Head-to-head clinical analysis & difference comparison: details on mechanism of action, dosing, half-life, interactions, and maternal-fetal safety.
AFINITOR vs AFINITOR DISPERZ
Clinician-reviewed, head-to-head comparison of mechanism, dosing, pharmacokinetics, and safety profiles.
Last clinically reviewed: July 2026 · OpiCalc Medical Review Team
Inhibitor of mammalian target of rapamycin (m TOR), specifically the m TORC1 complex, by binding to the FKBP-12 protein, reducing cell proliferation, angiogenesis, and glucose uptake.
Everolimus is an m TOR inhibitor that binds to FKBP-12, forming a complex that inhibits the m TOR serine-threonine kinase, thereby blocking cell cycle progression, angiogenesis, and cell growth.
Advanced hormone receptor-positive, HER2-negative breast cancer in postmenopausal women in combination with exemestane after failure of letrozole or anastrozole,Progressive neuroendocrine tumors of pancreatic origin (PNET) in unresectable, locally advanced or metastatic disease,Advanced renal cell carcinoma (RCC) after failure of sunitinib or sorafenib,Subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosis complex (TSC) in patients requiring therapeutic intervention but not amenable to curative resection
Advanced hormone receptor-positive, HER2-negative breast cancer (postmenopausal women, in combination with exemestane),Advanced neuroendocrine tumors of pancreatic origin (unresectable, locally advanced, or metastatic),Advanced neuroendocrine tumors of gastrointestinal or lung origin (unresectable, locally advanced, or metastatic),Renal angiomyolipoma and tuberous sclerosis complex (TSC) not requiring immediate surgery,Subependymal giant cell astrocytoma (SEGA) associated with TSC,Renal cell carcinoma (advanced, after failure of sunitinib or sorafenib),Prevention of organ rejection in renal and cardiac transplant recipients (off-label: liver transplant)
10 mg orally once daily for advanced breast cancer, neuroendocrine tumors, and renal cell carcinoma; 10 mg orally once daily for subependymal giant cell astrocytoma (SEGA) in adults; 5 mg/m^2 orally once daily for SEGA in pediatric patients (titrated to trough levels 5-15 ng/m L).
10 mg orally once daily for advanced hormone receptor-positive, HER2-negative breast cancer; 10 mg orally once daily for advanced pancreatic neuroendocrine tumors; 10 mg orally once daily for advanced renal cell carcinoma; 7.5 mg orally once daily for subependymal giant cell astrocytoma (SEGA); 5 mg orally once daily for tuberous sclerosis complex (TSC)-associated renal angiomyolipoma.
Terminal elimination half-life: 30 hours (range 15–40 hours) in healthy subjects; increases to 40–70 hours in moderate hepatic impairment.
Terminal half-life is approximately 30 hours (range 28-35 hours) in patients with advanced solid tumors, supporting once-daily dosing.
Substrate of CYP3A4; metabolized primarily by CYP3A4; also a substrate of P-glycoprotein (P-gp).
Everolimus is metabolized primarily by CYP3A4 and is a substrate of P-glycoprotein (P-gp). It is also a moderate inhibitor of CYP3A4 and P-gp.
Primarily fecal (80%) and renal (5%) as unchanged drug and metabolites. Biliary excretion is significant.
Primarily fecal (80%) with 22% as unchanged drug; renal excretion <5%.
74% bound to plasma proteins (primarily albumin and α1-acid glycoprotein).
Approximately 74% bound to plasma proteins (mainly albumin).
Mean steady-state Vd: 342 L (approx. 4.9 L/kg in a 70 kg adult), indicating extensive tissue distribution.
Mean apparent volume of distribution is 47 L (approximately 0.6 L/kg), indicating extensive tissue distribution.
Oral bioavailability: approximately 16% (low due to P-glycoprotein efflux and first-pass metabolism); food reduces variability but does not alter AUC significantly.
Absolute bioavailability of the tablet formulation is approximately 16% after a high-fat meal; dispersible tablet bioavailability is comparable when taken with food.
No dose adjustment for mild to moderate renal impairment (Cr Cl >=30 m L/min). For severe renal impairment (Cr Cl <30 m L/min): reduce dose to 5 mg once daily. End-stage renal disease (Cr Cl <15 m L/min): use with caution, no specific recommendation.
For Cr Cl 30-50 m L/min: no adjustment required. For Cr Cl <30 m L/min: contraindicated or not recommended due to lack of data. No specific GFR-based dose reduction recommended.
Child-Pugh A: no adjustment; Child-Pugh B: reduce dose to 5 mg daily; Child-Pugh C: reduce dose to 2.5 mg daily, or consider alternate therapy.
