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FARMACOCINETICA Y FARMACODINAMIA: Inhibidor esteroideo de la aromatasa, agente antineoplasico: El exemestano es un inactivador esteroideo de la aromatasa, irreversible, relacionado estructuralmente con el sustrato natural androstenediona. En mujeres posmenopausicas, los estrogenos se producen principalmente de la conversion de androgenos a estrogenos a traves de la enzima aromatasa en los tejidos perifericos. La privacion de estrogeno a traves de la inactivacion de la aromatasa es un tratamiento efectivo y selectivo para el cancer de mama dependiente de hormonas en mujeres posmenopausicas. En mujeres posmenopausicas, el exemestano redujo significativamente las concentraciones de estrogeno serico con una dosis inicial de 5 mg, y alcanzando la supresion maxima (> 90%) con dosis de 10-25 mg. En pacientes posmenopausicas con cancer de mama, tratadas con la dosis diaria de 25 mg, la aromatizacion completa del cuerpo se redujo en 98%. 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Se ha observado un ligero incremento en los niveles sericos de LH y FSH que no es dependiente de la dosis, aun con dosis bajas; este efecto es, sin embargo, el esperado para la clase farmacologica, y es probablemente el resultado de la retroalimentacion a nivel de la pituitaria, debido a la reduccion en los niveles de estrogeno que estimulan la secrecion de gonadotropinas en la pituitaria en mujeres posmenopausicas. 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