Chronic myelogenous leukemia (CML) is a myeloproliferative disease characterized by a specific translocation t(9;22)(q34;q11) that results in the transcription and translation of fusion proteins with constitutively activated tyrosine kinase activity and transduction along several signaling pathways. Identification and characterization of many of the members of this cascade of events has generated new drugs that are able to target specific segments of that chain. Most notable among these are the tyrosine kinase inhibitor compounds such as ST1571. Their activity in many CML patients who have become resistant to standard treatments such as interferon alfa or who have developed transformation into accelerated and blastic phases has recently been demonstrated in phase I clinical trials. Other agents and new drugs are being identified. This review provides a concise overview over some of these agents and their role in the treatment of CML today.