Yi-Bin Chen1, Ann S LaCasce. 1. Dana Farber Cancer Institute, Massachusetts General Hospital, GRB 740, 44 Binney Street, Boston, MA 02115, USA.
Abstract
BACKGROUND: Enzastaurin is a novel antineoplastic and antiangiogenic agent that acts through inhibition of protein kinase C (PKC). OBJECTIVE: This review summarizes the scientific rationale and current clinical evidence for the use of enzastaurin in oncology. METHODS: We performed a systematic review of the literature using the keywords protein kinase C-beta and enzastaurin in order to characterize the therapeutic target PKC-beta. We then reviewed the in-vitro, Phase I, and Phase II data for enzastaurin with a focus on hematologic malignancies. RESULTS/ CONCLUSIONS: After preliminary Phase I trials established a favorable toxicity profile, enzastaurin has been studied in completed and ongoing Phase II and III studies in solid and hematologic malignancies, including B-cell lymphomas where the rationale for its use is most promising.
BACKGROUND:Enzastaurin is a novel antineoplastic and antiangiogenic agent that acts through inhibition of protein kinase C (PKC). OBJECTIVE: This review summarizes the scientific rationale and current clinical evidence for the use of enzastaurin in oncology. METHODS: We performed a systematic review of the literature using the keywords protein kinase C-beta and enzastaurin in order to characterize the therapeutic target PKC-beta. We then reviewed the in-vitro, Phase I, and Phase II data for enzastaurin with a focus on hematologic malignancies. RESULTS/ CONCLUSIONS: After preliminary Phase I trials established a favorable toxicity profile, enzastaurin has been studied in completed and ongoing Phase II and III studies in solid and hematologic malignancies, including B-cell lymphomas where the rationale for its use is most promising.
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