β-Lapachone is an ortho-naphthoquinone and inhibits topoisomerase I. β-Lapachone is a classic quinone-containing antitumor NQO1-bioactivatable drug that directly kills NQO1-overexpressing cancer cells. NQO1 is an antioxidative enzyme that helps recover renal oxidative status. β-Lapachone reduces cisplatin-induced nephrotoxicity. In cancer cells, cisplatin forms cross-link with  DNA, which inhibits DNA  replication, and this genotoxic stress and  DNA damage are essential for its anticancer effect. Several studies revealed a synergistic effect when β-Lapachone is combined with other chemotherapeutic agents. Moreover, β-Lapachone not only reduces cisplatin-induced inflammatory responses but also synergistically enhanced cisplatin’s antitumor activity. In addition, β-Lapachone plays a beneficial role in the prevention of inflammatory-related diseases. β-Lapachone co-treatment attenuates cisplatin-induced pathologic alterations. β-Lapachone also markedly decreases cisplatin-induced renal cell apoptosis and DSBs formation. The β-lapachone+cisplatin group shows the highest MRN complex expression. Moreover, it increases the basal expression level of the MRN complex. β-Lapachone has positive effects on rheumatoid arthritis (RA) treatment. Furthermore, β-Lapachone attenuates lung inflammation induced by bleomycin and acute kidney injury mediated by cisplatin in mice. Anti-arthritic effect of β-Lapachone and the promising anti-inflammatory and anti-arthritic effects of β-Lapachone through suppression of edema and cell migration, NF-κB, TNF-α and reducing concentrations of pro-inflammatory cytokines such as IL-6. As well, β-Lapachone leads to a reduction in serum levels of NO which plays an important role in the pathogenesis of rheumatoid arthritis. β-Lapachone shows positive effects on the animal model of multiple sclerosis. In a word, β-Lapachone is a natural naphtaquinone with anti-oxidative stress, anti-cancer.  It has an inhibitory effect on various cancers. It includes epidermoid laryngeal cancer, as well as prostate, colon, ovarian, lung, and breast-cancer. In addition, β-Lapachonehas anti-inflammatory activities.