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. Author manuscript; available in PMC: 2023 Jun 2.
Published in final edited form as: Semin Cancer Biol. 2022 Dec 13;88:46–66. doi: 10.1016/j.semcancer.2022.12.002

Table 1.

Targeting extracellular matrix.

Drug/inhibitor Target Effectiveness Reference
Bivatuzumab CD44 Bivatuzumab can direct against CD44v6, blocking CD44-HA interaction [247,248]
RO5429083 CD44 A monoclonal CD44 antibody, block the interaction between CD44 and HA, which have been entered phase 1 clinical trial conducted among patients with CD44-expressing malignant tumors [249]
Verbascoside CD44 Verbascoside suppressed growth of glioblastoma cells by inhibiting CD44 dimerization, as well as suppress tumor stem cell formation [250]
7rh DDR1 Inhibition of DDR1 by 7rh reduces collagen-mediated tumorigenicity in pancreatic ductal adenocarcinoma [251]
WRG-28 DDR2 By targeting DDR2, WRG-28 can efficiently prevent disrupt DDR2 receptor-collagen ligand interaction and DDR- mediated tumor progression in preclinical models [252]
Imatinib, nilotinib and dasatinib DDR1 and DDR2 These 3 compounds are potent inhibitors of both DDR1 and DDR2 by inhibiting collagen- induced discoidin domain receptor 1 and 2 activation [253–255]
Fresolimumab Collagen An anti-TGF-β antibody, suppress TGF-β-regulated gene expression, decreases collagen synthesis, it is currently tested in a phase 1 clinical trial [256,257]
Losartan Collagen Losartan inhibits collagen I production via TGF-β pathways and improves the distribution and efficacy of nanotherapeuticsin tumors [258]
Simtuzumab LOXL2 Simtuzumab (GS-6624) is a selective inhibitor of LOXL2, which suppress LOXL2 enzymatic activity and inhibits collagen crosslinking, it is currently tested in a phase II clinical trial to test the efficacy and safety of GS-6624 combined with gemcitabine as first-line treatment for metastatic pancreatic adenocarcinoma [259,260]
(2-Chloropyridin-4- yl) methanamine hydrochloride LOXL2 (2-Chloropyridin-4-yl) methanamine hydrochloride is a small molecule inhibitor of LOXL2, it suppresses transformation abilities by repressing LOX2 induced EMT in cervical cancer [261]
CCT365623 LOX CCT365623 is a pharmacological inhibitor of LOX, it disrupts TGFβ1/ HTRA1/ MATN2/EGFR signaling axis and reduces tumor progression. [262]
Cilengitide αvβ3 and αvβ5 integrin Cilengitide is an inhibitor of αvβ3 and αvβ5 integrin, demonstrated modest antitumor activity among recurrent glioblastoma multiforme patients in a prior phase I study [263]
Curcumin αvβ3 integrin Curcumin is a natural derivative of turmeric, it influences αvβ3 integrin expression and up-regulation of PDK4 in Erlotinib resistant SW480 colon cancer cells [264]
Defactinib(VS-6063) FAK Defactinib is a FAK inhibitor which targets FAK catalytic activity, FAK is a key mediator of therapeutic resistance, it is a potential inhibitor to overcome adaptive resistance to chemotherapy, combinations with the other therapy drugs (such as Pembrolizumab; Paclitaxel and carboplatin; VS-6766) have been tested in the clinical trial phase I or II [265–267]
IN10018 FAK IN10018 is a highly selective oral inhibitor of FAK, it is currently tested in a phase Ib clinical trial to study of IN10018 in combination with pegylated liposomal doxorubicin in patients with platinum-resistant ovarian cancer [268]
GSK2256098 FAK GSK2256098 is an ATPcompetitive inhibitor that binds to the ATP-binding pocket of FAK, it is currently tested in a phase 1 clinical trial to study of GSK2256098 in patients with advanced solid tumors in the United Kingdom [269,270]
BI853520 FAK BI853520 is a highly selective ATP-competitive inhibitor of FAK, it is currently tested in a phase I clinical trial to study of BI853520 in patients with advanced or metastatic nonhematologic malignancies [271]