Drug Lead Identification + Optimization

SRI’s success in drug discovery is exemplified by its robust drug pipeline, with several marketed drugs, several in clinical and preclinical development, and numerous discovery programs. SRI has helped clients and partners advance more than 100 drugs into patient testing through aggressive lead identification and optimization.

SRI's laboratories routinely perform drug discovery through target identification and lead generation, computer-aided drug design, and design directed libraries to generate new small molecule leads. During lead optimization in drug discovery, SRI researchers improve the effectiveness, diminish the toxicity, and increase the absorption of the most promising compounds.

Lead identification and optimization ervices include:

  • Screening hits to leads

  • Lead optimization

  • Custom synthesis

  • Radiolabeled synthesis

  • Preformulation

  • Predictive Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) assays

Products + Solutions

researcher working in lab
SR16157: A Safer, More Effective Estrogen Inhibitor for Treating Breast Cancer

As an alternative to AIs, SRI has developed an estrogen inhibitor called SR16157. This rationally designed drug achieves more complete estrogen suppression by inhibiting estrogen in two ways.

Topics: Basic Cancer Research Cancer Drug Discovery Drug Discovery Drug Lead Identification + Optimization
researchers in lab coats working at a lab table
SR16388: A Novel Drug That Inhibits Tumor Growth by Targeting ERRalpha

SRI researchers have developed a novel steroidal compound, SR16388, which very selectively binds to and inhibits ERRalpha. This drug also regulates tumor energy metabolism by strongly inhibiting the protein HIF-1alpha, which promotes tumor cell survival in low-oxygen conditions.

Topics: Basic Cancer Research Cancer Drug Discovery Drug Discovery Drug Lead Identification + Optimization Pharmaceutical R+D
two researchers in lab coats working at equipment
TAS-108: A Better Anti-Estrogen Drug for Treating Breast Cancer

As a safer and more effective alternative to currently available drugs, SRI researchers have developed TAS-108, an oral anti-estrogen drug for the treatment of advanced breast cancer.

Topics: Basic Cancer Research Cancer Drug Discovery Drug Discovery Drug Lead Identification + Optimization

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