Event Schedule

12 October 2026

Target Validation and Hit Discovery

Session 1: "Unveiling Future Therapeutics by Targeting Orphan Nuclear Receptors"

Speaker: Ian Mitchelle S. De Vera, Ph.D. 

Assistant Professor, Director, Protein Core Facility

Department of Pharmacology & Physiology, Saint Louis University School of Medicine, MO, USA

Abstract

Targeting signaling mechanisms mediated by nuclear receptors (NRs) represents a promising strategy for developing new therapies for neurological disorders, multiple types of cancer, metabolic diseases, and other human conditions. The human nuclear receptor superfamily comprises 48 transcription factors that regulate diverse physiological and pathological processes. Ligand binding induces conformational changes in NRs that promote their interaction with specific genomic DNA sequences, known as nuclear receptor response elements, and facilitate the recruitment of co-regulatory proteins that ultimately modulate target-gene transcription. A subset of NRs is classified as orphan nuclear receptors (ONRs) because their endogenous ligands have not yet been conclusively identified or validated. Consequently, several of these receptors have historically been regarded as “undruggable.” However, the possibility that ONR activity can be selectively modulated by small-molecule ligands makes these receptors particularly compelling—and largely untapped —targets for therapeutic intervention. Here, an integrated arsenal of medium- to high-throughput biophysical approaches, in silico ligand docking, and structural elucidation techniques, including solution nuclear magnetic resonance (NMR) spectroscopy, was employed to identify small-molecule ligands that selectively bind to and modulate specific ONRs. These drug-discovery efforts were further complemented by medicinal chemistry, pharmacokinetic profiling, and in vivo evaluation in mouse models of disease. Together, these multidisciplinary approaches uncovered unexpected ligand–receptor interactions, revealed previously unrecognized regulatory pathways, and identified promising therapeutic opportunities with potential clinical applications

09 November 2026

Biologics Characterization and Developability

Session 2: Lab to Life: Discovery and Development of Biologic Therapy

Speaker: Jan Paulo Zaragosa, Ph.D. 

Associate Principal Scientist Molecular Discovery

Protein Characterization and Analytics Merck, CA, USA

Abstract

This presentation follows the development of clesrovimab (Enflonsia™), an FDA-approved antibody for RSV prevention in infants, as a real-world example of biologic therapies from discovery to patient impact. It covers engineered biologics, multiplex design strategies, and platforms like immunization, display methods, and computational modeling. Data engineering and machine learning, including generative AI tools, such as RFdiffusion and protein language models, are shown to accelerate drug development and enable de novo protein design. The talk highlights how interdisciplinary collaboration across chemistry, biology, engineering, computer science, and medicine advances modern drug discovery to meet medical needs and cure diseases.

07 December 2026

Session 3: High Throughput Analytical Workflows Enable Large Sample Size Screening in Early Drug Discovery Space

Speaker: Erwin G. Abucayan, Ph.D.

Associate Principal Scientist

Analytical R&D Discovery Analytical Research, Merck, NJ, USA

Abstract

Reliable Liquid Chromatography (LC) assays are critical for enabling the development of diverse therapeutic modalities, from highly polar small molecules to complex biologics such as antibody–drug conjugates (ADCs). To accelerate method development and derisk analytical deliverables, we implemented a workflow combining high-throughput column screening with multifactorial in silico method optimization. Column screening enables rapid identification of stationary phases capable of handling analytes with challenging physicochemical properties, while in silico multifactorial modeling optimizes key parameters for LC separations such as gradient profile, solvent composition, and temperature to achieve robust separations. This integrated approach enables systematic development of robust analytical methods and the timely deployment of fit-for-purpose assays across modalities. 

18 January 2027

Process Chemistry /API Manufacturing

Session 4: One Pot, Five Enzyme Cascade Enabling Access to Enlicitide Decanoate, The Largest Small Molecule Therapeutic for Lowering Cholesterol

Speaker: Jennifer V. Obligacion, Ph.D.

Associate Principal Scientist

Chemistry Discovery Process Chemistry, Merck, NJ, USA

Abstract

MK 0616 is an orally available macrocyclic peptide inhibitor of PCSK9 in development for the treatment of atherosclerotic cardiovascular disease. Its three fused macrocycles and high functional complexity make it extremely challenging to manufacture, with the first reported chemical route requiring 43 steps and delivered less than 1% overall yield. This talk will describe the development of a one pot, five enzyme cascade that enables protecting group free amidation, and reductive amination to access an advanced intermediate en route to MK-0616, ultimately enabling its long-term manufacture.

15 February 2027

Analytical Chemistry and Method Development

Session 5: Automated Screening and and Multifactorial Modelling for U/HPLC Assay Development across Drug Modalities

Speaker: Rodell C. Barrientos, Ph.D.

Associate Principal Scientist 

Analytical Research & Development, Merck, NJ, USA

Abstract

Reliable Liquid Chromatography (LC) assays are critical for enabling the development of diverse therapeutic modalities, from highly polar small molecules to complex biologics such as antibody–drug conjugates (ADCs). To accelerate method development and derisk analytical deliverables, we implemented a workflow combining high-throughput column screening with multifactorial in silico method optimization. Column screening enables rapid identification of stationary phases capable of handling analytes with challenging physicochemical properties, while in silico multifactorial modeling optimizes key parameters for LC separations such as gradient profile, solvent composition, and temperature to achieve robust separations. This integrated approach enables systematic development of robust analytical methods and the timely deployment of fit-for-purpose assays across modalities.

15 March 2027

Global Agency Engagements and Commercialization

Session 6: Chemistry in Regulatory Affairs CMC: Drug Registration, Strategies  and Documentation

Speaker: Llorente V. Bonaga, Ph.D.

Senior Director 

Global Regulatory Affairs CMC, Merck, NJ, USA

Abstract

The successful registration of pharmaceutical products requires the effective integration of scientific innovation, regulatory compliance, and robust Chemistry, Manufacturing, and Controls (CMC) strategies. As regulatory expectations continue to evolve, CMC professionals play a critical role in ensuring that the quality, safety, and efficacy of drug substances and drug products are consistently demonstrated throughout the product lifecycle, from development to commercialization and post-approval management. This presentation provides an overview of the fundamental principles and practical applications of chemistry within Regulatory Affairs CMC, highlighting how chemical and pharmaceutical sciences support global drug registration activities. Key topics include the development of regulatory CMC strategies, preparation and maintenance of Common Technical Document (CTD) submissions, management of product quality information, and the alignment of manufacturing and analytical development with regulatory requirements. The presentation also discusses the importance of risk-based approaches, lifecycle management, control strategy development, and the implementation of current international guidelines, including those from ICH and major health authorities such as FDA, EMA, and PMDA. Case studies will show how chemistry, CMC documentation, and cross-functional collaboration support global regulatory approvals and product lifecycle management.

12 April 2027

Session 7: The Process of Global Drug Registrations and Approvals

Speaker: Oscar Toress, Ph.D.

Associate Principal Scientist 

Global Regulatory Affairs CMC, Merck, NJ, USA

Abstract