Batimastat (BB-94) sodium salt is a broad-spectrum MMP inhibitor (IC50s: 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7, and MMP-3).

MMP1:3 nM , MMP7:6 nM , MMP2:4 nM , MMP9:4 nM , MMP3:20 nM

Batimastat inhibits gelatinases A and B (IC50s: 4 nM and 10 nM). The IC50 with the structurally similar collagenase Ht-d is 6 nM, which is comparable with values for MMP-1 (3 nM), MMP-8 (10 nM), and MMP-3 (20 nM) [2]. CD30 shedding from the cell line Karpas299 can effectively be blocked by the hydroxamic acid-based metalloproteinase inhibitor Batimastat (IC50: 230 nM) [3].

Matrix density is analyzed in saline- or Batimastat (40 mg/kg)-pretreated animals 4 h after E2 administration, the time point at which collagen density is observed to be at its lowest after hormone treatment [6]. Intraperitoneal administration of Batimastat effectively blocks the growth of human ovarian carcinoma xenografts and murine melanoma metastasis and delays the growth of primary tumors in an orthotopic model of human breast cancer without cytotoxicity and without affecting mRNA levels [2]. Batimastat has shown antineoplastic and antiangiogenic activity in various tumor models. Treatment with Batimastat (60 mg/kg i.p. every other day, for a total of eight injections) concomitantly with Cisplatin (4 mg/kg i.v., every 7 days for a total of three injections) completely prevents growth and spread of both xenografts, and all animals are alive and healthy on day 200[4]. Kaplan-Meier analysis of survival (at 48 h) shows that animals treated with Batimastat have increased survival (95.2%) in comparison with controls (75%), and differences are almost statistically significant (p=0.064) [5].

6. Russo LA, et al. Regulated expression of matrix metalloproteinases, inflammatory mediators, and endometrial matrix remodeling by 17beta-estradiol in the immature rat uterus. Reprod Biol Endocrinol. 2009 Nov 4;7:124.

http://www.ncbi.nlm.nih.gov/pubmed/19889233