Positive Results Reported for Novel Anticoagulant Drug

Pharmacokinetics of tecarfarin were not compromised by renal function like it was with warfarin.

Armetheon, Inc recently announced positive phase 1 results for its anticoagulation drug tecarfarin versus the standard treatment, warfarin.

Armetheon is a specialty pharmacy company that creates small molecule drugs to treat various cardiovascular diseases. Investigators in the clinical trial analyzed the effect of severe chronic kidney disease on the pharmacokinetics of tecarfarin and warfarin.

The pharmacokinetics, renal clearance and plasma half-life of tecarfarin was not seen to be compromised by renal impairment, according to a press release from Armetheon. However, investigators found that renal clearance was reduced, and an increased half-life was seen with warfarin.

Although warfarin is the standard anticoagulation treatment, a large number of patients have poorly controlled symptoms because of the drug, according to Armetheon. Findings suggest that the reason behind this phenomenon is because the drug can be affected greatly by renal function.

Other studies suggest that warfarin is the most commonly prescribed anticoagulant for patients with atrial fibrillation and venous thromboembolism, despite the availability of novel drugs. Warfarin is also known to interact with other medications, and even food.

Armetheon plans to enroll patients with chronic kidney disease (CKD) in an upcoming phase 3 trial called Tecarfarin for AntiCoagulation Trial (TACT). TACT is expected to enroll 3000 patients with any indication for the drug, according to the press release.

“For patients with chronic kidney disease, anticoagulation is a challenge, and warfarin is still widely used. Unfortunately, kidney disease complicates management with warfarin, and these patients tend to have more unstable anticoagulation with warfarin, which increases risk of stroke and bleeding,” said researcher Mintu Turakhia, MD, MAS. “The current study provides clear pharmacological evidence why warfarin works poorly in the presence of kidney disease, while tecarfarin was not really affected. This could have huge promise for the many patients with advanced kidney disease that presently do not have good treatment options.”

The phase 1 trial was designed to evaluate safety, tolerability, and pharmacokinetics of both drugs in 12 patients with stage 4 and 10 CKD, according to the press release. Patients with CKD were matched to 10 healthy patients.

“We are greatly encouraged by the results of this phase 1 study in CKD patients, which suggest that tecarfarin holds promise as an improved option for anticoagulation in these patients,” said Detlef Albrecht, MD, Armetheon’s chief medical officer and head of drug development. “The safety and pharmacokinetics findings support the broadening of our enrollment plan for TACT to include patients with severe renal impairment, which represent a growing subgroup among anticoagulated patients and who are often excluded from pivotal phase 3 cardiovascular studies of novel anticoagulant therapies.”