Table 1.
List of pharmacological molecules targeting autotaxin and LPA receptors validated in preclinical animal models
| Targets | Drug names | Diseases | References |
|---|---|---|---|
| LPA1 receptor | AM966 | Idiopathic pulmonary fibrosis | Swaney et al. (2010) |
| LPA1 receptor | AM095 | Dermal fibrosis | Castelino et al. (2011) |
| Lung fibrosis | Swaney et al. (2011) | ||
| Kidney fibrosis | Swaney et al. (2011) | ||
| LPA1 receptor | LA‐01 | Rheumatoid arthritis | Miyabe et al. (2013) |
| LPA2 receptor | DBIBB | Asthma | Knowlden et al. (2016) |
| LPA2 receptor | GRI977143 | Resistance to radiation | Kiss et al. (2013) |
| LPA5 receptor | H2L‐5765411 | Thrombosis | Williams et al. (2009) |
| LPA1, LPA3 receptors | VPC‐12249 | Renal ischaemia–reperfusion | Okusa et al. (2003) |
| LPA1, LPA3 receptors | Ki16425 | Rheumatoid arthritis | Orosa et al. (2014) |
| Hydrocephalus | Yung et al. (2011) | ||
| Renal interstitial fibrosis | Pradere et al. (2007) | ||
| Cancer: | |||
| Breast cancer bone metastasis | Boucharaba et al. (2004) | ||
| Renal cell carcinoma | Su et al. (2013) | ||
| LPA1, LPA3 receptors | Debio 0719 | Osteoporosis | David et al. (2014) |
| Cancer: | |||
| Breast cancer liver metastasis | Marshall et al. (2012) | ||
| Breast cancer lung metastasis | Marshall et al. (2012) and | ||
| David et al. (2012) | |||
| Breast cancer bone metastasis | David et al. (2012) | ||
| LPA1, LPA3 receptors | Ki16198 | Cancer: | |
| Pancreatic cancer | Komachi et al. (2012) | ||
| Pancreatic cancer lung, liver and brain metastases | Komachi et al. (2012) | ||
| All LPA receptors and autotaxin | BrP‐LPA | Rheumatoid arthritis | Nikitopoulou et al. (2013) |
| Cancer: | |||
| Breast cancer | Zhang et al. (2009) | ||
| Glioma | Schleicher et al. (2011) | ||
| Autotaxin | VPC8a202 | Cancer: | |
| Breast cancer lung metastasis | Peyruchaud et al. (2013) | ||
| Autotaxin | ONO‐8430506 | Cancer: | |
| Breast cancer | Benesch et al. (2014) | ||
| Breast cancer lung metastasis | Benesch et al. (2014) | ||
| Autotaxin | PF‐8380 | Inflammation | Gierse et al. (2010) |
| Cancer: | |||
| Glioblastoma | Bhave et al. (2013) | ||
| Autotaxin | 4PBPA | Cancer: | |
| Melanoma lung metastasis | Gupte et al. (2011) | ||
| Autotaxin | S32826 | Glaucoma | Iyer et al. (2012) |
| Autotaxin | BMP‐22 | Cancer: | |
| Breast cancer bone metastasis | Leblanc et al. (2014) | ||
| Autotaxin | Gintonin | Cancer: | |
| Melanoma lung metastasis | Hwang et al. (2013) | ||
| Autotaxin | GWJ‐A‐23 | Idiopathic pulmonary fibrosis | Oikonomou et al. (2012) |
| Asthma | Park et al. (2013) |