Despite huge increases in access to contraceptives globally more than 700,000 maternal deaths, most in developing countries and related to unintended pregnancies, occurred between 1995 and 2000. Eighty-five million women have unintended or unwanted pregnancies annually due to a failure of contraception. Steroidal contraceptives are unsuitable for many women, but pharmacological alternatives are not available. Many couples discontinue use after initiation because of method-related reasons such as side-effects, health concerns or inconvenience. The development of non-hormonal contraceptives with additional health benefits such as blocking sexually transmitted infections (STIs) are highly desirable. We have produced novel compounds that prevent the establishment of pregnancy and are currently being trialled in combination with anti-STIs. Sustained delivery of the compounds via nanoparticles is also being explored. If effective, this will offer new opportunities as pharmacological, non-hormonal dual-role contraceptives for women.