Compounds 1247–1301 (non-secosteroidal VDR ligands) [315] were analyzed and presented better therapeutic efficacy when compared to 1α,25(OH)2D3 in experimental models of cancer and osteoporosis with less induction of hypercalcemia, a major potential adverse effect in the clinical application of VDR ligands. The gene discussed is VDR; the disease is osteoporosis.