Lerozol® Tablet: Each film coated tablet contains Letrozole USP 2.5mg..
Letrozole is a nonsteroidal aromatase inhibitor. It exerts its antitumor effect by depriving estrogen-dependent breast cancer cells of their growth stimulus. It inhibits the conversion of androgens to estrogens. Letrozole inhibits the aromatase enzyme by competitively binding to the heme of the cytochrome P450 subunit of the enzyme, resulting in a reduction of estrogen biosynthesis in all tissues.
The recommended dose is one 2.5 mg tablet administered once a day, regardless to meals. In patients with advanced disease, treatment with Lerozol® should be continued until tumor progression is evident.
Treatment should be discontinued at tumor relapse.
No dose adjustment is required for elderly patients. Patients treated with Lerozol® do not require glucocorticoid or mineralocorticoid replacement therapy.
Renal Impairment:
No dosage adjustment is required for patients with renal impairment if creatinine clearance is 10 ml/min.
Hepatic Impairment:
No dosage adjustment is recommended for patients with mild to moderate hepatic impairment. The dose of Lerozole in patients with cirrhosis and severe hepatic dysfunction should be reduced by 50%. The recommended dose for such patients is 2.5 mg administered every other day. the effect of hepatic impairment of Lerozol® exposure in noncirrhotic cancer patients with elevated bilirubin levels has not been determined.
An interaction study with warfarin showed no clinically significant effect of letrozole on warfarin pharmacokinetics. In in-vitro experiments, Letrozole showed no significant inhibition in the metabolism of diazepam. Coadministration of Letrozole and tamoxifen 20 mg daily resulted in a reduction of letrozole plasma levels of 38% on average. Clinical experience in the second-line breast cancer pivotal trials indicates that the therapeutic effect of Letrozole therapy is not impaired if Letrozole is administered immediately after tamoxifen.
It is not known if Letrozole is exerted in human milk. Because many drugs are exerted in human milk, caution should be exercised when letrozole is administered to a nursing woman.
The safety and effectiveness in pediatric patients have not been established.
Since fatigue and dizziness have been observed with the use of letrozole and somnolence was uncommonly reported, caution is advised when driving or using machinery.
Store in a cool and dry place protected from light and moisture.
Lerozol® Tablet; Box containing 2 x 5 tablets in blister pack.