SGR-3515
Investigators interested in participating in this clinical program, please click below.
INVESTIGATIONAL WEE1/MYT1 INHIBITOR
Target
Wee1/Myt1
Program Type
Proprietary, small molecule
Indication
Solid tumors
Stage
Phase 1 clinical development
Overview
SGR-3515 is a Wee1/Myt1 inhibitor.
Wee1 and Myt1 (membrane associated tyrosine/threonine 1) kinases regulate the cell cycle and DNA damage response through phosphorylation and inactivation of cyclin dependent kinase 1 (CDK1), allowing cells to repair DNA damage before entering mitosis. Concurrent loss of function of Wee1 and Myt1 confers selective vulnerability in cancer cells, a mechanism referred to as synthetic lethality. Compounds inhibiting Wee1 and Myt1 have shown clinical benefit in gynecological and other cancers.
Our Approach
We leveraged our computational platform to identify multiple highly selective and structurally distinct Wee1 inhibitors with optimized physicochemical properties. Preclinical models confirmed strong pharmacodynamic responses and anti-tumor activity of SGR-3515 as a monotherapy and as part of combination therapy with other agents. SGR-3515 is a Wee1/Myt1 dual inhibitor with a differentiated biochemical, biophysical and functional profile, with sustained inhibition of Wee1 and Myt1 in tumor tissue. Myt1 co-inhibition enhances activity and leverages synthetic lethality, with potential to reduce tumor resistance. The profile of SGR-3515 enables dosing schedules optimized to maintain anti-tumor activity and limit hematological toxicity.
SGR-3515 is currently in clinical development in patients with advanced solid tumors.
Clinical trial information
Patient trial
A Phase 1 clinical trial of SGR-3515 is ongoing to evaluate the safety and tolerability and to determine the maximum tolerated dose/recommended dose in patients with advanced solid tumors.
Learn more at: CLINICALTRIALS.GOV
Presentations
Poster Presentation
Discovery of potent, selective, and orally available Wee1 inhibitors that demonstrate increased DNA damage, tumor cell mitosis and in vivo tumor regression
American Association of Cancer Research (AACR) 2022 Annual Meeting
Services
Explore resources for patients and physicians.
