Dasatinib

Rebecca VW, et al. iScience, 2026, 114669.

Dasatinib was evaluated for restoring BRAF/MEK inhibitor (BRAFi/MEKi) sensitivity in patient-derived xenograft (PDX) models of BRAFi/MEKi-resistant melanoma. Eleven clinically relevant compounds with pan-RTK, non-RTK, or PI3K-mTOR specificity were screened in vivo, identifying dasatinib as most effective in re-sensitizing resistant tumors. Tumor protein activity profiling revealed that high baseline expression of resistance-associated proteins (AXL, YAP, HSP70, phospho-AKT) predicted combination therapy efficacy. Dasatinib combined with BRAFi/MEKi suppressed resistant YAP+ subpopulations, restoring anti-tumor activity. This study demonstrates the application of dasatinib as a rational salvage therapy in preclinical PDX models and highlights the importance of protein-level analyses over genotypic profiling in guiding therapeutic interventions.

Eltahan DA, et al. Journal of Drug Delivery Science and Technology, 2025, 107, 106870.

A self-emulsifying drug delivery system (SEDDS) was developed to improve dasatinib solubility and intestinal absorption. Cinnamon oil was combined with Tween 80 surfactant and co-surfactants ethanol (F2) or PEG 200 (F3). Dasatinib solubility was assessed by titrating 25 mg of drug into oil/surfactant mixtures until complete dissolution, expressed as % w/w. Optimized SEDDS (50% cinnamon oil w/w) were prepared by accurate weighing and simple mixing, followed by aqueous dilution to form nanoscale emulsions. Particle size and zeta potential were characterized, and 100 mg dasatinib was incorporated to study dissolution behavior. F2 formulation demonstrated superior dissolution, indicating the potential of SEDDS to enhance oral bioavailability through nanoscale dispersion and improved permeability.

Khadke R, et al. International Journal of Pharmaceutics, 2025, 675, 125504.

Dasatinib-loaded oil-in-water nanoemulsions were prepared to improve ocular delivery and therapeutic efficacy. Oleic acid served as the oil phase, and a Smix of Tween 80 and propylene glycol (1:1 ratio) was combined under stirring. The aqueous phase (pH 7.4 phosphate buffer) was added rapidly to form a clear emulsion, with proportions guided by a pseudo-ternary phase diagram. Dasatinib was incorporated at 0.05-1% into the oil phase, followed by Smix addition and rapid aqueous dispersion under continuous stirring. Resulting nanoemulsions were characterized for clarity, droplet size, and stability. This method enabled efficient drug loading and nanoscale formulation, supporting dasatinib's anti-angiogenic and anti-inflammatory activity for ocular applications.