabling the discovery of target-specific, orally bioavailable peptides. This generalizable workflow, applicable to interactions with a functional readout, yielded sub-1 kDa peptides with high-affinity binding to proteases and good oral bioavailability in rats.

8:35 am

De novo Design of Oral Peptides Using Physics-Based Generative AI

Hans Melo, PhD, Co Founder & CEO, Menten AI

Cyclic peptides have long been considered attractive as a drug modality due to their medium size and combining the advantages of small molecules and biologics. However, membrane permeability remains a significant challenge. Recently, physics-based Generative AI has emerged as a promising technology to design cyclic peptides with specific properties in mind. Here we focus on applying this method to design de novo cyclic peptides with drug-like oral bioavailability.

9:05 am PANEL DISCUSSION:

GLP1-Related Drug Discovery & Development Challenges

PANEL MODERATOR:

Emel Adaligil, PhD, Principal Scientific Manager, Peptide Therapeutics, Genentech, Inc.

9:35 amCoffee Break in the Exhibit Hall with Poster Awards Announced (Sponsorship Opportunity Available)

10:30 am

Formulation & Delivery Considerations in Early Drug Discovery for Oral Peptides

Tahnee J. Dening, PhD, Principal Scientist, Genentech Inc.

Although once considered highly infeasible, oral administration of peptide drugs is now a reality, as evidenced by oral semaglutide (Rybelsus) and oral octreotide (Mycapssa) drug products. In this presentation, we will discuss formulation strategies (and peptide design rules) to enable the oral absorption of both high solubility/low permeability peptides and low solubility/high permeability peptides, with an emphasis on early drug discovery.

11:00 am

Advancements in Peptide Late-Stage Functionalization for Drug Discovery

Jennifer Hanisak, PhD, Senior Scientist, Peptide Chemistry, Merck

11:30 am

Next-Generation, Orally Bioavailable, PD-L1-Targeted Macrocyclic Peptide

Paul M. Scola, PhD, Senior Director, Drug Discovery, Bristol Myers Squibb Co.

12:00 pmClose of GLP1 & Oral Peptides Conference


For more details on the conference, please contact:

Anjani Shah, PhD

Senior Conference Director and Lead Content Director for Drug Discovery Chemistry

Cambridge Healthtech Institute

Phone: (+1) 781-247-6252

Email: ashah@healthtech.com

 

For sponsorship information, please contact:

Kristin Skahan

Senior Business Development Manager

Cambridge Healthtech Institute

Phone: (+1) 781-972-5431

Email: kskahan@healthtech.com