Head-to-head clinical analysis & difference comparison: details on mechanism of action, dosing, half-life, interactions, and maternal-fetal safety.
ASTAGRAF XL vs ELIDEL
Clinician-reviewed, head-to-head comparison of mechanism, dosing, pharmacokinetics, and safety profiles.
Last clinically reviewed: July 2026 · OpiCalc Medical Review Team
Calcineurin inhibitor that binds to FKBP-12, forming a complex that inhibits calcineurin, thereby preventing dephosphorylation and nuclear translocation of NFAT, which reduces T-cell activation and cytokine production (e.g., IL-2).
Inhibits T-cell activation by binding to macrophilin-12 (FKBP-12) and inhibiting calcineurin, thereby blocking cytokine transcription.
Prophylaxis of organ rejection in kidney transplant recipients,Prophylaxis of organ rejection in liver transplant recipients,Prophylaxis of organ rejection in heart transplant recipients
Atopic dermatitis unresponsive to or intolerant of other topical treatments,Off-label: psoriasis, vitiligo, rosacea, contact dermatitis, lichen sclerosus, cutaneous lupus erythematosus
Initial oral dose of 0.1-0.15 mg/kg/day divided every 12 hours, with subsequent adjustments based on trough levels. Typical maintenance dose 0.05-0.15 mg/kg/day.
Apply a thin layer of 1% cream to affected areas twice daily.
Terminal elimination half-life is approximately 43 hours (range 15.8–68.6 hours) in adult kidney transplant recipients. This long half-life supports once-daily dosing. In liver transplant patients, half-life ranges from 12 to 42 hours.
Terminal elimination half-life: 30–45 hours (mean 35 hours) following topical application; clinically, twice-daily dosing ensures therapeutic concentrations.
Primarily hepatic via CYP3A4 and CYP3A5; undergoes extensive first-pass metabolism. Substrate of P-glycoprotein.
Metabolized primarily by CYP3A4; major metabolite O-demethylated pimecrolimus.
Primarily fecal (94.6%) via biliary elimination. Renal excretion accounts for approximately 2.4% of the dose, mainly as metabolites. Less than 1% is excreted unchanged in urine.
Renal (negligible, <1% unchanged) and biliary/fecal (approximately 97% as metabolites); less than 1% of the dose is excreted renally as unchanged drug.
Approximately 99% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein.
99% bound to plasma proteins (primarily albumin and alpha-1-acid glycoprotein).
Volume of distribution is 3.5–4.5 L/kg (wide distribution, indicating extensive tissue binding). High Vd reflects distribution into erythrocytes, lymphocytes, and tissues.
Vd ~ 10 L/kg (extensive tissue distribution); suggests significant extravascular binding and penetration into tissues.
Oral bioavailability is highly variable, approximately 20–30% (range 5–89%). Absorption is incomplete and inconsistent; food decreases absorption by up to 33%. The modified-release formulation (Astagraf XL) has a lower peak and more sustained absorption compared to immediate-release.
Topical: Systemic bioavailability is approximately 4% (range 1–7%) of applied dose; absorption increases with extent of skin lesion and thickness of application.
For GFR <30 m L/min: reduce dose by 50% and monitor trough levels closely. No adjustment for GFR >30 m L/min.
No dose adjustment required for any degree of renal impairment.
Child-Pugh Class A: no adjustment. Class B: reduce dose by 25%. Class C: reduce dose by 50% and monitor trough levels frequently.
No formal studies in hepatic impairment; use caution in severe impairment.
Initial oral dose 0.15-0.2 mg/kg/day divided every 12 hours. Adjust to target trough levels of 5-15 ng/m L. Maximum dose 0.3 mg/kg/day.
Apply a thin layer of 1% cream twice daily for children aged 2 years and older; not indicated for children under 2 years.
Start at lower end of adult dosing range (0.05 mg/kg/day) and titrate slowly due to reduced renal function and increased risk of adverse effects. Monitor trough levels closely.
No specific dose adjustment recommended; apply a thin layer of 1% cream twice daily as for adults.
Increased susceptibility to infection and possible development of lymphoma and other malignancies, particularly of the skin, due to immunosuppression. Increased nephrotoxicity, especially when used with other nephrotoxic drugs.
Long-term safety of topical calcineurin inhibitors has not been established; rare cases of malignancy (e.g., lymphoma, skin cancer) have been reported; use should be limited to short-term and intermittent treatment.
Nephrotoxicity, neurotoxicity (tremor, headache, seizures), hypertension, hyperkalemia, hyperglycemia, increased risk of infections and malignancies (especially skin), and lymphoproliferative disorders. Monitor blood pressure, renal function, electrolytes, and drug levels.
Increased risk of infections (e.g., eczema herpeticum, varicella zoster); avoid use on malignant or premalignant skin conditions; lymphadenopathy; photosensitivity; not recommended in patients with Netherton syndrome; potential for systemic immunosuppression; monitor for local irritation.
Hypersensitivity to tacrolimus or any component of the formulation; concurrent use with cyclosporine or other calcineurin inhibitors.
Hypersensitivity to pimecrolimus or any component of the formulation; history of malignancy; application to areas of active infection; Netherton syndrome; immunocompromised patients.
