OncoPharm Apalutamide
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Feb 15, 2018 The discussion dives into the FDA approval of apalutamide for non-metastatic castrate-sensitive prostate cancer. It highlights its mechanism of action, dosing, and critical findings from the SPARTAN study. The potential drug interactions and side effects are also addressed, emphasizing the crucial role of pharmacists in monitoring patients. Additionally, updates from ASCO GU bring new insights into the use of DOACs in cancer treatment, adding further depth to the conversation.
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Apalutamide Mechanism And Dosing
- Apalutamide is a second-generation androgen receptor antagonist similar to enzalutamide that blocks androgen binding and receptor translocation.
- It is dosed 240 mg daily as four 60 mg tablets and taken with ongoing androgen-deprivation therapy.
Auto-Induction Alters Apalutamide PK
- Apalutamide reaches steady state in four weeks due to auto-induction despite a three-day half-life at steady state.
- Its major metabolic pathways are CYP2C8 and CYP3A4, roughly equally contributing to clearance.
Anticipate Broad Drug Interactions
- Expect major drug interactions because apalutamide is a potent CYP3A4 and CYP2C19 inducer and affects many common drugs.
- Monitor and adjust doses for statins, anticoagulants, antiplatelets, PPIs, and cardiovascular meds when patients start apalutamide.