Abstract: Grass pea (Lathyrus sativus) is a legume with various adverse adaptability and rich nutrition. However, it can lead to the human and animal neurotoxicity after longterm consumption due to its neurotoxin, β-N-oxalyl-L-α,β-diaminopropionic acid (β-ODAP), limiting its utilization. This paper summarized the influences of β-ODAP on osmotic adjustment and growth regulation in grass pea under drought stress, the research progress in analysis methods, toxicological mechanisms and practical utility of β-ODAP, and the breeding strategies for low and zero-β-ODAP. β-ODAP synthesis was found to be abundant in grass pea under drought stress and its content was enhanced gradually with the increasing extent of drought stress. β-ODAP could supply nitrogen for plant growth and seed development, scavenge reactive oxygen species (ROS), involve in osmotic adjustment as a soluble amino acid, transport zincions as a carrier molecule, and impact nodule development. However, increasing the content of sulfurcontaining amino acids (methionine and cysteine) could decrease the level of toxicity of grass pea. There were a lot of investigations on collecting genetic resources, cross breeding, tissue culture, and gene manipulation for low and zerotoxin in grass pea in recent years. Although β-ODAP could induce excitotoxicity by damaging intracellular Ca2+ homeostasis and as glutamate analogues, it has medicinal value on hemostasis and antitumor.