GLP1 & Oral Peptides | April 15-16, 2025 | San Diego, CA

Cambridge Healthtech Institute’s 13th Annual

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.

• Day 1
• Day 2
• Download Brochure

Tuesday, April 15

7:00 amRegistration Open and Morning Coffee

8:00 amWelcome Remarks

8:05 am

Chairperson's Remarks

Hao Wu, PhD, Director of Chemistry, Pinnacle Medicines

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.

9:40 amBreakout Discussions (In-Person Only)

Breakout Discussions are informal, moderated discussions, allowing participants to exchange ideas and experiences and develop future collaborations around a focused topic. Each breakout will be led by a facilitator/s who keeps the discussion on track and the group engaged. Please visit the Breakout Discussions page on the conference website for a complete listing of topics and descriptions. Breakout Discussions are offered in-person only. 

In-Person Only BREAKOUT DISCUSSION 7:

Macrocyclic Peptides: Discovery to Delivery

Rumit Maini, PhD, Senior Director, Peptide Discovery Team, Eli Lilly

• Lab-based v. AI/ML-based macrocyclic discovery platforms 
• Permeation enhancers v. passive permeability​

In-Person Only BREAKOUT DISCUSSION 8:

Peptide Drug Conjugates (PDCs)

Avinash Muppidi, PhD, Director, Peptide Therapeutics, Eli Lilly and Company

Keykavous Parang, PhD, Professor, Biomedical and Pharmaceutical Sciences, Chapman University

• PDCs next new drug modality?
• PDCs beyond radionuclide conjugates
• PDCs vs ADCs
• Getting PDCs into cells

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

Supporting a Peptide Pipeline: Enabling Development of an Orally Bioavailable PCSK9 Inhibitor

Scott Pollack, PhD, Associate Principal Scientist, Merck & Co., Inc.

The growth of peptide-based programs in drug discovery, and in particular those developed through mRNA display, has required the parallel development of new chemistries to enable access to non-canonical amino acids (ncAAs) and ultimately macrocyclic peptides. We describe our efforts to prepare a novel orally bioavailable PSCK9 inhibitor and how these approaches can be used to enable other peptide programs.

11:50 am PANEL DISCUSSION:

Peptide Therapeutics Opportunities and Challenges

PANEL MODERATOR:

Hao Wu, PhD, Director of Chemistry, Pinnacle Medicines

• How will growing attention to peptide therapeutics impact medicinal chemistry?
• Oral vs. injectable peptide (and GLP1) therapeutics: patient compliance and clinical implications
• Chemical and formulation innovations to enhance oral bioavailability of peptides
• Challenges in manufacturing cyclic peptides for oral delivery​

PANELISTS:

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

Katerina Leftheris, PhD, formerly Chief Scientific Officer, Vilya Therapeutics

Mark Murcko, PhD, Principal, Disruptive Biomedical LLC

Scott Pollack, PhD, Associate Principal Scientist, Merck & Co., Inc.

12:20 pmEnjoy Lunch on Your Own

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

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 and Company

Nisotirostide is a novel NPY2 receptor agonist designed to enhance the metabolic effects of GLP-1 receptor agonists in type 2 diabetes and obesity. In vitro studies showed selective activation of NPY2 receptor signaling, while in vivo studies demonstrated significant reductions in food intake and body weight in mice. Chronic administration in diet-induced obese mice resulted in dose-dependent weight loss and improved glucose homeostasis. These findings suggest that Nisotirostide has the potential to improve glycemic control and reduce body weight in patients with type 2 diabetes and obesity. Clinical evaluation is ongoing.

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

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

• Day 1
• Day 2
• Download Brochure

Wednesday, April 16

7:15 amRegistration Open and Morning Coffee

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

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

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

The discovery of BMS-986238, a second-generation macrocyclic peptide and a potent inhibitor of PD-L1, is described. The targeted profile of this asset included the property of tight binding kinetics to the PD-L1 receptor, but with a significantly modified pharmacokinetic profile and specifically a long plasma half-life. These properties were predicted to reduce the frequency of QD-dosing as compared to the first-generation inhibitor BMS-986189 and likewise enable oral administration.

9:05 am

Design of Bicyclic Peptide Tandems Mimicking the Homodimeric GDF15 Protein to Modulate the GDF15-GFRaL-RET Receptor Complex Cell Signaling

Anais FM Noisier, PhD, Associate Principal Scientist, AstraZeneca R&D

The GDF15-GFRaL-RET protein complex is involved in appetite control and is an attractive target for disease states such as obesity and cachexia. We describe the discovery of Bicycle peptides and the design of Bicycle tandems capable of mimicking the homodimeric GDF15 ligand and modulating the intracellular signaling response driven by the hexameric complex assembly.

9:35 amCoffee Break in the Exhibit Hall with Poster Awards Announced

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, Associate Principal Scientist, Peptide Chemistry, Merck & Co., Inc.

In macrocyclic peptide (MP) drug discovery, the ability to fine-tune structural features as well as physical chemical properties is crucial for developing drug-like candidates. Due to the limited availability of commercial non-canonical amino acids (ncAAs), the discovery of novel building blocks for these purposes is paramount. Late-stage functionalization (LSF) is a highly efficient strategy for identifying novel ncAAs but is restricted by the limited number of chemistries compatible with fully elaborated MPs. This presentation will highlight some of our recent accomplishments in expanding the LSF toolbox for MPs.

11:30 amClose of GLP1 & Oral Peptides Conference

• Day 1
• Day 2
• Download Brochure

No Agenda API URL configured.