Basiliximab

Basiliximab
Mass / length primary structure	143.8 kDa
Identifier
External IDs	CAS number : 179045-86-4;
Drug information
ATC code	L04 AA09
DrugBank	BTD00073
Drug class	Immunosuppressant

Basiliximab is a chimeric monoclonal antibody against the interleukin-2 receptor (CD25) that is used therapeutically to prevent acute rejection reactions after kidney and liver transplants .

Clinical information

Application areas (indications)

Basiliximab is used in adults and children in combination with ciclosporin and corticosteroids for the prevention of acute transplant rejection after kidney transplants. In adults, it can also be used as part of a long-term immunosuppressive treatment in combination with ciclosporin, corticosteroids and azathioprine or mycophenolate mofetil .

Currently, clinical trials for the treatment of ulcerative colitis carried out with basiliximab, for this indication , however, is currently not approved before.

Dosis, kind and Time of the Use

As soon as it is certain that the patient will receive the transplant, adults will be given 20 mg intravenous basiliximab two hours before the transplant . Another dose of 20 mg follows four days after the transplant.

Contraindications (contraindications)

Basiliximab must not be used in cases of known hypersensitivity to the antibody, or during pregnancy and breastfeeding .

Adverse effects (side effects)

Basiliximab leads to a variety of side effects; In addition to very frequent ones, such as pain or nausea, hypersensitivity reactions are observed, albeit rarely, which can be severe. Therefore, the antibody may only be used in clinics that are able to treat such hypersensitivity reactions. An increased number of infectious diseases or malignancies was not observed.

Pharmacological properties

Mechanism of action (pharmacodynamics)

Basiliximab binds and blocks the interleukin-2 receptor (CD25) on the surface of activated T lymphocytes . This interrupts the signal for T cell proliferation and weakens the immune response against the transplant. In clinical studies on a total of 590 patients, it was shown that the addition of basiliximab to a standard immunosuppressive treatment leads to a reduced number of acute transplant rejections. Another drug with the same mechanism of action is the humanized antibody daclizumab .

toxicology

In rhesus monkeys , single doses of up to 5 mg / kg and multiple doses of up to 24 mg / kg (more than a thousand times the exposure after the clinically recommended dose) showed no undesirable effects. In clinical studies, 60 mg as a single dose and 150 mg as a multiple dose did not show any undesirable effects.

Other Information

Chemical information

Basili ximab is a chimeric (mouse / human) antibody of the IgG ₁ type that is produced in cell culture in mouse myeloma cells . The finished drug also contains potassium dihydrogen phosphate, sodium monohydrogen phosphate, sodium chloride , sucrose, mannitol, glycine and water for injections as excipients .

History

The antibody was approved in the US in May 1998 and in the European Union in October 1998.

Trade names and dosage forms

Simulect

literature

European public assessment report on Simulect. (PDF; 42 kB)

Individual evidence

↑ B. Nashan, R. Moore, P. Amlot, AG Schmidt, K. Abeywickrama, JP Soulillou: Randomized trial of basiliximab versus placebo for control of acute cellular rejection in renal allograft recipients. CHIB 201 International Study Group. In: The Lancet . 350 (9086), Oct 25, 1997, pp. 1193-1198. Erratum in: Lancet. 350 (9089), Nov 15, 1997, p. 1484. PMID 9652559 .
↑ JR Thistlethwaite Jr, B. Nashan, M. Hall, L. Chodoff, TH Lin: Reduced acute rejection and superior 1-year renal allograft survival with basiliximab in patients with diabetes mellitus. The Global Simulect Study Group. In: transplant. 70 (5), Sep 15, 2000, pp. 784-790. PMID 11003358 .
↑ AC Webster, LP Ruster, R. McGee, SL Matheson, GY Higgins, NS Willis, JR Chapman, JC Craig: Interleukin 2 receptor antagonists for kidney transplant recipients. In: Cochrane Database Syst Rev. (1), Jan 20, 2010, Art. No. CD003897. Review. PMID 20091551 .
^ TJ Creed et al .: Basiliximab for the treatment of steroid-resistant ulcerative colitis: further experience in moderate and severe disease. In: Aliment Pharmacol Ther . 23 (10), May 15, 2006, pp. 1435-1442. PMID 16669958 .

[1] B. Nashan, R. Moore, P. Amlot, AG Schmidt, K. Abeywickrama, JP Soulillou: Randomized trial of basiliximab versus placebo for control of acute cellular rejection in renal allograft recipients. CHIB 201 International Study Group. In: The Lancet . 350 (9086), Oct 25, 1997, pp. 1193-1198. Erratum in: Lancet. 350 (9089), Nov 15, 1997, p. 1484. PMID 9652559 .

[2] JR Thistlethwaite Jr, B. Nashan, M. Hall, L. Chodoff, TH Lin: Reduced acute rejection and superior 1-year renal allograft survival with basiliximab in patients with diabetes mellitus. The Global Simulect Study Group. In: transplant. 70 (5), Sep 15, 2000, pp. 784-790. PMID 11003358 .

[3] AC Webster, LP Ruster, R. McGee, SL Matheson, GY Higgins, NS Willis, JR Chapman, JC Craig: Interleukin 2 receptor antagonists for kidney transplant recipients. In: Cochrane Database Syst Rev. (1), Jan 20, 2010, Art. No. CD003897. Review. PMID 20091551 .

[4] TJ Creed et al .: Basiliximab for the treatment of steroid-resistant ulcerative colitis: further experience in moderate and severe disease. In: Aliment Pharmacol Ther . 23 (10), May 15, 2006, pp. 1435-1442. PMID 16669958 .