Comprehensive medication guide to Astagraf XL including estimated pricing, availability information, side effects, and how to find it in stock at your local pharmacy.
Estimated Insurance Pricing
$0-$50 copay with commercial insurance plus the Astellas Cares copay card (up to $3,000/year savings); Medicare Part B covers 80% after deductible as a post-transplant immunosuppressive drug.
Estimated Cash Pricing
$95-$880/month retail depending on strength (0.5 mg to 5 mg, 30 capsules); approximately $174/month for 1 mg with SingleCare discount card. No generic commercially available as of 2026.
Medfinder Findability Score
55/100
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Astagraf XL is the brand name for tacrolimus extended-release capsules, manufactured by Astellas Pharma US. It was FDA-approved on July 19, 2013, making it the first once-daily oral tacrolimus formulation approved in the United States. It is available in 0.5 mg, 1 mg, and 5 mg strengths.
Astagraf XL is a calcineurin inhibitor immunosuppressant indicated for the prophylaxis of organ rejection in adult and pediatric kidney transplant patients who can swallow capsules, used in combination with other immunosuppressants. It is NOT approved for liver transplantation.
Astagraf XL is NOT interchangeable with tacrolimus immediate-release capsules (Prograf or generic), Envarsus XR extended-release tablets, or tacrolimus oral suspension. Substituting one formulation for another without physician supervision can cause organ rejection or toxicity.
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Astagraf XL contains tacrolimus, which works by binding to an intracellular protein called FKBP-12 (FK506-binding protein 12) inside T-lymphocytes. The resulting tacrolimus-FKBP-12 complex inhibits calcineurin, an enzyme critical for T-cell activation.
By blocking calcineurin, Astagraf XL prevents the activation of NFAT (Nuclear Factor of Activated T-cells) transcription factor, thereby suppressing the production of interleukin-2 and other cytokines responsible for driving T-cell proliferation and immune responses against the transplanted kidney.
The extended-release capsule formulation delivers tacrolimus continuously over 24 hours, providing more consistent blood level profiles compared to twice-daily immediate-release tacrolimus. Tacrolimus reaches steady state approximately 7 days after initiating or changing dosing. Regular whole blood trough concentration monitoring is essential because tacrolimus has a narrow therapeutic index.
0.5 mg — extended-release capsule
Light yellow cap, orange body; 30 capsules per bottle
1 mg — extended-release capsule
White cap, orange body; 30 capsules per bottle
5 mg — extended-release capsule
Grayish-red cap, orange body; 30 capsules per bottle
As of 2026, Astagraf XL is not on an active FDA or ASHP drug shortage list. Astellas confirms availability of all three strengths (0.5 mg, 1 mg, 5 mg). However, Astagraf XL has a findability score of 55 out of 100 due to its brand-only status, specialty pharmacy distribution, and the absence of a commercially available generic.
Many standard retail pharmacies do not consistently stock Astagraf XL, particularly in all three strengths. Patients are most likely to find it reliably at specialty pharmacies focused on transplant medications. Localized stocking gaps at retail chains are common. The strict non-interchangeability requirement means pharmacies cannot substitute another tacrolimus product without physician supervision.
If your pharmacy is out of stock, medfinder can call pharmacies near you to find which ones have Astagraf XL in your strength in stock, saving you hours of phone calls. Always refill 7-10 days before running out and consider using a transplant specialty pharmacy for more reliable access.
Astagraf XL is not a controlled substance, but its FDA prescribing information states it must be used under the supervision of a physician experienced in immunosuppressive therapy and organ transplant management. It is not appropriate for prescription by general practitioners without transplant expertise.
Telehealth follow-up is available for stable kidney transplant recipients already established on Astagraf XL therapy, but initiation and acute management require in-person care within a transplant center setting.
No. Astagraf XL (tacrolimus extended-release capsules) is not a controlled substance and is not scheduled under the DEA Controlled Substances Act. It does not have abuse potential and is not subject to the prescription refill restrictions that apply to Schedule II-V controlled substances.
However, Astagraf XL is a prescription-only medication that requires a physician experienced in immunosuppressive therapy. It cannot be prescribed by general practitioners without transplant expertise. The prescribing physician must monitor tacrolimus blood levels and kidney function regularly throughout treatment.
Astagraf XL carries an FDA Boxed Warning about increased risks of serious infections and malignancies, and increased mortality in female liver transplant patients. Common side effects include:
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Prograf (tacrolimus IR)
Twice-daily tacrolimus immediate-release capsules; original formulation with widely available generic. Not interchangeable with Astagraf XL without physician supervision.
Envarsus XR
Once-daily tacrolimus extended-release tablets by Veloxis. Not interchangeable with Astagraf XL; not FDA-approved for pediatric use.
Cyclosporine (Neoral/Gengraf)
Older calcineurin inhibitor; alternative for tacrolimus-intolerant patients. Causes more cosmetic side effects (hirsutism, gum overgrowth) but may cause less diabetes.
Mycophenolate mofetil (CellCept)
Antimetabolite immunosuppressant used in combination regimens alongside tacrolimus or cyclosporine, not as monotherapy.
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Azole antifungals (fluconazole, voriconazole, itraconazole)
majorCYP3A4 inhibitors that significantly increase tacrolimus blood levels. Dose reduction typically required.
Rifampin (rifampicin)
majorPotent CYP3A4 inducer; dramatically decreases tacrolimus levels, increasing rejection risk.
Phenytoin/phenobarbital/carbamazepine
majorCYP3A4 inducers; decrease tacrolimus levels requiring dose increases and close monitoring.
HIV protease inhibitors (ritonavir, lopinavir, nelfinavir)
majorStrong CYP3A4 inhibitors; significantly increase tacrolimus levels.
Grapefruit/grapefruit juice
majorInhibits intestinal CYP3A4, raising tacrolimus levels. Must be avoided completely.
Alcohol
majorDisrupts extended-release mechanism causing rapid tacrolimus release and toxic spikes.
NSAIDs (ibuprofen, naproxen, piroxicam)
moderateAdditive nephrotoxicity; reduces renal blood flow. Use acetaminophen instead.
Diltiazem/verapamil
moderateModerate CYP3A4 inhibitors; increase tacrolimus levels moderately. Monitor levels when starting or stopping.
St. John's Wort
majorPotent CYP3A4 inducer; drastically decreases tacrolimus levels. Contraindicated.
Cannabidiol (CBD)
moderateAffects CYP3A4 metabolism; can alter tacrolimus levels. Monitor closely if used.
Astagraf XL (tacrolimus extended-release capsules) is a cornerstone medication for kidney transplant recipients, providing the convenience of once-daily dosing while delivering effective immunosuppression. FDA-approved in 2013 and available in 73 countries, it has become a standard option in post-transplant care alongside twice-daily tacrolimus IR formulations.
Finding Astagraf XL can be challenging at standard retail pharmacies due to its brand-only, specialty-distributed status. Using a transplant specialty pharmacy and refilling early are the most reliable strategies. For commercially insured patients, the Astellas Cares copay card can reduce out-of-pocket costs to as little as $0 per fill with up to $3,000 in annual savings.
If you're having trouble finding Astagraf XL in stock, medfinder can call pharmacies near you to find which ones have your prescription ready to fill. Never skip doses or switch formulations without your transplant team's guidance -- consistent tacrolimus blood levels are essential to protecting your transplanted kidney.
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