Phase I trial of a novel matrix metalloproteinase inhibitor batimastat (BB-94) in patients with advanced cancer.

Abstract	Degradation of basement membrane and extracellular matrix by matrix metalloproteinases (MMPs) is believed to be required for tumor invasion, tumor-induced angiogenesis and vascular invasion. A synthetic hydroxamate, batimastat (also known as BB-94), inhibits MMPs by binding the zinc ion in the active site of the MMP. Batimastat inhibits at least 50% of MMP activity at concentrations less than or equal to 10 ng/ml in vitro. Batimastat retarded ascites accumulation and increased survival in mice with human ovarian tumor xenografts. Acute and long-term toxicological studies revealed no major toxicity in animals. Batimastat is poorly soluble and was administered intraperitoneally (i.p.) as a suspension. Previous studies in patients with malignant ascites have shown no major toxicities at doses as high as 1350 mg/m2.
Authors	S Wojtowicz-Praga, J Low, J Marshall, E Ness, R Dickson, J Barter, M Sale, P McCann, J Moore, A Cole, M J Hawkins
Journal	Investigational new drugs (Invest New Drugs) Vol. 14 Issue 2 Pg. 193-202 ( 1996) ISSN: 0167-6997 [Print] United States
PMID	8913840 (Publication Type: Clinical Trial, Clinical Trial, Phase I, Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)
Chemical References	Antineoplastic Agents Matrix Metalloproteinase Inhibitors Protease Inhibitors Thiophenes Phenylalanine batimastat Collagenases Gelatinases Metalloendopeptidases Matrix Metalloproteinase 2 Matrix Metalloproteinase 9
Topics	Adult Aged Antineoplastic Agents (adverse effects, pharmacokinetics, therapeutic use) Collagenases (blood) Drug Administration Schedule Female Gelatinases (antagonists & inhibitors, blood) Humans Injections, Intraperitoneal Male Matrix Metalloproteinase 2 Matrix Metalloproteinase 9 Matrix Metalloproteinase Inhibitors Metalloendopeptidases (antagonists & inhibitors, blood) Middle Aged Neoplasms (drug therapy, enzymology, metabolism) Phenylalanine (adverse effects, analogs & derivatives, pharmacokinetics, therapeutic use) Protease Inhibitors (adverse effects, pharmacokinetics, therapeutic use) Thiophenes (adverse effects, pharmacokinetics, therapeutic use)

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