Caco-2 colorectal adenocarcinoma cell line (Caco-2) (Caco-2)

Caco-2 is a human colorectal adenocarcinoma cell line that is widely utilized as an in vitro model of the human intestinal epithelial barrier [3.1.1, 3.1.4]. Although derived from a colon tumor, Caco-2 cells possess the unique ability to spontaneously differentiate into a polarized monolayer with morphological and functional characteristics of small intestinal enterocytes, including the presence of a brush border with microvilli and tight junctions [3.1.3, 3.2.5]. This differentiation makes them the gold standard for assessing the intestinal permeability and absorption of orally administered drug candidates [3.2.1, 3.2.2]. The cells express various metabolic enzymes and efflux transporters, most notably P-glycoprotein (ABCB1), which play critical roles in determining drug bioavailability and potential drug-drug interactions [3.2.4]. In research, the Caco-2 permeability assay is used to categorize drugs according to the Biopharmaceutics Classification System (BCS) [3.2.1]. It is important to clarify that "Caco-2" refers to the entire cell line rather than a specific protein or molecular target; thus, drugs do not "target" Caco-2 in a therapeutic sense but are instead evaluated for their transport properties across the Caco-2 cell layer [3.1.5, 3.2.1]. The cell line is also used in cancer research to study the mechanisms of colorectal tumor progression and response to chemotherapy [3.1.2, 3.2.3].

Other names

Caco-2Caco2Cancer coli-2Human colorectal adenocarcinoma cell line

The Caco-2 cell line serves as a model for intestinal absorption; drugs are evaluated for their ability to permeate the cell monolayer via passive diffusion or active transport mediated by proteins like P-glycoprotein. It is not a therapeutic target in the molecular sense, but rather a biological system used to predict drug bioavailability.