Richard D. Carvajal

TL;DR: Exposure at doses above 300 mg QD and 200 mg BID are in the efficacious range from preclinical projections and clinical PK demonstrates rapid absorption of LXS196 with Tmax of ~1 hr post dose and consistent terminal T1/2 across different doses (~ 11 hr).

TL;DR: Efficacy of single-agent ontuxizumab at these doses in melanoma was low and well tolerated, and the overall response rate was 3.1% at the 4 mg/kg dose, with clinical benefit achieved in 42.4% of response evaluable patients.

TL;DR: This phase II study met its primary endpoint with an 18-week DCR of 46% and demonstrates that combining a cytotoxic therapy (dacarbazine) with an antiangiogenic small molecule (sorafenib) is feasible and associated with favorable disease-control rates; however, it also increases the potential for significant toxicity.

TL;DR: This first-in-human trial of BVD-523 (ulixertinib), a selective ERK1/2 kinase inhibitor, was initiated based on its promising preclinical profile and aims to determination of dose-limiting toxicities, maximum tolerated dose, and recommended phase II dose.

TL;DR: BID dosing of CB-839 with meals provided optimal PK and tolerability and achieved robust inhibition of GLS in blood and tumors and after achieving strong GLS inhibition with acceptable toxicity and observing a TNBC patient with a 23% reduction in tumor burden on study for >18 months, a combination arm testing CB- 839 with Pac (Pac-CB) for TNBC was opened.