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Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3, MMP-13 and MMP-9 with Kis of 0.05 nM, 0.3 nM, 0.03 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity[1][2][3][4]. | [Definition]
ChEBI: Prinomastat hydrochloride is a hydrochloride resulting from the formal reaction of equimolar amounts of prinomastat and hydrogen chloride. A selective inhibitor with of matrix metalloproteinases (MMPs) 2, 3, 9, 13, and 14. It has a role as a matrix metalloproteinase inhibitor, an antineoplastic agent and an EC 3.4.24.35 (gelatinase B) inhibitor. It contains a prinomastat(1+). | [in vivo]
In a human fibrosarcoma mouse model (HT1080), the mice are treated therapeutically for 14-16 days with 50 mg/kg/day ip daily starting day 3 to 6 after tumour inoculation. Prinomastat is well tolerated by the animals, and there are no signs of weight loss or other adverse effects. Prinomastat has good tumour growth inhibition, with a short T1/2 of 1.6 hours[1]. | [IC 50]
MMP-9: 5 nM (IC50); MMP-9: 0.26 nM (Ki); MMP-2: 0.05 nM (Ki); MMP-1: 79 nM (IC50); MMP-13: 6.3 nM (IC50); MMP-13: 0.3 nM (Ki); collagenases 3: 0.03 nM (Ki) | [References]
[1] S?rensen MD, et al. Cyclic phosphinamides and phosphonamides, novel series of potent matrix metalloproteinase inhibitors with antitumour activity. Bioorg Med Chem. 2003 Dec 1;11(24):5461-84. DOI:10.1016/j.bmc.2003.09.015
[2] Blavier L, et al. Stromelysin-1 (MMP-3) is a target and a regulator of Wnt1-induced epithelial-mesenchymal transition (EMT). Cancer Biol Ther. 2010 Jul 15;10(2):198-208. DOI:10.4161/cbt.10.2.12193
[3] Shalinsky DR, et al. Broad antitumor and antiangiogenic activities of AG3340, a potent and selective MMP inhibitor undergoing advanced oncology clinical trials. Ann N Y Acad Sci. 1999 Jun 30;878:236-70. DOI:10.1111/j.1749-6632.1999.tb07689.x
[4] Ozerdem U, et al. The effect of prinomastat (AG3340), a potent inhibitor of matrix metalloproteinases, on a subacute model of proliferative vitreoretinopathy. Curr Eye Res. 2000 Jun;20(6):447-53. PMID:10980656 |
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