FASLODEX

Absorption: The single dose and multiple dose PK parameters for the 500 mg dosing regimen with an additional dose (AD) at Day 15 are reported in Table 11. The additional dose of FASLODEX given two weeks after the initial dose allows for steady state concentrations to be reached within the first month of dosing.

Table 11Summary of Fulvestrant Pharmacokinetic Parameters [gMean (CV%)] in Postmenopausal Advanced Breast Cancer Patients after Intramuscular Administration 500 mg + AD Dosing Regimen C...

The efficacy of FASLODEX 500 mg versus FASLODEX 250 mg was compared in CONFIRM. The efficacy of FASLODEX 250 mg was compared to 1 mg anastrozole in Studies 0020 and 0021. The efficacy of FASLODEX 500 mg was compared to 1 mg anastrozole in FALCON. The efficacy of FASLODEX 500 mg in combination with palbociclib 125 mg was compared to FASLODEX 500 mg plus placebo in PALOMA-3. The efficacy of FASLODEX 500 mg in combination with abemaciclib 150 mg was compared to FASLODEX 500 mg plus placebo in MONARCH 2. The efficacy of FASLODEX 500 mg in combination with ribociclib 600 mg was compared to FASLODEX...

The following adverse reactions are discussed in more detail in other sections of the labeling:

• Risk of Bleeding [see Warnings and Precautions (5.1) ]
• Increased Exposure in Patients with Hepatic Impairment [see Warnings and Precautions (5.2) ]
• Injection Site Reaction [see Warnings and Precautions (5.3) ]
• Embryo-Fetal Toxicity [see Warnings and Precautions (5.4) ]
• The most common adverse reactions occurring in ≥5% of patients receiving FASLODEX 500 mg were: injection site pain, nausea, ...

FASLODEX is contraindicated in patients with a known hypersensitivity to the drug or to any of its components. Hypersensitivity reactions, including urticaria and angioedema, have been reported in association with FASLODEX [see Adverse Reactions (6.2) ].

• Hypersensitivity. (4)

• Risk of Bleeding: Use with caution in patients with bleeding diatheses, thrombocytopenia, or anticoagulant use. (5.1)
• Increased Exposure in Patients with Hepatic Impairment: Use a 250 mg dose for patients with moderate hepatic impairment. ( 2.2 , 5.2 , 8.6 )
• Injection Site Reaction: Use caution while administering FASLODEX at the dorsogluteal injection site due to the proximity of the underlying sciatic nerve. (5.3)
• Embryo-Fetal Toxicity: Can cause fetal harm. Advise females of reproduct...

7 DRUG INTERACTIONS There are no known drug-drug interactions. Although, fulvestrant is metabolized by CYP 3A4 in vitro , drug interactions studies with ketoconazole or rifampin did not alter fulvestrant pharmacokinetics. Dose adjustment is not needed in patients co-prescribed CYP 3A4 inhibitors or inducers [see Clinical Pharmacology (12.3) ] .

• There are no known drug-drug interactions. (7)