Skip to main content
. 2024 Apr 24;22:382. doi: 10.1186/s12967-024-05199-3

Table 4.

inhibitors and drugs targeting collagen modifications

Therapy target Name drug Drug format Disease Research stage
P4HA1 Diethyl-pythiDC Small molecule inhibitor Colorectal cancer Preclinical [131]
P4HA2 Aspirin Small molecule inhibitor Hepatocellular carcinoma Preclinical [132]
P4H EDHB Small molecule inhibitor Breast cancer Preclinical [160]
BMP1.3 Anti-BMP1.3 mAb Myocardial infarction Preclinical [134]
LOX

BAPN (β-aminopropionitrile)

PXS-5505

Irreversible inhibitor

Small molecule inhibitor

Cancer

Pancreatic cancer

Preclinical [139]

Preclinical [161]

LOXL2

Simtuzumab

GS341

mAb

pAb

Fibrosis, Cancer

Phase II [162]

Preclinical [135, 163]

LOXL2

PXS-S1A

PXS-S2A

PAT-1251

PXS-5382A

Epigallocatechin gallate (EGCG)

Small molecule inhibitors Fibrosis, heart failure, glaucoma, oncological and angiogenic diseases

Phase II [135]

Phase II [135]

Phase I [164, 165]

Phase I [135]

Phase I [166]

Copper

tetrathiomolybdate (TM)I

d-penicillamine (D-pen)

Copper chelators

Cancer

Breast cancer

Phase I/II [140, 141, 167]

Phase II [136, 168]

Dual LOX/LOXL

PXS-5153A

CCT365623

Inhibitor

Fibrosis

Cancer

Preclinical [169]

Preclinical [170, 171]

MMP9

MMP9

MMP14

MMP1,

MMP2,

MMP3

Andecaliximab (GS-5745)

AB0041, AB0046,

DX-2400

Single Chain Fragment Variables

mAb

mAb

mAb

mAb

Cancer,

Colorectal cancer

Breast, melanoma, sarcoma

Breast cancer

Phase III [172, 173]

Preclinical [144, 174]

Preclinical [175]

Preclinical [176]

PAD4

PAD4

PAD4

PAD4

TDFA

TDCA

Cl-amidine

F-amidine

GSK199,

GSK484

JBI-589

Selective

Irreversible small molecule inhibitors

Reversible inhibitors

Small molecule

Inflammatory disorders and

Cancer

Cancer

Preclinical [177]

Preclinical [178, 179]

Preclinical [177]

Preclinical [114]