Purpose: To conduct a systematic review of available limited sampling strategies (LSSs) for all anticancer (other than platinum) agents and to assess the clinical utility of such models. Design: A literature search was conducted using PubMed and EMBASE up to November 2008. Relevant articles were then categorized according to modified level of evidence guidelines of the U.S. Preventive Services Task Force. Results: Fifty-one studies have been published suggesting LSSs for the estimation of pharmacokinetic (PK) parameters for 16 different anticancer agents. These include [number of studies (n) =1, unless otherwise denoted]: busulfan [levels II-1, II-2(n=6), III], cladribine (level II-1), cyclophosphamide (level II-1), docetaxel (level II-1, III), doxorubicin (level II-1), epirubicin [levels II-1, III(n=2)], etoposide [levels I(n=3), II-1(n=2), II-2, III], 5-fluorouracil [levels II-1, II-2, III(n=2)], irinotecan [levels I(n=2), II-2(n=3), III], melphalan (level I), methotrexate [level II-1(n=3), II-2], temozolamide (level I), thiotepa (level III), topotecan [levels I(n=3), II-1, II-2, III], vinblastine (level II-1) and vinorelbine [levels I, II-2(n=2)]. Conclusion: The 12 level I studies illustrate that when properly constructed and validated, LSSs have the ability to estimate PK parameters in cancer patients. However, the estimated PK parameters need to be related to clinical response or toxicity in order to demonstrate full clinical utility.