Role of nano-lipid formulation of CARP-1 mimetic, CFM-4.17 to improve systemic exposure and response in osimertinib resistant non-small cell lung cancer.

ABSTRACT:

Background

EGFR mutated NSCLCs have been shown to employ the use of CARP-1 in overriding the signaling inhibition of tyrosine kinase inhibitors (such as Osimertinib). CFM 4.17 is a CARP-1 inhibitor which has a promising role in overcoming Tyrosine Kinase Inhibitor (TKI) resistance when used as a pre-treatment through promoting apoptosis. Lack of solubility, hydrophobicity leading to poor systemic exposure are the limitations of CFM 4.17. This can be overcome by nano lipid-based formulation (NLPF) of CFM 4.17 which can enhance systemic exposure in preclinical animal models as well as improve therapeutic efficacy in drug-resistant cancer cell lines.

Methods

Molecular docking simulation studies were performed for CFM 4.17. CFM 4.17-NLPF was formulated by melt dispersion techniq

SUBMITTER: Kommineni N 

PROVIDER: S-EPMC7857068 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature