Tacrolimus

CAS 109581-93-3

About the API

Therapeutic category Immunology
Available formulations Injectables Oral Liquid Oral Solid Oral Solid Long-Acting Topical / Dermatological
Regulations CEP Flag CEP EU DMF Flag EU DMF Japan DMF Flag Japan DMF Korea DMF Flag Korea DMF Other Flag Other US DMF Flag US DMF

General Information

About Tacrolimus

Tacrolimus is a substance that is used to suppress immune cells, mainly T cells, to prevent rejection of certain organ transplants and to treat a host of other conditions.

The topical solution is prescribed for the second-line treatment of moderate to severe dermatitis (eczema). The 0.1% ointment is intended for adults, while the 0.03% ointment can also be used to treat children aged 2 to 15 years. Specific conditions vary according to country. Oral capsules for immediate release, oral solution and oral granules, as well as intravenous injectable, are used to prevent the rejection of heart, kidney and liver allogeneic transplants (i.e., from a human donor who is genetically non-identical, as in most transplants).

 

According to country, tacrolimus is also used to prevent rejection of other allogeneic organ transplants as well as bone marrow transplants, and to treat patients with graft-versus-host disease (GVHD), myasthenia gravis, rheumatoid arthritis, lupus nephritis, and ulcerative colitis.

 

The granules cater to young children and other patients who have trouble swallowing (granules are made into an oral suspension).

 

Once-daily extended-release capsules are used in patients who convert from tacrolimus immediate-release formulations (after their condition has stabilized), to prevent rejection of kidney transplants and ‘ in the EU, Japan, and other locations ‘ liver transplants as well.

Tacrolimus Studies

Studies have shown that the incidence of acute rejection is reduced by tacrolimus in comparison to cyclosporine. Clinical studies are ongoing for other indications.

Tacrolimus: FDA

Tacrolimus, a designated orphan drug for non-topical formulations, was approved by the FDA in 1994 as an oral capsule and injectable; in 2000 as a topical ointment; and in 2015 as an extended release tablet. Capsules have been approved for use in nearly 100 countries. In Japan in particular, tacrolimus is approved for numerous indications.

 

It is prepared by a fermentation process based on the microorganism S. tsukubaensis.