Relay Therapeutics

Relay Therapeutics is a clinical-stage precision medicine company distinguished by its motion-based drug discovery approach. Headquartered in Cambridge, Massachusetts, the company integrates molecular-level insights into protein dynamics with the drug discovery process. Its scientific framework combines structural biology, biophysics, chemistry, and biology with advanced computational modeling methods.

Relay Therapeutics’ core technology, the Dynamo® Platform, is based on the concept of Motion-Based Drug Design®. This platform aims to understand the conformational changes of proteins over time, model the functional consequences of these motions, and define how target proteins interact with potential drugs. The platform integrates physics-based simulations, long-timescale molecular dynamics, free energy perturbation (FEP) calculations, and machine learning–enhanced simulation models.

The Dynamo process consists of three stages:

1. Experimental characterization of the target protein’s structural and dynamic features using techniques such as cryo-electron microscopy (Cryo-EM) and room-temperature X-ray crystallography.
2. Hypothesis generation and virtual screening, where potential binding pockets and modulation strategies are identified, and suitable chemical starting points are selected through virtual screening and DNA-encoded library (REL-DEL) methods.
3. Optimization and validation, involving molecular simulations, biophysical assays, and medicinal chemistry to refine lead compounds into development candidates.

Relay Therapeutics develops small-molecule therapies for oncology and genetic diseases.

Key programs include:

• RLY-2608, a mutant-selective PI3Kα inhibitor, was evaluated in advanced breast cancer and PIK3CA-related overgrowth spectrum (PROS) disorders. It is currently in the global Phase 3 ReDiscover-2 trial for HR+, HER2-, PI3Kα-mutated breast cancer, in combination with fulvestrant.
• RLY-8161, targeting NRAS-driven solid tumors.
• Lirafugratinib (RLY-4008), an FGFR2 inhibitor licensed to Elevar Therapeutics.

Relay Therapeutics was founded at the intersection of three major scientific advances:

1. The identification of disease-causing targets through genomics.
2. The visualization of protein motion at atomic resolution via structural biology.
3. The computational capacity to perform molecular dynamics simulations on biological timescales.

Through the integration of these disciplines, the company develops novel therapeutic strategies targeting proteins previously considered “undruggable.”

Relay Therapeutics upholds a patient-centered philosophy through its Expanded Access Policy, which aims to broaden patient access to experimental treatments. The company collaborates closely with patients, families, and advocacy organizations, maintaining ethical transparency and clinical integrity throughout its research process.

Based in Cambridge, Massachusetts, Relay Therapeutics fosters an integrated culture uniting research, clinical development, and data science. By combining structural biology with AI-driven computational science, the company seeks to establish a new paradigm in the discovery and development of next-generation medicines.