Alestramustine

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A chemotherapeutic agent used in cancer treatment


Alestramustine
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Alestramustine is a chemotherapeutic agent that combines the properties of an alkylating agent and an estrogen. It is primarily used in the treatment of prostate cancer.

Mechanism of Action

Alestramustine is a prodrug that is metabolized into two active components: estradiol and normustine. The estradiol component acts as an estrogen, which can help in reducing the levels of testosterone, a hormone that can promote the growth of prostate cancer cells. The normustine component is an alkylating agent that works by damaging the DNA of cancer cells, thereby inhibiting their ability to divide and grow.

Pharmacokinetics

Upon administration, alestramustine is absorbed and metabolized in the body. The estradiol component is responsible for the hormonal effects, while the normustine component provides the cytotoxic effects. The drug is designed to target cancer cells more effectively by utilizing the affinity of estradiol for estrogen receptors, which are often overexpressed in certain types of cancer cells.

Clinical Use

Alestramustine is used in the treatment of hormone-sensitive prostate cancer. It is particularly useful in cases where other forms of hormone therapy have failed. The combination of hormonal and cytotoxic effects makes it a valuable option in the management of advanced prostate cancer.

Side Effects

The use of alestramustine can lead to several side effects, which are typical of both estrogenic and alkylating agents. Common side effects include:

More serious side effects can include:

Administration

Alestramustine is typically administered orally. The dosage and treatment regimen depend on the specific needs of the patient and the stage of the cancer.

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  • Alestramustine

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Contributors: Prab R. Tumpati, MD