It is an exciting time for cancer researchers in the field of apoptotic cell death. The avalanche of discoveries over the past decade or so regarding how apoptosis is regulated begins to be exploited for therapeutic benefit as the first apoptosis-targeted drugs enter early clinical trials. This chapter provides a selective review on the development of such drugs. We also outline issues regarding the regulation and design of early clinical trials of this type of molecularly targeted agent. Finally, we discuss the biomarkers and surrogate pharmacodynamic endpoint assays currently available to chart the efficacy of apoptosis-inducing anticancer therapy.