Tablet for oral suspension (Afinitor Disperz)
- Strengths
- 2, 3, 5 mg
- Product note
- Disperse in water; do not swallow intact. This formulation carries the seizure indication.
Everolimus
Afinitor Disperz · generic tablets for oral suspension
DailyMed-verified antiseizure indications
Indication / use
- Label / evidence summary
- Afinitor Disperz and corresponding generic tablets for oral suspension: adjunctive treatment of TSC-associated focal-onset seizures at age 2 years and older. Conventional Afinitor tablets do not have this seizure indication.
- Role
- Maintenance
- Class
- mTOR inhibitor
Indications checked 27 September 2026. Product, route, age, and treatment-role limits apply. A DailyMed listing alone does not establish FDA approval.
- Afinitor / Afinitor Disperz — brand-name package insert (DailyMed PDF) ↗
- Representative source · Everolimus tablets for oral suspension (Biocon) — DailyMed label (PDF) ↗
- Afinitor Disperz tablets for oral suspension U.S. label
Tuberous sclerosis syndrome · 2 years and older · MaintenanceAdjunctive treatment of TSC-associated focal-onset seizures only.
- Everolimus tablets for oral suspension (generic) U.S. label
Tuberous sclerosis syndrome · 2 years and older · MaintenanceAdjunctive TSC-associated focal-onset seizures; representative generic suspension-tablet label.
Formulations & strengths
U.S. product labels; strengths per dosage unit.
Tablet for oral suspension (generic everolimus)
- Strengths
- 2, 3, 5 mg
- Product note
- Representative Biocon label; prepare according to the exact product instructions.
Conventional tablet (Afinitor)
- Strengths
- 2.5, 5, 7.5, 10 mg
- Product note
- Other labeled indications; no seizure indication. Excluded from seizure-use matching.
Brand & formulation labels
Each link names the product and formulation it covers. Archived labels do not establish current availability.
Dosing & administration
- Adult / product-specific schedule
- For TSC-associated focal seizures: Afinitor Disperz starting dose 5 mg/m² orally once daily; adjust using whole-blood trough monitoring to 5–15 ng/mL. Dosing differs for other everolimus indications.
- Pediatric
- For the seizure indication, age 2 years and older: the same body-surface-area starting dose and trough target. Safety and effectiveness for this indication are not established below age 2.
- Titration / repeat dosing
- Check trough concentrations 1–2 weeks after initiation or a dose change. The label uses new dose = current dose × target / measured trough, with no increase greater than 5 mg at one titration. Reassess after interaction or hepatic-function changes; apply the label’s separate toxicity modifications.
Practical administration
- Product instructions
- Prepare suspension in water only, using the label’s oral-syringe or small-glass method. Take consistently with or without food. Do not combine Afinitor and Afinitor Disperz to achieve a dose.
Dose adjustment & concentrations
- Renal impairment
- Creatinine clearance 25–178 mL/min had no significant effect on oral clearance in the label analysis. Monitor renal function; renal failure is a serious precaution.
- Hepatic impairment
- For TSC-associated seizures with severe hepatic impairment (Child-Pugh C), the cited brand label recommends starting 2.5 mg/m² once daily, then adjusting by trough concentrations. Monitor troughs after changes in hepatic function.
- Serum reference information
- Whole-blood trough target for TSC-associated seizures: 5–15 ng/mL. Use the same assay and laboratory where possible.
Safety
- Boxed warning
- No boxed warning in the cited label.
- Contraindications
- Clinically significant hypersensitivity to everolimus, other rapamycin derivatives or product excipients.
- Serious precautions & monitoring
- Noninfectious pneumonitis; serious or opportunistic infections; stomatitis; renal failure; myelosuppression; hyperglycemia / dyslipidemia; impaired wound healing and embryo-fetal toxicity. Monitor blood counts, renal function, glucose, lipids and trough levels. Avoid live vaccines during treatment.
Common / selected adverse effects
- Stomatitis
- Respiratory infections
- Diarrhea
- Fever
- Cough / rash
Selected label-reported effects; frequencies cannot be compared across drugs.
