Tasquinimod
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| Biological half-life | 40 ± 16 hours |
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| Formula | C20H17F3N2O4 |
| Molar mass | 406.355 g/mol |
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Tasquinimod (ABR-215050, CID 54682876) is an experimental drug currently being investigated for the treatment of solid tumors. Tasquinimod has been mostly studied in prostate cancer, but its mechanism of action suggests that it could be used to treat other cancers. Castration-resistant prostate cancer (CRPC), formerly called hormone-resistant or hormone-refractory prostate cancer, is prostate cancer that grows despite medical or surgical androgen deprivation therapy. Tasquinimod targets the tumor microenvironment and counteracts cancer development by inhibiting angiogenesis and metastasis and by modulating the immune system. It is now in phase III development, following successful phase II trial outcomes.
Collaborative studies by laboratories at Johns Hopkins School of Medicine and Active Biotech Research AB identified tasquinimod as the lead agent for developing a treatment for prostate cancer. Tasquinimod was one of several second-generation quinoline-3-carboxamide variants synthesized using the drug roquinimex as a starting point, and it performed well in pre-clinical studies of cancer models.
In April 2011, Ipsen and Active Biotech entered into a broad partnership for the co-development of tasquinimod for the treatment of cancer. Active Biotech granted Ipsen exclusive rights to commercialize tasquinimod worldwide, except in North and South America and Japan where Active Biotech retained all commercial and marketing rights.
Tasquinimod is a novel small-molecule inhibitor that targets the tumor microenvironment by controlling the accumulation and immunosuppressive, pro-angiogenic and pro-metastatic functions of regulatory myeloid cells (also called myeloid-derived suppressor cells). It binds to and inhibits the interactions of S100A9, an immunomodulatory protein that promotes tumor development, influences suppressive and pro-angiogenic cells in the tumor microenvironment, and participates in the establishment of pre-metastatic niches.
Tasquinimod may also target the tumor microenvironment by suppressing the tumor hypoxic response, in which genes involved in the adaptation and survival of cells during hypoxia are induced. Tasquinimod reduces tumor angiogenesis; but its anti-angiogenic effects do not appear to be linked to vascular endothelial growth factor (VEGF) neutralization or VEGF receptor tyrosine kinase inhibition.
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