Agave salmiana Otto ex Salm-Dyck has traditionally been used for the production of fermented beverage known as "pulque" that has recently gained acceptance as a functional food. However, the plant requires up to 10 years to be used as raw material. The objective of this work was to evaluate the antioxidant and bioactive principles of Agave salmiana during different stages of development. Wild grown plants from Coahuila, Mexico, were identified based on leaf and spine traits to obtain a representative sample from six different stages of development (I-VI) from 1 to 7 years old. Total phenolic content (TPC), antioxidant activity (AOX), as well as composition and content of flavonols and saponins by HPLC-MS-TOF and HPLC-ELSD-PDA were evaluated. Concentrations of TPC were found to be between 5 to 13 mg gallic acid equivalents/g, reaching a maximum at stage II. The AOX presented a negative tendency from stage I to stage VI (from 148 to 50 μmol Trolox equivalents/g respectively). Kaempferol, quercetin and five saponins were identified. Similar to AOX, flavonols presented a negative concentration tendency with a reduction of 65% between the stage I and VI. Plants of stage III and IV presented the highest content of saponins, particularly chlorogenin glycoside, containing 3.19 and 2.90 mg protodioscin equivalents/g, respectively. These data suggest that plants from stages I to IV may be used as a source of antioxidant and bioactive principles, and that the content of these metabolites could be used as a marker to determine the developmental stage of the plant.