IPI-145 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) isoforms PI3Kγ and PI3Kδ (IC50s = 0.24 and 50 nM, respectively). It is orally bioavailable and selective. As PI3Kγ and PI3Kδ are preferentially expressed in immune cells, IPI-145 has profound effects in collagen-induced and adjuvant-induced arthritis, ovalbumin-induced asthma, and systemic lupus erythematosus animal models. It also has potential applications in immunotherapy and in certain cancers.