Child-Pugh A: reduce dose to 7.5 mg daily. Child-Pugh B: reduce dose to 5 mg daily. Child-Pugh C: contraindicated.
For SEGA: 5 mg/m^2 orally once daily, adjusted to achieve everolimus trough concentrations of 5-15 ng/m L. Dose adjustments per AUC or tolerability. Not approved for other indications in children.
For SEGA in TSC: weight-based dosing targeting AUC similar to adult 10 mg/day. Initial dose 2.5 mg/m² once daily, titrate to trough concentration 5-15 ng/m L. For TSC-associated renal angiomyolipoma: not established in pediatric patients.
No specific dose adjustment; start at recommended adult dose. Monitor for increased risk of infections, stomatitis, and metabolic effects due to age-related decline in organ function.
No specific dose adjustment required based on age alone; monitor renal function and dose adjust per renal/hepatic status. Elderly patients may have increased risk of adverse effects such as stomatitis, infections, and metabolic disturbances.
No black box warnings.
There is no FDA black box warning for Afinitor Disperz. However, serious infections, including opportunistic infections, may occur.
Non-infectious pneumonitis,Infections (including opportunistic infections),Hypersensitivity reactions including anaphylaxis,Angioedema,Renal failure,Impaired wound healing,Metabolic effects (hyperglycemia, dyslipidemia),Myelosuppression,Immunosuppression leading to increased risk of infections,Cases of fatal hemorrhage in patients with history of bleeding,Radiation sensitization and recall reactions, especially in patients with previous radiation therapy,Increased risk of pneumocystis jirovecii pneumonia (PJP) and other opportunistic infections; consider prophylaxis,Avoid live vaccines
Non-infectious pneumonitis (including interstitial lung disease) has been reported; monitor for symptoms and consider interruption or discontinuation.,Increased risk of infections, including opportunistic infections (e.g., Pneumocystis jirovecii, TB); monitor and treat promptly.,Increased serum creatinine and proteinuria may occur; monitor renal function.,Angioedema, including life-threatening cases, can occur, especially in patients taking ACE inhibitors.,Stomatitis and mouth ulcers are common; manage with topical treatments and dose modification.,Impaired wound healing; use with caution perioperatively.,Increased risk of bleeding, especially in patients with renal angiomyolipoma and TSC.,Fetal harm can occur; advise effective contraception during treatment.
Hypersensitivity to everolimus, sirolimus, or any component of the formulation
Hypersensitivity to everolimus, sirolimus, or any component of the formulation,Severe hepatic impairment (Child-Pugh class C) (relative contraindication; use with caution in moderate impairment)
Avoid grapefruit, grapefruit juice, and Seville oranges (including marmalade) due to CYP3A4 inhibition increasing everolimus levels. Take consistently with or without food, but high-fat meals reduce absorption. Avoid St. John's wort.
Avoid grapefruit, grapefruit juice, and Seville oranges due to CYP3A4 inhibition. Avoid high-fat meals, as they reduce absorption; take on empty stomach or with light fat-free meal. St. John's wort reduces everolimus levels and should be avoided.
Pregnancy Category D. Positive evidence of human fetal risk. Based on its mechanism of action (m TOR inhibitor) and animal studies, AFINITOR (everolimus) is embryotoxic and fetotoxic. First trimester exposure carries risk of structural anomalies; second and third trimester exposure may cause fetal growth restriction, oligohydramnios, and renal impairment. Use only if benefit outweighs risk.
Pregnancy Category D. Animal studies show embryotoxicity and fetotoxicity at subtherapeutic doses. First trimester: risk of major malformations. Second/third trimester: risk of fetal growth restriction, oligohydramnios, and spontaneous abortion.
No data on presence in human milk, effects on breastfed infant, or milk production. M/P ratio unknown. Breastfeeding is not recommended due to potential adverse effects on the developing immune system and growth.
No data on excretion in human milk; M/P ratio unknown. Due to potential serious adverse reactions in nursing infants (e.g., immunosuppression), breastfeeding is contraindicated during treatment and for 2 weeks after last dose.
No specific dose adjustments established for pregnancy. Pharmacokinetic changes in pregnancy (increased volume of distribution, altered hepatic metabolism) may reduce drug exposure; however, given the teratogenic risk, use during pregnancy should be avoided. If unavoidable, consider therapeutic drug monitoring if available and adjust dose to achieve target trough concentrations (typically 3-8 ng/m L for transplant indications; for oncology, refer to specific protocol).
No specific dose adjustments established for pregnancy. Pharmacokinetic changes (increased volume of distribution, altered metabolism) may reduce exposure; however, due to teratogenicity, use is not recommended unless benefit outweighs risk. Dose adjustments based on therapeutic drug monitoring are not validated.
