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XTANDI, Astellas, and the flying star logo are
registered trademarks of Astellas Pharma Inc.
XTANDI Access ServicesSM is a component of
Astellas Access ServicesSM.
XTANDI® (enzalutamide) capsules is indicated for the treatment of patients with metastatic
castration-resistant prostate cancer who have previously received docetaxel.
Important Safety Information
Contraindications-XTANDI can cause fetal harm when administered to a pregnant woman
based on its mechanism of action. XTANDI is not indicated for use in women. XTANDI is
contraindicated in women who are or may become pregnant.
Warnings and Precautions-In the randomized clinical trial, seizure occurred in 0.9% of
patients on XTANDI. No patients on the placebo arm experienced seizure. Patients experiencing
a seizure were permanently discontinued from therapy. All seizures resolved. Patients with a
history of seizure, taking medications known to decrease the seizure threshold, or with other risk
factors for seizure were excluded from the clinical trial. Because of the risk of seizure associated
with XTANDI use, patients should be advised of the risk of engaging in any activity where
sudden loss of consciousness could cause serious harm to themselves or others.
Adverse Reactions-The most common adverse drug reactions (;5%) reported in patients receiving
XTANDI in the randomized clinical trial were asthenia/fatigue, back pain, diarrhea, arthralgia,
hot flush, peripheral edema, musculoskeletal pain, headache, upper respiratory infection, muscular
weakness, dizziness, insomnia, lower respiratory infection, spinal cord compression and cauda
equina syndrome, hematuria, paresthesia, anxiety, and hypertension. Grade 1-4 neutropenia
occurred in 15% of XTANDI patients (1% Grade 3-4) and in 6% on placebo (no Grade 3-4). Grade
1-4 elevations in bilirubin occurred in 3% of XTANDI patients and 2% on placebo. One percent of
XTANDI patients compared to 0.3% on placebo died from infections or sepsis. Falls or injuries related
to falls occurred in 4.6% of XTANDI patients vs 1.3% on placebo. Falls were not associated with loss
of consciousness or seizure. Fall-related injuries were more severe in XTANDI patients and included
non-pathologic fractures, joint injuries, and hematomas. Grade 1 or 2 hallucinations occurred in
1.6% of XTANDI patients and 0.3% on placebo, with the majority on opioid-containing medications
at the time of the event.
Drug Interactions-Effect of Other Drugs on XTANDI: Administration of strong CYP2C8
inhibitors can increase the plasma exposure to XTANDI. Co-administration of XTANDI with strong
CYP2C8 inhibitors should be avoided if possible. If co-administration of XTANDI cannot be avoided,
reduce the dose of XTANDI. Co-administration of XTANDI with strong or moderate CYP3A4 and
CYP2C8 inducers can alter the plasma exposure of XTANDI and should be avoided if possible.
Effect of XTANDI on Other Drugs: XTANDI is a strong CYP3A4 inducer and a moderate
CYP2C9 and CYP2C19 inducer in humans. Avoid CYP3A4, CYP2C9 and CYP2C19 substrates
with a narrow therapeutic index, as XTANDI may decrease the plasma exposures of these drugs.
If XTANDI is co-administered with warfarin (CYP2C9 substrate), conduct additional INR monitoring.