Drug interactions: toxicity & clinical action
| Partner / combination | Clinical effect | Clinical action |
|---|---|---|
| Strong CYP3A / P-gp inhibitors | Substantially increased everolimus exposure. | Avoid combined use per label. |
| Moderate CYP3A / P-gp inhibitors; cannabidiol oral solution | Increased exposure; cannabidiol increased AUC about 2.5-fold in a label interaction study. | Apply product-specific dose reduction and repeat trough monitoring. |
| Strong CYP3A / P-gp inducers, including enzyme-inducing antiseizure medicines | Reduced everolimus exposure. | Follow the label’s induction-specific dose adjustments and monitor troughs. |
| ACE inhibitors | Higher angioedema risk. | Avoid combination per label. |
Selected interactions; consult the full label and complete medication list.
Pregnancy & contraception
- Fetal / neonatal risk
- Can cause fetal harm based on animal studies and mechanism; human pregnancy data are limited. Verify pregnancy status before treatment. Do not breastfeed during treatment or for 2 weeks after the last dose.
- Contraception
- Effective contraception during treatment and for 8 weeks after the last dose for females; for 4 weeks after the last dose for males with female partners of reproductive potential.
Clinical evidence
Research summaries describe studied populations and outcomes; they do not add indications or constitute treatment recommendations.
Direct pivotal trial
Trial summary
- Study design / duration
- EXIST-3: randomized, double-blind, placebo-controlled adjunctive trial in 366 patients with treatment-resistant TSC-associated focal seizures; 6-week titration and 12-week maintenance.
- Primary endpoint
- Reduction in focal-seizure frequency and proportion with at least 50% reduction.
- Results
- At least 50% seizure reduction occurred in 28.2% of the low-exposure group, 40.0% of the high-exposure group and 15.1% with placebo. These study exposure groups do not replace the current label’s trough target.
Trial publications
Comparative evidence
- Findings
- No head-to-head efficacy comparison is summarized.
Mechanism of action
- Everolimus binds FKBP12; the complex inhibits mTORC1 signaling.
- Tuberous sclerosis syndrome involves dysregulated mTOR signaling; the seizure indication is restricted to TSC-associated focal seizures.
Pharmacology
Adult values unless specified. Vd/F denotes apparent oral distribution volume.
Pharmacokinetics
- Bioavailability
- Absolute oral bioavailability is not quantified in the cited label. Exposure (AUC) is similar between Afinitor and Afinitor Disperz, but Disperz peak concentrations are 20–36% lower; this does not make their seizure indications interchangeable.
- Elimination half-life
- Mean elimination half-life approximately 30 hours.
- Volume of distribution
- Not quantified in the cited product label.
- Active metabolite(s)
- Six main circulating metabolites have approximately 100-fold less activity than everolimus; no clinically important active metabolite is established in the label.
- Active-metabolite half-life
- No clinically important active-metabolite half-life established in the label.
- Protein binding
- Approximately 74%.
- Metabolism / elimination
- CYP3A4 substrate; P-glycoprotein substrate. Predominantly fecal recovery of radiolabeled material; renal recovery is small.
Values reflect the cited product and study population; they are not interchangeable across formulations.
Molecular structure
NIH PubChem structure and record ↗
Product history
- Initial U.S. approval
- Afinitor Disperz: August 29, 2012 (NDA 203985); TSC-associated seizure indication added April 10, 2018.
- Market / formulation history
- Original everolimus approval preceded its seizure indication. Conventional Afinitor tablets and Disperz have different labeled uses.
- Brands
- Afinitor Disperz · generic tablets for oral suspension
- Manufacturer / marketer
- Novartis (Afinitor / Afinitor Disperz); Biocon (representative generic suspension tablets)
- Generic availability
- Yes — a representative tablets-for-oral-suspension label is linked.
- Related drugs
- Sirolimus is another mTOR inhibitor; it does not inherit this U.S. seizure indication.
Sources & review status
The Biocon suspension-tablet label is a representative generic source. Afinitor Disperz is linked to the original brand-name insert; conventional Afinitor tablets have different indications.
Brand reference: Afinitor / Afinitor Disperz ↗
Indications and DailyMed PDFs checked: 2026-09-27. Other profile sources reviewed: 2026-09-27 · label revision noted at that review: Current DailyMed brand and generic labels reviewed September 2026.. This is a draft reference; final review is pending.