BMS-135 / BMS - LARVOL DELTA

Enhancing the Oral Bioavailability of a Poorly Soluble Pan-CK2 Kinase Inhibitor: Leveraging a Phosphate Prodrug Strategy to Overcome Dissolution-Limited Absorption and Improve Systemic Exposure during Dose Escalation. (PubMed, J Med Chem) - "PK analyses revealed that systemic exposure was governed by both phosphate cleavage and intermediate hydrolysis rates, with steric factors critically influencing enzymatic activation. These findings support the continued development of BMS-135 as an orally bioavailable anticancer therapeutic and highlight the strategic utility of phosphate prodrugs for facilitating the oral delivery of poorly soluble kinase inhibitors."

Journal • Oncology