Description
Composition
1 tablet contains:
active substance: letrozole 2.50 mg;
excipients (core): lactose monohydrate 20.0 mg; microcrystalline cellulose 61.45 mg; carboxymethyl starch sodium 4.0 mg; colloidal silicon dioxide 0.5 mg; magnesium stearate 1.5 mg;
excipients (casing): hypromellose 0.68 mg; macrogol 0.34 mg; talc 0.34 mg; titanium dioxide 0.34 mg; yellow iron oxide colouring 0.30 mg.
Description
Round, biconvex film-coated tablets, pale yellow to dark yellow in colour. The cross-sectional core of the tablet is white or almost white in colour.
Pharmacotherapeutic group:
Antineoplastic agent – estrogen synthesis inhibitor
Mechanism of action
Elimination of estrogen-stimulating effects is a major factor in achieving a tumour response when the growth of tumour tissue depends on the presence of estrogen.
After menopause, estrogens are mainly produced under the influence of the enzyme aromatase, which converts androgens synthesised by the adrenal glands, mainly androstendione and testosterone, into estrone (E1) and estradiol (E2). Inhibition of estrogen synthesis in peripheral tissues and malignant tumour tissues can therefore be achieved by inhibition of the aromatase enzyme.
Letrozole is a non-steroidal aromatase inhibitor, and has anti-estrogenic activity by selectively inhibiting aromatase through highly specific competitive binding to the heme subunit of this enzyme, cytochrome P450. It blocks estrogen synthesis in all tissues.
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