Formulary
Apalutamide: Indications, Dosing, Side Effects and Interactions
Apalutamide is an androgen receptor inhibitor that decreases tumour cell proliferation and increases apoptosis.
MedNext Academy | 3 min read
Apalutamide: Indications, Dosing, Side Effects and Interactions
Apalutamide is an androgen receptor inhibitor that decreases tumour cell proliferation and increases apoptosis.
Drug action
Apalutamide is an androgen receptor inhibitor that decreases tumour cell proliferation and increases apoptosis.
Indications and dose
**Prostate cancer (specialist use only)**
- **Adult** (By Mouth): 240 mg once daily, for dose adjustments due to side-effects-consult product literature.
Cautions
History or risk of QT-interval prolongation; recent cardiovascular disease
Contraindications
History or risk of seizures
Side effects
Common or very common Acute coronary syndrome; alopecia; appetite decreased; arteriosclerosis; arthralgia; autoimmune thyroiditis; bone fractures; cardiovascular insufficiency; cerebrovascular insufficiency; conjunctivitis; costal cartilage fracture; diarrhoea; dyslipidaemia; fall; fatigue; genital rash; hemiparesis; hot flush; hypertension; hypothyroidism; ischaemic heart disease; muscle spasms; oral disorders; rash pustular; sacrum fracture; skin reactions; taste altered; weight decreased Uncommon Seizure (discontinue permanently); tongue biting Frequency not known QT interval prolongation; severe cutaneous adverse reactions (SCARs)
Interactions
**Other interactions (29):**
- The elimination of apalutamide and formation of its active metabolite, Ndesmethyl apalutamide, is mediated by both CYP2C8 and CYP3A4 to a similar extent at steady-state.
- Apalutamide is an inducer of enzymes and transporters and may lead to an increase in elimination of many commonly used medicinal products.
- Potential for other medicinal products to affect apalutamide exposures Medicinal products that inhibit CYP2C8 CYP2C8 plays a role in the elimination of apalutamide and in the formation of its active...
- In a drugdrug interaction study, the C max of apalutamide decreased by 21% while AUC increased by 68% following coadministration of apalutamide 240 mg single dose with gemfibrozil (strong CYP2C8...
- For the active moieties (sum of apalutamide plus the potency adjusted active metabolite), C max decreased by 21% while AUC increased by 45%.
- No initial dose adjustment is necessary when Erleada is coadministered with a strong inhibitor of CYP2C8 (e.g., gemfibrozil, clopidogrel) however, a reduction of the Erleada dose based on...
Hepatic impairment
Manufacturer advises avoid in severe impairment (no information available).
Renal impairment
Manufacturer advises caution in severe impairment (no information available).
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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