Androgen Receptor Inhibitor (Specialist Oncology Drug) Pregnancy: Contraindicated in women who are or may become pregnant. Based on an animal reproductive study and its mechanism of action, apalutamide may cause foetal harm and loss of pregnancy; there are no data in pregnant women. It is not known whether apalutamide or its metabolites are present in semen — patients having sex with female partners of reproductive potential should use a condom together with another highly effective contraceptive method during treatment and for 3 months after the last dose. Should not be used during breast-feeding. Based on animal studies, apalutamide may decrease fertility in males.

Apalutamide

Brand names: Erleada

Apalutamide is an oral androgen receptor inhibitor used in prostate cancer, including non-metastatic castration-resistant and metastatic hormone-sensitive disease, alongside androgen deprivation therapy.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 240 mg (one 240 mg tablet)

Route: Oral — the tablet should be swallowed whole, with or without food, and should not be crushed or split. For patients who cannot swallow it whole, the tablet may be dispersed in about 10 mL of non-fizzy water (wait 2 minutes, stir), then mixed with 30 mL of orange juice, green tea, applesauce, drinkable yogurt or additional water and swallowed immediately, rinsing the cup. It may also be given through a nasogastric tube 8 French or greater (place the whole tablet in a syringe of at least 20 mL with 10 mL non-fizzy water, wait 10 minutes, shake vigorously, administer immediately and flush).

Frequency: Once daily as a single daily dose

INITIATION: treatment should be initiated and supervised by a prescriber experienced in the treatment of prostate cancer. CONCOMITANT THERAPY: medical castration with a gonadotropin releasing hormone analogue (GnRHa) should be continued during treatment in patients who are not surgically castrated. MISSED DOSE: take as soon as possible on the same day and return to the normal schedule the following day; do not take extra tablets to make up a missed dose. TOXICITY: for Grade 3 or higher toxicity or an intolerable adverse reaction, HOLD dosing (rather than permanently discontinuing) until symptoms improve to Grade 1 or less or the original grade, then resume at the same dose or, if warranted, a reduced dose of 180 mg or 120 mg. ELDERLY: no dose adjustment necessary. HEPATIC: no adjustment for mild or moderate impairment (Child-Pugh A and B); for SEVERE hepatic impairment (Child-Pugh C) the recommended dose is 120 mg (two 60 mg tablets) orally once daily. PAEDIATRIC: there is no relevant use of apalutamide in the paediatric population.

Dose adjustments

Renal

No dose adjustment is necessary for mild to moderate renal impairment. Caution is required in severe renal impairment as apalutamide has not been studied in this population; if treatment is started, monitor for the adverse reactions listed in section 4.8 and dose reduce as per section 4.2.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

Hypersensitivity to the active substance or to any of the excipients
Women who are or may become pregnant

Side effects

Fatigue (26%)
Skin rash (26% any grade; 6% Grade 3 or 4)
Hypertension (22%) and hot flush (18%)
Arthralgia (17%) and fractures (11%)
Diarrhoea (16%)
Fall (13%) and weight decreased (13%)
Decreased appetite (11%) and hypothyroidism (8%); uncommon seizure; not known QT prolongation and agranulocytosis

Interactions

Strong CYP2C8 or CYP3A4 inhibitors — predicted to increase steady-state exposure of the active moieties; reduce the apalutamide dose as recommended for adverse reactions (US labelling)
Substrates of CYP3A4, CYP2C19, CYP2C9, P-gp, BCRP or OATP1B1 — apalutamide is a strong inducer of CYP3A4 and CYP2C19, a weak inducer of CYP2C9 and an inducer of P-gp, BCRP and OATP1B1, and decreases exposure of these substrates, which may cause loss of their effectiveness; consider alternative agents or evaluate for loss of activity (US labelling)
QT prolongation is listed as a not-known-frequency adverse reaction with cross-reference to UK SPC sections 4.4 and 4.5
NOTE: the fetched UK SPC extract did not include the full section 4.5 — the CYP entries come from the US prescribing information and should be checked against the UK SPC.

Clinical monograph

How it works

It binds the androgen receptor and inhibits androgen binding, receptor nuclear translocation, and DNA binding, thereby suppressing androgen-driven prostate cancer growth.

Prescribing in practice

Serious skin reactions, falls and fractures, and seizures are recognised risks, so assess fracture and seizure risk and counsel patients accordingly.
It is a strong enzyme inducer and has clinically important drug interactions, so review co-medications carefully.
Cardiovascular events and hypertension can occur and should be monitored.

Monitoring

Monitor for skin reactions, falls and fractures, seizures, cardiovascular events and blood pressure, and review concomitant medicines for interactions.

Counselling the patient

Report any severe rash, blistering, or skin peeling promptly.
Take care to reduce falls; report any blackout or seizure.
Tell pharmacists and doctors you take this drug, as it interacts with many medicines.

Evidence & guidelines

Use is supported by the SPARTAN and TITAN trials and relevant NICE guidance; consult the SPC for interactions and monitoring.

Reference: NICE TA585 (Apalutamide for non-metastatic castration-resistant prostate cancer, 2019); NICE TA740 (mCSPC, 2021); SPARTAN trial (NEJM 2018); TITAN trial (NEJM 2019); EAU Prostate Cancer Guidelines (2024); Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

Calculators

Pathways