The search for the ideal antihypertensive drug is ongoing. Since hypertension initially is a relatively symptom-free disease, it is important that any agent developed be not only efficacious but also safe, with minimal side effects. Additionally such a drug should ideally possess both primary and secondary cardiovascular preventive properties. This review discusses the most commonly used antihypertensive drugs in the light of these goals, and highlights the development of multiaction drugs. Carvedilol, which is a nonselective beta-blocking and α<sub>1</sub>-blocking drug, with additional Ca<sup>2+</sup>-antagonistic properties, is being developed as an antihypertensive, antianginal drug and as an adjunct therapy in congestive heart failure. The development challenges for this single-entity drug are discussed and evidence for its antihypertensive efficacy, as well as its antianginal efficacy, is presented. The cardioprotective potential of carvedilol based on preclinical experiments is addressed. Finally, the regulatory questions regarding the development of a multiaction drug are highlighted.