sirolimus (protein bound)

IV (Adults ): 100 mg/m² on Days 1 and 8 of each 21-day cycle; continue until disease progression or unacceptable toxicity. Concurrent use with moderate or weak CYP3A4 inhibitor: 56 mg/m² on Days 1 and 8 of each 21-day cycle; continue until disease progression or unacceptable toxicity.

Hepatic Impairment

IV (Adults ): Mild hepatic impairment (total bilirubin ≤upper limit of normal [ULN] with AST >ULN; or total bilirubin >1–1.5 times ULN with any AST: 75 mg/m² on Days 1 and 8 of each 21-day cycle; continue until disease progression or unacceptable toxicity. Moderate hepatic impairment (total bilirubin >1.5–3 times ULN with any AST): 56 mg/m² on Days 1 and 8 of each 21-day cycle; continue until disease progression or unacceptable toxicity.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as an inhibitor of mechanistic target of rapamycin kinase (mTOR), which reduces cell proliferation, angiogenesis, and glucose uptake. This formulation is bound to albumin, which may allow it to work differently and have a different side effect profile than other formulations of sirolimus.

Therapeutic effects:

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics, Immunosuppressant agents

Pharmacologic Classification: Mechanistic target of rapamycin kinase inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Unknown.

Protein Binding: >99%.

Metabolism/Excretion: Primarily metabolized in the liver via the CYP3A4 isoenzyme. 91% excreted in the feces and 2% in the urine.

Half-Life: 59 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
IV	rapid	end of infusion	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy.
Advise patient to discontinue sirolimus and notify health care professional immediately for symptoms of hypersensitivity (rash, difficulty breathing, flushing, chest pain, angioedema), severe bleeding or injury, ILD (shortness of breath), or serious infection.
Inform patient of the need to monitor labs frequently throughout therapy.
Inform patient to avoid live vaccines and contact with those who have received live vaccines during therapy.
Inform patient of ↑ risk of contracting infections during therapy.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Rep: May cause fetal harm. Advise women of reproductive potential to use effective contraception during therapy and for 12 wk after last dose. Advise patient not to breastfeed during therapy or for 2 wk after last dose and to notify health care professional if pregnancy is planned or suspected. May cause female and male infertility.