Factory Direct Supply 99% Purity Tacrolimus FK-506 powder CAS 104987-11-3 IN BULK

Chemical Identity: Tacrolimus (CAS No. 104987-11-3) Description: Tacrolimus is a macrolide lactone compound derived from the fermentation of the soil bacterium Streptomyces tsukubaensis. It is a potent immunosuppressant with a narrow therapeutic index.

Mechanism of Action:

• Tacrolimus exerts its immunosuppressive effects by inhibiting calcineurin, a phosphatase enzyme involved in the activation of T-lymphocytes.
• By inhibiting calcineurin, tacrolimus blocks the production of interleukin-2 (IL-2) and other cytokines, thereby suppressing T-cell activation and the immune response against transplanted organs.

Indications:

• Tacrolimus is indicated for the prophylaxis of organ rejection in patients receiving allogeneic liver, kidney, or heart transplants.
• It is typically used in combination with other immunosuppressive medications, such as corticosteroids and antimetabolites.

Dosage Forms:

• Tacrolimus is available in oral and intravenous formulations. The oral form is commonly available as immediate-release capsules and extended-release tablets.

Dosage and Administration:

• The dosage of tacrolimus is individualized based on factors such as the type of transplant, patient's body weight, renal function, and concomitant medications.
• It is usually administered twice daily, with doses adjusted to achieve target blood concentrations.

Monitoring:

• Therapeutic drug monitoring is essential for tacrolimus therapy to optimize efficacy and minimize toxicity. Blood concentrations of tacrolimus are measured regularly, and doses are adjusted accordingly.
• Monitoring may include measurement of trough levels (before the next dose) to ensure adequate immunosuppression and minimize the risk of rejection.

Adverse Effects:

• Common adverse effects of tacrolimus include nephrotoxicity, neurotoxicity, hypertension, gastrointestinal disturbances, hyperglycemia, and electrolyte imbalances.
• Long-term use of tacrolimus may also increase the risk of infections, malignancies (such as skin cancer and lymphoma), and metabolic complications.

Drug Interactions:

• Tacrolimus interacts with numerous drugs, including other immunosuppressants, antifungal agents, antibiotics, and drugs that affect cytochrome P450 enzymes.
• Concurrent use of tacrolimus with drugs that inhibit or induce CYP3A4 metabolism may alter tacrolimus blood concentrations, requiring dose adjustments.

Contraindications:

• Tacrolimus is contraindicated in patients with a known hypersensitivity to tacrolimus or any of its components.
• It should not be used in patients with uncontrolled infections or preexisting severe renal impairment.

Pregnancy and Lactation:

• Tacrolimus may cause fetal harm when administered during pregnancy and is classified as Pregnancy Category C. The benefits and risks should be carefully considered before using tacrolimus in pregnant women.
• Tacrolimus is excreted in breast milk, and breastfeeding is not recommended during tacrolimus therapy due to the potential risk of adverse effects in the infant.