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Basiliximab
| Monoclonal antibody |
| Type |
Whole antibody |
| Source |
Chimeric (mouse/human) |
| Target |
CD25 |
| Clinical data |
| Trade names |
Simulect |
| AHFS/Drugs.com |
Monograph |
Pregnancy
category |
- AU: D
- US: B (No risk in non-human studies)
|
| ATC code |
|
| Pharmacokinetic data |
| Biological half-life |
7.2 days |
| Identifiers |
| CAS Number |
|
| DrugBank |
|
| ChemSpider |
|
| UNII |
|
| ChEMBL |
|
| Chemical and physical data |
| Formula |
C6378H9844N1698O1997S48 |
| Molar mass |
143801.3 g/mol |
| NY (what is this?) (verify) |
Basiliximab (trade name Simulect) is a chimeric mouse-human monoclonal antibody to the α chain (CD25) of the IL-2 receptor of T cells. It is used to prevent rejection in organ transplantation, especially in kidney transplants. It is a Novartis product and was approved by the Food and Drug Administration (FDA) in 1998.
Contents
- 1 Uses
- 2 Mechanism of action
- 3 Chemistry
- 4 History
- 5 References and notes
Uses
Basiliximab is an immunosuppressant agent used to prevent immediate transplant rejection in people who are receiving kidney transplants, in combination with other agents.[1] It has been reported that some cases of lichen planus have been successfully treated with basiliximab as an alternative therapy to ciclosporin. No short-term side effects have been reported.[2]
Mechanism of action
Basiliximab competes with IL-2 to bind to the alpha chain subunit of the IL2 receptor on the surface of the activated T lymphocytes and thus prevents the receptor from signaling. This prevents T cells from replicating and also from activating B cells, which are responsible for the production of antibodies, which would bind to the transplanted organ and stimulate an immune response against the transplant.[3][4]
Chemistry
It is a chimeric CD25 monoclonal antibody of the IgG1 isotype.[3][4]
History
It is a Novartis product and was approved by the Food and Drug Administration (FDA) in 1998.[4][5]
References and notes
- ^ MedlinePlus. Last Revised - June 15, 2012 Basiliximab Injection
- ^ A.D. Katsambas, T.M. Lotti European handbook of dermatological treatments 2nd edition, 2003, page 291, ISBN 3-540-00878-0
- ^ a b Hardinger KL, Brennan DC, Klein CL. Selection of induction therapy in kidney transplantation. Transpl Int. 2013 Jul;26(7):662-72. PMID 23279211
- ^ a b c Basiliximab label
- ^ Waldman, Thomas A. (2003). Immunotherapy: past, present and future. Nature Medicine 9, 269-277.
|
Immunosuppressive drugs / Immunosuppressants (L04)
|
|
Intracellular
(initiation) |
| Antimetabolites |
- purine synthesis inhibitors: Azathioprine
- Mycophenolic acid
- pyrimidine synthesis inhibitors: Leflunomide
- Teriflunomide
|
|
Macrolides/
other IL-2 inhibitors |
- FKBP/Cyclophilin/Calcineurin: Tacrolimus
- Ciclosporin
- Pimecrolimus
|
|
| IMiDs |
- Lenalidomide
- Pomalidomide
- Thalidomide
- PDE4 inhibitor: Apremilast
|
|
|
Intracellular
(reception) |
| IL-1 receptor antagonists |
|
|
| mTOR |
- Sirolimus
- Everolimus
- Ridaforolimus
- Temsirolimus
- Umirolimus
- Zotarolimus
|
|
|
| Extracellular |
