Journal of the Korean Association of Oral and Maxillofacial Surgeons : eISSN 2234-5930 / pISSN 2234-7550

Table. 3.

Table. 3.

Comparison of cyclosporine and tacrolimus

Medication Cyclosporine Tacrolimus
Brand name Sandimmune (Novartis)
Neoral (Novartis)
Prograf (twice daily) (Astellas Pharma)
Advagraf (Astellas Pharma)
Astagraf XL (Astellas Pharma)
Graceptor (Astellas Pharma)
Prograf XL (Astellas Pharma)
Envarsus XR (once daily) (Veloxis Pharmaceuticals)
Pharmacologic profile Poor oral bioavailability with poor water solubility9,19
Metabolism: CYP3A4, CYPA5, P-glycoprotein19,25-27
Excretion mainly through the biliary route29
Route of administration Oral: oral solution, soft gel capsule, microemulsion
IV: administer with caution due to anaphylactic reaction13
Topical delivery (e.g., eye, skin)
Oral: IR, ER, XL
Sublingual: 50% of oral dosage23
IV: Administer with caution due to anaphylactic reaction20,21
Topical delivery (e.g., skin)
Mechanism of action Calcineurin/NFAT pathway inhibition: cyclosporin–cyclophilin complex inhibits calcineurin, leading to inhibition of nuclear translocation of NFAT family members3
JNK & p38 pathway inhibition: cyclosporine inhibits the upper stream of MAPKKK, leading to inhibition of p38 (MAPK14) and JNK (MAPK8) pathways43,44
Calcineurin/NFAT pathway inhibition: tacrolimus-FKBP12 complex inhibits calcineurin26
Inhibition of activation of B-cells and antibody generation45
Efficacy Compared to cyclosporine, tacrolimus shows similar qualitative effect at 20- to 50-fold lower concentration in clinical doses32
Acute rejection
Graft-survival
Acute rejection: lower for tacrolimus group46
1-year/2-year patient survival, graft survival: comparable46
3-year/5-year patient survival, graft survival: higher for tacrolimus group47
Adverse effects Nephrotoxicity (comparable with tacrolimus)2,52,53
Neurotoxicity55
Hyperlipidemia
Hypercholesterolemia
Hirsutism
Gingivitis/gingival hyperplasia57
Nephrotoxicity (IV route may have a higher risk)46
Neurotoxicity (higher rates shown in liver transplant patients)46
Gastrointestinal disturbance
Post-transplantation diabetes (higher than cyclosporine)46
Nerve regeneration Lack of peripheral nerve regenerative property61,64 FKBP-12, FKBP-52 may mediate peripheral axon, and myelin sheath regeneration61,65

(XL: extra-long, XR: extended-release, IV: intravenous, IR: immediate-release, ER: extended-release, NFAT: nuclear factor of activated T cell, JNK: Jun N-terminal kinase, MAPK: mitogen-activated protein kinase, MAPKKK: MAPK kinase kinase, FKBP: FK506 binding protein)

J Korean Assoc Oral Maxillofac Surg 2023;49:311~323
https://doi.org/10.5125/jkaoms.2023.49.6.311
© JKAOMS