EIK1005 / Eikon Therap - LARVOL DELTA

Preclinical development of EIK1005, a potent and selective inhibitor of Werner helicase (AACR 2026) - "Further studies elucidated several mechanisms of potential resistance to WRN inhibition. Overall, our preclinical characterization of EIK1005 demonstrates its strong activity and favorable pharmacologic profile that provide impetus to the ongoing clinical development of EIK1005 in patients with MSI-H cancers."

Preclinical • Microsatellite Instability • Oncology • GDF15 • MSI • WRN

EIK1005-002: A Clinical Research Study Evaluating EIK1005, a Werner Helicase Inhibitor, as Monotherapy and in Combination With Pembrolizumab in Participants With Advanced Solid Tumors Including Microsatellite Instability High (MSI-H) Tumors (clinicaltrials.gov) - P1/2 | N=160 | Recruiting | Sponsor: Eikon Therapeutics | Not yet recruiting ➔ Recruiting

Checkpoint inhibition • dMMR • Enrollment open • Mismatch repair • Monotherapy • MSI-H • Colorectal Cancer • Endometrial Cancer • Esophageal Cancer • Gastric Cancer • Microsatellite Instability • Oncology • Solid Tumor • MSI

EIK1005-002: A Clinical Research Study Evaluating EIK1005, a Werner Helicase Inhibitor, as Monotherapy and in Combination With Pembrolizumab in Participants With Advanced Solid Tumors Including Microsatellite Instability High (MSI-H) Tumors (clinicaltrials.gov) - P1/2 | N=160 | Not yet recruiting | Sponsor: Eikon Therapeutics

Checkpoint inhibition • dMMR • Mismatch repair • Monotherapy • MSI-H • New P1/2 trial • Colorectal Cancer • Endometrial Cancer • Esophageal Cancer • Gastric Cancer • Microsatellite Instability • Oncology • Solid Tumor

A novel, internally derived program targeting Werner (WRN) helicase for microsatellite unstable cancers and sensitive cancers that have other defects in DNA repair. EIK1005 is expected to begin Phase 1 clinical testing in Q4, 2025. (Businesswire)

New P1 trial • Microsatellite Instability • Solid Tumor

A Randomized, Double Blind, Single-Ascending Dose Study to Investigate the Safety, Tolerability, and Pharmacokinetic Profile of EIK1005 in Healthy Participants. (ANZCTR) - P1 | N=48 | Active, not recruiting | Sponsor: EIKON Therapeutics, Inc. | Not yet recruiting ➔ Active, not recruiting | Initiation date: Aug 2025

Enrollment closed • Trial initiation date • Microsatellite Instability • Solid Tumor

A Randomized, Double Blind, Single-Ascending Dose Study to Investigate the Safety, Tolerability, and Pharmacokinetic Profile of EIK1005 in Healthy Participants. (ANZCTR) - P1 | N=48 | Not yet recruiting | Sponsor: EIKON Therapeutics, Inc.

New P1 trial • Microsatellite Instability • Solid Tumor

Eikon Therapeutics Secures $350.7 Million Series D to Advance Clinical-Stage Programs and Future Pipeline (Businesswire) - "Eikon Therapeutics, Inc...announced the initial closing of a $350.7 million Series D financing. Since its founding in 2019, Eikon Therapeutics has privately raised in excess of $1.1 billion to support its mission of developing new medicines to address grievous illnesses....Eikon’s clinical portfolio is anchored by its lead program, EIK1001, a systemically administered co-agonist of toll-like receptors 7 and 8 now in a Phase III trial for advanced melanoma.... In parallel, the company is advancing EIK1003, a highly selective PARP1 inhibitor currently undergoing Phase 1 evaluation in patients with breast, ovarian, prostate, or pancreatic cancers, and EIK1004, a central nervous system-penetrant PARP1-selective inhibitor poised to initiate Phase 1 studies targeting brain cancers. Eikon’s early-stage pipeline features, among other undisclosed candidates, two androgen receptor antagonists and an internally derived WRN inhibitor (EIK1005)..."

Financing • Brain Cancer • Breast Cancer • Melanoma • Ovarian Cancer • Pancreatic Cancer • Prostate Cancer