| Antibodies |
| Monoclonal |
Serum target
(noncellular) |
- Complement component 5 (Eculizumab)
- TNF (Adalimumab
- Afelimomab
- Certolizumab pegol
- Golimumab
- Infliximab
- Nerelimomab)
- Interleukin 5 (Mepolizumab)
- Immunoglobulin E (Omalizumab)
- IL-12 and IL-23 (Lebrikizumab
- Ustekinumab)
|
|
| Cellular target |
- CD3 (Muromonab-CD3
- Otelixizumab
- Teplizumab
- Visilizumab)
- CD4 (Clenoliximab
- Keliximab
- Zanolimumab)
- CD11a (Efalizumab)
- CD18 (Erlizumab)
- CD20 (Obinutuzumab
- Rituximab
- Ocrelizumab
- Pascolizumab)
- CD23 (Gomiliximab
- Lumiliximab)
- CD40 (Teneliximab
- Toralizumab)
- CD62L/L-selectin (Aselizumab)
- CD80 (Galiximab)
- CD147/Basigin (Gavilimomab)
- CD154 (Ruplizumab)
- BLyS (Belimumab
- Blisibimod)
- CTLA-4 (Ipilimumab
- Tremelimumab)
- CAT (Bertilimumab
- Lerdelimumab
- Metelimumab)
- Integrin (Natalizumab)
- Interleukin-6 receptor (Tocilizumab)
- LFA-1 (Odulimomab)
- IL-2 receptor/CD25 (Basiliximab
- Daclizumab
- Inolimomab)
- T-lymphocyte (Zolimomab aritox)
|
|
| Unsorted |
- Atorolimumab
- Cedelizumab
- Fontolizumab
- Maslimomab
- Morolimumab
- Pexelizumab
- Reslizumab
- Rovelizumab
- Siplizumab
- Talizumab
- Telimomab aritox
- Vapaliximab
- Vepalimomab
|
|
|
| Polyclonal |
- Anti-thymocyte globulin
- Anti-lymphocyte globulin
|
|
|
| -cept (Fusion) |
- CTLA-4 (Abatacept
- Belatacept)
- TNF inhibitor (Etanercept
- Pegsunercept)
- Aflibercept
- Alefacept
- Rilonacept
|
|
|
Monoclonal antibodies for the immune system
|
|
| Immune system ("-l(i[m])-") |
|
|
| Interleukin ("-k(i[n])-") |
| Human ("-kinu-") |
- Brazikumab
- Briakinumab
- Canakinumab
- Fezakinumab
- Fletikumab
- Guselkumab
- Secukinumab
- Sirukumab
- Tralokinumab
- Ustekinumab
|
|
| Humanized ("-kizu-", "-kinzu-") |
- Anrukinzumab
- Clazakizumab
- Enokizumab
- Gevokizumab
- Ixekizumab
- Lebrikizumab
- Olokizumab
- Perakizumab
- Tildrakizumab
|
|
|
| Inflammatory lesions ("-les-") |
| Mouse ("-leso-") |
- Besilesomab
- Fanolesomab‡
- Lemalesomab
- Sulesomab
|
|
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
|
Interleukin receptor modulators
|
|
| IL-1 |
- Agonists: Interleukin 1 (α, β)
- Mobenakin
- Pifonakin
- Antagonists: AF-12198
- Anakinra
- IL-1RA
- Isunakinra
- Antibodies: Canakinumab
- Gevokizumab
- Lutikizumab
- Decoy receptors: Rilonacept (IL-1 Trap)
|
|
| IL-2 |
- Agonists: Adargileukin alfa
- Aldesleukin
- Celmoleukin
- Denileukin diftitox
- Interleukin 2
- Pegaldesleukin
- Teceleukin
- Tucotuzumab celmoleukin
- Antibodies: Basiliximab
- Daclizumab (dacliximab)
- Inolimomab
|
|
| IL-3 |
- Agonists: Daniplestim
- Interleukin 3
- Leridistim
- Milodistim
- Muplestim
- Promegapoietin
|
|
| IL-4 |
- Agonists: Binetrakin
- Interleukin 4
- Interleukin 13
- Antibodies: Dupilumab
- Pascolizumab
|
|
| IL-5 |
- Antibodies: Benralizumab
- Mepolizumab
- Reslizumab
- Antisense oligonucleotides: TPI ASM8
|
|
| IL-6 |
- Agonists: Atexakin alfa
- Interleukin 6
- Antibodies: ARGX-109
- Clazakizumab
- Elsilimomab
- mAb 1339
- Olokizumab
- Sarilumab
- Siltuximab
- Sirukumab
- Tocilizumab
|
|
| IL-7 |
|
|
| IL-8 |
- See CXCR1 (IL-8Rα) and CXCR2 (IL-8Rβ) here instead.
