Afinitor (Page 2 of 12)

2.10 Dosage Modifications for Hepatic Impairment

The recommended dosages of AFINITOR/AFINITOR DISPERZ for patients with hepatic impairment are described in Table 3 [see Use in Specific Populations (8.6)]:

Table 3: Recommended Dosage Modifications for Patients with Hepatic Impairment
Indication Dose Modification for AFINITOR/AFINITOR DISPERZ
Breast Cancer, NET, RCC, and TSC-Associated Renal Angiomyolipoma
  • Mild hepatic impairment (Child-Pugh class A) – 7.5 mg orally once daily; decrease the dose to 5 mg orally once daily if a dose of 7.5 mg once daily is not tolerated.
  • Moderate hepatic impairment (Child-Pugh class B) – 5 mg orally once daily; decrease the dose to 2.5 mg orally once daily if a dose of 5 mg once daily is not tolerated.
  • Severe hepatic impairment (Child-Pugh class C) – 2.5 mg orally once daily if the desired benefit outweighs the risk; do not exceed a dose of 2.5 mg once daily.
TSC-Associated SEGA and TSC-Associated Partial-Onset Seizures
  • Severe hepatic impairment (Child-Pugh class C) – 2.5 mg/m2 orally once daily.
  • Adjust dose based on everolimus trough concentrations as recommended [see Dosage and Administration (2.8)].

2.11 Dosage Modifications for P-gp and CYP3A4 Inhibitors

  • Avoid the concomitant use of P-gp and strong CYP3A4 inhibitors [see Drug Interactions (7.1)].
  • Avoid ingesting grapefruit and grapefruit juice.
  • Reduce the dose for patients taking AFINITOR/AFINITOR DISPERZ with a P-gp and moderate CYP3A4 inhibitor as recommended in Table 4 [see Drug Interactions (7.1), Clinical Pharmacology (12.3)].
Table 4: Recommended Dosage Modifications for Concurrent Use of AFINITOR/AFINITOR DISPERZ with a P-gp and Moderate CYP3A4 Inhibitor
Indication Dose Modification for AFINITOR/AFINITOR DISPERZ
Breast Cancer, NET, RCC, and TSC-Associated Renal Angiomyolipoma
  • Reduce dose to 2.5 mg once daily.
  • May increase dose to 5 mg once daily if tolerated.
  • Resume dose administered prior to inhibitor initiation, once the inhibitor is discontinued for 3 days.
TSC-Associated SEGA and TSC-Associated Partial-Onset Seizures
  • Reduce the daily dose by 50%.
  • Change to every other day dosing if the reduced dose is lower than the lowest available strength.
  • Resume dose administered prior to inhibitor initiation, once the inhibitor is discontinued for 3 days.
  • Assess trough concentrations when initiating and discontinuing the inhibitor [see Dosage and Administration (2.8)].

2.12 Dosage Modifications for P-gp and CYP3A4 Inducers

  • Avoid concomitant use of St. John’s Wort (Hypericum perforatum).
  • Increase the dose for patients taking AFINITOR/AFINITOR DISPERZ with a P-gp and strong CYP3A4 inducer as recommended in Table 5 [see Drug Interactions (7.1), Clinical Pharmacology (12.3)].
Table 5: Recommended Dosage Modifications for Concurrent Use of AFINITOR/AFINITOR DISPERZ with P-gp and Strong CYP3A4 Inducers
Indication Dose Modification for AFINITOR/AFINITOR DISPERZ
Breast Cancer, NET, RCC, and TSC-Associated Renal Angiomyolipoma
  • Avoid coadministration where alternatives exist.
  • If coadministration cannot be avoided, double the daily dose using increments of 5 mg or less. Multiple increments may be required.
  • Resume the dose administered prior to inducer initiation, once an inducer is discontinued for 5 days.
TSC-Associated SEGA and TSC-Associated Partial-Onset Seizures
  • Double the daily dose using increments of 5 mg or less. Multiple increments may be required.
  • Addition of another strong CYP3A4 inducer in a patient already receiving treatment with a strong CYP3A4 inducer may not require additional dosage modification.
  • Assess trough concentrations when initiating and discontinuing the inducer [see Dosage and Administration (2.8)].
  • Resume the dose administered before starting any inducer, once all inducers are discontinued for 5 days.

2.13 Administration and Preparation

  • Administer AFINITOR/AFINITOR DISPERZ at the same time each day.
  • Administer AFINITOR/AFINITOR DISPERZ consistently either with or without food [see Clinical Pharmacology (12.3)].
  • If a dose of AFINITOR/AFINITOR DISPERZ is missed, it can be administered up to 6 hours after the time it is normally administered. After more than 6 hours, the dose should be skipped for that day. The next day, AFINITOR/AFINITOR DISPERZ should be administered at its usual time. Double doses should not be administered to make up for the dose that was missed.

AFINITOR

  • AFINITOR should be swallowed whole with a glass of water. Do not break or crush tablets.

AFINITOR DISPERZ

  • Wear gloves to avoid possible contact with everolimus when preparing suspensions of AFINITOR DISPERZ for another person.
  • Administer as a suspension only.
  • Administer suspension immediately after preparation. Discard suspension if not administered within 60 minutes after preparation.
  • Prepare suspension in water only.

Using an Oral Syringe to Prepare Oral Suspension:

  • Place the prescribed dose into a 10-mL syringe. Do not exceed a total of 10 mg per syringe. If higher doses are required, prepare an additional syringe. Do not break or crush tablets.
  • Draw approximately 5 mL of water and 4 mL of air into the syringe.
  • Place the filled syringe into a container (tip up) for 3 minutes, until the tablets are in suspension.
  • Gently invert the syringe 5 times immediately prior to administration.
  • After administration of the prepared suspension, draw approximately 5 mL of water and 4 mL of air into the same syringe, and swirl the contents to suspend remaining particles. Administer the entire contents of the syringe.

Using a Small Drinking Glass to Prepare Oral Suspension:

  • Place the prescribed dose into a small drinking glass (maximum size 100 mL) containing approximately 25 mL of water. Do not exceed a total of 10 mg per glass. If higher doses are required, prepare an additional glass. Do not break or crush tablets.
  • Allow 3 minutes for suspension to occur.
  • Stir the contents gently with a spoon, immediately prior to drinking.
  • After administration of the prepared suspension, add 25 mL of water and stir with the same spoon to re-suspend remaining particles. Administer the entire contents of the glass.

3 DOSAGE FORMS AND STRENGTHS

AFINITOR

Tablets, white to slightly yellow and elongated with a bevelled edge:

  • 2.5 mg: engraved with “LCL” on one side and “NVR” on the other.
  • 5 mg: engraved with “5” on one side and “NVR” on the other.
  • 7.5 mg: engraved with “7P5” on one side and “NVR” on the other.
  • 10 mg: engraved with “UHE” on one side and “NVR” on the other.

AFINITOR DISPERZ

Tablets for oral suspension, white to slightly yellowish, round, and flat with a bevelled edge:

  • 2 mg: engraved with “D2” on one side and “NVR” on the other.
  • 3 mg: engraved with “D3” on one side and “NVR” on the other.
  • 5 mg: engraved with “D5” on one side and “NVR” on the other.

4 CONTRAINDICATIONS

AFINITOR/AFINITOR DISPERZ is contraindicated in patients with clinically significant hypersensitivity to everolimus or to other rapamycin derivatives [see Warnings and Precautions (5.3)].

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