MMP	Pseudonym	Substrates
1	Collagenase-1, interstitial C	1-Antichymotrypsin, types I, II, III, VII, and X collagen, gelatin, 1-proteinase inhibitor[13-17]
2	Gelatinase A	Denatured collagen, types IV and V collagen, elastin, fibronectin, gelatin, laminin, proteoglycan, pro-MMP-9, pro-MMP-13[18-21]
3	Stromelysin-1	1-Antichymotrypsin, carboxymethylated transferrin, type IV collagen, type I procollagen, fibronectin, gelatin, laminin, 1-proteinase inhibitor, proteoglycan, pro-MMP-1, pro-MMP-7, pro-MMP-9[17, 22-25, 27-30]
7	Matrilysin	Casein, type IV collagen, elastin, fibronectin, type I gelatin, laminin, nidogen, proteoglycan, pro-MMP-1, pro-MMP-9[11, 26, 27]
8	Collagenase-2, neutrophil C	Aggrecan, type I collagen, fibrinogen, gelatin[28, 29, 31]
9	Gelatinase B	Denatured collagen, types IV and V collagen, elastin, type I gelatin[19, 32-34]
10	Stromelysin-2	Carboxymethylated transferrin, casein, gelatin, pro-MMP-1, pro-MMP-7, pro-MMP-8, pro-MMP-9[30, 35]
11	Stromelysin-3	Not known
12	Macrophage metalloelastase	Apolipoprotein(a), factor XII, fibrinogen[31, 36]
13	Collagenase-3	1-Antichymotrypsin, types I, II, and III collagen, factor XII, fibrinogen, gelatin, plasminogen activator inhibitor-2[28, 29, 31, 37]
14	MT1-MMP	Aggrecan, types I, III, and III collagen, cassein, factor XII, fibronectin, fibrinogen, gelatin, laminin, 1-macroglobulin, nidogen, perlecan, 1-proteinase inhibitor, pro-MMP-2, pro-MMP-13, proteoglycan, large tenascin-C, pro-TNF-, vitronectin[11, 21, 27, 31, 38-40]
15	MT2-MMP	Aggrecan, fibronectin, laminin, nidogen, perlecan, large tenascin-C, pro-TNF-[11]
16	MT3-MMP	Pro-MMP-212
17	MT4-MMP	Fibrin, fibrinogen, gelatin, pro-MMP-2, pro-TNF-[41, 42]
18		Not known[43]
19		Casein, type IV collagen, fibrin, fibronectin, fibrinogen, gelatin, laminin, nidogen, large tenascin-C[44]
20	Enamelysin	Amelogenin[45]
21		Not known[46]
23		Not known[10]
24	MT5-MMP	Gelatin, pro-MMP-2[47, 48]
25	MT6-MMP, leukolysin	Type IV collagen, fibrin, fibronectin, gelatin, pro-MMP-2[49, 50]
26	Endometase, matrilysin-2	Type IV collagen, fibronectin, fibrinogen, type I gelatin, a1-proteinase inhibitor, pro-MMP-9[9, 51]
28	Epilysin	Casein[46, 52]

MMP = matrix metalloproteinase; MT = membrane-type; TNF = tumor necrosis factor.

Agent (route)	Dosage	Cmax (ng/ml)	Half-life (hrs)	PPB (%)	Vd/F (L)	Cl/F (ml/min)	Remarks
Batimastat    (i.p.)[110, 111]	150 mg/m2 1800 mg/m2	300 1570	349-743	96	0.7-5.4	0.00001-0.00012	Poorly solubility, not orally bioavailable
BAY 12-9566    (oral)[112, 113]	100 mg q.d. 400 mg q.d. 800 mg b.i.d.	50,000 50,000 160,000	60.7	99.99	--	--	Nonlinear pharmacokinetics (possibly due to saturable absorption)
BMS-275291    (oral)[114, 115]	600 mg/day 2400 mg/day	-	~24-50a	46-77	--	--	Linear pharmacokinetics up to 1200 and 2400 mg/day in healthy subjects and patients with cancer, respectively
Marimastat    (oral)[117, 123]	25 mg b.i.d. 50 mg b.i.d. 100 mg b.i.d.	184 196 540	3.7-11.3	--	66-444	1600-12633	Linear pharmacokinetics up to 200 mg (single dose) in healthy subjects
Metastat    (oral)[116]	36 mg/m2/day 70 mg/m2/day	1036 2465	23.7-144.4	94.5	490.9-2222.7b	81.8-668.1b	Linear pharmacokinetics up to 70 mg/m2/day; potential saturable absorption
MMI270(B)    (oral)[118, 119]	150 mg b.i.d. 600 mg b.i.d.	941.9 9155.9	1.6	--	383.8c	2771c	Linear pharmacokinetics up to 600 mg t.i.d.
Prinomastat    (oral)[120]	25 mg b.i.d.	513	2.0-3.0	69	91d	422d	Linear 100 mg b.i.d.

i.p. = intraperitoneal;C_max = maximum plasma concentration; PPB = plasma protein binding; V_d/F = apparent volume of distribution; Cl/F = apparent clearance.
^aBased on statement that steady state was achieved by day 15 in patients with cancer or day 7 in healthy subjects.^{[114, 115]} Calculated as time to reach steady state equals 7 times half-life.^[122]
bBased on 75-kg person. Both Cl_T/F (apparent total clearance) and Vd_pss/F (apparent pseudo-steady-state volume of distribution) are corrected for plasma protein binding.
^cBased on fasting The AUC_0-8 hr = 2422 ± 1246 ng·hr/ml at a dose of 400 mg.^[119] Estimated using Cl_T/F = dose/AUC_0- and Vdpss/F = (Cl_T/F)/k_e.^[122]
dBased on historical data of AG-3340 AUC = 987 ± 366 ng·hr/ml at a dose of 25 mg.^[120] Calculated using Cl_T/F = dose/AUC_0- and Vd_pss/F = (Cl_T/F)/k_e.^[122]