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Batimastat

Description of Batimastat: batimastat (BB-94) is a broad spectrum peptide inhibitor of MMPs. Batimastat (BB-94) has been shown to inhibit tumor growth and metastasis in mice. 

Current developer:   British Biotech.

Batimastat is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor (IC₅₀ values are 3, 4, 4, 6 and 20 nM for MMP -1, -2, -9, -7 and -3 respectively). Exhibits antiproliferative, anti-invasive and antimetastatic activity in human ovarian carcinoma xenografts in vivo.

1: van Beusekom HM, Post MJ, Whelan DM, de Smet BJ, Duncker DJ, van der Giessen WJ. Metalloproteinase inhibition by batimastat does not reduce neointimal thickening in stented atherosclerotic porcine femoral arteries. Cardiovasc Radiat Med. 2003 Oct-Dec;4(4):186-91. PubMed PMID: 15321056.

2: Björnsson MJ, Havemose-Poulsen A, Stoltze K, Holmstrup P. Influence of the matrix metalloproteinase inhibitor batimastat (BB-94) on periodontal bone destruction in Sprague-Dawley rats. J Periodontal Res. 2004 Aug;39(4):269-74. PubMed PMID: 15206921.

3: Rucavado A, Escalante T, Gutiérrez JM. Effect of the metalloproteinase inhibitor batimastat in the systemic toxicity induced by Bothrops asper snake venom: understanding the role of metalloproteinases in envenomation. Toxicon. 2004 Mar 15;43(4):417-24. PubMed PMID: 15051405.

4: Santucci MB, Ciaramella A, Mattei M, Sumerska T, Fraziano M. Batimastat reduces Mycobacterium tuberculosis-induced apoptosis in macrophages. Int Immunopharmacol. 2003 Nov;3(12):1657-65. PubMed PMID: 14555290.

5: Herget J, Novotna J, Bibova J, Povysilova V, Vankova M, Hampl V. Metalloproteinase inhibition by Batimastat attenuates pulmonary hypertension in chronically hypoxic rats. Am J Physiol Lung Cell Mol Physiol. 2003 Jul;285(1):L199-208. Epub 2003 Mar 28. PubMed PMID: 12665462.

6: Mirzaie M, Herse B, Oster O, Schöndube F. The matrix metalloproteinase inhibitor batimastat inhibits the lung colonisation of orthotopically implanted malignant pancreatic tumor cells in SCID mice. Swiss Surg. 2002;8(4):165-70. PubMed PMID: 12227109.

7: Eikesdal HP, Bjorkhaug ST, Dahl O. Hyperthermia exhibits anti-vascular activity in the s.c. BT4An rat glioma: lack of interaction with the angiogenesis inhibitor batimastat. Int J Hyperthermia. 2002 Mar-Apr;18(2):141-52. PubMed PMID: 11911484.

8: Holst-Hansen C, Low JA, Stephens RW, Johnson MD, Carmeliet P, Frandsen TL, Brünner N, Dickson RB. Increased stromal expression of murine urokinase plasminogen activator in a human breast cancer xenograft model following treatment with the matrix metalloprotease inhibitor, batimastat. Breast Cancer Res Treat. 2001 Aug;68(3):225-37. PubMed PMID: 11727959.

9: Corbel M, Lanchou J, Germain N, Malledant Y, Boichot E, Lagente V. Modulation of airway remodeling-associated mediators by the antifibrotic compound, pirfenidone, and the matrix metalloproteinase inhibitor, batimastat, during acute lung injury in mice. Eur J Pharmacol. 2001 Aug 24;426(1-2):113-21. PubMed PMID: 11525779.

10: Di Sebastiano P, di Mola FF, Artese L, Rossi C, Mascetta G, Pernthaler H, Innocenti P. Beneficial effects of Batimastat (BB-94), a matrix metalloproteinase inhibitor, in rat experimental colitis. Digestion. 2001;63(4):234-9. PubMed PMID: 11435723.

11: Rucavado A, Escalante T, Franceschi A, Chaves F, León G, Cury Y, Ovadia M, Gutiérrez JM. Inhibition of local hemorrhage and dermonecrosis induced by Bothrops asper snake venom: effectiveness of early in situ administration of the peptidomimetic metalloproteinase inhibitor batimastat and the chelating agent CaNa2EDTA. Am J Trop Med Hyg. 2000 Nov-Dec;63(5-6):313-9. PubMed PMID: 11421384.

12: Corbel M, Caulet-Maugendre S, Germain N, Molet S, Lagente V, Boichot E. Inhibition of bleomycin-induced pulmonary fibrosis in mice by the matrix metalloproteinase inhibitor batimastat. J Pathol. 2001 Apr;193(4):538-45. PubMed PMID: 11276015.

13: Krüger A, Soeltl R, Sopov I, Kopitz C, Arlt M, Magdolen V, Harbeck N, Gänsbacher B, Schmitt M. Hydroxamate-type matrix metalloproteinase inhibitor batimastat promotes liver metastasis. Cancer Res. 2001 Feb 15;61(4):1272-5. PubMed PMID: 11245418.