Grapefruit juice significantly increases tacrolimus AUC and Cmax; avoid concurrent use. High-fat meals may decrease absorption; maintain consistent fat intake with each dose to ensure stable levels. Avoid taking with alcohol or herbal supplements like St. John's wort, which may reduce efficacy.
No known food interactions. Avoid grapefruit juice as it may increase drug levels (CYP3A4 inhibition).
Tacrolimus is classified as FDA Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. In animal studies, tacrolimus caused maternal toxicity and embryotoxicity at doses higher than those used clinically. First trimester exposure is associated with an increased risk of congenital anomalies, including cardiac malformations. Second and third trimester use has been linked with intrauterine growth restriction, preterm delivery, and transient neonatal hyperkalemia and renal dysfunction. Postnatal immunosuppression in the neonate may occur.
FDA Pregnancy Category C. Systemic exposure is minimal after topical application, but animal studies have shown developmental toxicity. No adequate human studies; risk cannot be excluded. Avoid in pregnancy unless clearly needed.
Tacrolimus is excreted into human breast milk with a milk-to-plasma (M/P) ratio of approximately 0.3. Limited data suggest low infant exposure (relative infant dose 0.5% of maternal weight-adjusted dose). However, because of potential for infant immunosuppression and growth effects, breastfeeding is generally not recommended unless benefits outweigh risks. Monitor infant for trough levels if breastfeeding.
Not recommended. Pimecrolimus is excreted in milk in animal studies; unknown in humans. M/P ratio not available. Potential for serious adverse reactions in nursing infants.
Pregnancy increases tacrolimus clearance due to expanded plasma volume and altered cytochrome P450 3A4 activity. Dose requirements may increase by 25-50% during the second and third trimesters. Therapeutic drug monitoring is essential, targeting trough levels 5-10 ng/m L. Postpartum, doses should be reduced to prepregnancy levels within 1-2 weeks as clearance normalizes.
No dose adjustment necessary; use minimal amount to control symptoms. Systemic absorption is negligible, so pharmacokinetic changes in pregnancy do not alter dosing.
Monitor trough levels 5-15 ng/m L; avoid using with sirolimus due to increased risk of thrombotic microangiopathy; conversion from tacrolimus immediate-release is 1:1 (mg:mg) but monitor levels closely for 2 weeks; administer consistently with or without food to avoid fluctuations.
Topical calcineurin inhibitor for atopic dermatitis, reserved as second-line therapy for mild-to-moderate eczema due to boxed warning for rare malignancy risk. Apply thin layer only; avoid occlusive dressings. Do not use in immunocompromised patients. Intermittent use is recommended; continuous long-term use safety not established.
Take at the same time every day, consistently with or without food.,Do not crush, chew, or split the extended-release capsules; swallow whole.,Avoid grapefruit and grapefruit juice as they can increase drug levels and toxicity.,Report signs of infection (fever, sore throat), tremors, or changes in urine output immediately.,Minimize sun exposure and use sunscreen due to increased risk of skin cancer.,Do not change brand or formulation without consulting your transplant team.,Keep all appointments for blood level monitoring.
Apply only to affected skin areas; avoid eyes, mouth, and open wounds.,Use for short durations; do not use continuously for extended periods.,Avoid sun exposure and tanning beds; use sunscreen on treated areas.,Do not cover treated skin with bandages or wraps unless instructed.,Report any signs of infection, skin burning, or new skin growths to your doctor.,This drug is for external use only; wash hands after application unless treating hands.,Do not use if you have a weakened immune system or active skin infection.
No interactions on record
No interactions on record
Explore head-to-head clinical comparisons of other medications in the same therapeutic classes.
Common clinical questions about ASTAGRAF XL vs ELIDEL, answered by our medical review team.
ASTAGRAF XL is a Immunosuppressant, Calcineurin Inhibitor that works by Calcineurin inhibitor that binds to FKBP-12, forming a complex that inhibits calcineurin, thereby preventing dephosphorylation and nuclear translocation of NFAT, which reduces T-cell activation and cytokine production (e.g., IL-2).. ELIDEL is a Topical Calcineurin Inhibitor that works by Inhibits T-cell activation by binding to macrophilin-12 (FKBP-12) and inhibiting calcineurin, thereby blocking cytokine transcription.. They differ in pharmacokinetic profiles, FDA-approved indications, and side effect profiles.
Potency comparisons between ASTAGRAF XL and ELIDEL depend on the specific clinical indication. These are agents from distinct pharmacological classes and are not directly interchangeable by dose. A physician or clinical pharmacist should guide any therapeutic switching decisions.
The standard adult dose of ASTAGRAF XL is: Initial oral dose of 0.1-0.15 mg/kg/day divided every 12 hours, with subsequent adjustments based on trough levels. Typical maintenance dose 0.05-0.15 mg/kg/day.. The standard adult dose of ELIDEL is: Apply a thin layer of 1% cream to affected areas twice daily.. 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 ASTAGRAF XL and ELIDEL 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. ASTAGRAF XL is classified as Category C. Tacrolimus is classified as FDA Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. In animal studies, tacrolimus caused maternal toxicity an. ELIDEL is classified as Category C. FDA Pregnancy Category C. Systemic exposure is minimal after topical application, but animal studies have shown developmental toxicity. No adequate human studies; risk cannot be ex. Always consult a maternal-fetal medicine specialist before taking either drug during pregnancy or lactation.