TABLE 1.

Drugs targeting SDC-1 or SDC-1-related proteins.

Target	Drug name	Chemical type	Mechanism of action	Effect	Cancer	References
SDC-1	Zoledronic acid	Resembles endogenous pyrophosphate	Disruption of SDC-1/integrins cross-talk	Inhibition of SDC-1 and ανβ3 integrin protein expression	Myeloma cells; breast cancer	Dedes et al. (2012)
	Nimesulide	Non-steroidal anti-inflammatory drug	Inhibition of SDC-1 expression	Inhibition of cell migration	Primary effusion lymphoma	George Paul et al. (2011)
	Indatuximab ravtansine (BT062-DM4)	Antibody-drug conjugate to cytotoxic agent (DM4)	Cytotoxic action in the target cell	Specific SDC-1+ cell death; inhibition of tumor cell growth and proliferation	Multiple myeloma	Schönfeld et al. (2017), Jagannath et al. (2019)
	OC-46F2	Recombinant antibody	Inhibition of SDC-1/VEGFR2 interaction	Inhibition of vascular maturation and tumor growth	Malignant melanoma and ovarian cancer	Orecchia et al. (2013)
	(CDB-HepII) polypeptide	Polypeptide	Reduction in αVβ3 integrin and SDC-1, interaction	Inhibition of pulmonary metastasis	Melanoma	Gong et al. (2008)
	Synstatin	Peptide	Competition with SDC-1 to bind receptors	Blockage of the SDC-1 core protein active site; suppression of the EGFR/α6β4 integrin complex; inhibition of angiogenesis	Multiple myeloma; mammary tumors	Beauvais et al. (2009), Rapraeger (2013), Rapraeger et al. (2013), Gao et al. (2021)
Shed SDC-1	Batimastat (BB-94)	Small molecule	MMP inhibition	Inhibition of SDC-1 shedding; prevention of tumor progression	Breast, ovarian, and colorectal cancer	Macaulay et al. (1999)
	NCS 405020	Small molecule	Inhibit the homodimerization of MT1-MMP	Reduction in SDC-1 shedding; suppression of tumor growth and invasion	Breast cancer	Remacle et al. (2012)
	All-trans retinoic acid (A-TRA)	Micronutrient	-	Reduction in SDC-1 shedding; inhibition of cancer invasion/metastasis	Lung	Ramya et al. (2012)
	Tranexamic acid	Synthetic lysine analogue	Inhibition of serine protease	Reduction in SDC-1 shedding; prevention of cancer metastasis	-	Diebel et al. (2018)
	Antithrombin III	Protein	-	Prevention of SDC-1 shedding; inhibition of metastasis	-	Lopez et al. (2020)
Heparan Sulfate	Heparin	Anticoagulant drug	Inhibition of heparanase activity	Hampering VEGF and FGF-2 activity, anti-angiogenesis	Myeloma	Casu et al. (2007)
	SST0001	Modified heparin	Inhibition of heparanase	Inhibition of HGF, VEGF, and anti-angiogenesis	Human pediatric sarcoma models	Cassinelli et al. (2013)
	M402	Modified heparin	Inhibition of heparanase	Anti-angiogenesis; inhibition of metastasis	Melanoma	Zhou et al. (2011), Kaur et al. (2021)
	9E8, H1023	Heparanase-neutralizing monoclonal antibodies	Neutralization of heparanase enzymatic activity	Inhibition of metastasis	Lymphoma	Weissmann et al. (2016)
	PG545	Sulfated synthetic tetrasaccharide	Inhibition of heparanase	Suppression of proliferation and migration	Ovarian cancer	Winterhoff et al. (2015)
	Suramin	Polysulfonated naphthylurea-based small molecule	Suppression of the activity of heparinase activity	Inhibition of caspase-3/8/9 activity; inhibition of FGF-2; suppression of both intrinsic and extrinsic apoptotic pathways	Hepatocellular carcinoma	Tayel et al. (2014)
	PI-88	Sulfated oligosaccharide	Inhibition of heparanase activity	Prevention of cancer recurrence and metastasis of cancer	Hepatocellular carcinoma	Liao et al. (2016)
	4-MMI	Triazolo–thiadiazole compounds	Inhibition of heparanase activity	Prevention of carcinoma cell invasion and metastasis; downregulation of VEGF expression	Glioma; breast cancer; myeloma	Barash et al. (2021)