Everolimus

AFINITOR

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Pronunciation: e-ver-OE-li-mus (a-FIN-it-or)

Everolimus ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Everolimus ballicule

Everolimus AFINITOR mascot mnemonic cartoon — Visual mnemonic: Everolimus mascot
**“Every lima’s A finisher”**

What it ismTOR inhibitor; transplant, renal and breast cancer, and tuberous sclerosis.

Why this oneIt is both an immunosuppressant and an antiproliferative, and it treats the tumors of tuberous sclerosis.

What limits itStomatitis is common and often dose-limiting. Non-infectious pneumonitis; hyperglycemia and hyperlipidemia.

Everolimus molecular structure (skeletal formula) — Molecular structure: Everolimus

FDA-approved for

cancer/transplant (2009)

FDA label

Read the full label on DailyMed ↗

FDA dosing	Population	Start	Target	Max
Renal cell carcinoma (RCC)	adult	10 mg QD	10 mg QD until progression/toxicity	10 mg QD
TSC-associated renal angiomyolipoma	adult	10 mg QD	10 mg QD until progression/toxicity	10 mg QD

Renal Undefined (monitor renal function before and periodically)

Hepatic Mild (Child-Pugh A) 7.5 mg QD (reduce to 5 mg if not tolerated); Moderate (B) 5 mg QD (reduce to 2.5 mg); Severe (C) 2.5 mg QD if benefit outweighs risk

Instructions

Swallow tablets whole; take consistently with or without food
Do not combine tablets and tablets for oral suspension to reach the dose
Start dexamethasone alcohol-free mouthwash for stomatitis prophylaxis
Withhold >=1 week before elective surgery

Available strengths

tab 0.25, 0.5, 0.75, 1, 2, 2.5, 3, 5, 7.5, 10 mg

Cautions

Non-infectious pneumonitis
Infections (may be serious/fatal)
Severe hypersensitivity reactions
Angioedema (increased risk with concomitant ACE inhibitors)
Stomatitis / oral ulceration
Renal failure
Impaired wound healing
Metabolic disorders (hyperglycemia, hyperlipidemia)
Myelosuppression
Radiation sensitization / recall
Embryo-fetal toxicity

Adverse reactions

Stomatitis
Infections
Rash
Fatigue / asthenia
Diarrhea
Edema
Abdominal pain, nausea
Fever, cough, headache, decreased appetite

Pregnancy Can cause fetal harm (animal data, mechanism); advise pregnant women of risk and use effective contraception.

Lactation Do not breastfeed during treatment and for 2 weeks after the last dose.

Cost

Everolimus (AFINITOR)

What pharmacies pay · NADAC 9/30/26

Strength		#/mo	generic $/mo	CostPlus
0.25 mg	tab	30 qd	$53.56	offered
0.5 mg	tab	30 qd	$105.74	offered
0.75 mg	tab	30 qd	$125.48	offered
1 mg	tab	30 qd	$157.59	offered
2 mg	tab	30 qd		offered
2.5 mg	tab	30 qd		offered
3 mg	tab	30 qd		not offered
5 mg	tab	30 qd	$443.12	offered
7.5 mg	tab	30 qd		offered
10 mg	tab	30 qd	$789.73	offered

Generic entry2018

⚠ BOXED WARNINGS

Immunosuppression, infection and lymphoma
Kidney graft thrombosis; nephrotoxicity with cyclosporine

No boxed warning for Afinitor, the oncology product, but Zortress, the transplant product carries a boxed warning for immunosuppression, infection and lymphoma, graft thrombosis and nephrotoxicity with cyclosporine.

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryD

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

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Memory aids: interaction avatars

CYP3A4 substrate

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