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Inositol phosphates regulate essential cellular processes such as insulin signaling, nucleotide synthesis, DNA damage response, and phosphate homeostasis. Given this wide spectrum of physiological roles, the kinases responsible for inositol phosphate biosynthesis\u2014namely IP3Ks, IPMK, ITPK1, IP5\u20102\u2009K, IP6Ks, and PPIP5Ks\u2014have attracted increased interest over the past decade. Accumulating evidence supports their potential as drug targets in the treatment of obesity, cancer, and aging\u2010related conditions. In this review, structure\u2010guided strategies, particularly those informed by high\u2010resolution crystal structures, are examined for their role in accelerating the discovery and development of small\u2010molecule inhibitors targeting inositol phosphate kinases. 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