Home » Drug Information » FDA Approved Drugs » 2009
Medical Areas: Obstetrics/Gynecology (Women’s Health)
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Lysteda (tranexamic acid)
The following drug information is obtained from various newswires, published
medical journal articles, and medical conference presentations.
Company: Xanodyne Pharmaceuticals
Approval Status: Approved November 2009
Treatment Area: heavy menstrual bleeding
Lysteda is a non-hormonal antifibrinolytic drug. It works by stabilizing a protein that helps blood to clot.
Lysteda is specifically indicated for the treatment of cyclic heavy menstrual bleeding.
Lysteda is supplied as a tablet for oral administration. The recommended dose for women with normal renal function is two 650 mg tablets taken three times daily (3900 mg/day) for a maximum of 5 days during monthly menstruation. Lysteda may be administered without regard to meals. Tablets should be swallowed whole and not chewed or broken apart.
The FDA approval of Lysteda was based on one 3-cycle treatment and one 6-cycle treatment, randomized, double-blind, placebo-controlled studies. Heavy menstrual bleeding was defined as an average menstrual blood loss of > 80 mL. The primary outcome measure was menstrual blood loss (MBL), measured using the alkaline hematin method. The endpoint was change from baseline in MBL, calculated by subtracting the mean MBL during treatment from the mean pretreatment MBL.
Three-Cycle Treatment Study
This study compared the effects of two doses of Lysteda given daily for up to 5 days during each menstrual period versus placebo on MBL over a 3-cycle treatment duration. Of 294 evaluable subjects, 112 received Lysteda 1950 mg/day, 115 subjects received Lysteda 3900 mg/day and 67 subjects received placebo. MBL was statistically significantly reduced in patients treated with 3900 mg/day Lysteda compared to placebo (p<0.001). Lysteda also statistically significantly reduced limitations on social, leisure, and physical activities in the 3900 mg/day dose group compared to placebo (p <0.05).
Six-Cycle Treatment Study
This study compared the effects of Lysteda 3900 mg/day given daily for up to 5 days during each menstrual period versus placebo on MBL over a 6-cycle treatment duration. Data are from 187 evaluable subjects. MBL was statistically significantly reduced in patients treated with 3900 mg/day compared to placebo (p<0.001). Limitations on social, leisure, and physical activities were also statistically significantly reduced in the Lysteda group compared to placebo (p <0.05).
Adverse events associated with the use of Lysteda may include, but are not limited to, the following:
- Nasal and Sinus Symptoms
- Back pain
- Abdominal Pain
Mechanism of Action
Lysteda (tranexamic acid) is a synthetic lysine amino acid derivative, which diminishes the dissolution of hemostatic fibrin by plasmin. In the presence of tranexamic acid, the lysine receptor binding sites of plasmin for fibrin are occupied, preventing binding to fibrin monomers, thus preserving and stabilizing fibrin’s matrix structure.
The antifibrinolytic effects of tranexamic acid are mediated by reversible interactions at multiple binding sites within plasminogen. Native human plasminogen contains 4 to 5 lysine binding sites with low affinity for tranexamic acid (Kd = 750 umol/L) and 1 with high affinity (Kd = 1.1 umol/L). The high affinity lysine site of plasminogen is involved in its binding to fibrin. Saturation of the high affinity binding site with tranexamic acid displaces plasminogen from the surface of fibrin. Although plasmin may be formed by conformational changes in plasminogen, its binding to and dissolution of the fibrin matrix is inhibited.
For additional information regarding Lysteda or heavy menstrual bleeding, please visit the Lysteda web page.