Ormeloxifene (also known as centchroman) is a selective estrogen receptor modulator. It is a once-a-week non-steroidal oral contraceptive agent marketed in India and other countries under the brand names Novex-DS, Centron, and Sevista. Ormeloxifene has been investigated in the management of benign breast diseases such as mastalgia. The l-isomer, levormeloxifene, which has oestrogenic effects, has been investigated in the management of postmenopausal osteoporosis, but development appears to have been discontinued because of adverse effects. Recent studies have shown Ormeloxifene`s potent anti-cancer activities in breast, head and neck, and chronic myeloid leukemia cells. Several in vivo and clinical studies have reported that ormeloxifene possesses an excellent therapeutic index and has been well-tolerated, without any haematological, biochemical or histopathological toxicity, even with chronic administration. In India, ormeloxifene has been available as birth control since the early 1990s, and it is currently marketed there under the trade name Saheli. Ormeloxifene has also been licensed under the trade names Centron and Sevista. Ormeloxifene acts on oestrogen receptors. It has a weak estrogenic and potent antiestrogenic actions. It is expected to exert a contraceptive effect and normalise the bleeding from uterine cavity by regularising the expression of oestrogen receptors on the endometrium. As a contraceptive, it prevents proliferation and decidualisation of the endometrium, enhances blastocyst formation and slightly increases embryo transport through the oviducts.