Tinya Abrams

TL;DR: The pharmacokinetic/pharmacodynamic relationship established for SU11248 in these preclinical studies has aided in the design, selection, and evaluation of dosing regimens being tested in human trials.

TL;DR: It is suggested that SU11248 may have clinical potential in the treatment of SCLC via direct antitumor activity mediated via KIT as well as tumor angiogenesis via vascular endothelial growth factor receptor FLK1/KDR and PDGFRbeta.

TL;DR: Data suggest that SU11248 may be an effective and tolerated therapy to inhibit growth of breast cancer bone metastases, with the additional advantage of inhibiting tumor-associated osteolysis.

TL;DR: It is demonstrated that SU11248 is effective in preclinical breast cancer models and suggested that it may be useful in the treatment of breast cancer in the clinic, and in combination with conventional cytotoxic agents.

TL;DR: The design and synthesis of a series of potent benzothiophene-containing compounds that exhibit oral bioavailability and preclinical activity as SERDs are described, culminating in the identification of LSZ102, a compound in clinical development for the treatment of ERα positive breast cancer.