Tasquinimod Looks Promising in Trials

Tasquinimod is a small molecule with anti angiogenic activity that interupts blood vessel formation in tumours and cuts off their blood supply. Current Phase 2 clinical trials look promising and demonstrate that Tasquinimod has significant anticancer activity and showed antimetastatic activity. Tasquinimod is active at very low doses and a dose of 1 mg daily was the maximum used in the trials. It has dose limiting toxcity above 1 mg daily so this is the maximum that can be safely used.

Molecular structure of Tasquinimod which is a quinoline carboxamide.

Tasquinimod is an analogue of the drug Roquinimex also known as Linomide. Roquinimex has immunostimulant actvity as well as anti angiogenic activity. It also inhibits TNF alpha production. It is deactivated by metabolic 4-hydroxylation, a process that is blocked by a trifluoromethyl group in Tasquinimod.

Molecular Structure of Roquinimex

The precise mechanism of action of Tasquinimod is not known but it does have anti angiogenic activity and stops the development of new vasculature to the tumours.

Tasquinimod  phase II clinical trial  in men with minimally symptomatic metastatic castrate-resistant prostate cancer. A randomized, double-blind, placebo-controlled phase II trial  was conducted in men assigned (at a ratio of two to one) to either oral once-daily tasquinimod (TASQ) 0.25 mg/d escalating to 1.0 mg/d over 4 weeks or placebo. The primary end point was the proportion of patients without disease progression at 6 months, or pain criteria, excluding prostate-specific antigen. Two hundred one men (134 assigned to TASQ; 67 to placebo) were evaluable, and baseline characteristics were well balanced. Six-month progression-free proportions for TASQ and placebo groups were 69% and 37%, respectively, and median progression-free survival (PFS) was 7.6 versus 3.3 months. TASQ significantly slowed progression and improved PFS in patients with metastatic CRPC with an acceptable AE profile.