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Astagraf XL

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Astagraf XL

ASTAGRAF XL™
(tacrolimus) Extended-release Capsules

WARNING

MALIGNANCIES; SERIOUS INFECTIONS; AND MORTALITY IN FEMALE LIVER TRANSPLANT RECIPIENTS

  • Only physicians experienced in immunosuppressive therapy and management of organ transplant patients should prescribe ASTAGRAF XL. Patients receiving the drug should be managed in facilities equipped and staffed with adequate laboratory and supportive medical resources. The physician responsible for maintenance therapy should have complete information requisite for the follow-up of the patient [see WARNINGS AND PRECAUTIONS].

Malignancies and Serious Infections

  • Increased susceptibility to infection and the possible development of malignancies such as lymphoma and skin cancer may result from immunosuppression [see WARNINGS AND PRECAUTIONS].

Mortality in Liver Transplantation

  • Increased mortality in female transplant recipients was observed in a clinical trial of liver transplantation. Use in liver transplantation is not recommended [see WARNINGS AND PRECAUTIONS].

DRUG DESCRIPTION

ASTAGRAF XL is available for oral administration as hard gelatin capsules (tacrolimus extended-release capsules) containing the equivalent of 0.5 mg, 1 mg or 5 mg of anhydrous tacrolimus USP. Inactive ingredients include ethylcellulose NF, hypromellose USP, magnesium stearate NF and lactose monohydrate NF. The ingredients are directly proportional across all capsule strengths. The capsule shell contains gelatin NF, titanium dioxide USP, ferric oxide NF, and sodium lauryl sulfate. The capsule shell also has a trace of printing ink, Opacode S-1-15083 Red.

Tacrolimus is the active ingredient in ASTAGRAF XL. Tacrolimus is a macrolide immunosuppressant produced by Streptomyces tsukubaensis. Chemically, tacrolimus is designated as [3S – [3R*[E(1S*, 3S*, 4S*)], 4S*, 5R*, 8S*, 9E, 12R*, 14R*, 15S*, 16R*, 18S*, 19S*, 26aR*]] – 5, 6, 8, 11, 12, 13, 14, 15, 16, 17, 18, 19, 24, 25, 26, 26a – hexadecahydro – 5, 19 – dihydroxy – 3 – [2 – (4 – hydroxy – 3 – methoxycyclo – hexyl) – 1 – methylethenyl] – 14, 16 – dimethoxy – 4, 10, 12, 18 – tetramethyl – 8 – (2 – propenyl) – 15, 19 – epoxy – 3H – pyrido[2, 1 – c][1, 4]oxaazacyclotricosine – 1, 7, 20, 21(4H, 23H) – tetrone, monohydrate.

The chemical structure of tacrolimus is:

ASTAGRAF XL™ (tacrolimus) Structural Formula Illustration

Tacrolimus has an empirical formula of C44H69NO12•H2O and a formula weight of 822.03. Tacrolimus appears as white crystals or crystalline powder. It is practically insoluble in water, freely soluble in ethanol, and very soluble in methanol and chloroform.

Last reviewed on RxList: 3/18/2014
This monograph has been modified to include the generic and brand name in many instances.

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