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Apalutamide: Mechanism, Dosage & Side Effects

Apalutamide is a medication used to treat prostate cancer. It blocks androgen receptors, inhibiting tumor growth, and is used in non-metastatic and metastatic castration-resistant prostate cancer.

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Things worth knowing about "Apalutamide"

Apalutamide is a medication used to treat prostate cancer. It blocks androgen receptors, inhibiting tumor growth, and is used in non-metastatic and metastatic castration-resistant prostate cancer.

What is Apalutamide?

Apalutamide is a second-generation androgen receptor inhibitor used in the treatment of prostate cancer. It belongs to the class of non-steroidal antiandrogens and has been approved by both the European Medicines Agency (EMA) and the US Food and Drug Administration (FDA). It is marketed under the brand name Erleada®.

Indications

Apalutamide is approved for the treatment of:

Non-metastatic castration-resistant prostate cancer (nmCRPC): Prostate cancer that continues to progress despite hormone therapy (castration) and has not yet spread to distant organs.
Metastatic castration-resistant prostate cancer (mCRPC): Prostate cancer that progresses despite hormone therapy and has already formed metastases, used in combination with androgen deprivation therapy (ADT).
Metastatic hormone-sensitive prostate cancer (mHSPC): First-line therapy in combination with androgen deprivation therapy.

Mechanism of Action

Apalutamide selectively binds with high affinity to the androgen receptor (AR), blocking multiple steps in the signaling pathway that drives tumor growth:

Inhibition of androgen binding (male sex hormones such as testosterone and dihydrotestosterone) to the receptor
Prevention of nuclear translocation of the androgen receptor
Blockade of DNA binding and transcription of androgen-dependent genes

This multi-step inhibition significantly slows or halts the proliferation of prostate cancer cells. Compared to older antiandrogens, apalutamide has a substantially higher binding affinity for the androgen receptor.

Dosage and Administration

Apalutamide is typically administered as an oral tablet at a daily dose of 240 mg (four 60 mg tablets). It can be taken with or without food. Treatment is usually combined with androgen deprivation therapy (ADT) to suppress testosterone production. Dose reductions may be considered in the event of adverse effects, under medical supervision.

Side Effects

Like all medications, apalutamide can cause side effects. The most common include:

Skin rash (very common, affecting a large proportion of patients)
Fatigue and exhaustion
Hypertension (high blood pressure)
Weight loss and decreased appetite
Joint pain (arthralgia)
Bone fragility and increased risk of fractures
Thyroid disorders (hypothyroidism)
Seizures (rare but a significant risk factor)

Patients with a history of seizures should use apalutamide only with particular caution and under close medical supervision.

Drug Interactions

Apalutamide is a potent inducer of the enzyme CYP3A4 and a moderate inducer of CYP2C19. This means it can accelerate the metabolism of many other medications in the body, reducing their efficacy. Affected substances include:

Certain anticoagulants (blood thinners)
Statins for cholesterol reduction
Certain antibiotics and antifungal agents
Other cancer medications

A thorough review of all medications being taken by the treating physician is essential before starting therapy.

Clinical Studies

The approval of apalutamide is based on the results of several large clinical trials:

SPARTAN Study: Demonstrated a significant improvement in metastasis-free survival in nmCRPC.
TITAN Study: Demonstrated improved overall survival in metastatic hormone-sensitive prostate cancer (mHSPC) in combination with ADT.

References

European Medicines Agency (EMA): Erleada (Apalutamide) - Summary of Product Characteristics. EMA, 2018. Available at: www.ema.europa.eu
Smith MR et al. - Apalutamide Treatment and Metastasis-free Survival in Prostate Cancer. New England Journal of Medicine, 2018; 378(15):1408-1418.
Chi KN et al. - Apalutamide for Metastatic, Castration-Sensitive Prostate Cancer. New England Journal of Medicine, 2019; 381(1):13-24.

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