Monitor renal function and blood glucose regularly; Afinitor (everolimus) can cause non-infectious pneumonitis, so obtain baseline chest imaging and assess for new or worsening respiratory symptoms. Adjust dose for moderate hepatic impairment (Child-Pugh B). Avoid live vaccines during treatment.
AFINITOR DISPERZ (everolimus) is an m TOR inhibitor; tablets for oral suspension are not interchangeable with regular tablets due to different pharmacokinetics. Monitor for non-infectious pneumonitis, rash, stomatitis, metabolic effects (hyperglycemia, hyperlipidemia), and renal impairment. Dose adjustments required for hepatic impairment and concurrent strong CYP3A4/P-gp inhibitors or inducers. Avoid live vaccines during treatment.
Take Afinitor at the same time each day, consistently either with or without food.,Avoid grapefruit, grapefruit juice, and Seville oranges during treatment.,Report any new or worsening cough, chest pain, or difficulty breathing immediately.,Monitor for signs of infection such as fever, chills, or sore throat; avoid large crowds and sick individuals.,Use effective contraception during treatment and for 8 weeks after stopping.,Do not crush or chew tablets; swallow whole with a glass of water.
Take exactly as prescribed; do not crush or chew tablets for oral suspension.,Mix dose with water only, do not mix with juice or other liquids.,Avoid grapefruit, grapefruit juice, and Seville oranges during treatment.,Report any new or worsening shortness of breath, cough, or chest pain immediately.,Use effective non-hormonal contraception during and for 8 weeks after last dose.,Avoid live vaccines and close contact with recently vaccinated individuals.,Monitor for mouth sores; use alcohol-free mouthwash and soft toothbrush.,Do not take St. John's wort or strong CYP3A4/P-gp inhibitors/inducers without consulting doctor.
No interactions on record
No interactions on record
Common clinical questions about AFINITOR vs AFINITOR DISPERZ, answered by our medical review team.
AFINITOR is a mTOR Inhibitor Antineoplastic that works by Inhibitor of mammalian target of rapamycin (m TOR), specifically the m TORC1 complex, by binding to the FKBP-12 protein, reducing cell proliferation, angiogenesis, and glucose uptake.. AFINITOR DISPERZ is a mTOR Inhibitor Antineoplastic that works by Everolimus is an m TOR inhibitor that binds to FKBP-12, forming a complex that inhibits the m TOR serine-threonine kinase, thereby blocking cell cycle progression, angiogenesis, and cell growth.. They differ in pharmacokinetic profiles, FDA-approved indications, and side effect profiles.
Potency comparisons between AFINITOR and AFINITOR DISPERZ depend on the specific clinical indication. These are both mTOR Inhibitor Antineoplastic agents and are not directly interchangeable by dose. A physician or clinical pharmacist should guide any therapeutic switching decisions.
The standard adult dose of AFINITOR is: 10 mg orally once daily for advanced breast cancer, neuroendocrine tumors, and renal cell carcinoma; 10 mg orally once daily for subependymal giant cell astrocytoma (SEGA) in adults; 5 mg/m^2 orally once daily for SEGA in pediatric patients (titrated to trough levels 5-15 ng/m L).. The standard adult dose of AFINITOR DISPERZ is: 10 mg orally once daily for advanced hormone receptor-positive, HER2-negative breast cancer; 10 mg orally once daily for advanced pancreatic neuroendocrine tumors; 10 mg orally once daily for advanced renal cell carcinoma; 7.5 mg orally once daily for subependymal giant cell astrocytoma (SEGA); 5 mg orally once daily for tuberous sclerosis complex (TSC)-associated renal angiomyolipoma.. Dosing should always be individualized based on indication, renal and hepatic function, age, and other patient factors.
No direct drug-drug interaction has been formally documented between AFINITOR and AFINITOR DISPERZ in current clinical databases. However, individual patient risk factors including other medications, organ function, and comorbidities should always be evaluated by a qualified healthcare provider.
The maternal-fetal safety profiles differ. AFINITOR is classified as Category C. Pregnancy Category D. Positive evidence of human fetal risk. Based on its mechanism of action (mTOR inhibitor) and animal studies, AFINITOR (everolimus) is embryotoxic and fetotoxi. AFINITOR DISPERZ is classified as Category C. Pregnancy Category D. Animal studies show embryotoxicity and fetotoxicity at subtherapeutic doses. First trimester: risk of major malformations. Second/third trimester: risk of fet. Always consult a maternal-fetal medicine specialist before taking either drug during pregnancy or lactation.