|
|
| IL-9 |
|
|
| IL-10 |
- Agonists: Ilodecakin
- Interleukin 10 (CSIF)
|
|
| IL-11 |
- Agonists: Interleukin 11 (AGIF)
- Oprelvekin
|
|
| IL-12 |
- Agonists: Edodekin alfa
- Interleukin 12
- Antibodies: Briakinumab
- Ustekinumab
|
|
| IL-13 |
- Agonists: Binetrakin
- Cintredekin besudotox
- Interleukin 4
- Interleukin 13
- Antibodies: Anrukinzumab
- Lebrikizumab
- Tralokinumab
|
|
| IL-15 |
- Agonists: ALT-803
- Interleukin 15
|
|
| IL-17 |
- Agonists: Interleukin 17 (A, B, C, D, E (interleukin 25), F)
- Antibodies: Brodalumab
- Ixekizumab
- Perakizumab
- Remtolumab
- Secukinumab
- Vunakizumab
|
|
| IL-18 |
- Agonists: Iboctadekin
- Interleukin 18
- Interleukin 37
- Tadekinig
|
|
| IL-20 |
- Agonists: Interleukin 19
- Interleukin 20
- Interleukin 24
- Antibodies: Fletikumab (against IL-20)
|
|
| IL-21 |
- Agonists: Denenicokin
- Interleukin 21
- Antibodies: NNC0114-0005
- NNC0114-0006
|
|
| IL-22 |
- Antibodies: Fezakinumab (against IL-22)
|
|
| IL-23 |
- Agonists: Interleukin 23 (SGRF)
- Antibodies: Brazikumab
- Briakinumab
- Guselkumab
- Tildrakizumab
- Ustekinumab
|
|
| IL-27 |
- Agonists: Interleukin 27 (interleukin 30)
|
|
| IL-28 |
- Agonists: Interferon λ4 (IFN-λ4)
- Interleukin 28 (A (IFN-λ2), B (IFN-λ3))
- Interleukin-29 (IFN-λ1)
|
|
| IL-31 |
|
|
| IL1RL1 |
|
|
| IL1RL2 |
- Agonists: Interleukin 36 (α, β, γ)
- Interleukin 38
|
|
| Others |
|
JAK
|
|
|
|
Others
|
- Interleukin 14 (taxilin alpha, HMW-BCGF)
- Interleukin 16 (signals through CD4)
- Interleukin 24 (signals through IL-22Rα1/IL-20Rβ heterodimer)
- Interleukin 26 (signals through IL-20Rα/IL-10Rβ heterodimer)
- Interleukin 32
- Interleukin 34 (signals through M-CSFR/CSF1R)
- Interleukin 35
|
|
|
- See also: Cytokine receptor modulators
- Peptide receptor modulators
|
UpToDate Contents
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- 1. 成人における肝移植：免疫抑制の概要 liver transplantation in adults overview of immunosuppression
- 2. 成人の腎移植における免疫抑制誘導療法 induction immunosuppressive therapy in renal transplantation in adults
- 3. 肺移植後の免疫抑制の導入 induction immunosuppression following lung transplantation
- 4. 急性移植片対宿主病の治療 treatment of acute graft versus host disease
- 5. 心臓移植における免疫抑制療法の導入および維持 induction and maintenance of immunosuppressive therapy in cardiac transplantation
English Journal
- Induction therapy of basiliximab versus antithymocyte globulin in renal allograft: a systematic review and meta-analysis.
- Wang K1, Xu X2, Fan M1.
- Clinical and experimental nephrology.Clin Exp Nephrol.2018 Jun;22(3):684-693. doi: 10.1007/s10157-017-1480-z. Epub 2017 Oct 6.
- PMID 28986715
- Tacrolimus-induced asymptomatic thrombotic microangiopathy diagnosed by laboratory tests in pig-to-rhesus corneal xenotransplantation: A case report.
- Kim JM1,2,3,4, Kim J5,6,7, Choi SH5,6, Shin JS1,2,3,4,8, Min BH1,3,8, Jeong WY1, Lee GE1, Kim MS1, Kwon S1, Kim MK1,5,6, Park CG1,2,3,4,8,9.
- Xenotransplantation.Xenotransplantation.2018 May 18:e12404. doi: 10.1111/xen.12404. [Epub ahead of print]
- PMID 29777547
- Advagraf® with or without an induction therapy for de novo kidney-transplant recipients.
- Noble J1,2, Jouve T1,2, Rostaing L1,2, Malvezzi P1.
- Expert review of clinical immunology.Expert Rev Clin Immunol.2018 May 14. doi: 10.1080/1744666X.2018.1476850. [Epub ahead of print]
- PMID 29757021
Japanese Journal
- ABO血液型不適合腎移植の術前後の管理 : DFPPによる合併症について(<特集>白血球系細胞除去療法の最近の展開)
- OP4-006 Basiliximab(Simulect)を用いた早期ステロイドオフ免疫抑制療法の臨床的検討(一般演題(口演))
- Basiliximab(シムレクト^【○!R】)の腎移植後1カ月間の拒絶反応抑制効果ならびに外国臨床データの国内への外挿可能性の考察
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