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 deciphers the dynamic behavior of proteins at the molecular level and integrates this knowledge into the drug discovery process. The company’s scientific approach combines advanced experimental methods in structural biology, biophysics, chemistry, and biology with powerful computational modeling workflows.

Relay Therapeutics’ core technology, the Dynamo® Platform, is grounded in the concept of “Motion-Based Drug Design®.” This platform aims to understand conformational changes in proteins over time, model the functional consequences of these motions, and determine the mechanisms by which drugs interact with target proteins. The platform is supported by physics-based simulations, long-timescale molecular dynamics analyses, free energy perturbation calculations (FEP), and machine learning algorithms integrated into simulation models.

The Dynamo process consists of three stages. The first stage involves the experimental determination of the structural and dynamic properties of the target protein, utilizing techniques such as cryo-electron microscopy (Cryo-EM) and ambient-temperature X-ray crystallography. In the second stage, potential binding sites and target modulation hypotheses are developed; appropriate chemical starting points are then identified through virtual screening and DNA-encoded molecular libraries (REL-DEL). In the final stage, advanced molecular simulations, biophysical assays, and medicinal chemistry efforts are integrated to optimize lead candidates.

Relay Therapeutics is developing innovative small-molecule drug candidates primarily in the fields of oncology and genetic diseases. One of the company’s leading candidates, RLY-2608, is a mutant-selective PI3Kα inhibitor currently under clinical investigation for both advanced breast cancer and PIK3CA mutation-associated vascular malformations (PROS). RLY-2608 is being evaluated in combination with fulvestrant in the global Phase 3 ReDiscover-2 trial for patients with HR+, HER2-, PI3Kα-mutated breast cancer. Other candidates in the company’s clinical pipeline include RLY-8161 (targeting NRAS-driven solid tumors) and Lirafugratinib (RLY-4008) (an FGFR2 inhibitor licensed to Elevar Therapeutics).

The founding of Relay Therapeutics emerged at the intersection of three key scientific advances: the identification of disease-causing targets through genomic data, the development of structural biology techniques enabling atomic-resolution visualization of protein motions, and progress in computational power allowing molecular dynamics simulations across biological timescales. By integrating these three domains, the company is developing novel therapeutic strategies against protein targets previously deemed “undruggable.”

Relay Therapeutics maintains an “Expanded Access Policy” program aimed at increasing treatment access. The company prioritizes ethical sensitivity and patient-centricity in its clinical research processes through collaboration with patients, families, and patient advocacy groups.

Relay Therapeutics is headquartered in Cambridge, Massachusetts, and fosters an integrated work culture combining research, clinical development, and data science teams. The company seeks to establish a new paradigm in drug discovery by uniting structural biology with artificial intelligence-driven computational science.